Details
Stereochemistry | ACHIRAL |
Molecular Formula | C26H23FIN5O4 |
Molecular Weight | 615.3948 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C(=O)C(C)=C2N(C(=O)N(C3CC3)C(=O)C2=C1NC4=CC=C(I)C=C4F)C5=CC(NC(C)=O)=CC=C5
InChI
InChIKey=LIRYPHYGHXZJBZ-UHFFFAOYSA-N
InChI=1S/C26H23FIN5O4/c1-13-22-21(23(31(3)24(13)35)30-20-10-7-15(28)11-19(20)27)25(36)33(17-8-9-17)26(37)32(22)18-6-4-5-16(12-18)29-14(2)34/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34)
Molecular Formula | C26H23FIN5O4 |
Molecular Weight | 615.3948 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/?term=24875464; http://www.ncbi.nlm.nih.gov/pubmed/23846731
Curator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/?term=24875464; http://www.ncbi.nlm.nih.gov/pubmed/23846731
Trametinib is a reversible and specific inhibitor of mitogen-activated protein kinase kinases MEK1 and MEK2 which are involved in a RAS/RAF/MEK/ERK signaling pathway and control cell growth, survival, and differentiation. By inhibiting MEK1 and MEK2 trametinib blocks dual phosphorylation of ERK1/2 and stops cell cycling. In addition, trametinib blocks BRAF pathway in the cells with BRAF V600E mutations. Trametinib (as a single agent and in combination with dabrafenib) is approved for the treatment of unresectable or metastatic melanoma with BRAF V600E or V600K mutations.
CNS Activity
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=24875464
Curator's Comment: Trametinib crosses blood-brain barrier and has anticancer activity in the CNS
Originator
Sources: http://www.ncbi.nlm.nih.gov/pubmed/23846731
Curator's Comment: Originally developed by Japan Tobacco, GlaxoSmithKline has licensed exclusive worldwide rights to the compound and conducted development in a number of different cancer types.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: Q02750 Gene ID: 5604.0 Gene Symbol: MAP2K1 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4747351/ |
0.9 nM [IC50] | ||
Target ID: P36507 Gene ID: 5605.0 Gene Symbol: MAP2K2 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4747351/ |
1.8 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | MEKINIST Approved UseIndicated, as a single agent or in combination with dabrafenib, for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations Launch Date2013 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
9.5 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23893461 |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
TRAMETINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
8.03 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24606567 |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
TRAMETINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
498 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23893461 |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
TRAMETINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
525 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24606567 |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
TRAMETINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
127 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23893461 |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
TRAMETINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
264 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24606567 |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
TRAMETINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5% EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24606567 |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
TRAMETINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Disc. AE: Left ventricular dysfunction, Cardiac failure... AEs leading to discontinuation/dose reduction: Left ventricular dysfunction (0.9%) Sources: Page: 204114Orig1s000MedR.pdf - p.92Cardiac failure (0.5%) Myocardial infarction (0.5%) Tachycardia (0.5%) ALT increased (0.5%) Bilirubin increased (0.5%) GGT increased (0.5%) CPK increased (0.5%) Pneumonitis (0.9%) Renal failure (0.9%) Rash (0.9%) Erythema nodosum (0.5%) Chorioretinopathy (0.5%) Retinal detachment (0.5%) Hepatic failure (0.5%) Hepatitis (0.5%) Hepatobiliary disease (0.5%) Duodenal perforation (0.5%) Esophagitis (0.5%) Vomiting (0.5%) Diarrhea (0.5%) Abdominal pain upper (0.5%) Face edema (0.5%) Edema peripheral (0.5%) Fatigue (0.5%) Pyrexia (0.5%) Decreased appetite (0.5%) Hyponatremia (0.5%) Cell death (0.5%) Hypersensitivity (0.5%) Corneal graft rejection (0.5%) Anemia (0.5%) |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Disc. AE: Rash, Diarrhea... Other AEs: Hypertension, Rash... AEs leading to discontinuation/dose reduction: Rash (4%) Other AEs:Diarrhea (2%) Peripheral edema (2%) Transaminases increased (1%) Cardiac disorder (1%) Cellulitis (1%) Nausea (1%) Pyrexia (1%) Rash (9%) Acne (0.9%) Dermatitis acneiform (0.9%) Pruritus (0.9%) Erythema (0.5%) Rash maculo-papular (0.5%) Rash papular (0.5%) Skin ulcer (0.5%) Toxic skin eruption (0.5%) ALT increased (3%) AST increased (0.9%) CPK increased (0.9%) Alkaline phosphatase increased (0.5%) Electrocardiogram abnormal (0.5%) Decreased hemoglobin (0.5%) Stomatitis (0.9%) Abdominal pain (0.5%) Anal ulcer (0.5%) Diarrhea (0.5%) Lip ulceration (0.5%) Oral pain (0.5%) Rash pustular (0.9%) Folliculitis (0.5%) Klebsiella infection (0.5%) Nail infection (0.5%) Pulpitis dental (0.5%) Fatigue (0.9%) Mucosal inflammation (0.9%) Pyrexia (0.5%) Rhabdomyolysis (0.9%) Neck pain (0.5%) Exertional dyspnea (0.5%) Interstitial lung disease (0.5%) Nasal ulcer (0.5%) Conduction disorder (0.5%) Left ventricular dysfunction (0.5%) Hypertension (0.9%) Central serous retinopathy (0.5%) Hypertriglyceridemia (0.5%) Rash (grade 3, 7%) Acne (grade 3, 0.5%) Pruritus (grade 3, 0.9%) Rash papular (grade 3, 0.5%) ALT increased (grade 3, 0.9%) CPK increased (grade 3, 0.5%) Decreased hemoglobin (grade 3, 0.5%) Stomatitis (grade 3, 0.5%) Abdominal pain (grade 3, 0.5%) Lip ulceration (grade 3, 0.5%) Oral pain (grade 3, 0.5%) Rash pustular (grade 3, 0.5%) Folliculitis (grade 3, 0.5%) Klebsiella infection (grade 3, 0.5%) Fatigue (grade 3, 0.9%) Mucosal inflammation (grade 3, 0.9%) Rhabdomyolysis (grade 3, 0.9%) Exertional dyspnea (grade 3, 0.5%) Interstitial lung disease (grade 3, 0.5%) Conduction disorder (grade 3, 0.5%) Hypertension (grade 3, 0.9%) Hypertriglyceridemia (grade 3, 0.5%) Hypertension (grade 3, 13%) Sources: Page: 204114Orig1s000MedR.pdf - p.99Rash (grade 3, 8%) Fatigue (grade 3, 4%) Anemia (grade 3, 2%) Dehydration (grade 3, 1%) ALT increased (grade 3, 2%) Dyspnea (grade 3, 1%) Hypoalbuminemia (grade 3, 1%) Pruritus (grade 3, 2%) Vomiting (grade 3, 1%) CPK increased (grade 3, 1%) Cellulitis (grade 3, 1%) Infection (grade 3, 1%) Rash (grade 4, 0.5%) Dehydration (grade 4, 0.5%) Dyspnea (grade 4, 0.5%) |
2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
Other AEs: Skin rash, Skin rash... Other AEs: Skin rash (grade 3, 7.1%) Sources: Page: 204114Orig1s000SumR.pdf - p.21Skin rash (grade 4, 0.5%) Fatigue (grade 3, 4%) Peripheral edema (grade 3, 1%) Acneiform dermatitis (grade 3, 1%) Nausea (grade 3, 1%) Alopecia (grade 3, <1%) Hypertension (grade 3, 12%) Vomiting (grade 3, 1%) |
2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: |
Other AEs: Detachment of retinal pigment epithelium, Retinal vein occlusion... Other AEs: Detachment of retinal pigment epithelium (0.5%) Sources: Retinal vein occlusion (0.6%) Interstitial lung disease (2.4%) Skin rash (6%) |
2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
Other AEs: Cardiomyopathy... Other AEs: Cardiomyopathy (7%) Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
10 mg 1 times / day multiple, oral Highest studied dose Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 4 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 4 Sources: |
DLT: Central serous retinopathy, Diarrhoea... Dose limiting toxicities: Central serous retinopathy (grade 2) Sources: Diarrhoea (grade 3) Rash (grade 3) |
10 mg 1 times / day multiple, oral Highest studied dose Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 4 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 4 Sources: |
Other AEs: Detachment of retinal pigment epithelium... Other AEs: Detachment of retinal pigment epithelium (28%) Sources: |
4 mg 1 times / day multiple, oral Highest studied dose Dose: 4 mg, 1 times / day Route: oral Route: multiple Dose: 4 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 3 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 3 Sources: |
DLT: Central serous retinopathy... Dose limiting toxicities: Central serous retinopathy (grade 2) Sources: |
4 mg 1 times / day multiple, oral Highest studied dose Dose: 4 mg, 1 times / day Route: oral Route: multiple Dose: 4 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 3 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 3 Sources: |
|
3 mg 1 times / day multiple, oral MTD Dose: 3 mg, 1 times / day Route: oral Route: multiple Dose: 3 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 12 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 12 Sources: |
Disc. AE: Fatigue... AEs leading to discontinuation/dose reduction: Fatigue (8.3%) Sources: |
2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Other AEs: Acneiform dermatitis, Diarrhoea... Other AEs: Acneiform dermatitis (grade 1, 49%) Sources: Diarrhoea (grade 1, 34%) Fatigue (grade 1, 19%) Peripheral oedema (grade 1, 26%) Nausea (grade 1, 20%) Vomiting (grade 1, 7%) Pruritus (grade 1, 14%) Fissures of skin (grade 1, 16%) Decreased appetite (grade 1, 9%) Eye disorders NEC (grade 1, 9%) Mucosal inflammation (grade 1, 4%) Constipation (grade 1, 3%) Left ventricular ejection fraction decreased (grade 1, 3%) Periorbital oedema (grade 1, 7%) Thrombocytopenia (grade 1, 1%) Dry mouth (grade 1, 3%) Acneiform dermatitis (grade 2, 31%) Diarrhoea (grade 2, 10%) Fatigue (grade 2, 10%) Peripheral oedema (grade 2, 3%) Nausea (grade 2, 6%) Vomiting (grade 2, 4%) Pruritus (grade 2, 6%) Fissures of skin (grade 2, 6%) Decreased appetite (grade 2, 1%) Constipation (grade 2, 1%) Left ventricular ejection fraction decreased (grade 2, 6%) Acneiform dermatitis (grade 3, 4%) Diarrhoea (grade 3, 1%) Fatigue (grade 3, 1%) Vomiting (grade 3, 1%) Eye disorders NEC (grade 3, 1%) Left ventricular ejection fraction decreased (grade 3, 1%) |
2 mg 1 times / day multiple, oral Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 3 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 3 Sources: |
DLT: Rash... |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
ALT increased | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Abdominal pain upper | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Anemia | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Bilirubin increased | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
