Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C53H83NO14 |
| Molecular Weight | 958.2244 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 15 / 15 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CC[C@@H](C)[C@@](O)(O1)C(=O)C(=O)N3CCCC[C@H]3C(=O)O[C@@H](CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)\[C@H](C2)OC)[C@H](C)C[C@@H]4CC[C@@H](OCCO)[C@@H](C4)OC
InChI
InChIKey=HKVAMNSJSFKALM-GKUWKFKPSA-N
InChI=1S/C53H83NO14/c1-32-16-12-11-13-17-33(2)44(63-8)30-40-21-19-38(7)53(62,68-40)50(59)51(60)54-23-15-14-18-41(54)52(61)67-45(35(4)28-39-20-22-43(66-25-24-55)46(29-39)64-9)31-42(56)34(3)27-37(6)48(58)49(65-10)47(57)36(5)26-32/h11-13,16-17,27,32,34-36,38-41,43-46,48-49,55,58,62H,14-15,18-26,28-31H2,1-10H3/b13-11+,16-12+,33-17+,37-27+/t32-,34-,35-,36-,38-,39+,40+,41+,43-,44+,45+,46-,48-,49+,53-/m1/s1
DescriptionSources: http://www.drugbank.ca/drugs/DB01590Curator's Comment: Description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022334s036lbl.pdf
Sources: http://www.drugbank.ca/drugs/DB01590
Curator's Comment: Description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022334s036lbl.pdf
Everolimus is a derivative of Rapamycin (sirolimus), it is a mTOR inhibitor that binds with high affinity to the FK506 binding protein-12 (FKBP-12), thereby forming a drug complex that inhibits the activation of mTOR. This inhibition reduces the activity of effectors downstream, which leads to a blockage in the progression of cells from G1 into S phase, and subsequently inducing cell growth arrest and apoptosis. Everolimus also inhibits the expression of hypoxia-inducible factor, leading to a decrease in the expression of vascular endothelial growth factor. The result of everolimus inhibition of mTOR is a reduction in cell proliferation, angiogenesis, and glucose uptake. Everolimus is indicated for the treatment of postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer (advanced HR+ BC) in combination with exemestane, after failure of treatment with letrozole or anastrozole. Indicated for the treatment of adult patients with progressive neuroendocrine tumors of pancreatic origin (PNET) with unresectable, locally advanced or metastatic disease. Indicated for the treatment of adult patients with advanced renal cell carcinoma (RCC) after failure of treatment with sunitinib or sorafenib. Indicated for the treatment of adult patients with renal angiomyolipoma and tuberous sclerosis complex (TSC), not requiring immediate surgery. Indicated in pediatric and adult patients with tuberous sclerosis complex (TSC) for the treatment of subependymal giant cell astrocytoma (SEGA) that requires therapeutic intervention but cannot be curatively resected. Everolimus is marketed by Novartis under the tradenames Zortress (USA) and Certican (Europe and other countries) in transplantation medicine, and as Afinitor (general tumours) and Votubia (tumours as a result of TSC) in oncology. Everolimus is also available from Biocon, with the brand name Evertor, from Natco Pharma, with the brand name Temonat, from Ranbaxy Laboratories, with the brand name of Imozide, from Emcure Pharmaceuticals, with the brand name of Temcure, among over 20 different brands.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2842 Sources: http://www.drugbank.ca/drugs/DB01590 |
|||
Target ID: GO:0001649 |
13.5 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | AFINITOR Approved UseAFINITOR is a kinase inhibitor indicated for the treatment of:
postmenopausal women with advanced hormone receptor-positive, HER2 negative breast cancer (advanced HR+ BC) in combination with exemestane after failure of treatment with letrozole or anastrozole.
adults with progressive neuroendocrine tumors of pancreatic origin (PNET) and adults with progressive, well-differentiated, non-functional neuroendocrine tumors (NET) of gastrointestinal (GI) or lung origin that are unresectable, locally advanced or metastatic.
adults with advanced renal cell carcinoma (RCC) after failure of treatment with sunitinib or sorafenib.
adults with renal angiomyolipoma and tuberous sclerosis complex (TSC), not requiring immediate surgery. Launch Date2009 |
|||
| Primary | AFINITOR Approved UseAFINITOR is a kinase inhibitor indicated for the treatment of:
postmenopausal women with advanced hormone receptor-positive, HER2 negative breast cancer (advanced HR+ BC) in combination with exemestane after failure of treatment with letrozole or anastrozole.
adults with progressive neuroendocrine tumors of pancreatic origin (PNET) and adults with progressive, well-differentiated, non-functional neuroendocrine tumors (NET) of gastrointestinal (GI) or lung origin that are unresectable, locally advanced or metastatic.
adults with advanced renal cell carcinoma (RCC) after failure of treatment with sunitinib or sorafenib.
adults with renal angiomyolipoma and tuberous sclerosis complex (TSC), not requiring immediate surgery. Launch Date2009 |
|||
| Primary | AFINITOR Approved UseAFINITOR is a kinase inhibitor indicated for the treatment of:
postmenopausal women with advanced hormone receptor-positive, HER2 negative breast cancer (advanced HR+ BC) in combination with exemestane after failure of treatment with letrozole or anastrozole.
