Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C22H24BrFN4O2 |
| Molecular Weight | 475.354 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC2=C(C=C1OCC3CCN(C)CC3)N=CN=C2NC4=CC=C(Br)C=C4F
InChI
InChIKey=UHTHHESEBZOYNR-UHFFFAOYSA-N
InChI=1S/C22H24BrFN4O2/c1-28-7-5-14(6-8-28)12-30-21-11-19-16(10-20(21)29-2)22(26-13-25-19)27-18-4-3-15(23)9-17(18)24/h3-4,9-11,13-14H,5-8,12H2,1-2H3,(H,25,26,27)
| Molecular Formula | C22H24BrFN4O2 |
| Molecular Weight | 475.354 |
| 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
https://www.ncbi.nlm.nih.gov/pubmed/25982012
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/25982012
Vandetanib, 4-anilinoquinazoline, is an anti-cancer drug that with the potential for use in a broad range of tumour types. In 2011 vandetanib (trade name Caprelsa) was approved by the FDA to treat nonresectable, locally advanced, or metastatic medullary thyroid cancer in adult patients. In vitro studies have shown that vandetanib inhibits the tyrosine kinase activity of the EGFR and VEGFR families, RET, BRK, TIE2, and members of the EPH receptor and Src kinase families. These receptor tyrosine kinases are involved in both normal cellular function and pathologic processes such as oncogenesis, metastasis, tumor angiogenesis, and maintenance of the tumor microenvironment. Vandetanib was shown to inhibit epidermal growth factor (EGF)-stimulated receptor tyrosine kinase phosphorylation in tumor cells and endothelial cells and VEGF-stimulated tyrosine kinase phosphorylation in endothelial cells. Vandetanib administration reduced tumor cell-induced angiogenesis, tumor vessel permeability, and inhibited tumor growth and metastasis in mouse models of cancer.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: P00533|||Q9GZX1 Gene ID: 1956.0 Gene Symbol: EGFR Target Organism: Homo sapiens (Human) |
0.5 µM [IC50] | ||
Target ID: P35968 Gene ID: 3791.0 Gene Symbol: KDR Target Organism: Homo sapiens (Human) |
0.04 µM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | CAPRELSA Approved UseIndicated for the treatment of symptomatic or progressive medullary thyroid cancer in patients with unresectable locally advanced or metastatic disease. Use CAPRELSA in patients with indolent, asymptomatic or slowly progressing disease only after careful consideration of the treatment related
risks of CAPRELSA. Launch Date2011 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2024 ng/mL |
300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VANDETANIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
130 ng/mL |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
VANDETANIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
38611 ng × h/mL |
300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VANDETANIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
22030 ng × h/mL |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
VANDETANIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
7.6 day |
300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VANDETANIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
204 h |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
VANDETANIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
6% |
300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VANDETANIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
1200 mg 1 times / day single, oral Highest studied dose Dose: 1200 mg, 1 times / day Route: oral Route: single Dose: 1200 mg, 1 times / day Sources: |
healthy, mean age 34.4 years n = 5 Health Status: healthy Age Group: mean age 34.4 years Sex: M Population Size: 5 Sources: |
Other AEs: Rash, Blood pressure systolic increased... Other AEs: Rash Sources: Blood pressure systolic increased Blood pressure diastolic increased |
300 mg 1 times / day single, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: single Dose: 300 mg, 1 times / day Sources: |
healthy, mean age 34.4 years n = 6 Health Status: healthy Age Group: mean age 34.4 years Sex: M Population Size: 6 Sources: |
Disc. AE: Vomiting... AEs leading to discontinuation/dose reduction: Vomiting (grade 2) Sources: |
400 mg 1 times / day single, oral Dose: 400 mg, 1 times / day Route: oral Route: single Dose: 400 mg, 1 times / day Sources: |
healthy, mean age 34.4 years n = 6 Health Status: healthy Age Group: mean age 34.4 years Sex: M Population Size: 6 Sources: |
Disc. AE: Eczema... AEs leading to discontinuation/dose reduction: Eczema (grade 1) Sources: |
800 mg 1 times / day single, oral Dose: 800 mg, 1 times / day Route: oral Route: single Dose: 800 mg, 1 times / day Sources: |
