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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	4225	319460-85-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: axitinib inlyta AG 013736 AG-013736	A benzamide and indazole derivative that acts as a TYROSINE KINASE inhibitor of the VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR. It is used in the treatment of advanced RENAL CELL CARCINOMA. Molecular weight: 386.47 Formula: C22H18N4OS CLOGP: 3.19 LIPINSKI: 0 HAC: 5 HDO: 2 TPSA: 70.67 ALOGS: -5.85 ROTB: 5 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

axitinib
inlyta
AG 013736
AG-013736

A benzamide and indazole derivative that acts as a TYROSINE KINASE inhibitor of the VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR. It is used in the treatment of advanced RENAL CELL CARCINOMA.

Molecular weight: 386.47
Formula: C22H18N4OS
CLOGP: 3.19
LIPINSKI: 0
HAC: 5
HDO: 2
TPSA: 70.67
ALOGS: -5.85
ROTB: 5

Status: ONP

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

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	5 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	4.30 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Hosey CM, Chan R, Benet LZ
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma)	0.00 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Jan. 27, 2012	FDA	PFIZER

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
Neoplasm progression	606.52	23.51	212	7838	36216	63444756
Diarrhoea	346.84	23.51	436	7614	714930	62766042
Disease progression	305.38	23.51	191	7859	122567	63358405
Death	291.56	23.51	293	7757	374088	63106884
Hypertension	223.10	23.51	222	7828	279081	63201891
Palmar-plantar erythrodysaesthesia syndrome	218.55	23.51	89	7961	22926	63458046
Dysphonia	181.69	23.51	98	7952	47516	63433456
Decreased appetite	149.53	23.51	171	7879	250881	63230091
Stomatitis	140.42	23.51	126	7924	138599	63342373
Blood pressure increased	134.85	23.51	132	7918	161930	63319042

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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
Neoplasm progression	1278.46	19.50	485	19457	22815	34914174
Dysphonia	1133.82	19.50	445	19497	22938	34914051
Disease progression	793.07	19.50	582	19360	107495	34829494
Diarrhoea	696.78	19.50	971	18971	388941	34548048
Hypertension	512.35	19.50	500	19442	135943	34801046
Fatigue	493.01	19.50	806	19136	369847	34567142
Death	461.11	19.50	814	19128	397235	34539754
Palmar-plantar erythrodysaesthesia syndrome	361.23	19.50	181	19761	16614	34920375
Decreased appetite	314.33	19.50	428	19514	165964	34771025
Blood pressure increased	268.22	19.50	289	19653	87813	34849176

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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
Neoplasm progression	1793.44	19.43	667	26058	51015	79666648
Dysphonia	1213.07	19.43	517	26208	56355	79661308
Disease progression	1012.68	19.43	677	26048	183685	79533978
Diarrhoea	954.36	19.43	1308	25417	879181	78838482
Death	821.85	19.43	975	25750	565539	79152124
Hypertension	635.46	19.43	661	26064	330331	79387332
Fatigue	572.69	19.43	1070	25655	928657	78789006
Palmar-plantar erythrodysaesthesia syndrome	546.96	19.43	252	26473	32882	79684781
Decreased appetite	463.91	19.43	571	26154	341847	79375816
Blood pressure increased	372.32	19.43	404	26321	210956	79506707

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01EK01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:38637	tyrosine kinase inhibitors
CHEBI has role	CHEBI:65207	vascular endothelial growth factor receptor inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000020000	Receptor Tyrosine Kinase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors

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

Disease	Relation	SNOMED_ID	DOID
Renal cell carcinoma	indication	702391001	DOID:4450

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.57	acidic
pKa2	12.18	acidic
pKa3	4.85	Basic
pKa4	1.98	Basic

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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
1MG	INLYTA	PF PRISM CV	N202324	Jan. 27, 2012	RX	TABLET	ORAL	10570202	Feb. 3, 2035	IN COMBINATION WITH PEMBROLIZUMAB FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA
1MG	INLYTA	PF PRISM CV	N202324	Jan. 27, 2012	RX	TABLET	ORAL	10869924	Jan. 12, 2037	AXITINIB IN COMBINATION WITH AVELUMAB FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA
5MG	INLYTA	PF PRISM CV	N202324	Jan. 27, 2012	RX	TABLET	ORAL	10570202	Feb. 3, 2035	IN COMBINATION WITH PEMBROLIZUMAB FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA
5MG	INLYTA	PF PRISM CV	N202324	Jan. 27, 2012	RX	TABLET	ORAL	10869924	Jan. 12, 2037	AXITINIB IN COMBINATION WITH AVELUMAB FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Vascular endothelial growth factor receptor 3	Kinase	P35916	VGFR3_HUMAN	INHIBITOR	Kd	6.77	CHEMBL	CHEMBL
Vascular endothelial growth factor receptor 1	Kinase	P17948	VGFR1_HUMAN	INHIBITOR	Kd	8.24	CHEMBL	CHEMBL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN	INHIBITOR	Kd	8.23	CHEMBL	CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN		Kd	9.31	CHEMBL
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		Kd	5.64	CHEMBL
Breakpoint cluster region protein	Kinase	P11274	BCR_HUMAN		Kd	6.73	CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	5.57	CHEMBL
Tyrosine-protein kinase Yes	Kinase	P07947	YES_HUMAN		Kd	5.57	CHEMBL
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN		Kd	7.51	CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		Kd	7	CHEMBL

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External reference:

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ID	Source
AXI	PDB_CHEM_ID
014143	NDDF
1242999	RXNORM
187097	MMSL
28294	MMSL
4031332	VUID
4031332	VANDF
427882000	SNOMEDCT_US
429507005	SNOMEDCT_US
5659	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
INLYTA	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0145	TABLET, FILM COATED	1 mg	ORAL	NDA	32 sections
INLYTA	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0145	TABLET, FILM COATED	1 mg	ORAL	NDA	32 sections
INLYTA	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0151	TABLET, FILM COATED	5 mg	ORAL	NDA	32 sections
INLYTA	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0151	TABLET, FILM COATED	5 mg	ORAL	NDA	32 sections
INLYTA	HUMAN PRESCRIPTION DRUG LABEL	1	63539-026	TABLET, FILM COATED	1 mg	ORAL	NDA	32 sections
INLYTA	HUMAN PRESCRIPTION DRUG LABEL	1	63539-026	TABLET, FILM COATED	1 mg	ORAL	NDA	32 sections
INLYTA	HUMAN PRESCRIPTION DRUG LABEL	1	63539-044	TABLET, FILM COATED	5 mg	ORAL	NDA	32 sections
INLYTA	HUMAN PRESCRIPTION DRUG LABEL	1	63539-044	TABLET, FILM COATED	5 mg	ORAL	NDA	32 sections

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