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cabozantinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	4715	849217-68-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: cabozantinib malate cabozantinib (S)-malate cabozantinib cometriq XL184 cabozantinib S-malate cabometyx	Cabozantinib inhibits the tyrosine kinase activity of MET, VEGFR-1, -2 and -3, AXL, RET, ROS1, TYRO3, MER, KIT, TRKB, FLT-3, and TIE-2. These receptor tyrosine kinases are involved in both normal cellular function and pathologic processes such as oncogenesis, metastasis, tumor angiogenesis, drug resistance, and maintenance of the tumor microenvironment. Molecular weight: 501.51 Formula: C28H24FN3O5 CLOGP: 4.44 LIPINSKI: 1 HAC: 8 HDO: 2 TPSA: 98.78 ALOGS: -5.40 ROTB: 8 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

cabozantinib malate
cabozantinib (S)-malate
cabozantinib
cometriq
XL184
cabozantinib S-malate
cabometyx

Cabozantinib inhibits the tyrosine kinase activity of MET, VEGFR-1, -2 and -3, AXL, RET, ROS1, TYRO3, MER, KIT, TRKB, FLT-3, and TIE-2. These receptor tyrosine kinases are involved in both normal cellular function and pathologic processes such as oncogenesis, metastasis, tumor angiogenesis, drug resistance, and maintenance of the tumor microenvironment.

Molecular weight: 501.51
Formula: C28H24FN3O5
CLOGP: 4.44
LIPINSKI: 1
HAC: 8
HDO: 2
TPSA: 98.78
ALOGS: -5.40
ROTB: 8

Status: ONP

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

Drug dosage:

Dose	Unit	Route
60	mg	O

ADMET properties:

None

Approvals:

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Date	Agency	Company
March 21, 2014	EMA	TMC Pharma Services Ltd
March 25, 2020	PMDA	Takeda Pharmaceutical Company Limited
Nov. 29, 2012	FDA	EXELIXIS

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FDA Adverse Event Reporting System (Female)

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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
Palmar-plantar erythrodysaesthesia syndrome	899.15	25.15	265	9018	22750	63456989
Malignant neoplasm progression	688.52	25.15	302	8981	81819	63397920
Diarrhoea	335.93	25.15	462	8821	714904	62764835
Hepatic function abnormal	214.94	25.15	106	9177	37036	63442703
Decreased appetite	205.27	25.15	216	9067	250836	63228903
Hypothyroidism	170.44	25.15	95	9188	42537	63437202
Taste disorder	160.09	25.15	64	9219	13598	63466141
Hypertension	139.52	25.15	187	9096	279116	63200623
Stomatitis	134.31	25.15	131	9152	138594	63341145
Hair colour changes	121.71	25.15	36	9247	3091	63476648

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FDA Adverse Event Reporting System (Male)

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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
Palmar-plantar erythrodysaesthesia syndrome	2324.70	20.55	723	22192	16072	34917944
Malignant neoplasm progression	1210.67	20.55	738	22177	87308	34846708
Diarrhoea	772.46	20.55	1097	21818	388815	34545201
Hypothyroidism	592.24	20.55	284	22631	20618	34913398
Hepatic function abnormal	589.94	20.55	365	22550	43998	34890018
Decreased appetite	494.72	20.55	575	22340	165817	34768199
Hypertension	421.00	20.55	481	22434	135962	34798054
Stomatitis	397.62	20.55	281	22634	42233	34891783
Taste disorder	381.88	20.55	152	22763	7003	34927013
Proteinuria	341.51	20.55	189	22726	18453	34915563

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FDA Adverse Event Reporting System (Geriatric)

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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
Palmar-plantar erythrodysaesthesia syndrome	2856.79	21.03	853	26439	32281	79684815
Malignant neoplasm progression	1027.60	21.03	616	26676	135374	79581722
Diarrhoea	898.08	21.03	1285	26007	879204	78837892
Hepatic function abnormal	809.59	21.03	426	26866	72681	79644415
Hypothyroidism	736.92	21.03	359	26933	52033	79665063
Decreased appetite	610.43	21.03	664	26628	341754	79375342
Hypertension	501.14	21.03	590	26702	330402	79386694
Taste disorder	484.90	21.03	188	27104	15635	79701461
Proteinuria	401.25	21.03	204	27088	32298	79684798
Stomatitis	350.51	21.03	334	26958	146423	79570673

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01EX07	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:38637	tyrosine kinase inhibitors
CHEBI has role	CHEBI:50266	Prodrugs
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000175076	Protein Kinase Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Liver cell carcinoma	indication	109841003	DOID:684
Medullary thyroid carcinoma	indication	255032005	DOID:3973
Renal cell carcinoma	indication	702391001	DOID:4450
Metastatic renal cell carcinoma	indication	702392008