healthy, mean age 34.4 years n = 6 Health Status: healthy Age Group: mean age 34.4 years Sex: M Population Size: 6 Sources: |
Disc. AE: Folliculitis... AEs leading to discontinuation/dose reduction: Folliculitis (grade 2) Sources: |
200 mg 1 times / day multiple, oral Recommended|MTD Dose: 200 mg, 1 times / day Route: oral Route: multiple Dose: 200 mg, 1 times / day Sources: |
unhealthy, mean age 45.6 years n = 8 Health Status: unhealthy Condition: cancer Age Group: mean age 45.6 years Sex: M+F Population Size: 8 Sources: |
DLT: Hypophosphatemia, Diarrhea... Dose limiting toxicities: Hypophosphatemia (grade 3, 12.5%) Sources: Diarrhea (grade 2, 12.5%) |
600 mg 1 times / day multiple, oral Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: |
unhealthy, mean age 50.6 years n = 8 Health Status: unhealthy Condition: cancer Age Group: mean age 50.6 years Sex: M+F Population Size: 8 Sources: |
DLT: Intestinal obstruction, Diarrhea... Dose limiting toxicities: Intestinal obstruction (grade 3, 12.5%) Sources: Diarrhea (grade 3, 25%) Colitis (grade 3, 12.5%) Hypertension (grade 3, 12.5%) Fatigue (grade 3, 12.5%) Thrombocytopenia (grade 3, 12.5%) |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
Disc. AE: Skin disorder, Asthenia... Other AEs: Rash, Acneiform dermatitis... AEs leading to discontinuation/dose reduction: Skin disorder (2.5%) Other AEs:Asthenia (1.7%) Fatigue (0.9%) Pyrexia (0.9%) Diarrhea (0.9%) Creatinine increased (0.9%) Electrocardiogram QTc interval prolonged (0.9%) Hypertension (0.9%) General physical health deterioration (0.4%) Dysphagia (0.4%) Nausea (0.4%) Pancreatitis (0.4%) Peritonitis (0.4%) Small intestinal perforation (0.4%) Vomiting (0.4%) Systolic dysfunction (0.4%) Chylothorax (0.4%) Cough (0.4%) Dysphonia (0.4%) Dyspnea (0.4%) Pneumonitis (0.4%) Peripheral ischemia (0.4%) Peripheral sensorimotor neuropathy (0.4%) Vision blurred (0.4%) Arthralgia (0.4%) Germ cell cancer (0.4%) Rash (grade 3, 3.9%) Sources: Page: 022405Orig1s000MedR.pdf - p.71Acneiform dermatitis (grade 3, 0.9%) Photosensitivity reaction (grade 3, 1.7%) Generalized erythema (grade 3, 1.3%) Skin exfoliation (grade 3, 0.4%) Palmar-plantar erythrodysaesth. (grade 3, 0.4%) Dermatitis bullous (grade 3, 0.4%) Skin candida (grade 3, 0.4%) Erysipelas (grade 3, 0.4%) Pneumonitis (grade 3, 0.4%) Dyspnea (grade 3, 1.7%) Respiratory failure (grade 3, 0.8%) Diarrhea (grade 3, 3%) Nausea (grade 3, 1%) Hypertension (grade 3, 6%) Headache (grade 3, 1%) Fatigue (grade 3, 6%) Decreased appetite (grade 3, 4%) Dermatitis acneiform (grade 3, <1%) Vomiting (grade 3, 1%) Asthenia (grade 3, 3%) Abdominal pain (grade 3, 2%) QT interval prolonged (grade 3, 8%) Photosensitivity reaction (grade 3, 2%) Hypocalcaemia (grade 3, 2%) Pruritus (grade 3, 1%) Weight decreased (grade 3, 1%) Depression (grade 3, 2%) ALT increased (grade 3, 2%) Calcium decreased (grade 3, 6%) Calcium increased (grade 3, 9%) Glucose increased (grade 3, 2%) Magnesium decreased (grade 3, <1%) Potassium decreased (grade 3, <1%) Potassium increased (grade 3, <1%) Hemoglobin decreased (grade 3, <1%) Neutrophil count decreased (grade 3, <1%) WBC decreased (grade 3, <1%) |
500 mg 1 times / day multiple, oral Dose: 500 mg, 1 times / day Route: oral Route: multiple Dose: 500 mg, 1 times / day Sources: |
unhealthy, mean age 51.6 years n = 8 Health Status: unhealthy Condition: cancer Age Group: mean age 51.6 years Sex: M+F Population Size: 8 Sources: |
DLT: Diarrhea, Folliculitis... Disc. AE: Folliculitis... Dose limiting toxicities: Diarrhea (grade 2, 12.5%) AEs leading toFolliculitis (grade 2, 12.5%) ALT increased (grade 3, 12.5%) Rash (grade 3, 12.5%) discontinuation/dose reduction: Folliculitis (grade 3, 12.5%) Sources: |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, mean age 57.7 years n = 25 Health Status: unhealthy Condition: cancer Age Group: mean age 57.7 years Sex: M+F Population Size: 25 Sources: |
DLT: Rash... Disc. AE: Congestive cardiac failure... Dose limiting toxicities: Rash (grade 2, 4%) AEs leading todiscontinuation/dose reduction: Congestive cardiac failure (grade 3, 4%) Sources: |
100 mg 1 times / day multiple, oral Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, median age 50 years n = 3 Health Status: unhealthy Condition: solid tumors Age Group: median age 50 years Sex: M+F Population Size: 3 Sources: |
Other AEs: Lymphopenia... |
200 mg 1 times / day multiple, oral Recommended|MTD Dose: 200 mg, 1 times / day Route: oral Route: multiple Dose: 200 mg, 1 times / day Sources: |
unhealthy, median age 52.5 years n = 6 Health Status: unhealthy Condition: solid tumors Age Group: median age 52.5 years Sex: M+F Population Size: 6 Sources: |
