Apatinib

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Apatinib is a drug catalogued in DrugCentral. DrugCentral lists 7 molecular targets, including KDR, RET and KIT. Recorded indications include Secondary malignant neoplasm of stomach.

• Molecular targets: KDR, RET, KIT and CSK (7 listed in DrugCentral).
• Indications: Secondary malignant neoplasm of stomach.
• ATC code: L01EK05 (Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors).
• Molecular formula: C24H23N5O; molecular weight 397.48 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Secondary malignant neoplasm of stomach

Mechanism & targets

Molecular targets (7)

Target	Gene	Action	Activity
Vascular endothelial growth factor receptor 2	KDR	inhibitor	IC50 9.00
Proto-oncogene tyrosine-protein kinase receptor Ret	RET	inhibitor	IC50 7.89
Mast/stem cell growth factor receptor Kit	KIT	inhibitor	IC50 6.37
Tyrosine-protein kinase CSK	CSK	inhibitor	IC50 6.28
Proto-oncogene tyrosine-protein kinase Src	SRC	inhibitor	IC50 6.28
Receptor-interacting serine/threonine-protein kinase 3	RIPK3	unknown	Kd 5.62
Mitogen-activated protein kinase kinase kinase MLT	ZAK	unknown	Kd 5.32

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
—	China Food and Drug Administration (CFDA)	—	—

ATC classification

ATC code	Therapeutic hierarchy
L01EK05	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Neurotoxicity	191.4
Palmar-plantar erythrodysaesthesia syndrome	162.2
Myelosuppression	159.2
Proteinuria	109.7
Bone marrow failure	68.8
Alopecia	66.0

Chemical structure

• Molecular formula: C₂₄H₂₃N₅O
• Molecular weight: 397.48 g/mol
• CAS number: —
• InChIKey: WPEWQEMJFLWMLV-UHFFFAOYSA-N
• PubChem CID: 45139106

O=C(NC1=CC=C(C=C1)C1(CCCC1)C#N)C1=CC=CN=C1NCC1=CC=NC=C1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Apatinib used for?

DrugCentral lists the following indications for Apatinib: Secondary malignant neoplasm of stomach.

How does Apatinib work?

Its molecular targets in DrugCentral include KDR (inhibitor), RET (inhibitor), KIT (inhibitor) and CSK (inhibitor).

What is the chemical formula of Apatinib?

Apatinib has the molecular formula C24H23N5O and a molecular weight of 397.48 g/mol.

Sources

• DrugCentral drug card 5211 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3186534 — compound record and bioactivity
• PubChem CID 45139106 — chemical identifiers
• DrugBank DB14765 — drug record
• FDA UNII 5S371K6132 — substance identity
• UniProt P35968 (KDR) — target protein
• UniProt P07949 (RET) — target protein
• UniProt P10721 (KIT) — target protein
• UniProt P41240 (CSK) — target protein
• UniProt P12931 (SRC) — target protein
• UniProt Q9Y572 (RIPK3) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.