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.15	acidic
pKa2	11.76	acidic
pKa3	4.95	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 20MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	8497284	Sept. 24, 2024	TREATMENT OF ADVANCED RENAL CELL CARCINOMA
EQ 20MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	8497284	Sept. 24, 2024	TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 20MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	8497284	Sept. 24, 2024	TREATMENT OF RENAL CELL CARCINOMA
EQ 20MG BASE	COMETRIQ	EXELIXIS	N203756	Nov. 29, 2012	RX	CAPSULE	ORAL	11098015	Jan. 15, 2030	METHOD OF TREATING MEDULLARY THYROID CANCER
EQ 20MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	11098015	Jan. 15, 2030	TREATMENT OF ADVANCED RENAL CELL CARCINOMA
EQ 20MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	11098015	Jan. 15, 2030	TREATMENT OF DIFFERENTIATED THYROID CANCER THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY
EQ 20MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	11098015	Jan. 15, 2030	TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 20MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	11098015	Jan. 15, 2030	TREATMENT OF RENAL CELL CARCINOMA
EQ 20MG BASE	COMETRIQ	EXELIXIS	N203756	Nov. 29, 2012	RX	CAPSULE	ORAL	8877776	Oct. 8, 2030	METHOD OF TREATING MEDULLARY THYROID CANCER
EQ 20MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	8877776	Oct. 8, 2030	TREATMENT OF DIFFERENTIATED THYROID CANCER THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 20MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	Jan. 22, 2024	FOR THE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA, AS A FIRST-LINE TREATMENT IN COMBINATION WITH NIVOLUMAB
EQ 20MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	Sept. 17, 2024	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH LOCALLY ADVANCED OR METASTATIC DIFFERENTIATED THYROID CANCER (DTC) THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY OR INELIGIBLE
EQ 20MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	Jan. 14, 2026	INDICATED FOR TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 20MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	Sept. 17, 2028	THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH LOCALLY ADVANCED OR METASTATIC DIFFERENTIATED THYROID CANCER (DTC) THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY OR INELIGIBLE
EQ 40MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	Jan. 22, 2024	FOR THE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA, AS A FIRST-LINE TREATMENT IN COMBINATION WITH NIVOLUMAB
EQ 40MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	Sept. 17, 2024	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH LOCALLY ADVANCED OR METASTATIC DIFFERENTIATED THYROID CANCER (DTC) THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY OR INELIGIBLE
EQ 40MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	Jan. 14, 2026	INDICATED FOR TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB
EQ 40MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	Sept. 17, 2028	THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH LOCALLY ADVANCED OR METASTATIC DIFFERENTIATED THYROID CANCER (DTC) THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY OR INELIGIBLE
EQ 60MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	Jan. 22, 2024	FOR THE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA, AS A FIRST-LINE TREATMENT IN COMBINATION WITH NIVOLUMAB
EQ 60MG BASE	CABOMETYX	EXELIXIS INC	N208692	April 25, 2016	RX	TABLET	ORAL	Sept. 17, 2024	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH LOCALLY ADVANCED OR METASTATIC DIFFERENTIATED THYROID CANCER (DTC) THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY OR INELIGIBLE

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN	INHIBITOR	IC50	8.34	WOMBAT-PK	DRUG LABEL
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN	INHIBITOR	IC50	7.95	WOMBAT-PK	DRUG LABEL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN	INHIBITOR	IC50	8.28	WOMBAT-PK	DRUG LABEL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN	INHIBITOR	IC50	10.46	WOMBAT-PK	DRUG LABEL
Angiopoietin-1 receptor	Kinase	Q02763	TIE2_HUMAN	INHIBITOR	IC50	7.85	WOMBAT-PK	DRUG LABEL
Hepatocyte growth factor receptor	Kinase	P08581	MET_HUMAN	INHIBITOR	IC50	8.89	WOMBAT-PK	DRUG LABEL
Ephrin type-A receptor 2	Kinase	P29317	EPHA2_HUMAN		Kd	6.13	CHEMBL
Vascular endothelial growth factor receptor 1	Kinase	P17948	VGFR1_HUMAN		IC50	7.92	CHEMBL
Vascular endothelial growth factor receptor 3	Kinase	P35916	VGFR3_HUMAN		IC50	8.22	CHEMBL
Tyrosine-protein kinase HCK	Kinase	P08631	HCK_HUMAN		Kd	5.96	CHEMBL

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External reference:

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ID	Source
014768	NDDF
014782	NDDF
1140909-48-3	SECONDARY_CAS_RN
1363267	RXNORM
194795	MMSL
1C39JW444G	UNII
240294	MMSL
25102847	PUBCHEM_CID
28993	MMSL
31609	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
CABOMETYX	HUMAN PRESCRIPTION DRUG LABEL	1	42388-023	TABLET	60 mg	ORAL	NDA	27 sections
CABOMETYX	HUMAN PRESCRIPTION DRUG LABEL	1	42388-023	TABLET	60 mg	ORAL	NDA	27 sections
CABOMETYX	HUMAN PRESCRIPTION DRUG LABEL	1	42388-023	TABLET	60 mg	ORAL	NDA	27 sections
CABOMETYX	HUMAN PRESCRIPTION DRUG LABEL	1	42388-024	TABLET	20 mg	ORAL	NDA	27 sections
CABOMETYX	HUMAN PRESCRIPTION DRUG LABEL	1	42388-024	TABLET	20 mg	ORAL	NDA	27 sections
CABOMETYX	HUMAN PRESCRIPTION DRUG LABEL	1	42388-024	TABLET	20 mg	ORAL	NDA	27 sections
CABOMETYX	HUMAN PRESCRIPTION DRUG LABEL	1	42388-025	TABLET	40 mg	ORAL	NDA	27 sections
CABOMETYX	HUMAN PRESCRIPTION DRUG LABEL	1	42388-025	TABLET	40 mg	ORAL	NDA	27 sections
CABOMETYX	HUMAN PRESCRIPTION DRUG LABEL	1	42388-025	TABLET	40 mg	ORAL	NDA	27 sections
COMETRIQ	HUMAN PRESCRIPTION DRUG LABEL	1	42388-013	CAPSULE	20 mg	ORAL	NDA	27 sections

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