DLT: Hypertension... Other AEs: Fatigue... Dose limiting toxicities: Hypertension (grade 3, 33.3%) Other AEs:Fatigue (grade 3, 16.7%) Sources: |
400 mg 1 times / day multiple, oral Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: |
unhealthy, median age 53 years n = 3 Health Status: unhealthy Condition: solid tumors Age Group: median age 53 years Sex: M+F Population Size: 3 Sources: |
DLT: Hypertension, Alanine aminotransferase increased... Dose limiting toxicities: Hypertension (grade 3, 33.3%) Sources: Alanine aminotransferase increased (grade 3, 33.3%) |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, median age 55.5 years n = 6 Health Status: unhealthy Condition: solid tumors Age Group: median age 55.5 years Sex: M+F Population Size: 6 Sources: |
DLT: Hypertension, Diarrhea... Dose limiting toxicities: Hypertension (grade 3, 33.3%) Sources: Diarrhea (grade 3, 33.3%) Headache (grade 3, 33.3%) Toxic skin eruption (grade 2, 33.3%) |
300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
Disc. AE: Rash, Dyspnea... Other AEs: Diarrhea, Diarrhea... AEs leading to discontinuation/dose reduction: Rash (1.3%) Other AEs:Dyspnea (1%) Pneumonia (1.1%) Diarrhea (50%) Sources: Diarrhea (grade 3-4, 5%) Rash (28%) Rash (grade 3-4, 3%) Nausea (23%) Nausea (grade 3-4, 1%) Anorexia (20%) Anorexia (grade 3-4, 2%) Fatigue (20%) Fatigue (grade 3-4, 4%) Dyspnea (15%) Dyspnea (grade 3-4, 4%) Cough (13%) Cough (grade 3-4, 0.8%) Dermatitis acneiform (12%) Dermatitis acneiform (grade 3-4, 0.6%) Vomiting (14%) Vomiting (grade 3-4, 2%) Constipation (9%) Dry skin (10%) Dry skin (grade 3-4, 0.3%) Hypertension (16%) Hypertension (grade 3-4, 4%) Pruritus (6%) Pruritus (grade 3-4, 0.5%) |
300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
Other AEs: QT interval prolonged, Torsades de pointes... Other AEs: QT interval prolonged (5.1%) Sources: Torsades de pointes (0.2%) Sudden death (grade 5, 0.2%) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Blood pressure diastolic increased | 1200 mg 1 times / day single, oral Highest studied dose Dose: 1200 mg, 1 times / day Route: oral Route: single Dose: 1200 mg, 1 times / day Sources: |
healthy, mean age 34.4 years n = 5 Health Status: healthy Age Group: mean age 34.4 years Sex: M Population Size: 5 Sources: |
|
| Blood pressure systolic increased | 1200 mg 1 times / day single, oral Highest studied dose Dose: 1200 mg, 1 times / day Route: oral Route: single Dose: 1200 mg, 1 times / day Sources: |
healthy, mean age 34.4 years n = 5 Health Status: healthy Age Group: mean age 34.4 years Sex: M Population Size: 5 Sources: |
|
| Rash | 1200 mg 1 times / day single, oral Highest studied dose Dose: 1200 mg, 1 times / day Route: oral Route: single Dose: 1200 mg, 1 times / day Sources: |
healthy, mean age 34.4 years n = 5 Health Status: healthy Age Group: mean age 34.4 years Sex: M Population Size: 5 Sources: |
|
| Vomiting | grade 2 Disc. AE |
300 mg 1 times / day single, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: single Dose: 300 mg, 1 times / day Sources: |
healthy, mean age 34.4 years n = 6 Health Status: healthy Age Group: mean age 34.4 years Sex: M Population Size: 6 Sources: |
| Eczema | grade 1 Disc. AE |
400 mg 1 times / day single, oral Dose: 400 mg, 1 times / day Route: oral Route: single Dose: 400 mg, 1 times / day Sources: |
healthy, mean age 34.4 years n = 6 Health Status: healthy Age Group: mean age 34.4 years Sex: M Population Size: 6 Sources: |
| Folliculitis | grade 2 Disc. AE |
800 mg 1 times / day single, oral Dose: 800 mg, 1 times / day Route: oral Route: single Dose: 800 mg, 1 times / day Sources: |
healthy, mean age 34.4 years n = 6 Health Status: healthy Age Group: mean age 34.4 years Sex: M Population Size: 6 Sources: |
| Diarrhea | grade 2, 12.5% DLT |
200 mg 1 times / day multiple, oral Recommended|MTD Dose: 200 mg, 1 times / day Route: oral Route: multiple Dose: 200 mg, 1 times / day Sources: |
unhealthy, mean age 45.6 years n = 8 Health Status: unhealthy Condition: cancer Age Group: mean age 45.6 years Sex: M+F Population Size: 8 Sources: |
| Hypophosphatemia | grade 3, 12.5% DLT |
200 mg 1 times / day multiple, oral Recommended|MTD Dose: 200 mg, 1 times / day Route: oral Route: multiple Dose: 200 mg, 1 times / day Sources: |
unhealthy, mean age 45.6 years n = 8 Health Status: unhealthy Condition: cancer Age Group: mean age 45.6 years Sex: M+F Population Size: 8 Sources: |
| Colitis | grade 3, 12.5% DLT |
600 mg 1 times / day multiple, oral Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: |
unhealthy, mean age 50.6 years n = 8 Health Status: unhealthy Condition: cancer Age Group: mean age 50.6 years Sex: M+F Population Size: 8 Sources: |
