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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	658.70	27.44	399	7013	195957	46482693
Malignant neoplasm progression	593.79	27.44	260	7152	64666	46613984
Proteinuria	424.47	27.44	141	7271	16412	46662238
Decreased appetite	344.47	27.44	267	7145	193569	46485081
Palmar-plantar erythrodysaesthesia syndrome	277.99	27.44	109	7303	20342	46658308
Hepatic encephalopathy	214.95	27.44	75	7337	10082	46668568
Diarrhoea	145.92	27.44	291	7121	559311	46119339
Blood pressure increased	94.17	27.44	108	7304	126558	46552092
Platelet count decreased	93.05	27.44	96	7316	99928	46578722
Stomatitis	89.05	27.44	79	7333	68218	46610432
Cholecystitis	85.39	27.44	43	7369	14423	46664227
Hypothyroidism	84.72	27.44	56	7356	31282	46647368
Tumour haemorrhage	79.11	27.44	22	7390	1393	46677257
Tracheal fistula	69.04	27.44	11	7401	37	46678613
Drug ineffective	65.66	27.44	14	7398	677824	46000826
Fatigue	64.66	27.44	227	7185	608470	46070180
Arterial haemorrhage	49.44	27.44	16	7396	1702	46676948
Pneumothorax	46.59	27.44	29	7383	14600	46664050
Oral pain	43.30	27.44	34	7378	24763	46653887
Blood thyroid stimulating hormone increased	42.28	27.44	20	7392	5849	46672801
Fistula	42.02	27.44	22	7390	7988	46670662
Ascites	39.25	27.44	38	7374	36546	46642104
Vomiting	38.82	27.44	158	7254	452636	46226014
Dehydration	37.54	27.44	80	7332	159460	46519190
Epistaxis	35.06	27.44	47	7365	64258	46614392
Nephrotic syndrome	33.11	27.44	16	7396	4905	46673745
Tracheal haemorrhage	32.23	27.44	7	7405	156	46678494
Dysphonia	30.57	27.44	34	7378	38380	46640270
Protein urine present	29.53	27.44	15	7397	5116	46673534
Malaise	29.44	27.44	117	7295	331115	46347535
Ammonia increased	28.75	27.44	14	7398	4363	46674287
Drug hypersensitivity	28.12	27.44	3	7409	243822	46434828
Cerebral haemorrhage	27.70	27.44	28	7384	28343	46650307

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	671.71	24.02	504	10608	149406	29791960
Malignant neoplasm progression	635.89	24.02	371	10741	71916	29869450
Hepatic encephalopathy	601.02	24.02	218	10894	13974	29927392
Proteinuria	433.06	24.02	178	10934	15967	29925399
Hypertension	394.36	24.02	339	10773	121015	29820351
Palmar-plantar erythrodysaesthesia syndrome	392.16	24.02	162	10950	14708	29926658
Diarrhoea	336.45	24.02	506	10606	333597	29607769
Hypothyroidism	200.89	24.02	102	11010	14861	29926505
Fatigue	174.00	24.02	372	10740	320301	29621065
Tumour haemorrhage	157.86	24.02	52	11060	2476	29938890
Blood pressure increased	141.60	24.02	153	10959	71775	29869591
Dysphonia	131.34	24.02	84	11028	18948	29922418
Liver carcinoma ruptured	111.46	24.02	22	11090	116	29941250
Malaise	102.01	24.02	204	10908	166758	29774608
Oesophageal varices haemorrhage	93.21	24.02	37	11075	3014	29938352
Ascites	91.69	24.02	88	11024	35833	29905533
Hepatic failure	89.93	24.02	85	11027	33958	29907408
Ammonia increased	81.47	24.02	37	11075	4204	29937162
Stomatitis	74.44	24.02	80	11032	37199	29904167
Cholecystitis	70.34	24.02	44	11068	9535	29931831
Drug ineffective	69.94	24.02	20	11092	340367	29600999
Dehydration	67.13	24.02	144	10968	123395	29817971
Renal cancer	64.45	24.02	31	11081	4009	29937357
Blood thyroid stimulating hormone increased	61.52	24.02	27	11085	2829	29938537
Oral pain	58.45	24.02	39	11073	9430	29931936
Epistaxis	56.40	24.02	83	11029	52898	29888468
Pneumothorax	55.77	24.02	47	11065	16146	29925220
Blood bilirubin increased	55.21	24.02	68	11044	36568	29904798
Cholangitis	52.70	24.02	34	11078	7768	29933598
Tumour rupture	50.98	24.02	12	11100	159	29941207
Weight decreased	49.33	24.02	145	10967	150776	29790590
Hepatic function abnormal	46.50	24.02	67	11045	41878	29899488
Hyperammonaemia	42.15	24.02	26	11086	5494	29935872
Condition aggravated	37.05	24.02	4	11108	137862	29803504
Toxicity to various agents	37.04	24.02	10	11102	177173	29764193
Vomiting	36.79	24.02	170	10942	219648	29721718
Tracheal fistula	36.42	24.02	8	11104	76	29941290
Portal vein thrombosis	36.20	24.02	20	11092	3444	29937922
Drug interaction	35.25	24.02	15	11097	199553	29741813
Rhythm idioventricular	31.17	24.02	9	11103	274	29941092
Protein urine present	30.27	24.02	20	11092	4755	29936611
Platelet count decreased	29.08	24.02	96	11016	106033	29835333
Off label use	28.89	24.02	30	11082	249260	29692106
Cholecystitis acute	28.32	24.02	20	11092	5297	29936069
Gastrointestinal perforation	27.52	24.02	17	11095	3599	29937767
Tracheo-oesophageal fistula	27.44	24.02	9	11103	422	29940944
Nausea	27.42	24.02	196	10916	296761	29644605
Haemobilia	26.39	24.02	8	11104	289	29941077
Taste disorder	25.56	24.02	16	11096	3467	29937899

Pharmacologic Action:

Source	Code	Description
ATC	L01EX08	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors
FDA MoA	N0000020000	Receptor Tyrosine Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
CHEBI has role	CHEBI:35610	cytostatic
CHEBI has role	CHEBI:62434	alk inhibitor
CHEBI has role	CHEBI:63457	fibroblast growth factor receptor antagonists
CHEBI has role	CHEBI:65207	vegfr inhibitors
CHEBI has role	CHEBI:71031	orphan drugs

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)

None

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	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
857890-39-2	SECONDARY_CAS_RN
4034239	VANDF
C2606791	UMLSCUI
CHEBI:85994	CHEBI
LEV	PDB_CHEM_ID
CHEMBL1289601	ChEMBL_ID
CHEMBL2105704	ChEMBL_ID
DB09078	DRUGBANK_ID
C531958	MESH_SUPPLEMENTAL_RECORD_UI
9823820	PUBCHEM_CID
7426	IUPHAR_LIGAND_ID
9361	INN_ID
EE083865G2	UNII
1603296	RXNORM
232716	MMSL
294829	MMSL
294831	MMSL
30895	MMSL
d08346	MMSL
015899	NDDF
015900	NDDF
714108002	SNOMEDCT_US
714109005	SNOMEDCT_US
735068004	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Lenvima	HUMAN PRESCRIPTION DRUG LABEL	1	62856-704	CAPSULE	4 mg	ORAL	NDA	29 sections
Lenvima	HUMAN PRESCRIPTION DRUG LABEL	1	62856-708	CAPSULE	4 mg	ORAL	NDA	29 sections
Lenvima	HUMAN PRESCRIPTION DRUG LABEL	1	62856-710	CAPSULE	10 mg	ORAL	NDA	29 sections
Lenvima	HUMAN PRESCRIPTION DRUG LABEL	1	62856-712	CAPSULE	4 mg	ORAL	NDA	29 sections
Lenvima	HUMAN PRESCRIPTION DRUG LABEL	1	62856-720	CAPSULE	10 mg	ORAL	NDA	29 sections