CPK increased | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Cardiac failure | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Cell death | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Chorioretinopathy | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Corneal graft rejection | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Decreased appetite | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Diarrhea | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Duodenal perforation | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Edema peripheral | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Erythema nodosum | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Esophagitis | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Face edema | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Fatigue | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
GGT increased | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Hepatic failure | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Hepatitis | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Hepatobiliary disease | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Hypersensitivity | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Hyponatremia | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Myocardial infarction | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Pyrexia | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Retinal detachment | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Tachycardia | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Vomiting | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Left ventricular dysfunction | 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Pneumonitis | 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Rash | 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Renal failure | 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.92 |
Abdominal pain | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Alkaline phosphatase increased | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Anal ulcer | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Central serous retinopathy | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Conduction disorder | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Decreased hemoglobin | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Diarrhea | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Electrocardiogram abnormal | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Erythema | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Exertional dyspnea | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Folliculitis | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Hypertriglyceridemia | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Interstitial lung disease | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Klebsiella infection | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Left ventricular dysfunction | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Lip ulceration | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Nail infection | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Nasal ulcer | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Neck pain | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Oral pain | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Pulpitis dental | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Pyrexia | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Rash maculo-papular | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Rash papular | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Skin ulcer | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Toxic skin eruption | 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
AST increased | 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Acne | 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
CPK increased | 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Dermatitis acneiform | 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Fatigue | 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Hypertension | 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Mucosal inflammation | 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Pruritus | 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Rash pustular | 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Rhabdomyolysis | 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Stomatitis | 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Cardiac disorder | 1% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Cellulitis | 1% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Nausea | 1% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Pyrexia | 1% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Transaminases increased | 1% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Diarrhea | 2% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Peripheral edema | 2% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
ALT increased | 3% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Rash | 4% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Rash | 9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Abdominal pain | grade 3, 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Acne | grade 3, 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
