All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5211	811803-05-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: rivoceranib apatinib apatinib mesylate apatinib mesilate YN968D1	Apatinib is an oral tyrosine kinase inhibitor approved in China for the treatment of patients with advanced metastatic gastric cancer. Molecular weight: 397.48 Formula: C24H23N5O CLOGP: 3.72 LIPINSKI: 0 HAC: 6 HDO: 2 TPSA: 90.70 ALOGS: -4.52 ROTB: 6

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
None	China Food and Drug Administration (CFDA)

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
Myelosuppression	88.37	69.88	19	170	23684	63465149

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
Bone marrow failure	69.72	59.48	17	116	29236	34927562

FDA Adverse Event Reporting System (Geriatric)

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	90.05	61.41	22	316	33112	79710938
Myelosuppression	80.87	61.41	21	317	40275	79703775
Bone marrow failure	62.25	61.41	18	320	51089	79692961

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors

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

Disease	Relation	SNOMED_ID	DOID
Secondary malignant neoplasm of stomach	indication	94606003

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.66	acidic
pKa2	6.69	Basic
pKa3	4.82	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN	INHIBITOR	IC50	9		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Mitogen-activated protein kinase kinase kinase MLT	Kinase	Q9NYL2	MLTK_HUMAN		Kd	5.32		CHEMBL
Receptor-interacting serine/threonine-protein kinase 3	Kinase	Q9Y572	RIPK3_HUMAN		Kd	5.62		CHEMBL
Tyrosine-protein kinase CSK	Kinase	P41240	CSK_HUMAN	INHIBITOR	IC50	6.28		IUPHAR
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN	INHIBITOR	IC50	6.28		SCIENTIFIC LITERATURE
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN	INHIBITOR	IC50	7.89		SCIENTIFIC LITERATURE
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN	INHIBITOR	IC50	6.37		SCIENTIFIC LITERATURE

External reference:

ID	Source
C2346836	UMLSCUI
CHEMBL3186534	ChEMBL_ID
11315474	PUBCHEM_CID
DB14765	DRUGBANK_ID
CHEMBL3545414	ChEMBL_ID
7648	IUPHAR_LIGAND_ID
018934	NDDF
10596	INN_ID
C553458	MESH_SUPPLEMENTAL_RECORD_UI
5S371K6132	UNII

Pharmaceutical products:

None