| Fatigue | grade 3, 12.5% DLT |
600 mg 1 times / day multiple, oral Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: |
unhealthy, mean age 50.6 years n = 8 Health Status: unhealthy Condition: cancer Age Group: mean age 50.6 years Sex: M+F Population Size: 8 Sources: |
| Hypertension | grade 3, 12.5% DLT |
600 mg 1 times / day multiple, oral Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: |
unhealthy, mean age 50.6 years n = 8 Health Status: unhealthy Condition: cancer Age Group: mean age 50.6 years Sex: M+F Population Size: 8 Sources: |
| Intestinal obstruction | grade 3, 12.5% DLT |
600 mg 1 times / day multiple, oral Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: |
unhealthy, mean age 50.6 years n = 8 Health Status: unhealthy Condition: cancer Age Group: mean age 50.6 years Sex: M+F Population Size: 8 Sources: |
| Thrombocytopenia | grade 3, 12.5% DLT |
600 mg 1 times / day multiple, oral Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: |
unhealthy, mean age 50.6 years n = 8 Health Status: unhealthy Condition: cancer Age Group: mean age 50.6 years Sex: M+F Population Size: 8 Sources: |
| Diarrhea | grade 3, 25% DLT |
600 mg 1 times / day multiple, oral Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: |
unhealthy, mean age 50.6 years n = 8 Health Status: unhealthy Condition: cancer Age Group: mean age 50.6 years Sex: M+F Population Size: 8 Sources: |
| Arthralgia | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Chylothorax | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Cough | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Dysphagia | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Dysphonia | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Dyspnea | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| General physical health deterioration | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Germ cell cancer | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Nausea | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Pancreatitis | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Peripheral ischemia | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Peripheral sensorimotor neuropathy | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Peritonitis | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Pneumonitis | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Small intestinal perforation | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Systolic dysfunction | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Vision blurred | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Vomiting | 0.4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Creatinine increased | 0.9% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Diarrhea | 0.9% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Electrocardiogram QTc interval prolonged | 0.9% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Fatigue | 0.9% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Hypertension | 0.9% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Pyrexia | 0.9% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Asthenia | 1.7% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Skin disorder | 2.5% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Dermatitis bullous | grade 3, 0.4% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Erysipelas | grade 3, 0.4% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Palmar-plantar erythrodysaesth. | grade 3, 0.4% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Pneumonitis | grade 3, 0.4% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Skin candida | grade 3, 0.4% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Skin exfoliation | grade 3, 0.4% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Respiratory failure | grade 3, 0.8% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Acneiform dermatitis | grade 3, 0.9% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Headache | grade 3, 1% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Nausea | grade 3, 1% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Pruritus | grade 3, 1% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Vomiting | grade 3, 1% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Weight decreased | grade 3, 1% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Generalized erythema | grade 3, 1.3% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Dyspnea | grade 3, 1.7% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Photosensitivity reaction | grade 3, 1.7% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| ALT increased | grade 3, 2% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Abdominal pain | grade 3, 2% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Depression | grade 3, 2% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Glucose increased | grade 3, 2% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Hypocalcaemia | grade 3, 2% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Photosensitivity reaction | grade 3, 2% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Asthenia | grade 3, 3% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Diarrhea | grade 3, 3% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Rash | grade 3, 3.9% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Decreased appetite | grade 3, 4% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Calcium decreased | grade 3, 6% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Fatigue | grade 3, 6% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Hypertension | grade 3, 6% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| QT interval prolonged | grade 3, 8% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Calcium increased | grade 3, 9% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Dermatitis acneiform | grade 3, <1% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Hemoglobin decreased | grade 3, <1% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Magnesium decreased | grade 3, <1% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Neutrophil count decreased | grade 3, <1% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Potassium decreased | grade 3, <1% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Potassium increased | grade 3, <1% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| WBC decreased | grade 3, <1% | 300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
unhealthy, mean age 50.7 years n = 231 Health Status: unhealthy Condition: medullary thyroid cancer Age Group: mean age 50.7 years Sex: M+F Population Size: 231 Sources: Page: 022405Orig1s000MedR.pdf - p.71 |
| Diarrhea | grade 2, 12.5% DLT |
500 mg 1 times / day multiple, oral Dose: 500 mg, 1 times / day Route: oral Route: multiple Dose: 500 mg, 1 times / day Sources: |
unhealthy, mean age 51.6 years n = 8 Health Status: unhealthy Condition: cancer Age Group: mean age 51.6 years Sex: M+F Population Size: 8 Sources: |
| Folliculitis | grade 2, 12.5% DLT |
500 mg 1 times / day multiple, oral Dose: 500 mg, 1 times / day Route: oral Route: multiple Dose: 500 mg, 1 times / day Sources: |
unhealthy, mean age 51.6 years n = 8 Health Status: unhealthy Condition: cancer Age Group: mean age 51.6 years Sex: M+F Population Size: 8 Sources: |
| ALT increased | grade 3, 12.5% DLT |
500 mg 1 times / day multiple, oral Dose: 500 mg, 1 times / day Route: oral Route: multiple Dose: 500 mg, 1 times / day Sources: |
unhealthy, mean age 51.6 years n = 8 Health Status: unhealthy Condition: cancer Age Group: mean age 51.6 years Sex: M+F Population Size: 8 Sources: |
| Rash | grade 3, 12.5% DLT |
500 mg 1 times / day multiple, oral Dose: 500 mg, 1 times / day Route: oral Route: multiple Dose: 500 mg, 1 times / day Sources: |
unhealthy, mean age 51.6 years n = 8 Health Status: unhealthy Condition: cancer Age Group: mean age 51.6 years Sex: M+F Population Size: 8 Sources: |
| Folliculitis | grade 3, 12.5% Disc. AE |
500 mg 1 times / day multiple, oral Dose: 500 mg, 1 times / day Route: oral Route: multiple Dose: 500 mg, 1 times / day Sources: |
unhealthy, mean age 51.6 years n = 8 Health Status: unhealthy Condition: cancer Age Group: mean age 51.6 years Sex: M+F Population Size: 8 Sources: |
| Rash | grade 2, 4% DLT |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, mean age 57.7 years n = 25 Health Status: unhealthy Condition: cancer Age Group: mean age 57.7 years Sex: M+F Population Size: 25 Sources: |
| Congestive cardiac failure | grade 3, 4% Disc. AE |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, mean age 57.7 years n = 25 Health Status: unhealthy Condition: cancer Age Group: mean age 57.7 years Sex: M+F Population Size: 25 Sources: |
| Lymphopenia | grade 3, 33.3% | 100 mg 1 times / day multiple, oral Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, median age 50 years n = 3 Health Status: unhealthy Condition: solid tumors Age Group: median age 50 years Sex: M+F Population Size: 3 Sources: |
| Fatigue | grade 3, 16.7% | 200 mg 1 times / day multiple, oral Recommended|MTD Dose: 200 mg, 1 times / day Route: oral Route: multiple Dose: 200 mg, 1 times / day Sources: |
unhealthy, median age 52.5 years n = 6 Health Status: unhealthy Condition: solid tumors Age Group: median age 52.5 years Sex: M+F Population Size: 6 Sources: |
| Hypertension | grade 3, 33.3% DLT |
200 mg 1 times / day multiple, oral Recommended|MTD Dose: 200 mg, 1 times / day Route: oral Route: multiple Dose: 200 mg, 1 times / day Sources: |
unhealthy, median age 52.5 years n = 6 Health Status: unhealthy Condition: solid tumors Age Group: median age 52.5 years Sex: M+F Population Size: 6 Sources: |
| Alanine aminotransferase increased | grade 3, 33.3% DLT |
400 mg 1 times / day multiple, oral Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: |
unhealthy, median age 53 years n = 3 Health Status: unhealthy Condition: solid tumors Age Group: median age 53 years Sex: M+F Population Size: 3 Sources: |
| Hypertension | grade 3, 33.3% DLT |
400 mg 1 times / day multiple, oral Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: |
unhealthy, median age 53 years n = 3 Health Status: unhealthy Condition: solid tumors Age Group: median age 53 years Sex: M+F Population Size: 3 Sources: |
| Toxic skin eruption | grade 2, 33.3% DLT |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, median age 55.5 years n = 6 Health Status: unhealthy Condition: solid tumors Age Group: median age 55.5 years Sex: M+F Population Size: 6 Sources: |
| Diarrhea | grade 3, 33.3% DLT |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, median age 55.5 years n = 6 Health Status: unhealthy Condition: solid tumors Age Group: median age 55.5 years Sex: M+F Population Size: 6 Sources: |
| Headache | grade 3, 33.3% DLT |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, median age 55.5 years n = 6 Health Status: unhealthy Condition: solid tumors Age Group: median age 55.5 years Sex: M+F Population Size: 6 Sources: |
| Hypertension | grade 3, 33.3% DLT |
300 mg 1 times / day multiple, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, median age 55.5 years n = 6 Health Status: unhealthy Condition: solid tumors Age Group: median age 55.5 years Sex: M+F Population Size: 6 Sources: |
| Dyspnea | 1% Disc. AE |
300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Pneumonia | 1.1% Disc. AE |
300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Rash | 1.3% Disc. AE |
300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Dry skin | 10% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Dermatitis acneiform | 12% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Cough | 13% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Vomiting | 14% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Dyspnea | 15% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Hypertension | 16% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Anorexia | 20% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Fatigue | 20% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Nausea | 23% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Rash | 28% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Diarrhea | 50% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Pruritus | 6% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Constipation | 9% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Dry skin | grade 3-4, 0.3% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Pruritus | grade 3-4, 0.5% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Dermatitis acneiform | grade 3-4, 0.6% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Cough | grade 3-4, 0.8% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Nausea | grade 3-4, 1% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Anorexia | grade 3-4, 2% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Vomiting | grade 3-4, 2% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Rash | grade 3-4, 3% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Dyspnea | grade 3-4, 4% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Fatigue | grade 3-4, 4% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Hypertension | grade 3-4, 4% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Diarrhea | grade 3-4, 5% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Torsades de pointes | 0.2% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| QT interval prolonged | 5.1% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
| Sudden death | grade 5, 0.2% | 300 mg/day 1 times / day multiple, oral Recommended Dose: 300 mg/day, 1 times / day Route: oral Route: multiple Dose: 300 mg/day, 1 times / day Sources: |
unhealthy, median age 61 years n = 623 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 61 years Sex: M+F Population Size: 623 Sources: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| weak [IC50 52 uM] | ||||
| weak | unlikely Comment: less than 40% effect at 2uM in vitro |
|||
| weak | unlikely Comment: less than 40% effect at 2uM in vitro |
|||
| weak | unlikely Comment: less than 40% effect at 2uM in vitro |
|||
| yes [IC50 18.3 uM] | ||||
| yes [IC50 5.5 uM] |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| minor | ||||
| minor | ||||
| minor | ||||
| minor | ||||
| minor | ||||
| no | ||||
| no | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | yes (co-administration study) Comment: Itraconazole does not increased exposure to vandetanib; rifampicin reduced exposure to vandetanib by 48% but increased exposure to the active N-desmethyl metabolite |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors. | 2002 Mar 14 |
|
| Antitumor effects of ZD6474, a small molecule vascular endothelial growth factor receptor tyrosine kinase inhibitor, with additional activity against epidermal growth factor receptor tyrosine kinase. | 2003 Apr |
|
| [Anti angiogenesis]. | 2004 Apr |
|
| Anticancer effects of ZD6474, a VEGF receptor tyrosine kinase inhibitor, in gefitinib ("Iressa")-sensitive and resistant xenograft models. | 2004 Dec |
|
| ZD6474, a potent inhibitor of vascular endothelial growth factor signaling, combined with radiotherapy: schedule-dependent enhancement of antitumor activity. | 2004 Dec 15 |
|
| Small in-frame deletion in the epidermal growth factor receptor as a target for ZD6474. | 2004 Dec 15 |
|
| Hormonal regulation and functional role of vascular endothelial growth factor a in the rat testis. | 2004 Feb |
|
| Efficacy of combined antiangiogenic and vascular disrupting agents in treatment of solid tumors. | 2004 Nov 15 |
|
| The tyrosine kinase inhibitor ZD6474 inhibits tumour growth in an intracerebral rat glioma model. | 2004 Sep 13 |
|
| ZD6474 headed for phase III trials in the fall. | 2005 Aug |
|
| Gateways to clinical trials. | 2005 Dec |
|
| ZD6474--clinical experience to date. | 2005 Jun |
|
| Gateways to clinical trials. | 2005 Mar |
|
| Sequence-dependent antiproliferative effects of cytotoxic drugs and epidermal growth factor receptor inhibitors. | 2005 May |
|
| Molecule-kinase interaction map. | 2005 Nov |
|
| Update on angiogenesis inhibitors. | 2005 Nov |
|
| Phase II data with ZD6474, a small-molecule kinase inhibitor of epidermal growth factor receptor and vascular endothelial growth factor receptor, in previously treated advanced non-small-cell lung cancer. | 2005 Sep |
|
| Anti-tumor activity of the combination of cetuximab, an anti-EGFR blocking monoclonal antibody and ZD6474, an inhibitor of VEGFR and EGFR tyrosine kinases. | 2006 Aug |
|
| Tissue distribution and metabolism of the tyrosine kinase inhibitor ZD6474 (Zactima) in tumor-bearing nude mice following oral dosing. | 2006 Aug |
|
| Toxicities of antiangiogenic therapy in non-small-cell lung cancer. | 2006 Dec |
|
| ZD6474, an inhibitor of VEGFR and EGFR tyrosine kinase activity in combination with radiotherapy. | 2006 Jan 1 |
|
| Gateways to clinical trials. | 2006 Mar |
|
| Antiangiogenic drugs in non-small cell lung cancer treatment. | 2006 Mar |
|
| Gateways to clinical trials. | 2006 Nov |
|
| Targeting the EGF/VEGF-R system by tyrosine-kinase inhibitors--a novel antiproliferative/antiangiogenic strategy in thyroid cancer. | 2006 Nov |
|
| Gateways to clinical trials. | 2006 Sep |
|
| American Society of Clinical Oncology--43rd annual meeting. Research into therapeutics: Part 3. | 2007 Aug |
|
| Micronodular transformation as a novel mechanism of VEGF-A-induced metastasis. | 2007 Aug 23 |
|
| Role of anti-angiogenesis agents in treating NSCLC: focus on bevacizumab and VEGFR tyrosine kinase inhibitors. | 2007 Feb |
|
| Rationale and clinical results of multi-target treatments in oncology. | 2007 Jan-Mar |
|
| Pharmacology of epidermal growth factor inhibitors. | 2007 Jan-Mar |
|
| A transplantable human medullary thyroid carcinoma as a model for RET tyrosine kinase-driven tumorigenesis. | 2007 Jun |
|
| Drug insight: VEGF as a therapeutic target for breast cancer. | 2007 Mar |
|
| 1H-1,2,4-triazol-3-yl-anilines: novel potent inhibitors of vascular endothelial growth factor receptors 1 and 2. | 2007 May |
|
| Induction of cell cycle arrest and apoptosis in human nasopharyngeal carcinoma cells by ZD6474, an inhibitor of VEGFR tyrosine kinase with additional activity against EGFR tyrosine kinase. | 2007 Nov 1 |
Sample Use Guides
300 mg once daily may be taken with or without food. Dosage reduction may be necessary in the event of severe toxicities or QTc interval prolongation. The starting dose is 200 mg in patients with moderate to severe renal impairment.
