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Details

Stereochemistry ACHIRAL
Molecular Formula C21H19ClN4O4
Molecular Weight 426.8537
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LENVATINIB

SMILES

COc1cc2c(cc1C(=N)O)c(ccn2)Oc3ccc(c(c3)Cl)NC(=NC4CC4)O

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)

HIDE SMILES / InChI

Molecular Formula C21H19ClN4O4
Molecular Weight 426.8537
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
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.

CNS Activity

Curator's Comment:: The drug is able to cross the blood brain barrier, at least at low levels.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
LENVIMA

Approved Use

LENVIMA 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 Date

1.42369921E12
Primary
LENVIMA

Approved Use

LENVIMA 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 Date

1.42369921E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
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

AUC

ValueDoseCo-administeredAnalytePopulation
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

T1/2

ValueDoseCo-administeredAnalytePopulation
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

Funbound

ValueDoseCo-administeredAnalytePopulation
1.5%
LENVATINIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse 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%)
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%)
Sources:
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%)
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%)
Sources:
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)
Fatigue (grade 3, 1 patient)
Sources:
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%)
Asthenia (1.15%)
Hypertension (13%)
Proteinuria (11%)
Decreased appetite (10%)
Diarrhea (10%)
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: 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%)
Renal 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%)
Sources: Page: p. 108
40 mg single, oral
Highest studied dose
Dose: 40 mg
Route: oral
Route: single
Dose: 40 mg
Sources:
unhealthy, adult
AEs

AEs

AESignificanceDosePopulation
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
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 >100 uM]
no [IC50 >30 uM]
no [IC50 >30 uM]
no [IC50 >30 uM]
no [IC50 >30 uM]
no [IC50 >30 uM]
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
weak [IC50 >100 uM]
weak [IC50 >100 uM]
weak [IC50 >100 uM]
weak [IC50 >100 uM]
weak [IC50 >100 uM]
weak [IC50 >100 uM]
unlikely
Comment: no clinically important effect of lenvatinib on midazolam
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
yes [IC50 10.6 uM]
yes [IC50 14 uM]
yes
yes
yes
yes
yes
yes
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
yes
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
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
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

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.
2012 Dec 27
Neuroendocrine cancer: SELECT—lenvatinib in thyroid cancer.
2015 Apr
Patents

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
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 Sat Jun 26 00:43:40 UTC 2021
Edited
by admin
on Sat Jun 26 00:43:40 UTC 2021
Record UNII
EE083865G2
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LENVATINIB
DASH   INN   MI   USAN   WHO-DD  
USAN   INN  
Official Name English
4-(3-CHLORO-4-((CYCLOPROPYLAMINOCARBONYL)AMINO)PHENOXY)-7-METHOXY-6-QUINOLINECARBOXAMIDE
Systematic Name English
6-QUINOLINECARBOXAMIDE, 4-(3-CHLORO-4-(((CYCLOPROPYLAMINO)CARBONYL)AMINO)PHENOXY)-7-METHOXY-
Systematic Name English
LENVATINIB [INN]
Common Name English
ER-203492-00
Code English
LENVATINIB [WHO-DD]
Common Name English
E-7080
Code English
LENVATINIB [MI]
Common Name English
LENVATINIB [USAN]
Common Name English
6-QUINOLINECARBOXAMIDE, 4-(3-CHLORO-4-(((CYCLOPROPYLAMINO)CARBONYL)AMINO)PHENOXY)- 7-METHOXY-
Systematic Name English
E7080
Code English
4-(3-CHLORO-4-((CYCLOPROPYLCARBAMOYL)AMINO)PHENOXY)-7-METHOXYQUINOLINE-6-CARBOXAMIDE
Systematic Name English
N-(4-((6-CARBAMOYL-7-METHOXYQUINOLIN-4-YL)OXY)-2-CHLOROPHENYL)-N'-CYCLOPROPYLUREA
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
FDA ORPHAN DRUG 423614
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
NCI_THESAURUS C93259
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
WHO-ATC L01XE29
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
FDA ORPHAN DRUG 378412
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
NDF-RT N0000175605
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
FDA ORPHAN DRUG 423714
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
EU-Orphan Drug EU/3/15/1460
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
Code System Code Type Description
FDA UNII
EE083865G2
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
PRIMARY
CAS
417716-92-8
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
PRIMARY
INN
9361
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
PRIMARY
ChEMBL
CHEMBL1289601
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
PRIMARY
LACTMED
Lenvatinib
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
PRIMARY
MERCK INDEX
M6764
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
PRIMARY Merck Index
WIKIPEDIA
LENVATINIB
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
PRIMARY
DRUG BANK
DB09078
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
PRIMARY
IUPHAR
7426
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
PRIMARY
RXCUI
1603296
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
PRIMARY RxNorm
DRUG CENTRAL
4942
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
PRIMARY
EVMPD
SUB64419
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
PRIMARY
NCI_THESAURUS
C95124
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
PRIMARY
NDF-RT
N0000020000
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
PRIMARY Receptor Tyrosine Kinase Inhibitors [MoA]
EPA CompTox
417716-92-8
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
PRIMARY
PUBCHEM
9823820
Created by admin on Sat Jun 26 00:43:40 UTC 2021 , Edited by admin on Sat Jun 26 00:43:40 UTC 2021
PRIMARY
Related Record Type Details
BINDER->LIGAND
BINDING
INHIBITOR -> METABOLIC ENZYME
INHIBITOR
PLASMA
SALT/SOLVATE -> PARENT
TARGET -> INHIBITOR
INHIBITOR -> METABOLIC ENZYME
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 LESS ACTIVE -> PARENT
MAJOR
PLASMA
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC