Apatinib

Apatinib

File:Apatinib.svg
Systematic (IUPAC) name
N-[4-(1-cyanocyclopentyl) phenyl-2-(4-picolyl)amino-3-Nicotinamide methanesulphonate
Clinical data
Routes of administration	Oral
Identifiers
ATC code	none
Chemical data
Formula	C25H27N5O3S
Molar mass	493.58 g/mol[[]]

Apatinib, also known as YN968D1, is a tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor (VEGFR). It is an orally bioavailable, small molecule agent which is thought to bind to the VEGFR inhibiting angiogenesis in cancer cells, specifically by inhibiting VEGF-mediated endothelial cell migration and proliferation decreasing tumor microvessel density. This agent also mildly inhibits c-Kit and c-SRC tyrosine kinases.

Apatinib was first synthesized by Advenchen Laboratories in California, USA and is being developed by Jiangsu Hengrui Medicine (China), LSK BioPartners (US) and Bukwang Pharmaceutical Company (Korea). It is an investigational cancer drug currently undergoing clinical trials as a potential targeted treatment for metastatic gastric carcinoma.

Phase I/II clinical study

The principle investigator from Fudan University, China, presented results of Phase I/II human clinical studies at the 2009 CSCO Meeting (October 17, 2009). Cancer patients were administered varied doses of Apatinib daily for 28 days. Apatinib was well tolerated at doses below 750mg/day, 3 of 3 dose limiting toxicities were reported at 1000mg/day and the maximum tolerated dose is determined to be 850mg/day. The investigator also reported of 65 cancer patients treated in Phase I/II, 1.54% had a complete response, 12.31% had a partial response, 66.15% had stable disease and 20% had progressive disease .

Current status

There is a Phase II/III study recruiting patients in China to determine whether apatinib can improve progression free survival compared with placebo in patients with metastatic gastric carcinoma who have failed two lines of chemotherapy (September, 2009) .