Details
Stereochemistry | ACHIRAL |
Molecular Formula | C24H23N5O.CH4O3S |
Molecular Weight | 493.578 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CS(O)(=O)=O.O=C(NC1=CC=C(C=C1)C2(CCCC2)C#N)C3=CC=CN=C3NCC4=CC=NC=C4
InChI
InChIKey=FYJROXRIVQPKRY-UHFFFAOYSA-N
InChI=1S/C24H23N5O.CH4O3S/c25-17-24(11-1-2-12-24)19-5-7-20(8-6-19)29-23(30)21-4-3-13-27-22(21)28-16-18-9-14-26-15-10-18;1-5(2,3)4/h3-10,13-15H,1-2,11-12,16H2,(H,27,28)(H,29,30);1H3,(H,2,3,4)
Apatinib is an orally bioavailable, small molecule tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor-2 and used for the treatment of metastatic gastric cancer or gastroesophageal junction cancer that has progressed or relapsed after chemotherapy. To date, second-line ramucirumab and third-line Apatinib are the only anti-angiogenic approaches that have significantly improved the survival of patients with metastatic gastric cancer. Apatinib exhibited potent, highly-selective inhibition of VEGFR-2, c-kit, c-src, and RET tyrosine kinases. The efficacy of Apatinib monotherapy in patients with metastatic gastric cancer or gastroesophageal junction cancer for whom at least two prior chemotherapy regimens had failed was demonstrated in randomized open-label or double-blind phase II trials and a pivotal placebo-controlled phase III trial, all of which were conducted in China. Further clinical experience and long-term pharmacovigilance are required to definitively establish the efficacy and safety profile of Apatinib, including its use in combination with other chemotherapeutic agents.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: P35968 Gene ID: 3791.0 Gene Symbol: KDR Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/21443688 |
1.0 nM [IC50] |
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Classification Tree | Code System | Code | ||
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EU-Orphan Drug |
EU/3/17/1840
Created by
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FDA ORPHAN DRUG |
579117
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admin on Sat Dec 16 03:22:18 GMT 2023 , Edited by admin on Sat Dec 16 03:22:18 GMT 2023
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45139106
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FG-24
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CHEMBL3186534
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TK02X14ASJ
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APATINIB
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DTXSID80153427
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100000172343
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C74012
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1218779-75-9
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ACTIVE MOIETY
SUBSTANCE RECORD