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lenvatinib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	4942	417716-92-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: E-7080 E 7080 lenvatinib lenvima ER-203492-00 E7080 lenvatinib mesylate lenvatinib mesilate	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) Molecular weight: 426.86 Formula: C21H19ClN4O4 CLOGP: 3.35 LIPINSKI: 0 HAC: 8 HDO: 3 TPSA: 115.57 ALOGS: -4.84 ROTB: 6 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

E-7080
E 7080
lenvatinib
lenvima
ER-203492-00
E7080
lenvatinib mesylate
lenvatinib mesilate

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)

Molecular weight: 426.86
Formula: C21H19ClN4O4
CLOGP: 3.35
LIPINSKI: 0
HAC: 8
HDO: 3
TPSA: 115.57
ALOGS: -4.84
ROTB: 6

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
May 28, 2015	EMA	Eisai Europe Ltd
Feb. 13, 2015	FDA	EISAI INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hypertension	1111.91	60.19	295	1432	27066	2329292
Malignant neoplasm progression	832.26	60.19	200	1527	11928	2344430
Decreased appetite	629.86	60.19	193	1534	28698	2327660
Proteinuria	541.90	60.19	109	1618	2741	2353617
Diarrhoea	400.84	60.19	184	1543	83380	2272978
Palmar-plantar erythrodysaesthesia syndrome	389.54	60.19	89	1638	4112	2352246
Hepatic encephalopathy	284.12	60.19	58	1669	1549	2354809
Fatigue	279.25	60.19	145	1582	84728	2271630
Platelet count decreased	248.47	60.19	83	1644	15730	2340628
Vomiting	211.02	60.19	114	1613	71488	2284870
Nausea	195.26	60.19	127	1600	112062	2244296
Stomatitis	176.47	60.19	57	1670	9653	2346705
Malaise	159.02	60.19	87	1640	55498	2300860
Blood pressure increased	156.00	60.19	60	1667	16926	2339432
Hypothyroidism	113.82	60.19	34	1693	4423	2351935
Cholecystitis	112.22	60.19	29	1698	2211	2354147
Dehydration	107.94	60.19	50	1677	22245	2334113
Tumour haemorrhage	106.69	60.19	20	1707	334	2356024
Ascites	101.95	60.19	33	1694	5587	2350771
Weight decreased	99.39	60.19	51	1676	28320	2328038
Pyrexia	88.09	60.19	59	1668	53649	2302709
Pneumothorax	87.58	60.19	24	1703	2288	2354070
Abdominal pain	87.48	60.19	50	1677	34324	2322034
Arterial haemorrhage	84.32	60.19	15	1712	184	2356174
Asthenia	82.84	60.19	54	1673	46872	2309486
Oral pain	74.22	60.19	23	1704	3374	2352984
Tracheal fistula	74.15	60.19	10	1717	12	2356346
Epistaxis	70.23	60.19	29	1698	9750	2346608
Pneumonia	68.60	60.19	49	1678	49247	2307111
Hepatic function abnormal	68.41	60.19	25	1702	6067	2350291
Fistula	61.59	60.19	17	1710	1662	2354696
Headache	61.07	60.19	56	1671	80123	2276235

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Decreased appetite	1056.84	56.10	343	2381	23528	1720529
Malignant neoplasm progression	885.95	56.10	266	2458	13892	1730165
Diarrhoea	784.71	56.10	343	2381	53509	1690548
Hypertension	730.54	56.10	248	2476	19200	1724857
Hepatic encephalopathy	626.74	56.10	140	2584	2152	1741905
Proteinuria	586.12	56.10	138	2586	2706	1741351
Fatigue	530.36	56.10	258	2466	50523	1693534
Palmar-plantar erythrodysaesthesia syndrome	404.52	56.10	107	2617	3400	1740657
Malaise	299.31	56.10	148	2576	29417	1714640
Blood pressure increased	293.83	56.10	109	2615	10644	1733413
Hypothyroidism	238.00	56.10	66	2658	2494	1741563
Dehydration	219.39	56.10	102	2622	17556	1726501
Nausea	196.99	56.10	137	2587	51059	1692998
Weight decreased	189.11	56.10	100	2624	22653	1721404
Dysphonia	182.87	56.10	58	2666	3497	1740560
Pyrexia	168.53	56.10	120	2604	46280	1697777
Vomiting	150.35	56.10	104	2620	38211	1705846
Stomatitis	147.95	56.10	55	2669	5349	1738708
Platelet count decreased	138.08	56.10	73	2651	16450	1727607
Tumour haemorrhage	134.08	56.10	31	2693	548	1743509
Ascites	128.21	56.10	50	2674	5536	1738521
Epistaxis	125.06	56.10	55	2669	8251	1735806
Ammonia increased	122.11	56.10	31	2693	823	1743234
Hepatic failure	122.05	56.10	49	2675	5854	1738203
Asthenia	112.59	56.10	84	2640	34586	1709471
Oesophageal varices haemorrhage	108.15	56.10	26	2698	547	1743510
Cholecystitis	98.92	56.10	30	2694	1550	1742507
Pneumonia	97.38	56.10	87	2637	46095	1697962
Hepatic function abnormal	97.32	56.10	44	2680	7030	1737027
Renal cancer	96.08	56.10	27	2697	1064	1742993
Blood thyroid stimulating hormone increased	95.32	56.10	24	2700	615	1743442
Liver carcinoma ruptured	93.02	56.10	16	2708	51	1744006
Pneumothorax	90.57	56.10	32	2692	2680	1741377
Death	89.67	56.10	112	2612	87331	1656726
Abdominal pain	85.49	56.10	59	2665	21431	1722626
Oral pain	84.60	56.10	26	2698	1404	1742653
Blood bilirubin increased	74.06	56.10	35	2689	6175	1737882
Constipation	71.20	56.10	46	2678	14954	1729103
C-reactive protein increased	66.60	56.10	32	2692	5853	1738204
Dyspnoea	65.15	56.10	74	2650	51985	1692072
Aspartate aminotransferase increased	63.72	56.10	38	2686	10718	1733339
Cholangitis	63.52	56.10	20	2704	1169	1742888
Rash	60.64	56.10	62	2662	38631	1705426

Pharmacologic Action:

Source	Code	Description
ATC	L01XE29	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Protein kinase inhibitors
CHEBI has role	CHEBI:71031	orphan drug
CHEBI has role	CHEBI:35610	antineoplastic agent
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000020000	Receptor Tyrosine Kinase Inhibitors

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Follicular thyroid carcinoma	indication	255028004	DOID:3962
Papillary thyroid carcinoma	indication	255029007	DOID:3969
Renal cell carcinoma	indication	702391001	DOID:4450

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.09	acidic
pKa2	12.74	acidic
pKa3	13.02	acidic
pKa4	4.67	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 10MG BASE	LENVIMA	EISAI INC	N206947	Feb. 13, 2015	RX	CAPSULE	ORAL	9006256	July 27, 2027	METHOD FOR TREATING THYROID CARCINOMA INCLUDING DIFFERENTIATED THYROID CANCER
EQ 4MG BASE	LENVIMA	EISAI INC	N206947	Feb. 13, 2015	RX	CAPSULE	ORAL	9006256	July 27, 2027	METHOD FOR TREATING THYROID CARCINOMA INCLUDING DIFFERENTIATED THYROID CANCER

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 10MG BASE	LENVIMA	EISAI INC	N206947	Feb. 13, 2015	RX	CAPSULE	ORAL	Feb. 13, 2020	NEW CHEMICAL ENTITY
EQ 4MG BASE	LENVIMA	EISAI INC	N206947	Feb. 13, 2015	RX	CAPSULE	ORAL	Feb. 13, 2020	NEW CHEMICAL ENTITY
EQ 10MG BASE	LENVIMA	EISAI INC	N206947	Feb. 13, 2015	RX	CAPSULE	ORAL	Aug. 15, 2021	FIRST-LINE TREATMENT OF PATIENTS WITH UNRESECTABLE HEPATOCELLULAR CARCINOMA (HCC)
EQ 4MG BASE	LENVIMA	EISAI INC	N206947	Feb. 13, 2015	RX	CAPSULE	ORAL	Aug. 15, 2021	FIRST-LINE TREATMENT OF PATIENTS WITH UNRESECTABLE HEPATOCELLULAR CARCINOMA (HCC)
EQ 10MG BASE	LENVIMA	EISAI INC	N206947	Feb. 13, 2015	RX	CAPSULE	ORAL	Feb. 13, 2022	TREATMENT OF PATIENTS WITH LOCALLY RECURRENT OR METASTATIC, PROGRESSIVE, RADIOACTIVE IODINE REFRACTORY DIFFERENTIATED THYROID CANCER
EQ 4MG BASE	LENVIMA	EISAI INC	N206947	Feb. 13, 2015	RX	CAPSULE	ORAL	Feb. 13, 2022	TREATMENT OF PATIENTS WITH LOCALLY RECURRENT OR METASTATIC, PROGRESSIVE, RADIOACTIVE IODINE REFRACTORY DIFFERENTIATED THYROID CANCER
EQ 10MG BASE	LENVIMA	EISAI INC	N206947	Feb. 13, 2015	RX	CAPSULE	ORAL	Sept. 17, 2022	TREATMENT OF ADVANCED ENDOMETRIAL CARCINOMA THAT IS NOT MICROSATELLITE INSTABILITY-HIGH OR MISMATCH REPAIR DEFICIENT, WHO HAVE DISEASE PROGRESSION FOLLOWING PRIOR SYSTEMIC THERAPY AND ARE NOT CANDIDATES FOR CURATIVE SURGERY OR RADIATION
EQ 4MG BASE	LENVIMA	EISAI INC	N206947	Feb. 13, 2015	RX	CAPSULE	ORAL	Sept. 17, 2022	TREATMENT OF ADVANCED ENDOMETRIAL CARCINOMA THAT IS NOT MICROSATELLITE INSTABILITY-HIGH OR MISMATCH REPAIR DEFICIENT, WHO HAVE DISEASE PROGRESSION FOLLOWING PRIOR SYSTEMIC THERAPY AND ARE NOT CANDIDATES FOR CURATIVE SURGERY OR RADIATION
EQ 10MG BASE	LENVIMA	EISAI INC	N206947	Feb. 13, 2015	RX	CAPSULE	ORAL	Aug. 15, 2025	INDICATED FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH UNRESECTABLE HEPATOCELLULAR CARCINOMA (HCC)
EQ 4MG BASE	LENVIMA	EISAI INC	N206947	Feb. 13, 2015	RX	CAPSULE	ORAL	Aug. 15, 2025	INDICATED FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH UNRESECTABLE HEPATOCELLULAR CARCINOMA (HCC)