adults with progressive neuroendocrine tumors of pancreatic origin (PNET) and adults with progressive, well-differentiated, non-functional neuroendocrine tumors (NET) of gastrointestinal (GI) or lung origin that are unresectable, locally advanced or metastatic.
adults with advanced renal cell carcinoma (RCC) after failure of treatment with sunitinib or sorafenib.
adults with renal angiomyolipoma and tuberous sclerosis complex (TSC), not requiring immediate surgery. Launch Date2009 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
61.5 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28762135 |
10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
EVEROLIMUS blood | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
18.84 ng/mL |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
EVEROLIMUS plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
435 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28762135 |
10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
EVEROLIMUS blood | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
45.74 h |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
EVEROLIMUS plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
27% EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27299325 |
EVEROLIMUS plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
70 mg 1 times / week multiple, oral MTD|Highest studied dose Dose: 70 mg, 1 times / week Route: oral Route: multiple Dose: 70 mg, 1 times / week Co-administed with:: cetuximab(250 mg/m2 IV: 4 weeks) Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
unhealthy, mean age 60 years n = 16 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 16 Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
DLT: Rash, Mucositis... Other AEs: Fatigue, Phosphatase alkaline increased... Dose limiting toxicities: Rash (grade 3, 2.9%) Other AEs:Mucositis (grade 3, 1.4%) Fatigue (grade 3, 1.4%) Sources: Page: 022334s000_MedR_P2.pdf - p.19Phosphatase alkaline increased (grade 3, 1.4%) Hypoalbuminemia (grade 3, 1.4%) Hypersensitivity (grade 3, 2.9%) Thrombocytopenia (grade 3, 2.9%) AST increased (grade 3, 1.4%) Hyperbilirubinemia (grade 3, 1.4%) Anorexia (grade 3, 1.4%) Dehydration (grade 3, 1.4%) Dyspnea (grade 3, 2.9%) |
30 mg 1 times / week multiple, oral Dose: 30 mg, 1 times / week Route: oral Route: multiple Dose: 30 mg, 1 times / week Co-administed with:: (250 mg/m2 IV: 4 weeks) Sources: |
unhealthy, mean age 60 years n = 6 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 6 Sources: |
Other AEs: Hypersensitivity... |
50 mg 1 times / week multiple, oral Dose: 50 mg, 1 times / week Route: oral Route: multiple Dose: 50 mg, 1 times / week Co-administed with:: (250 mg/m2 IV: 4 weeks) Sources: |
unhealthy, mean age 60 years n = 7 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 7 Sources: |
DLT: Hypokalemia... Other AEs: Anemia, Hypersensitivity... Dose limiting toxicities: Hypokalemia (grade 3, 2%) Other AEs:Anemia (grade 3, 2%) Sources: Hypersensitivity (grade 3, 2%) Hyperbilirubinemia (grade 3, 2%) |
10 mg 1 times / day multiple, oral MTD|Highest studied dose Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 51 years n = 5 Health Status: unhealthy Condition: neuroendocrine tumors Age Group: median age 51 years Sex: M+F Population Size: 5 Sources: |
|
2.5 mg 1 times / day multiple, oral Dose: 2.5 mg, 1 times / day Route: oral Route: multiple Dose: 2.5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 51 years n = 4 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 51 years Sex: M+F Population Size: 4 Sources: |
DLT: Neutropenia, Febrile neutropenia... Other AEs: Neutropenia, Leukopenia... Dose limiting toxicities: Neutropenia (grade 3, 25%) Other AEs:Febrile neutropenia (grade 4, 25%) Neutropenia (grade 3, 50%) Sources: Leukopenia (grade 3, 50%) Anemia (grade 3, 25%) |
50 mg 1 times / week multiple, oral MTD Dose: 50 mg, 1 times / week Route: oral Route: multiple Dose: 50 mg, 1 times / week Sources: |
unhealthy, median age 55.5 years n = 3 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 55.5 years Sex: M+F Population Size: 3 Sources: |
|
20 mg 1 times / week multiple, oral Dose: 20 mg, 1 times / week Route: oral Route: multiple Dose: 20 mg, 1 times / week Sources: |
unhealthy, median age 55.5 years n = 7 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 55.5 years Sex: M+F Population Size: 7 Sources: |
DLT: Interstitial pneumonitis... Dose limiting toxicities: Interstitial pneumonitis (grade 2, 14.3%) Sources: |
35 mg 1 times / week multiple, oral (mean) Dose: 35 mg, 1 times / week Route: oral Route: multiple Dose: 35 mg, 1 times / week Sources: |
unhealthy, median age 55.5 years n = 10 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 55.5 years Sex: M+F Population Size: 10 Sources: |
Other AEs: Dermatitis, Oesophagitis... Other AEs: Dermatitis (grade 3, 20%) Sources: Oesophagitis (grade 3, 10%) Asthenia (grade 3, 10%) |
20 mg 1 times / week multiple, oral Recommended Dose: 20 mg, 1 times / week Route: oral Route: multiple Dose: 20 mg, 1 times / week Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 56 years n = 5 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 56 years Sex: M+F Population Size: 5 Sources: |
Other AEs: Neutropenia, Leukopenia... Other AEs: Neutropenia (grade 3, 80%) Sources: Leukopenia (grade 3, 20%) Anemia (grade 3, 20%) Hypokalemia (grade 3, 40%) |
30 mg 1 times / week multiple, oral Dose: 30 mg, 1 times / week Route: oral Route: multiple Dose: 30 mg, 1 times / week Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 56 years n = 13 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 56 years Sex: M+F Population Size: 13 Sources: |
DLT: Neutropenia, Neutropenia... Other AEs: Neutropenia, Leukopenia... Dose limiting toxicities: Neutropenia (grade 3, 15%) Other AEs:Neutropenia (grade 4, 7%) Febrile neutropenia (grade 4, 7%) Neutropenia (grade 3, 62%) Sources: Leukopenia (grade 3, 15%) Thrombocytopenia (grade 3, 23%) Anemia (grade 3, 23%) Febrile neutropenia (grade 3, 15%) Hypokalemia (grade 3, 23%) |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
Disc. AE: Pneumonitis, Dyspnea... Other AEs: Stomatitis, Anemia... AEs leading to discontinuation/dose reduction: Pneumonitis (2.6%) Other AEs:Dyspnea (1.9%) Lung disorder (1.5%) Fatigue (1.1%) Renal failure (0.4%) Stomatitis (4.5%) Pneumonitis (3.3%) Dyspnea (3%) Mucosal inflammation (3%) Asthenia (2.2%) Pneumonia (2.2%) Thrombocytopenia (2.2%) Anemia (1.9%) Diarrhea (1.9%) Rash (1.5%) Pyrexia (1.5%) Vomiting (1.1%) Dehydration (1.1%) Blood creatinine increased (1.1%) Constipation (1.1%) Fatigue (1.1%) Interstitial lung disease (1.1%) Nausea (1.1%) Abdominal pain (0.7%) Anorexia (0.7%) Arthralgia (0.7%) Edema peripheral (0.7%) Pruritus (0.7%) Pleural effusion (0.4%) Stomatitis (grade 3, 3.3%) Sources: Anemia (grade 3, 4.5%) Thrombocytopenia (grade 3, 1.1%) Lymphopenia (grade 3, 1.5%) Platelet count decreased (grade 3, 0.4%) Rash (grade 3, 0.7%) Erythema (grade 3, 0.7%) Hypercholesterolemia (grade 3, 1.9%) Hypertriglyceridemia (grade 3, 0.7%) Hyperglycemia (grade 3, 2.2%) Hyperlipidemia (grade 3, 0.4%) Blood glucose increased (grade 3, 0.7%) Blood triglycerides increased (grade 3, 0.7%) Diabetes mellitus (grade 3, 1.1%) Pancreatitis acute (grade 4, 0.4%) Blood creatinine increased (grade 3, 0.4%) Renal failure (grade 3, 0.7%) Renal failure acute (grade 4, 0.4%) Pneumonitis (grade 3, 2.6%) Interstitial lung disease (grade 3, 0.4%) Lung infiltration (grade 3, 0.7%) Pulmonary alveolar hemorrhage (grade 3, 0.4%) Deep vein thrombosis (grade 3, 0.4%) AST increased (grade 3, 0.7%) ALT increased (grade 3, 0.4%) Hepatic failure (grade 3, 0.4%) Diarrhea (grade 3, 1.5%) Dry skin (grade 3, 0.4%) Pruritus (grade 3, 0.4%) Palmar-plantar erythrodysaesthesia syndrome (grade 3, 0.4%) Fatigue (grade 3, 3%) Asthenia (grade 3, 1.5%) Mucosal inflammation (grade 3, 1.1%) Anorexia (grade 3, 0.4%) Dyspnea (grade 3, 1.5%) Infection (grade 3, 2.2%) Infection (grade 4, 1.1%) Hemoglobin decreased (grade 3, 8.9%) Hemoglobin decreased (grade 4, 0.4%) Alkaline phosphatase increased (grade 3, 0.7%) Phosphate decreased (grade 3, 4.5%) Sodium decreased (grade 3, 0.4%) Calcium increased (grade 3, 0.4%) Bilirubin increased (grade 3, 0.7%) Bilirubin increased (grade 4, 0.4%) Sodium increased (grade 3, 0.4%) |
2.5 mg 1 times / day multiple, oral Dose: 2.5 mg, 1 times / day Route: oral Route: multiple Dose: 2.5 mg, 1 times / day Sources: |
unhealthy, median age 62 years n = 6 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 62 years Sex: M+F Population Size: 6 Sources: |
DLT: Interstitial pneumonitis... Dose limiting toxicities: Interstitial pneumonitis (grade 2, 16.7%) Sources: |
5 mg 1 times / day multiple, oral Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Sources: |
unhealthy, median age 62 years n = 5 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 62 years Sex: M+F Population Size: 5 Sources: |
DLT: Oesophagitis, Interstitial pneumonitis... Other AEs: Dysphagia... Dose limiting toxicities: Oesophagitis (grade 3, 20%) Other AEs:Interstitial pneumonitis (grade 3, 20%) Dyspnoea (grade 4, 20%) Dysphagia (grade 3) Sources: |
5 mg 1 times / day multiple, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 62.5 years n = 6 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 62.5 years Sex: M+F Population Size: 6 Sources: |
DLT: Neutropenia, Febrile neutropenia... Other AEs: Neutropenia, Leukopenia... Dose limiting toxicities: Neutropenia (grade 3, 17%) Other AEs:Febrile neutropenia (grade 4, 17%) Thrombocytopenia (grade 4, 17%) Neutropenia (grade 3, 67%) Sources: Leukopenia (grade 3, 50%) Thrombocytopenia (grade 3, 67%) Anemia (grade 3, 17%) Febrile neutropenia (grade 3, 50%) Lymphopenia (grade 3, 33%) Pneumonia (grade 3, 33%) |
4 mg 1 times / day single, oral Highest studied dose Dose: 4 mg, 1 times / day Route: oral Route: single Dose: 4 mg, 1 times / day Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
healthy n = 4 Health Status: healthy Population Size: 4 Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
50 mg 1 times / day single, oral Highest studied dose Dose: 50 mg, 1 times / day Route: oral Route: single Dose: 50 mg, 1 times / day Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
healthy n = 61 Health Status: healthy Population Size: 61 Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| AST increased | grade 3, 1.4% | 70 mg 1 times / week multiple, oral MTD|Highest studied dose Dose: 70 mg, 1 times / week Route: oral Route: multiple Dose: 70 mg, 1 times / week Co-administed with:: cetuximab(250 mg/m2 IV: 4 weeks) Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
unhealthy, mean age 60 years n = 16 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 16 Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
| Anorexia | grade 3, 1.4% | 70 mg 1 times / week multiple, oral MTD|Highest studied dose Dose: 70 mg, 1 times / week Route: oral Route: multiple Dose: 70 mg, 1 times / week Co-administed with:: cetuximab(250 mg/m2 IV: 4 weeks) Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
unhealthy, mean age 60 years n = 16 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 16 Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
| Dehydration | grade 3, 1.4% | 70 mg 1 times / week multiple, oral MTD|Highest studied dose Dose: 70 mg, 1 times / week Route: oral Route: multiple Dose: 70 mg, 1 times / week Co-administed with:: cetuximab(250 mg/m2 IV: 4 weeks) Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
unhealthy, mean age 60 years n = 16 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 16 Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
| Fatigue | grade 3, 1.4% | 70 mg 1 times / week multiple, oral MTD|Highest studied dose Dose: 70 mg, 1 times / week Route: oral Route: multiple Dose: 70 mg, 1 times / week Co-administed with:: cetuximab(250 mg/m2 IV: 4 weeks) Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
unhealthy, mean age 60 years n = 16 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 16 Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
| Hyperbilirubinemia | grade 3, 1.4% | 70 mg 1 times / week multiple, oral MTD|Highest studied dose Dose: 70 mg, 1 times / week Route: oral Route: multiple Dose: 70 mg, 1 times / week Co-administed with:: cetuximab(250 mg/m2 IV: 4 weeks) Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
unhealthy, mean age 60 years n = 16 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 16 Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
| Hypoalbuminemia | grade 3, 1.4% | 70 mg 1 times / week multiple, oral MTD|Highest studied dose Dose: 70 mg, 1 times / week Route: oral Route: multiple Dose: 70 mg, 1 times / week Co-administed with:: cetuximab(250 mg/m2 IV: 4 weeks) Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
unhealthy, mean age 60 years n = 16 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 16 Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
| Phosphatase alkaline increased | grade 3, 1.4% | 70 mg 1 times / week multiple, oral MTD|Highest studied dose Dose: 70 mg, 1 times / week Route: oral Route: multiple Dose: 70 mg, 1 times / week Co-administed with:: cetuximab(250 mg/m2 IV: 4 weeks) Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
unhealthy, mean age 60 years n = 16 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 16 Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
| Mucositis | grade 3, 1.4% DLT |
70 mg 1 times / week multiple, oral MTD|Highest studied dose Dose: 70 mg, 1 times / week Route: oral Route: multiple Dose: 70 mg, 1 times / week Co-administed with:: cetuximab(250 mg/m2 IV: 4 weeks) Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
unhealthy, mean age 60 years n = 16 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 16 Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
| Dyspnea | grade 3, 2.9% | 70 mg 1 times / week multiple, oral MTD|Highest studied dose Dose: 70 mg, 1 times / week Route: oral Route: multiple Dose: 70 mg, 1 times / week Co-administed with:: cetuximab(250 mg/m2 IV: 4 weeks) Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
unhealthy, mean age 60 years n = 16 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 16 Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
| Hypersensitivity | grade 3, 2.9% | 70 mg 1 times / week multiple, oral MTD|Highest studied dose Dose: 70 mg, 1 times / week Route: oral Route: multiple Dose: 70 mg, 1 times / week Co-administed with:: cetuximab(250 mg/m2 IV: 4 weeks) Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
unhealthy, mean age 60 years n = 16 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 16 Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
| Thrombocytopenia | grade 3, 2.9% | 70 mg 1 times / week multiple, oral MTD|Highest studied dose Dose: 70 mg, 1 times / week Route: oral Route: multiple Dose: 70 mg, 1 times / week Co-administed with:: cetuximab(250 mg/m2 IV: 4 weeks) Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
unhealthy, mean age 60 years n = 16 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 16 Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
| Rash | grade 3, 2.9% DLT |
70 mg 1 times / week multiple, oral MTD|Highest studied dose Dose: 70 mg, 1 times / week Route: oral Route: multiple Dose: 70 mg, 1 times / week Co-administed with:: cetuximab(250 mg/m2 IV: 4 weeks) Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
unhealthy, mean age 60 years n = 16 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 16 Sources: Page: 022334s000_MedR_P2.pdf - p.19 |
| Hypersensitivity | grade 3, 16.7% | 30 mg 1 times / week multiple, oral Dose: 30 mg, 1 times / week Route: oral Route: multiple Dose: 30 mg, 1 times / week Co-administed with:: (250 mg/m2 IV: 4 weeks) Sources: |
unhealthy, mean age 60 years n = 6 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 6 Sources: |
| Anemia | grade 3, 2% | 50 mg 1 times / week multiple, oral Dose: 50 mg, 1 times / week Route: oral Route: multiple Dose: 50 mg, 1 times / week Co-administed with:: (250 mg/m2 IV: 4 weeks) Sources: |
unhealthy, mean age 60 years n = 7 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 7 Sources: |
| Hyperbilirubinemia | grade 3, 2% | 50 mg 1 times / week multiple, oral Dose: 50 mg, 1 times / week Route: oral Route: multiple Dose: 50 mg, 1 times / week Co-administed with:: (250 mg/m2 IV: 4 weeks) Sources: |
unhealthy, mean age 60 years n = 7 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 7 Sources: |
| Hypersensitivity | grade 3, 2% | 50 mg 1 times / week multiple, oral Dose: 50 mg, 1 times / week Route: oral Route: multiple Dose: 50 mg, 1 times / week Co-administed with:: (250 mg/m2 IV: 4 weeks) Sources: |
unhealthy, mean age 60 years n = 7 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 7 Sources: |
| Hypokalemia | grade 3, 2% DLT |
50 mg 1 times / week multiple, oral Dose: 50 mg, 1 times / week Route: oral Route: multiple Dose: 50 mg, 1 times / week Co-administed with:: (250 mg/m2 IV: 4 weeks) Sources: |
unhealthy, mean age 60 years n = 7 Health Status: unhealthy Condition: advanced cancer Age Group: mean age 60 years Sex: M+F Population Size: 7 Sources: |
| Anemia | grade 3, 25% | 2.5 mg 1 times / day multiple, oral Dose: 2.5 mg, 1 times / day Route: oral Route: multiple Dose: 2.5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 51 years n = 4 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 51 years Sex: M+F Population Size: 4 Sources: |
| Neutropenia | grade 3, 25% DLT |
2.5 mg 1 times / day multiple, oral Dose: 2.5 mg, 1 times / day Route: oral Route: multiple Dose: 2.5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 51 years n = 4 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 51 years Sex: M+F Population Size: 4 Sources: |
| Leukopenia | grade 3, 50% | 2.5 mg 1 times / day multiple, oral Dose: 2.5 mg, 1 times / day Route: oral Route: multiple Dose: 2.5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 51 years n = 4 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 51 years Sex: M+F Population Size: 4 Sources: |
| Neutropenia | grade 3, 50% | 2.5 mg 1 times / day multiple, oral Dose: 2.5 mg, 1 times / day Route: oral Route: multiple Dose: 2.5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 51 years n = 4 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 51 years Sex: M+F Population Size: 4 Sources: |
| Febrile neutropenia | grade 4, 25% DLT |
2.5 mg 1 times / day multiple, oral Dose: 2.5 mg, 1 times / day Route: oral Route: multiple Dose: 2.5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 51 years n = 4 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 51 years Sex: M+F Population Size: 4 Sources: |
| Interstitial pneumonitis | grade 2, 14.3% DLT, Disc. AE |
20 mg 1 times / week multiple, oral Dose: 20 mg, 1 times / week Route: oral Route: multiple Dose: 20 mg, 1 times / week Sources: |
unhealthy, median age 55.5 years n = 7 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 55.5 years Sex: M+F Population Size: 7 Sources: |
| Asthenia | grade 3, 10% | 35 mg 1 times / week multiple, oral (mean) Dose: 35 mg, 1 times / week Route: oral Route: multiple Dose: 35 mg, 1 times / week Sources: |
unhealthy, median age 55.5 years n = 10 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 55.5 years Sex: M+F Population Size: 10 Sources: |
| Oesophagitis | grade 3, 10% | 35 mg 1 times / week multiple, oral (mean) Dose: 35 mg, 1 times / week Route: oral Route: multiple Dose: 35 mg, 1 times / week Sources: |
unhealthy, median age 55.5 years n = 10 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 55.5 years Sex: M+F Population Size: 10 Sources: |
| Dermatitis | grade 3, 20% | 35 mg 1 times / week multiple, oral (mean) Dose: 35 mg, 1 times / week Route: oral Route: multiple Dose: 35 mg, 1 times / week Sources: |
unhealthy, median age 55.5 years n = 10 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 55.5 years Sex: M+F Population Size: 10 Sources: |
| Anemia | grade 3, 20% | 20 mg 1 times / week multiple, oral Recommended Dose: 20 mg, 1 times / week Route: oral Route: multiple Dose: 20 mg, 1 times / week Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 56 years n = 5 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 56 years Sex: M+F Population Size: 5 Sources: |
| Leukopenia | grade 3, 20% | 20 mg 1 times / week multiple, oral Recommended Dose: 20 mg, 1 times / week Route: oral Route: multiple Dose: 20 mg, 1 times / week Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 56 years n = 5 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 56 years Sex: M+F Population Size: 5 Sources: |
| Hypokalemia | grade 3, 40% | 20 mg 1 times / week multiple, oral Recommended Dose: 20 mg, 1 times / week Route: oral Route: multiple Dose: 20 mg, 1 times / week Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 56 years n = 5 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 56 years Sex: M+F Population Size: 5 Sources: |
| Neutropenia | grade 3, 80% | 20 mg 1 times / week multiple, oral Recommended Dose: 20 mg, 1 times / week Route: oral Route: multiple Dose: 20 mg, 1 times / week Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 56 years n = 5 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 56 years Sex: M+F Population Size: 5 Sources: |
| Febrile neutropenia | grade 3, 15% | 30 mg 1 times / week multiple, oral Dose: 30 mg, 1 times / week Route: oral Route: multiple Dose: 30 mg, 1 times / week Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 56 years n = 13 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 56 years Sex: M+F Population Size: 13 Sources: |
| Leukopenia | grade 3, 15% | 30 mg 1 times / week multiple, oral Dose: 30 mg, 1 times / week Route: oral Route: multiple Dose: 30 mg, 1 times / week Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 56 years n = 13 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 56 years Sex: M+F Population Size: 13 Sources: |
| Neutropenia | grade 3, 15% DLT |
30 mg 1 times / week multiple, oral Dose: 30 mg, 1 times / week Route: oral Route: multiple Dose: 30 mg, 1 times / week Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 56 years n = 13 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 56 years Sex: M+F Population Size: 13 Sources: |
| Anemia | grade 3, 23% | 30 mg 1 times / week multiple, oral Dose: 30 mg, 1 times / week Route: oral Route: multiple Dose: 30 mg, 1 times / week Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 56 years n = 13 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 56 years Sex: M+F Population Size: 13 Sources: |
| Hypokalemia | grade 3, 23% | 30 mg 1 times / week multiple, oral Dose: 30 mg, 1 times / week Route: oral Route: multiple Dose: 30 mg, 1 times / week Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 56 years n = 13 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 56 years Sex: M+F Population Size: 13 Sources: |
| Thrombocytopenia | grade 3, 23% | 30 mg 1 times / week multiple, oral Dose: 30 mg, 1 times / week Route: oral Route: multiple Dose: 30 mg, 1 times / week Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 56 years n = 13 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 56 years Sex: M+F Population Size: 13 Sources: |
| Neutropenia | grade 3, 62% | 30 mg 1 times / week multiple, oral Dose: 30 mg, 1 times / week Route: oral Route: multiple Dose: 30 mg, 1 times / week Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 56 years n = 13 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 56 years Sex: M+F Population Size: 13 Sources: |
| Febrile neutropenia | grade 4, 7% DLT |
30 mg 1 times / week multiple, oral Dose: 30 mg, 1 times / week Route: oral Route: multiple Dose: 30 mg, 1 times / week Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 56 years n = 13 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 56 years Sex: M+F Population Size: 13 Sources: |
| Neutropenia | grade 4, 7% DLT |
30 mg 1 times / week multiple, oral Dose: 30 mg, 1 times / week Route: oral Route: multiple Dose: 30 mg, 1 times / week Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 56 years n = 13 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 56 years Sex: M+F Population Size: 13 Sources: |
| Pleural effusion | 0.4% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Renal failure | 0.4% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Abdominal pain | 0.7% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Anorexia | 0.7% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Arthralgia | 0.7% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Edema peripheral | 0.7% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Pruritus | 0.7% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Blood creatinine increased | 1.1% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Constipation | 1.1% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Dehydration | 1.1% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Fatigue | 1.1% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Fatigue | 1.1% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Interstitial lung disease | 1.1% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Nausea | 1.1% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Vomiting | 1.1% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Lung disorder | 1.5% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Pyrexia | 1.5% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Rash | 1.5% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Anemia | 1.9% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Diarrhea | 1.9% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Dyspnea | 1.9% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Asthenia | 2.2% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Pneumonia | 2.2% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Thrombocytopenia | 2.2% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Pneumonitis | 2.6% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Dyspnea | 3% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Mucosal inflammation | 3% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Pneumonitis | 3.3% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Stomatitis | 4.5% Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| ALT increased | grade 3, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Anorexia | grade 3, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Blood creatinine increased | grade 3, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Calcium increased | grade 3, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Deep vein thrombosis | grade 3, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Dry skin | grade 3, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Hepatic failure | grade 3, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Hyperlipidemia | grade 3, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Interstitial lung disease | grade 3, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Palmar-plantar erythrodysaesthesia syndrome | grade 3, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Platelet count decreased | grade 3, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Pruritus | grade 3, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Pulmonary alveolar hemorrhage | grade 3, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Sodium decreased | grade 3, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Sodium increased | grade 3, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| AST increased | grade 3, 0.7% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Alkaline phosphatase increased | grade 3, 0.7% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Bilirubin increased | grade 3, 0.7% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Blood glucose increased | grade 3, 0.7% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Blood triglycerides increased | grade 3, 0.7% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Erythema | grade 3, 0.7% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Hypertriglyceridemia | grade 3, 0.7% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Lung infiltration | grade 3, 0.7% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Rash | grade 3, 0.7% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Renal failure | grade 3, 0.7% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Diabetes mellitus | grade 3, 1.1% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Mucosal inflammation | grade 3, 1.1% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Thrombocytopenia | grade 3, 1.1% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Asthenia | grade 3, 1.5% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Diarrhea | grade 3, 1.5% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Dyspnea | grade 3, 1.5% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Lymphopenia | grade 3, 1.5% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Hypercholesterolemia | grade 3, 1.9% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Hyperglycemia | grade 3, 2.2% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Infection | grade 3, 2.2% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Pneumonitis | grade 3, 2.6% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Fatigue | grade 3, 3% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Stomatitis | grade 3, 3.3% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Anemia | grade 3, 4.5% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Phosphate decreased | grade 3, 4.5% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Hemoglobin decreased | grade 3, 8.9% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Bilirubin increased | grade 4, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Hemoglobin decreased | grade 4, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Pancreatitis acute | grade 4, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Renal failure acute | grade 4, 0.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Infection | grade 4, 1.1% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, median age 61 years n = 269 Health Status: unhealthy Condition: kidney cancer Age Group: median age 61 years Sex: M+F Population Size: 269 Sources: |
| Interstitial pneumonitis | grade 2, 16.7% DLT, Disc. AE |
2.5 mg 1 times / day multiple, oral Dose: 2.5 mg, 1 times / day Route: oral Route: multiple Dose: 2.5 mg, 1 times / day Sources: |
unhealthy, median age 62 years n = 6 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 62 years Sex: M+F Population Size: 6 Sources: |
| Dysphagia | grade 3 | 5 mg 1 times / day multiple, oral Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Sources: |
unhealthy, median age 62 years n = 5 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 62 years Sex: M+F Population Size: 5 Sources: |
| Interstitial pneumonitis | grade 3, 20% DLT |
5 mg 1 times / day multiple, oral Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Sources: |
unhealthy, median age 62 years n = 5 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 62 years Sex: M+F Population Size: 5 Sources: |
| Oesophagitis | grade 3, 20% DLT |
5 mg 1 times / day multiple, oral Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Sources: |
unhealthy, median age 62 years n = 5 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 62 years Sex: M+F Population Size: 5 Sources: |
| Dyspnoea | grade 4, 20% DLT |
5 mg 1 times / day multiple, oral Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Sources: |
unhealthy, median age 62 years n = 5 Health Status: unhealthy Condition: non-small-cell lung cancer Age Group: median age 62 years Sex: M+F Population Size: 5 Sources: |
| Anemia | grade 3, 17% | 5 mg 1 times / day multiple, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 62.5 years n = 6 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 62.5 years Sex: M+F Population Size: 6 Sources: |
| Neutropenia | grade 3, 17% DLT |
5 mg 1 times / day multiple, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 62.5 years n = 6 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 62.5 years Sex: M+F Population Size: 6 Sources: |
| Lymphopenia | grade 3, 33% | 5 mg 1 times / day multiple, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 62.5 years n = 6 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 62.5 years Sex: M+F Population Size: 6 Sources: |
| Pneumonia | grade 3, 33% | 5 mg 1 times / day multiple, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 62.5 years n = 6 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 62.5 years Sex: M+F Population Size: 6 Sources: |
| Febrile neutropenia | grade 3, 50% | 5 mg 1 times / day multiple, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 62.5 years n = 6 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 62.5 years Sex: M+F Population Size: 6 Sources: |
| Leukopenia | grade 3, 50% | 5 mg 1 times / day multiple, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 62.5 years n = 6 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 62.5 years Sex: M+F Population Size: 6 Sources: |
| Neutropenia | grade 3, 67% | 5 mg 1 times / day multiple, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 62.5 years n = 6 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 62.5 years Sex: M+F Population Size: 6 Sources: |
| Thrombocytopenia | grade 3, 67% | 5 mg 1 times / day multiple, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 62.5 years n = 6 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 62.5 years Sex: M+F Population Size: 6 Sources: |
| Febrile neutropenia | grade 4, 17% DLT |
5 mg 1 times / day multiple, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 62.5 years n = 6 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 62.5 years Sex: M+F Population Size: 6 Sources: |
| Thrombocytopenia | grade 4, 17% DLT |
5 mg 1 times / day multiple, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Co-administed with:: cisplatin(75 mg/m2 IV; 1 per 3 weeks) Sources: etoposide(100 mg/m2 IV; 2 per 3 weeks) |
unhealthy, median age 62.5 years n = 6 Health Status: unhealthy Condition: small-cell lung cancer Age Group: median age 62.5 years Sex: M+F Population Size: 6 Sources: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| yes [IC50 9.42 uM] | ||||
| yes [Ki 1.7 uM] | unlikely Comment: In vitro everolimus inhibited CYP3A and 2D6, however, based on Ki values a significant effect on the metabolism of CYP3A or 2D6 is not expected. Page: - |
|||
| yes [Ki 2.3 uM] | unlikely Comment: In vitro everolimus inhibited CYP3A and 2D6, however, based on Ki values a significant effect on the metabolism of CYP3A or 2D6 is not expected. Page: - |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| yes | yes (co-administration study) Comment: Based on the results from the drug-drug interaction studies with ketoconazole, erythromycin and verapamil no dose adjustments wil be provided in the label since the increases in everolimus exposures can not be adjusted by lowering the dose to 5 mg QD. For strong CYP3A4 inducers, a dose increase to 20 mg would compensate for the decrease in everolimus exposure. For strong CYP3A4 inhibitors because of the significant increase in exposure labeling instructions co-administration is not recom Page: - |
|||
| yes | yes (co-administration study) Comment: verapamil increase AUC 240% Page: - |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| Reduced BCL2 and CCND1 mRNA expression in human cervical cancer HeLa cells treated with a combination of everolimus and paclitaxel. | 2016 |
|
| Long-term acquired everolimus resistance in pancreatic neuroendocrine tumours can be overcome with novel PI3K-AKT-mTOR inhibitors. | 2016 Mar 15 |
|
| mTOR inhibitors response and mTOR pathway in pancreatic neuroendocrine tumors. | 2016 Nov |
Sample Use Guides
Advanced HR+ BC, advanced NET, advanced RCC, or renal angiomyolipoma
with TSC:
10 mg once daily with or without food.
Route of Administration:
Oral
| Name | Type | Language | ||
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Brand Name | English | ||
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| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
FDA ORPHAN DRUG |
374012
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
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|
NDF-RT |
N0000175625
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
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|
WHO-ATC |
L04AA18
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
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|
EU-Orphan Drug |
EU/3/07/488
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
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|
FDA ORPHAN DRUG |
315410
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
WHO-VATC |
QL04AA18
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
EMA ASSESSMENT REPORTS |
VOTUBIA (AUTHORIZED: TUBEROUS SCLEROSIS)
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
NDF-RT |
N0000175605
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
NCI_THESAURUS |
C574
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
NCI_THESAURUS |
C2201
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
EMA ASSESSMENT REPORTS |
AFINITOR (AUTHORIZED: CARCINOMA, RENAL CELL)
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
WHO-ATC |
L01XE10
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
FDA ORPHAN DRUG |
283609
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
FDA ORPHAN DRUG |
254107
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
EMA ASSESSMENT REPORTS |
AFINITOR (AUTHORIZED: PANCREATIC NEOPLASMS)
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
FDA ORPHAN DRUG |
489715
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
NDF-RT |
N0000175076
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
FDA ORPHAN DRUG |
340111
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
NCI_THESAURUS |
C1742
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
FDA ORPHAN DRUG |
431214
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
WHO-VATC |
QL01XE10
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
||
|
LIVERTOX |
NBK548857
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
9HW64Q8G6G
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
8255
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
m5220
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | Merck Index | ||
|
CHEMBL1908360
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
N0000182141
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | Cytochrome P450 3A4 Inhibitors [MoA] | ||
|
MM-04
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
9HW64Q8G6G
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
DB01590
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
7863
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
159351-69-6
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
5889
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
EVEROLIMUS
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
C107135
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
DTXSID0040599
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
6442177
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
1118
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
N0000182137
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | Cytochrome P450 2D6 Inhibitors [MoA] | ||
|
100000092327
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
1268976
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
SUB02065MIG
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
N0000185503
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | P-Glycoprotein Inhibitors [MoA] | ||
|
141704
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | RxNorm | ||
|
68478
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
C48387
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY | |||
|
Everolimus
Created by
admin on Sat Dec 16 17:11:59 GMT 2023 , Edited by admin on Sat Dec 16 17:11:59 GMT 2023
|
PRIMARY |
ACTIVE MOIETY
METABOLITE (PARENT)
METABOLITE (PARENT)