CPK increased | grade 3, 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Conduction disorder | grade 3, 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Decreased hemoglobin | grade 3, 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Exertional dyspnea | grade 3, 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Folliculitis | grade 3, 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Hypertriglyceridemia | grade 3, 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Interstitial lung disease | grade 3, 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Klebsiella infection | grade 3, 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Lip ulceration | grade 3, 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Oral pain | grade 3, 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Rash papular | grade 3, 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Rash pustular | grade 3, 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Stomatitis | grade 3, 0.5% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
ALT increased | grade 3, 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Fatigue | grade 3, 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Hypertension | grade 3, 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Mucosal inflammation | grade 3, 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Pruritus | grade 3, 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Rhabdomyolysis | grade 3, 0.9% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
CPK increased | grade 3, 1% | 2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Cellulitis | grade 3, 1% | 2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Dehydration | grade 3, 1% | 2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Dyspnea | grade 3, 1% | 2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Hypoalbuminemia | grade 3, 1% | 2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Infection | grade 3, 1% | 2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Vomiting | grade 3, 1% | 2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Hypertension | grade 3, 13% | 2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
ALT increased | grade 3, 2% | 2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Anemia | grade 3, 2% | 2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Pruritus | grade 3, 2% | 2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Fatigue | grade 3, 4% | 2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Rash | grade 3, 7% Disc. AE |
2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Rash | grade 3, 8% | 2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Dehydration | grade 4, 0.5% | 2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Dyspnea | grade 4, 0.5% | 2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Rash | grade 4, 0.5% | 2 mg 2 times / day multiple, oral Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
unhealthy, median age 54.5 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 54.5 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000MedR.pdf - p.99 |
Acneiform dermatitis | grade 3, 1% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
Nausea | grade 3, 1% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
Peripheral edema | grade 3, 1% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
Vomiting | grade 3, 1% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
Hypertension | grade 3, 12% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
Fatigue | grade 3, 4% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
Skin rash | grade 3, 7.1% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
Alopecia | grade 3, <1% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
Skin rash | grade 4, 0.5% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
Detachment of retinal pigment epithelium | 0.5% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: |
Retinal vein occlusion | 0.6% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: |
Interstitial lung disease | 2.4% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: |
Skin rash | 6% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: |
Cardiomyopathy | 7% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
unhealthy, median age 55 years n = 211 Health Status: unhealthy Condition: melanoma Age Group: median age 55 years Sex: M+F Population Size: 211 Sources: Page: 204114Orig1s000SumR.pdf - p.21 |
Central serous retinopathy | grade 2 DLT |
10 mg 1 times / day multiple, oral Highest studied dose Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 4 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 4 Sources: |
Diarrhoea | grade 3 DLT |
10 mg 1 times / day multiple, oral Highest studied dose Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 4 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 4 Sources: |
Rash | grade 3 DLT |
10 mg 1 times / day multiple, oral Highest studied dose Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 4 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 4 Sources: |
Detachment of retinal pigment epithelium | 28% | 10 mg 1 times / day multiple, oral Highest studied dose Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 4 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 4 Sources: |