Route of Administration:
Oral
Used in in vitro co-culture tubule formation model consisting of HUVECs and human fibroblasts vandetanib potently inhibited each of the tubule growth parameters measured (number of branch points [IC50 = 33.23 nM], total vessel length [IC50 = 60.97 nM], tubule area [IC50 = 92.70 nM]), at potencies consistent with the potency of vandetanib for inhibition of VEGF-stimulated proliferation of HUVECs.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:02:00 GMT 2023
by
admin
on
Fri Dec 15 16:02:00 GMT 2023
|
| Record UNII |
YO460OQ37K
|
| Record Status |
Validated (UNII)
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| Record Version |
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-
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| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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EMA ASSESSMENT REPORTS |
CAPRELSA (AUTHORIZED: THYROID NEOPLASMS)
Created by
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LIVERTOX |
NBK548169
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NDF-RT |
N0000175605
Created by
admin on Fri Dec 15 16:02:00 GMT 2023 , Edited by admin on Fri Dec 15 16:02:00 GMT 2023
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NCI_THESAURUS |
C1742
Created by
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NCI_THESAURUS |
C2167
Created by
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EU-Orphan Drug |
EU/3/05/344
Created by
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WHO-ATC |
L01XE12
Created by
admin on Fri Dec 15 16:02:00 GMT 2023 , Edited by admin on Fri Dec 15 16:02:00 GMT 2023
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NCI_THESAURUS |
C93259
Created by
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FDA ORPHAN DRUG |
211005
Created by
admin on Fri Dec 15 16:02:00 GMT 2023 , Edited by admin on Fri Dec 15 16:02:00 GMT 2023
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WHO-VATC |
QL01XE12
Created by
admin on Fri Dec 15 16:02:00 GMT 2023 , Edited by admin on Fri Dec 15 16:02:00 GMT 2023
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| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
5717
Created by
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PRIMARY | |||
|
N0000185503
Created by
admin on Fri Dec 15 16:02:00 GMT 2023 , Edited by admin on Fri Dec 15 16:02:00 GMT 2023
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PRIMARY | P-Glycoprotein Inhibitors [MoA] | ||
|
SUB29174
Created by
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PRIMARY | |||
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CHEMBL24828
Created by
admin on Fri Dec 15 16:02:00 GMT 2023 , Edited by admin on Fri Dec 15 16:02:00 GMT 2023
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PRIMARY | |||
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744325
Created by
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PRIMARY | |||
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SS-07
Created by
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PRIMARY | |||
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4178
Created by
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PRIMARY | |||
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N0000187061
Created by
admin on Fri Dec 15 16:02:00 GMT 2023 , Edited by admin on Fri Dec 15 16:02:00 GMT 2023
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PRIMARY | Organic Cation Transporter 2 Inhibitors [MoA] | ||
|
C2737
Created by
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PRIMARY | |||
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443913-73-3
Created by
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PRIMARY | |||
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8198
Created by
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PRIMARY | |||
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YO460OQ37K
Created by
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PRIMARY | |||
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Vandetanib
Created by
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PRIMARY | |||
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760766
Created by
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PRIMARY | |||
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8365
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PRIMARY | |||
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DTXSID1046681
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PRIMARY | |||
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m11387
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PRIMARY | Merck Index | ||
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Vandetanib
Created by
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PRIMARY | |||
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DB05294
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PRIMARY | |||
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3081361
Created by
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PRIMARY | |||
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100000090715
Created by
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PRIMARY | |||
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49960
Created by
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PRIMARY | |||
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YO460OQ37K
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PRIMARY | |||
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1098413
Created by
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PRIMARY | RxNorm | ||
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C452423
Created by
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PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
TARGET -> INHIBITOR | |||
|
TRANSPORTER -> SUBSTRATE | |||
|
METABOLIC ENZYME -> SUBSTRATE | |||
|
METABOLIC ENZYME -> SUBSTRATE | |||
|
TRANSPORTER -> INHIBITOR | |||
|
TARGET -> INHIBITOR | |||
|
TARGET -> INHIBITOR | |||
|
TARGET -> INHIBITOR |
IC50
|
||
|
TARGET -> INHIBITOR RESISTANT |
IC50
|
||
|
EXCRETED UNCHANGED |
Within a 21-day collection period after a single dose of 14C-vandetanib, approximately 69% was recovered with 44% in feces and 25% in urine.
FECAL
|
||
|
TRANSPORTER -> INHIBITOR |
|
||
|
EXCRETED UNCHANGED |
Within a 21-day collection period after a single dose of 14C-vandetanib, approximately 69% was recovered with 44% in feces and 25% in urine.
URINE
|
||
|
BINDER->LIGAND |
BINDING
|
||
|
TARGET -> INHIBITOR | |||
|
METABOLIC ENZYME -> SUBSTRATE | |||
|
TARGET -> INHIBITOR RESISTANT |
IC50
|
||
|
TARGET -> INHIBITOR |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
METABOLITE INACTIVE -> PARENT |
FECAL; PLASMA; URINE
|
||
|
|
METABOLITE ACTIVE -> PARENT |
MAJOR
FECAL; PLASMA; URINE
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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ACTIVE MOIETY |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Volume of Distribution | PHARMACOKINETIC |
|
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| Tmax | PHARMACOKINETIC |
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| Biological Half-life | PHARMACOKINETIC |
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