Details
Stereochemistry | ACHIRAL |
Molecular Formula | C21H19ClN4O4 |
Molecular Weight | 426.853 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC2=C(C=C1C(N)=O)C(OC3=CC=C(NC(=O)NC4CC4)C(Cl)=C3)=CC=N2
InChI
InChIKey=WOSKHXYHFSIKNG-UHFFFAOYSA-N
InChI=1S/C21H19ClN4O4/c1-29-19-10-17-13(9-14(19)20(23)27)18(6-7-24-17)30-12-4-5-16(15(22)8-12)26-21(28)25-11-2-3-11/h4-11H,2-3H2,1H3,(H2,23,27)(H2,25,26,28)
Molecular Formula | C21H19ClN4O4 |
Molecular Weight | 426.853 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.drugbank.ca/drugs/DB09078Curator's Comment: Description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/206947s003lbl.pdf
Sources: https://www.drugbank.ca/drugs/DB09078
Curator's Comment: Description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/206947s003lbl.pdf
Lenvatinib, developed by Eisai Co., is a receptor tyrosine kinase (RTK) inhibitor that inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4). Lenvatinib also inhibits other RTKs that have been implicated in pathogenic angiogenesis, tumor growth, and cancer progression in addition to their normal cellular functions, including fibroblast growth factor (FGF) receptors FGFR1, 2, 3, and 4; the platelet derived growth factor receptor alpha (PDGFRα), KIT, and RET. These receptor tyrosine kinases (RTKs) located in the cell membrane play a central role in the activation of signal transduction pathways involved in the normal regulation of cellular processes, such as cell proliferation, migration, apoptosis and differentiation, and in pathogenic angiogenesis, lymphogenesis, tumour growth and cancer progression. In particular, VEGF has been identified as a crucial regulator of both physiologic and pathologic angiogenesis and increased expression of VEGF is associated with a poor prognosis in many types of cancers. Lenvatinib is indicated for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine (RAI)-refractory differentiated thyroid cancer. Most patients with thyroid cancer have a very good prognosis with treatment (98% 5 year survival rate) involving surgery and hormone therapy. However, for patients with RAI-refractory thyroid cancer, treatment options are limited and the prognosis is poor, leading to a push for the development of more targeted therapies such as lenvatinib. Lenvatinib is marketed under the trade name Lenvima, it is indicated for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL279 |
4.0 nM [IC50] | ||
Target ID: CHEMBL1955 |
5.2 nM [IC50] | ||
Target ID: CHEMBL1868 |
22.0 nM [IC50] | ||
Target ID: CHEMBL1913 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17943726 |
39.0 nM [IC50] | ||
Target ID: CHEMBL4142 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25197551 |
8.2 nM [Ki] | ||
Target ID: CHEMBL3650 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25197551 |
22.0 nM [Ki] | ||
Target ID: CHEMBL2742 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25197551 |
15.0 nM [Ki] | ||
Target ID: CHEMBL1936 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25197551 |
11.0 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | LENVIMA Approved UseLENVIMA is a kinase inhibitor that is indicated for:
• Differentiated Thyroid Cancer (DTC): single agent for patients with locally recurrent or metastatic, progressive, radioactive iodine-refractory DTC.
• Renal Cell Cancer (RCC): in combination with everolimus, for patients with advanced RCC following one prior anti-angiogenic therapy. Launch Date2015 |
|||
Primary | LENVIMA Approved UseLENVIMA is a kinase inhibitor that is indicated for:
• Differentiated Thyroid Cancer (DTC): single agent for patients with locally recurrent or metastatic, progressive, radioactive iodine-refractory DTC.
• Renal Cell Cancer (RCC): in combination with everolimus, for patients with advanced RCC following one prior anti-angiogenic therapy. Launch Date2015 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
325 ng/mL |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
LENVATINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3010 ng × h/mL |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
LENVATINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
28 h |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
LENVATINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.5% |
LENVATINIB plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 7 Sources: |
DLT: Proteinuria... Other AEs: Hypertension, Nausea... Dose limiting toxicities: Proteinuria (grade 3, 2 patients) Other AEs:Hypertension (57%) Sources: Nausea (43%) Diarrhoea (57%) Stomatitis (57%) Proteinuria (43%) Vomiting (14%) Lethargy (29%) Dysphonia (43%) Dry skin (14%) Fatigue (14%) Anorexia (29%) Constipation (14%) Headache (29%) |
25 mg 1 times / day steady, oral MTD Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 24 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 24 Sources: |
Other AEs: Hypertension, Nausea... Other AEs: Hypertension (63%) Sources: Nausea (58%) Diarrhoea (50%) Stomatitis (63%) Proteinuria (29%) Vomiting (33%) Lethargy (38%) Dysphonia (46%) Dry skin (46%) Fatigue (21%) Anorexia (21%) Constipation (33%) Headache (29%) Abdominal pain (29%) |
12.5 mg 1 times / day steady, oral Dose: 12.5 mg, 1 times / day Route: oral Route: steady Dose: 12.5 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 21 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 21 Sources: |
DLT: Thrombocytopenia... Dose limiting toxicities: Thrombocytopenia (grade 4, 1 patient) Sources: |
16 mg 1 times / day steady, oral Dose: 16 mg, 1 times / day Route: oral Route: steady Dose: 16 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 30 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 30 Sources: |
DLT: Hypertension, Fatigue... Dose limiting toxicities: Hypertension (grade 3, 1 patient) Sources: Fatigue (grade 3, 1 patient) |
6.4 mg 1 times / day steady, oral Dose: 6.4 mg, 1 times / day Route: oral Route: steady Dose: 6.4 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 21 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 21 Sources: |
DLT: Febrile neutropenia... Dose limiting toxicities: Febrile neutropenia (grade 3, 1 patient) Sources: |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: |
Disc. AE: Hypertension, Asthenia... AEs leading to discontinuation/dose reduction: Hypertension (1.15%) Sources: Asthenia (1.15%) Hypertension (13%) Proteinuria (11%) Decreased appetite (10%) Diarrhea (10%) |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Disc. AE: Proteinuria, Renal failure acute... AEs leading to discontinuation/dose reduction: Proteinuria (0.77%) Sources: Page: p. 108Renal failure acute (0.77%) Sepsis (0.77%) Abdominal pain upper (0.38%) Accidental overdose (0.38%) Acute myocardial infarction (0.38%) Acute respiratory failure (0.38%) Ataxia (0.38%) Blood alkaline phosphatase increased (0.38%) Cardio-respiratory arrest (0.38%) Cerebral microangiopathy (0.38%) Dizziness (0.38%) Epilepsy (0.38%) QT interval prolonged (0.38%) Fatigue (0.38%) Glossitis (0.38%) Hemorrhagic stroke (0.38%) Hyponatremia (0.38%) Laryngeal necrosis (0.38%) Memory impairment (0.38%) Myalgia (0.38%) Myocardial infarction (0.38%) Oropharyngeal pain (0.38%) Pneumonia (0.38%) Pulmonary embolism (0.38%) Sciatica (0.38%) Skin ulcer (0.38%) Spinal cord compression (0.38%) Stomatitis (0.38%) Vascular pseudoaneurysm (0.38%) Weight decreased (14.6%) Nausea (14.2%) Palmar-plantar erythrodysesthesia syndrome (12.3%) Asthenia (10.3%) Fatigue (9.9%) Stomatitis (8.8%) Vomiting (8%) Headache (5.4%) Arthralgia (5%) Abdominal pain (3.8%) Dehydration (3.5%) Myalgia (3%) Pneumonia (3%) Dysphonia (2.7%) Thrombocytopenia (2.7%) Dizziness (2.3%) Dysgeusia (2.3%) Dyspepsia (2.3%) Dysphagia (2.3%) Edema peripheral (2.3%) Oropharyngeal pain (2.3%) Platelet count decreased (2.3%) |
40 mg single, oral Highest studied dose Dose: 40 mg Route: oral Route: single Dose: 40 mg Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Constipation | 14% | 32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 7 Sources: |
Dry skin | 14% | 32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 7 Sources: |
Fatigue | 14% | 32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 7 Sources: |
Vomiting | 14% | 32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 7 Sources: |
Anorexia | 29% | 32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 7 Sources: |
Headache | 29% | 32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 7 Sources: |
Lethargy | 29% | 32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 7 Sources: |
Dysphonia | 43% | 32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 7 Sources: |
Nausea | 43% | 32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 7 Sources: |
Proteinuria | 43% | 32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 7 Sources: |
Diarrhoea | 57% | 32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 7 Sources: |
Hypertension | 57% | 32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 7 Sources: |
Stomatitis | 57% | 32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 7 Sources: |
Proteinuria | grade 3, 2 patients DLT |
32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 7 Sources: |
Anorexia | 21% | 25 mg 1 times / day steady, oral MTD Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 24 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 24 Sources: |
Fatigue | 21% | 25 mg 1 times / day steady, oral MTD Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 24 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 24 Sources: |
Abdominal pain | 29% | 25 mg 1 times / day steady, oral MTD Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 24 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 24 Sources: |
Headache | 29% | 25 mg 1 times / day steady, oral MTD Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 24 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 24 Sources: |
Proteinuria | 29% | 25 mg 1 times / day steady, oral MTD Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 24 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 24 Sources: |
Constipation | 33% | 25 mg 1 times / day steady, oral MTD Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 24 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 24 Sources: |
Vomiting | 33% | 25 mg 1 times / day steady, oral MTD Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 24 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 24 Sources: |
Lethargy | 38% | 25 mg 1 times / day steady, oral MTD Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 24 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 24 Sources: |
Dry skin | 46% | 25 mg 1 times / day steady, oral MTD Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 24 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 24 Sources: |
Dysphonia | 46% | 25 mg 1 times / day steady, oral MTD Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 24 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 24 Sources: |
Diarrhoea | 50% | 25 mg 1 times / day steady, oral MTD Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 24 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 24 Sources: |
Nausea | 58% | 25 mg 1 times / day steady, oral MTD Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 24 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 24 Sources: |
Hypertension | 63% | 25 mg 1 times / day steady, oral MTD Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 24 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 24 Sources: |
Stomatitis | 63% | 25 mg 1 times / day steady, oral MTD Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 24 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 24 Sources: |
Thrombocytopenia | grade 4, 1 patient DLT |
12.5 mg 1 times / day steady, oral Dose: 12.5 mg, 1 times / day Route: oral Route: steady Dose: 12.5 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 21 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 21 Sources: |
Fatigue | grade 3, 1 patient DLT |
16 mg 1 times / day steady, oral Dose: 16 mg, 1 times / day Route: oral Route: steady Dose: 16 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 30 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 30 Sources: |
Hypertension | grade 3, 1 patient DLT |
16 mg 1 times / day steady, oral Dose: 16 mg, 1 times / day Route: oral Route: steady Dose: 16 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 30 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 30 Sources: |
Febrile neutropenia | grade 3, 1 patient DLT |
6.4 mg 1 times / day steady, oral Dose: 6.4 mg, 1 times / day Route: oral Route: steady Dose: 6.4 mg, 1 times / day Sources: |
unhealthy, 54 years (range 25–84 years) n = 21 Health Status: unhealthy Condition: advanced solid tumours Age Group: 54 years (range 25–84 years) Sex: M+F Population Size: 21 Sources: |
Asthenia | 1.15% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: |
Hypertension | 1.15% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: |
Decreased appetite | 10% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: |
Diarrhea | 10% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: |
Proteinuria | 11% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: |
Hypertension | 13% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: |
Abdominal pain upper | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Accidental overdose | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Acute myocardial infarction | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Acute respiratory failure | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Ataxia | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Blood alkaline phosphatase increased | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Cardio-respiratory arrest | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Cerebral microangiopathy | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Dizziness | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Epilepsy | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Fatigue | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Glossitis | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Hemorrhagic stroke | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Hyponatremia | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Laryngeal necrosis | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Memory impairment | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Myalgia | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Myocardial infarction | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Oropharyngeal pain | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Pneumonia | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Pulmonary embolism | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
QT interval prolonged | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Sciatica | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Skin ulcer | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Spinal cord compression | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Stomatitis | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Vascular pseudoaneurysm | 0.38% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Proteinuria | 0.77% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Renal failure acute | 0.77% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Sepsis | 0.77% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Asthenia | 10.3% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Palmar-plantar erythrodysesthesia syndrome | 12.3% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Nausea | 14.2% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Weight decreased | 14.6% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Dizziness | 2.3% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Dysgeusia | 2.3% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Dyspepsia | 2.3% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Dysphagia | 2.3% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Edema peripheral | 2.3% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Oropharyngeal pain | 2.3% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Platelet count decreased | 2.3% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Dysphonia | 2.7% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Thrombocytopenia | 2.7% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Myalgia | 3% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Pneumonia | 3% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Dehydration | 3.5% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Abdominal pain | 3.8% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Arthralgia | 5% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Headache | 5.4% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Vomiting | 8% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Stomatitis | 8.8% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Fatigue | 9.9% Disc. AE |
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: Page: p. 108 |
unhealthy, 64 years n = 261 Health Status: unhealthy Age Group: 64 years Sex: M+F Population Size: 261 Sources: Page: p. 108 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 34.0 |
no [IC50 >100 uM] | |||
Page: 34.0 |
no [IC50 >30 uM] | |||
Page: 34, 35 |
no [IC50 >30 uM] | |||
Page: 34.0 |
no [IC50 >30 uM] | |||
Page: 34.0 |
no [IC50 >30 uM] | |||
Page: 34.0 |
no [IC50 >30 uM] | |||
Page: 34.0 |
no | |||
Page: 34.0 |
no | |||
Page: 34.0 |
no | |||
Page: 34.0 |
no | |||
Page: 33.0 |
no | |||
Page: 34.0 |
no | |||
Page: 34.0 |
no | |||
Page: 34.0 |
no | |||
Page: 34.0 |
no | |||
Page: 33.0 |
no | |||
Page: 34, 35 |
no | |||
Page: 34.0 |
no | |||
Page: 34.0 |
no | |||
Page: 34.0 |
no | |||
Page: 34.0 |
no | |||
Page: 34.0 |
no | |||
Page: 34.0 |
no | |||
Page: 33.0 |
weak [IC50 >100 uM] | |||
Page: 33.0 |
weak [IC50 >100 uM] | |||
Page: 33.0 |
weak [IC50 >100 uM] | |||
Page: 33.0 |
weak [IC50 >100 uM] | |||
Page: 33.0 |
weak [IC50 >100 uM] | |||
Page: 9, 33 |
weak [IC50 >100 uM] | unlikely Comment: no clinically important effect of lenvatinib on midazolam Page: 9, 33 |
||
Page: 9, 33 |
yes [IC50 10.1 uM] | unlikely Comment: no clinically important effect of lenvatinib on repaglinide; IC50 from human liver microsome experiments Page: 9, 33 |
||
Page: 34.0 |
yes [IC50 10.6 uM] | |||
Page: 34.0 |
yes [IC50 14 uM] | |||
Page: 34, 35 |
yes | |||
Page: 34.0 |
yes | |||
Page: 34.0 |
yes | |||
Page: 34, 35 |
yes | |||
Page: 34, 35 |
yes | |||
Page: 34, 35 |
yes | |||
Page: 34, 35 |
yes | |||
Page: 34, 35 |
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 8, 33, 34 |
no | |||
Page: 8, 33, 34 |
no | |||
Page: 8, 33, 34 |
no | |||
Page: 8, 33, 34 |
no | |||
Page: 8, 33, 34 |
no | |||
Page: 8, 33, 34 |
no | |||
Page: 8, 33, 34 |
no | |||
Page: 8, 33 |
yes | |||
Page: 4, 8, 9, 33, 34 |
yes | no (co-administration study) Comment: no dose adjustment is recommended for lenvatinib when co-administered with inhibitors of BCRP Page: 4, 8, 9, 33, 34 |
||
Page: 4, 9, 33 |
yes | no (co-administration study) Comment: no dose adjustment is recommended for lenvatinib when co-administered with inhibitors or inducers of CYP3A; coadministration with ketoconazole increased lenvatinib AUC by 15% and Cmax by 19% Page: 4, 9, 33 |
||
Page: 4, 8, 9, 33, 34 |
yes | no (co-administration study) Comment: no dose adjustment is recommended for lenvatinib when co-administered with inhibitors or inducers of P-gp; coadministration with rifampicin increased lenvatinib AUC by 31% and Cmax by 33% Page: 4, 8, 9, 33, 34 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 25, 49, 120 |
PubMed
Title | Date | PubMed |
---|---|---|
E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. | 2008 Feb 1 |
|
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. | 2012 Dec 27 |
|
Lenvatinib: first global approval. | 2015 Apr |
Sample Use Guides
Recommended Dose for DTC
The recommended daily dose of LENVIMA (Lenvatinib) is 24 mg (two 10 mg capsules and one 4 mg capsule) orally taken once daily with or without food. Continue LENVIMA until disease progression or until unacceptable toxicity. Take LENVIMA at the same time each day. If a dose is missed and cannot be taken within 12 hours, skip that dose and take the next dose at the usual time of administration.
Recommended Dose for RCC
The recommended daily dose of LENVIMA (Lenvatinib) is 18 mg (one 10 mg capsule and two 4 mg capsules) in combination with 5 mg everolimus orally taken once daily with or without food
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25197551
Lenvatinib inhibited VEGF induced proliferation and tube formation of HUVECs with IC50 values of 3.4 and 2.7 nM, respectively
Substance Class |
Chemical
Created
by
admin
on
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on
Fri Dec 15 15:48:19 GMT 2023
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Record UNII |
EE083865G2
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Validated (UNII)
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C129825
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FDA ORPHAN DRUG |
423614
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NCI_THESAURUS |
C93259
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WHO-ATC |
L01XE29
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FDA ORPHAN DRUG |
378412
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FDA ORPHAN DRUG |
423714
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NDF-RT |
N0000175605
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EU-Orphan Drug |
EU/3/15/1460
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Code System | Code | Type | Description | ||
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85994
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PRIMARY | |||
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XX-26
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EE083865G2
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417716-92-8
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9361
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CHEMBL1289601
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Lenvatinib
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m6764
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LENVATINIB
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PRIMARY | |||
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DB09078
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7426
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1603296
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4942
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SUB64419
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C95124
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85995
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N0000020000
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PRIMARY | Receptor Tyrosine Kinase Inhibitors [MoA] | ||
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DTXSID50194605
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PRIMARY | |||
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9823820
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EE083865G2
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100000134793
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PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
TRANSPORTER -> SUBSTRATE |
|
||
|
METABOLIC ENZYME -> SUBSTRATE |
Predicted no effect with other CYP2C8 substrates at clinical dose of Lenvatinib
|
||
|
TRANSPORTER -> SUBSTRATE |
|
||
|
BINDER->LIGAND |
BINDING
|
||
|
METABOLIC ENZYME -> INHIBITOR |
INHIBITOR
PLASMA
|
||
|
SALT/SOLVATE -> PARENT | |||
|
TARGET -> INHIBITOR | |||
|
METABOLIC ENZYME -> INHIBITOR |
Time-dependent inhibition. significant effect with other drugs which are substrate of CYP3A4 at clinical dose of Lenvatinib
MAJOR
PLASMA
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE INACTIVE -> PARENT |
MINOR
PLASMA
|
||
|
METABOLITE LESS ACTIVE -> PARENT |
MINOR
PLASMA
|
||
|
METABOLITE LESS ACTIVE -> PARENT |
MINOR
URINE
|
||
|
METABOLITE LESS ACTIVE -> PARENT |
MINOR
PLASMA
|
||
|
METABOLITE LESS ACTIVE -> PARENT |
MINOR
FECAL
|
||
|
METABOLITE LESS ACTIVE -> PARENT |
MAJOR
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
MINOR
PLASMA
|
||
|
METABOLITE LESS ACTIVE -> PARENT |
MINOR
PLASMA
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Biological Half-life | PHARMACOKINETIC |
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