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN	INHIBITOR	Ki	8.82	CHEMBL	DRUG LABEL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN	INHIBITOR	IC50	8.40	SCIENTIFIC LITERATURE	DRUG LABEL
Vascular endothelial growth factor receptor 3	Kinase	P35916	VGFR3_HUMAN	INHIBITOR	IC50	8.28	SCIENTIFIC LITERATURE	DRUG LABEL
Fibroblast growth factor receptor 1	Kinase	P11362	FGFR1_HUMAN	INHIBITOR	IC50	7.34	SCIENTIFIC LITERATURE	DRUG LABEL
Platelet-derived growth factor receptor alpha	Kinase	P16234	PGFRA_HUMAN	INHIBITOR	IC50	7.29	SCIENTIFIC LITERATURE	DRUG LABEL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN	INHIBITOR	IC50	7	SCIENTIFIC LITERATURE	DRUG LABEL
Vascular endothelial growth factor receptor 1	Kinase	P17948	VGFR1_HUMAN	INHIBITOR	IC50	7.66	SCIENTIFIC LITERATURE	DRUG LABEL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN	INHIBITOR	IC50	7.41	SCIENTIFIC LITERATURE
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN	INHIBITOR	IC50	5.19	SCIENTIFIC LITERATURE

External reference:

ID	Source
D09919	KEGG_DRUG
4034239	VUID
N0000191429	NUI
C2986924	UMLSCUI
3J78384F61	UNII
857890-39-2	SECONDARY_CAS_RN
714109005	SNOMEDCT_US
1603296	RXNORM
015899	NDDF
4034239	VANDF
d08346	MMSL
714108002	SNOMEDCT_US
9823820	PUBCHEM_CID
CHEBI:85994	CHEBI
9361	INN_ID
LEV	PDB_CHEM_ID
DB09078	DRUGBANK_ID
CHEMBL1289601	ChEMBL_ID
CHEMBL2105704	ChEMBL_ID
7426	IUPHAR_LIGAND_ID
C531958	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Lenvima	HUMAN PRESCRIPTION DRUG LABEL	1	62856-704	CAPSULE	4 mg	ORAL	NDA	18 sections
Lenvima	HUMAN PRESCRIPTION DRUG LABEL	1	62856-708	CAPSULE	4 mg	ORAL	NDA	18 sections
Lenvima	HUMAN PRESCRIPTION DRUG LABEL	1	62856-710	CAPSULE	10 mg	ORAL	NDA	18 sections
Lenvima	HUMAN PRESCRIPTION DRUG LABEL	1	62856-712	CAPSULE	4 mg	ORAL	NDA	18 sections
Lenvima	HUMAN PRESCRIPTION DRUG LABEL	2	62856-714	KIT	10 mg	None	NDA	18 sections
Lenvima	HUMAN PRESCRIPTION DRUG LABEL	2	62856-714	KIT	4 mg	None	NDA	18 sections
Lenvima	HUMAN PRESCRIPTION DRUG LABEL	2	62856-718	KIT	4 mg	None	NDA	18 sections
Lenvima	HUMAN PRESCRIPTION DRUG LABEL	2	62856-718	KIT	10 mg	None	NDA	18 sections
Lenvima	HUMAN PRESCRIPTION DRUG LABEL	1	62856-720	CAPSULE	10 mg	ORAL	NDA	18 sections
Lenvima	HUMAN PRESCRIPTION DRUG LABEL	2	62856-724	KIT	10 mg	None	NDA	18 sections
Lenvima	HUMAN PRESCRIPTION DRUG LABEL	2	62856-724	KIT	4 mg	None	NDA	18 sections