U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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
Structure of LENVATINIB

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)

HIDE SMILES / InChI
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

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

CNS Penetrant
2554
Curator's Comment: The drug is able to cross the blood brain barrier, at least at low levels.

Originator

Approval Year

2015
471
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2778
 4.0 nM [IC50]
Antagonist
2778
 5.2 nM [IC50]
Antagonist
2778
 22.0 nM [IC50]
Antagonist
2778
 39.0 nM [IC50]
Antagonist
2778
 8.2 nM [Ki]
Antagonist
2778
 22.0 nM [Ki]
Antagonist
2778
 15.0 nM [Ki]
Antagonist
2778
 11.0 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
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

2015
Primary
Approved
8429
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

2015
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
325 ng/mL
OTHER GOV
https://www.ema.europa.eu/en/documents/assessment-report/lenvima-epar-public-assessment-report_en.pdf
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
OTHER GOV
https://www.ema.europa.eu/en/documents/assessment-report/lenvima-epar-public-assessment-report_en.pdf
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
OTHER GOV
https://www.ema.europa.eu/en/documents/assessment-report/lenvima-epar-public-assessment-report_en.pdf
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%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206947s007lbl.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
DLT: Thrombocytopenia...
Dose limiting toxicities:
Thrombocytopenia (grade 4, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/22516948
16 mg 1 times / day steady, oral
Dose: 16 mg, 1 times / day
Route: oral
Route: steady
Dose: 16 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
DLT: Hypertension, Fatigue...
Dose limiting toxicities:
Hypertension (grade 3, 1 patient)
Fatigue (grade 3, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
DLT: Febrile neutropenia...
Dose limiting toxicities:
Febrile neutropenia (grade 3, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
40 mg single, oral
Highest studied dose
Dose: 40 mg
Route: oral
Route: single
Dose: 40 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://pubmed.ncbi.nlm.nih.gov/22516948
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
unhealthy, 64 years
n = 261
Health Status: unhealthy
Age Group: 64 years
Sex: M+F
Population Size: 261
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206947Orig1s000MedR.pdf
Page: p. 108
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737

inhibitor
1587
inhibitor
1767

activator
22

inducer
389
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP3A
214

CYP2C8
911

P-gp
1461

BCRP
699

UGT1A1
204

UGT1A4
77

UGT1A6
108

UGT1A9
116

UGT2B7
146

OAT1
599

OAT3
642

OCT1
512

OCT2
647

OATP1B1
788

BSEP
402

OATP1B3
706

aldehyde oxidase
7

CYP1A2
1524

CYP2B6
810

CYP2C19
1478

CYP2A6
707

CYP2E1
882
P-gp
1537

BCRP
561

aldehyde oxidase
16

OAT1
326

OAT3
339

OATP1B1
406

OATP1B3
350

OCT1
327

OCT2
355

BSEP
52
UGT1A1
69

UGT1A4
8

UGT1A6
34

UGT1A9
9

UGT2B7
14

P-gp
257

CYP1A1
108

CYP1A2
701

CYP2B6
547
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
aldehyde oxidase
8
 no [IC50 >100 uM]
BCRP
773
 no [IC50 >30 uM]
P-gp
1650
 no [IC50 >30 uM]
UGT1A6
141
 no [IC50 >30 uM]
UGT1A9
121
 no [IC50 >30 uM]
UGT2B7
157
 no [IC50 >30 uM]
CYP1A1
218
 no
CYP1A1
218
 no
CYP1A2
1692
 no
CYP1A2
1692
 no
CYP2A6
739
 no
CYP2B6
1001
 no
CYP2B6
1001
 no
CYP2C9
1819
 no
CYP2C9
1819
 no
CYP2E1
970
 no
OATP1B3
715
 no
P-gp
1650
 no
UGT1A1
254
 no
UGT1A4
80
 no
UGT1A6
141
 no
UGT1A9
121
 no
UGT2B7
157
 no
CYP1A2
1692
 weak [IC50 >100 uM]
CYP2B6
1001
 weak [IC50 >100 uM]
CYP2C19
1553
 weak [IC50 >100 uM]
CYP2C9
1819
 weak [IC50 >100 uM]
CYP2D6
1891
 weak [IC50 >100 uM]
CYP3A
298
 weak [IC50 >100 uM]
unlikely
Comment: no clinically important effect of lenvatinib on midazolam
Page: 9, 33
CYP2C8
965
 yes [IC50 10.1 uM]
unlikely
Comment: no clinically important effect of lenvatinib on repaglinide; IC50 from human liver microsome experiments
Page: 9, 33
UGT1A1
254
 yes [IC50 10.6 uM]
UGT1A4
80
 yes [IC50 14 uM]
BSEP
403
 yes
CYP3A
298
 yes
CYP3A4
1925
 yes
OAT1
603
 yes
OAT3
644
 yes
OATP1B1
803
 yes
OCT1
543
 yes
OCT2
648
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
BSEP
52
 no
OAT1
326
 no
OAT3
339
 no
OATP1B1
406
 no
OATP1B3
350
 no
OCT1
327
 no
OCT2
355
 no
aldehyde oxidase
16
 yes
BCRP
561
 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
CYP3A4
1737
 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
P-gp
1537
 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
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:85994
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:85994
ChemicalBook
CB12484883
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB12484883
MolPort
MolPort-009-679-469
https://www.molport.com/shop/molecule-link/MolPort-009-679-469
Selleck Chemicals
E7080
http://www.selleckchem.com/products/E7080.html
ZINC
ZINC000003816292
http://zinc15.docking.org/substances/ZINC000003816292
eMolecules
31507658
https://www.emolecules.com/cgi-bin/more?vid=31507658
PubMed