Central serous retinopathy | grade 2 DLT |
4 mg 1 times / day multiple, oral Highest studied dose Dose: 4 mg, 1 times / day Route: oral Route: multiple Dose: 4 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 3 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 3 Sources: |
Fatigue | 8.3% Disc. AE |
3 mg 1 times / day multiple, oral MTD Dose: 3 mg, 1 times / day Route: oral Route: multiple Dose: 3 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 12 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 12 Sources: |
Thrombocytopenia | grade 1, 1% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Pruritus | grade 1, 14% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Fissures of skin | grade 1, 16% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Fatigue | grade 1, 19% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Nausea | grade 1, 20% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Peripheral oedema | grade 1, 26% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Constipation | grade 1, 3% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Dry mouth | grade 1, 3% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Left ventricular ejection fraction decreased | grade 1, 3% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Diarrhoea | grade 1, 34% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Mucosal inflammation | grade 1, 4% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Acneiform dermatitis | grade 1, 49% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Periorbital oedema | grade 1, 7% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Vomiting | grade 1, 7% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Decreased appetite | grade 1, 9% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Eye disorders NEC | grade 1, 9% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Constipation | grade 2, 1% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Decreased appetite | grade 2, 1% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Diarrhoea | grade 2, 10% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Fatigue | grade 2, 10% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Peripheral oedema | grade 2, 3% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Acneiform dermatitis | grade 2, 31% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Vomiting | grade 2, 4% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Fissures of skin | grade 2, 6% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Left ventricular ejection fraction decreased | grade 2, 6% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Nausea | grade 2, 6% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Pruritus | grade 2, 6% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Diarrhoea | grade 3, 1% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Eye disorders NEC | grade 3, 1% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Fatigue | grade 3, 1% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Left ventricular ejection fraction decreased | grade 3, 1% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Vomiting | grade 3, 1% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Acneiform dermatitis | grade 3, 4% | 2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 70 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 70 Sources: |
Rash | grade 3 DLT |
2 mg 1 times / day multiple, oral Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: |
unhealthy, median age 58.5 years n = 3 Health Status: unhealthy Condition: advanced solid tumour Age Group: median age 58.5 years Sex: M+F Population Size: 3 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
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OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
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Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes [EC50 2.7 uM] | no (co-administration study) Comment: Based on cross-study comparisons, oral administration of trametinib 2 mg QD with everolimus (sensitive CYP3A4 substrate) 5 mg QD had no clinically important effect on the exposure (AUC and Cmax) of everolimus. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/204114Orig1s000ClinPharmR.pdf#page=8 Page: - |
|||
yes [IC50 0.34 uM] | ||||
yes [IC50 0.94 uM] | ||||
yes [IC50 1.1 uM] | ||||
yes [IC50 1.3 uM] | ||||
yes [IC50 4.1 uM] | ||||
yes [IC50 5 uM] | ||||
yes [IC50 5.5 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. | 2011 Jul |
|
GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition. | 2011 Mar 1 |
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Combination small molecule MEK and PI3K inhibition enhances uveal melanoma cell death in a mutant GNAQ- and GNA11-dependent manner. | 2012 Aug 15 |
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Trametinib (GSK1120212) in the treatment of melanoma. | 2013 Apr |
|
MEK and the inhibitors: from bench to bedside. | 2013 Apr 12 |
Patents
Sample Use Guides
Confirm the presence of BRAF V600E or V600K mutation in tumor specimens prior to initiation of treatment with MEKINIST. The recommended dosage regimens of MEKINIST are 2 mg orally once daily as a single agent or in combination with dabrafenib 150 mg orally twice daily.Take MEKINIST at least 1 hour before or at least 2 hours after a meal.
Route of Administration:
Oral
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4747351/
A375 and SK-MEL-28 untransfected or transfected with Mcl-1 plasmid were treated with 2 nM trametinib for 72 hours. The cell survival was evaluated by sulforhodamine B assay.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 20:39:48 GMT 2023
by
admin
on
Fri Dec 15 20:39:48 GMT 2023
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Record UNII |
33E86K87QN
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Record Status |
Validated (UNII)
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Record Version |
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-
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Code | English | ||
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Common Name | English |
Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C69145
Created by
admin on Fri Dec 15 20:39:48 GMT 2023 , Edited by admin on Fri Dec 15 20:39:48 GMT 2023
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NCI_THESAURUS |
C129825
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FDA ORPHAN DRUG |
376812
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WHO-ATC |
L01XE25
Created by
admin on Fri Dec 15 20:39:48 GMT 2023 , Edited by admin on Fri Dec 15 20:39:48 GMT 2023
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EMA ASSESSMENT REPORTS |
MEKINIST (AUTHORIZED: MELANOMA)
Created by
admin on Fri Dec 15 20:39:48 GMT 2023 , Edited by admin on Fri Dec 15 20:39:48 GMT 2023
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FDA ORPHAN DRUG |
882722
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admin on Fri Dec 15 20:39:48 GMT 2023 , Edited by admin on Fri Dec 15 20:39:48 GMT 2023
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FDA ORPHAN DRUG |
495915
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WHO-VATC |
QL01XE25
Created by
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FDA ORPHAN DRUG |
325410
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admin on Fri Dec 15 20:39:48 GMT 2023 , Edited by admin on Fri Dec 15 20:39:48 GMT 2023
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FDA ORPHAN DRUG |
521616
Created by
admin on Fri Dec 15 20:39:48 GMT 2023 , Edited by admin on Fri Dec 15 20:39:48 GMT 2023
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NDF-RT |
N0000175605
Created by
admin on Fri Dec 15 20:39:48 GMT 2023 , Edited by admin on Fri Dec 15 20:39:48 GMT 2023
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Code System | Code | Type | Description | ||
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75998
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PRIMARY | |||
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TRAMETINIB
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PRIMARY | |||
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33E86K87QN
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PRIMARY | |||
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100000143251
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PRIMARY | |||
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DTXSID901007381
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PRIMARY | |||
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SUB119776
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PRIMARY | |||
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9421
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PRIMARY | |||
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75991
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PRIMARY | |||
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33E86K87QN
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PRIMARY | |||
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11707110
Created by
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PRIMARY | |||
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C77908
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PRIMARY | |||
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Trametinib
Created by
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PRIMARY | |||
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4802
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PRIMARY | |||
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m11718
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PRIMARY | |||
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CHEMBL2103875
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PRIMARY | |||
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DB08911
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PRIMARY | |||
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1425099
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PRIMARY | RxNorm | ||
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XX-79
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PRIMARY | |||
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6495
Created by
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PRIMARY | |||
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871700-17-3
Created by
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PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
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SALT/SOLVATE -> PARENT |
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SALT/SOLVATE -> PARENT | |||
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TARGET -> INHIBITOR | |||
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TARGET -> INHIBITOR |
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE INACTIVE -> PARENT |
AMOUNT ADMINISTERED
PLASMA
|
||
|
METABOLITE -> PARENT |
STUDIED IN TWO PATIENTS NOT DETECTED IN ONE PATIENT
AMOUNT EXCRETED
URINE
|
||
|
METABOLITE -> PARENT |
PLASMA
|
||
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METABOLITE ACTIVE -> PARENT |
TWO PATIENTS STUDIED METABOLITE BELOW LLQ IN ONE PATIENT
MINOR
URINE
|
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|
METABOLITE -> PARENT |
STUDIED IN TWO PATIENTS NOT DETECTED IN ONE PATIENT
AMOUNT EXCRETED
FECAL
|
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|
METABOLITE -> PARENT |
NO QUANTITY LISTED
MINOR
URINE
|
||
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METABOLITE -> PARENT |
FECAL; PLASMA; URINE
|
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METABOLITE ACTIVE -> PARENT |
FECAL; PLASMA; URINE
|
||
|
METABOLITE INACTIVE -> PARENT |
ONLY DETECT IN ONE PATIENT
AMOUNT EXCRETED
URINE
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |