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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	2544	557795-19-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: sunitinib sunitinib malate sutent SU-011248 SU-010398 PHA-290940AD	An indole and pyrrole derivative that inhibits VEGFR-2 and PDGFR BETA RECEPTOR TYROSINE KINASES. It is used as an antineoplastic agent for the treatment of GASTROINTESTINAL STROMAL TUMORS, and for treatment of advanced or metastatic RENAL CELL CARCINOMA. Molecular weight: 398.48 Formula: C22H27FN4O2 CLOGP: 3 LIPINSKI: 0 HAC: 6 HDO: 3 TPSA: 77.23 ALOGS: -4.11 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

sunitinib
sunitinib malate
sutent
SU-011248
SU-010398
PHA-290940AD

An indole and pyrrole derivative that inhibits VEGFR-2 and PDGFR BETA RECEPTOR TYROSINE KINASES. It is used as an antineoplastic agent for the treatment of GASTROINTESTINAL STROMAL TUMORS, and for treatment of advanced or metastatic RENAL CELL CARCINOMA.

Molecular weight: 398.48
Formula: C22H27FN4O2
CLOGP: 3
LIPINSKI: 0
HAC: 6
HDO: 3
TPSA: 77.23
ALOGS: -4.11
ROTB: 7

Status: OFP

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

Drug dosage:

Dose	Unit	Route
33	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	54.50 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	4 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	25 mg/mL	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.34 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Jan. 26, 2006	FDA	CPPI CV
July 19, 2006	EMA	Pfizer Limited

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
Disease progression	1124.34	19.62	704	29024	122054	63337240
Palmar-plantar erythrodysaesthesia syndrome	828.87	19.62	335	29393	22680	63436614
Neoplasm progression	714.30	19.62	346	29382	36082	63423212
Death	553.85	19.62	772	28956	373609	63085685
Dysgeusia	406.46	19.62	260	29468	46450	63412844
Oral pain	402.97	19.62	217	29511	28177	63431117
Hypothyroidism	385.12	19.62	243	29485	42389	63416905
Yellow skin	359.76	19.62	101	29627	2179	63457115
Diarrhoea	345.21	19.62	915	28813	714451	62744843
Thrombocytopenia	322.61	19.62	375	29353	150782	63308512

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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
Disease progression	2105.45	14.82	1470	45202	106607	34803652
Neoplasm progression	1330.45	14.82	640	46032	22660	34887599
Palmar-plantar erythrodysaesthesia syndrome	1241.74	14.82	552	46120	16243	34894016
Death	772.56	14.82	1657	45015	396392	34513867
Dysgeusia	688.60	14.82	433	46239	26064	34884195
Yellow skin	476.42	14.82	157	46515	1965	34908294
Diarrhoea	453.88	14.82	1339	45333	388573	34521686
Stomatitis	444.96	14.82	403	46269	42111	34868148
Osteonecrosis of jaw	431.36	14.82	279	46393	17610	34892649
Oral pain	383	14.82	216	46456	10611	34899648

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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
Disease progression	2503.55	15.69	1674	64428	182688	79495598
Palmar-plantar erythrodysaesthesia syndrome	1838.46	15.69	773	65329	32361	79645925
Neoplasm progression	1818.81	15.69	877	65225	50805	79627481
Dysgeusia	1008.58	15.69	614	65488	56563	79621723
Death	889.77	15.69	1639	64463	564875	79113411
Diarrhoea	766.62	15.69	2008	64094	878481	78799805
Oral pain	701.70	15.69	395	65707	31403	79646883
Yellow skin	700.72	15.69	212	65890	3293	79674993
Hypothyroidism	630.48	15.69	443	65659	51949	79626337
Stomatitis	610.80	15.69	678	65424	146079	79532207

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01EX01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:48422	angiogenesis antagonist
CHEBI has role	CHEBI:50846	Immunologic factor
CHEBI has role	CHEBI:62434	ALK inhibitor
CHEBI has role	CHEBI:63726	neuroprotective agents
CHEBI has role	CHEBI:65207	vascular endothelial growth factor receptor inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000175076	Protein Kinase Inhibitors
MeSH PA	D020533	Angiogenesis 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
Gastrointestinal stromal tumor	indication	420120006	DOID:9253
Renal cell carcinoma	indication	702391001	DOID:4450
Pancreatic Neuroendocrine Tumor	indication	717919005
Acute hemorrhage	contraindication	8573003
Hyperkalemia	contraindication	14140009
Hyperbilirubinemia	contraindication	14783006	DOID:2741
Torsades de pointes	contraindication	31722008
Hyperthyroidism	contraindication	34486009	DOID:7998
Hypothyroidism	contraindication	40930008	DOID:1459
Hypokalemia	contraindication	43339004

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🐶 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	10.52	acidic
pKa2	11.68	acidic
pKa3	12.32	acidic
pKa4	9.32	Basic

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Orange Book patent data (new drug applications)

None

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
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN	INHIBITOR	Kd	9.66	CHEMBL	CHEMBL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN	INHIBITOR	Kd	9.70	CHEMBL	CHEMBL
Vascular endothelial growth factor receptor 3	Kinase	P35916	VGFR3_HUMAN	INHIBITOR	Ki	7.77	CHEMBL	CHEMBL
Macrophage colony-stimulating factor 1 receptor	Kinase	P07333	CSF1R_HUMAN	INHIBITOR	Kd	8.70	CHEMBL	CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN	INHIBITOR	Kd	10.12	CHEMBL	CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN	INHIBITOR	Kd	9.68	CHEMBL	CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN	INHIBITOR	IC50	8.80	IUPHAR	DRUG LABEL
Vascular endothelial growth factor receptor 1	Kinase	P17948	VGFR1_HUMAN	INHIBITOR	IC50	7.23	SCIENTIFIC LITERATURE	DRUG LABEL
Platelet-derived growth factor receptor alpha	Kinase	P16234	PGFRA_HUMAN	INHIBITOR	IC50	6.96	SCIENTIFIC LITERATURE	DRUG LABEL
Pyridoxal kinase	Kinase	O00764	PDXK_HUMAN		Kd	5.22	CHEMBL

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External reference:

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ID	Source
B49	PDB_CHEM_ID
011192	NDDF
011193	NDDF
20930	MMSL
21012	MMSL
341031-54-7	SECONDARY_CAS_RN
349534	MMSL
357977	RXNORM
4025079	VUID
4025079	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Sunitinib Malate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-8199	CAPSULE	12.50 mg	ORAL	ANDA	31 sections
Sunitinib Malate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-8224	CAPSULE	25 mg	ORAL	ANDA	31 sections
Sunitinib Malate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-8229	CAPSULE	37.50 mg	ORAL	ANDA	31 sections
Sunitinib Malate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-8231	CAPSULE	50 mg	ORAL	ANDA	31 sections
Sunitinib Malate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-6678	CAPSULE	12.50 mg	ORAL	ANDA	30 sections
Sunitinib Malate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-6678	CAPSULE	12.50 mg	ORAL	ANDA	30 sections
Sunitinib Malate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-6679	CAPSULE	25 mg	ORAL	ANDA	30 sections
Sunitinib Malate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-6679	CAPSULE	25 mg	ORAL	ANDA	30 sections
Sunitinib Malate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-6680	CAPSULE	50 mg	ORAL	ANDA	30 sections
Sunitinib Malate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-6680	CAPSULE	50 mg	ORAL	ANDA	30 sections

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