PubMed

TitleDatePubMed
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.
2012 Dec 27
Lenvatinib: first global approval.
2015 Apr
Patents

Patents

07550483
2
07612208
2
07683172
2
07994159
2
08058474
2
20040053908
3
20040253205
2
20060135486
5
JP2010280713A
2

Sample Use Guides

In Vivo Use Guide
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
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 Fri Dec 15 15:48:19 GMT 2023
Edited
by admin
on Fri Dec 15 15:48:19 GMT 2023
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
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
Lenvatinib [WHO-DD]
Common 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 Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
FDA ORPHAN DRUG 423614
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
NCI_THESAURUS C93259
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
WHO-ATC L01XE29
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
FDA ORPHAN DRUG 378412
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
FDA ORPHAN DRUG 423714
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
NDF-RT N0000175605
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
EU-Orphan Drug EU/3/15/1460
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
Code System Code Type Description
CHEBI
85994
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
USAN
XX-26
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
FDA UNII
EE083865G2
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
CAS
417716-92-8
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
INN
9361
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
ChEMBL
CHEMBL1289601
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
LACTMED
Lenvatinib
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
MERCK INDEX
m6764
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY Merck Index
WIKIPEDIA
LENVATINIB
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
DRUG BANK
DB09078
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
IUPHAR
7426
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
RXCUI
1603296
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY RxNorm
DRUG CENTRAL
4942
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
EVMPD
SUB64419
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
NCI_THESAURUS
C95124
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
CHEBI
85995
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
NDF-RT
N0000020000
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY Receptor Tyrosine Kinase Inhibitors [MoA]
EPA CompTox
DTXSID50194605
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
PUBCHEM
9823820
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
DAILYMED
EE083865G2
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
SMS_ID
100000134793
Created by admin on Fri Dec 15 15:48:19 GMT 2023 , Edited by admin on Fri Dec 15 15:48:19 GMT 2023
PRIMARY
Related Record Type Details
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> SUBSTRATE
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
Predicted no effect with other CYP2C8 substrates at clinical dose of Lenvatinib
ATP-BINDING CASSETTE SUB-FAMILY G MEMBER 2
TRANSPORTER -> SUBSTRATE
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
CYTOCHROME P450 2C8
METABOLIC ENZYME -> INHIBITOR
INHIBITOR
PLASMA
Structure of LENVATINIB MESYLATE
SALT/SOLVATE -> PARENT
VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2
TARGET -> INHIBITOR
CYTOCHROME P450 3A4
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
Structure of ME-92
METABOLITE INACTIVE -> PARENT
MINOR
PLASMA
Structure of 4-(4-((AMINOCARBONYL)AMINO)-3-CHLOROPHENOXY)-7-METHOXY-6-QUINOLINECARBOXAMIDE
METABOLITE LESS ACTIVE -> PARENT
MINOR
PLASMA
Structure of 4-(3-CHLORO-4-(((CYCLOPROPYLAMINO)CARBONYL)AMINO)PHENOXY)-1,2-DIHYDRO-7-METHOXY-2-OXO-6-QUINOLINECARBOXAMIDE
METABOLITE LESS ACTIVE -> PARENT
MINOR
URINE
Structure of ME-107
METABOLITE LESS ACTIVE -> PARENT
MINOR
PLASMA
Structure of 4-(3-CHLORO-4-(((CYCLOPROPYLAMINO)CARBONYL)AMINO)PHENOXY)-1,2-DIHYDRO-7-METHOXY-2-OXO-6-QUINOLINECARBOXAMIDE
METABOLITE LESS ACTIVE -> PARENT
MINOR
FECAL
Structure of 4-(3-CHLORO-4-(((CYCLOPROPYLAMINO)CARBONYL)AMINO)PHENOXY)-7-HYDROXY-6-QUINOLINECARBOXAMIDE
METABOLITE LESS ACTIVE -> PARENT
MAJOR
PLASMA
Structure of 1,4-DIHYDRO-7-METHOXY-4-OXO-6-QUINOLINECARBOXAMIDE
METABOLITE INACTIVE -> PARENT
MINOR
PLASMA
Structure of 4-(4-AMINO-3-CHLOROPHENOXY)-7-METHOXY-6-QUINOLINECARBOXAMIDE
METABOLITE LESS ACTIVE -> PARENT
MINOR
PLASMA
Related Record Type Details
Structure of LENVATINIB
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966