Drug intelligence / Profile preview

apatinib + raltitrexed + oxaliplatin

Development stage
Unknown
Lead developer
Guigang People's Hospital
Modality
Small Molecules
Administration
Oral, Intra-arterial, Intravenous
01

Overview

A combination therapy consisting of the VEGFR-2 inhibitor apatinib, the thymidylate synthase inhibitor raltitrexed, and the platinum-based alkylating agent oxaliplatin. This regimen is primarily investigated for the treatment of primary liver cancer, specifically hepatocellular carcinoma (HCC). Apatinib is an oral small molecule that selectively inhibits vascular endothelial growth factor receptor-2 (VEGFR-2), thereby suppressing tumor-associated angiogenesis. Raltitrexed is a folate-based antimetabolite that specifically inhibits thymidylate synthase, an enzyme essential for DNA synthesis. Oxaliplatin is a third-generation platinum compound that forms intra- and inter-strand DNA cross-links, leading to the inhibition of DNA replication and transcription. In clinical studies conducted by the Department of Oncology at Guigang City People’s Hospital and The Eighth Affiliated Hospital of Guangxi Medical University, this combination is often administered using a protocol where raltitrexed and oxaliplatin are delivered via hepatic arterial infusion chemotherapy (HAIC) or transarterial chemoembolization (TACE), supplemented by systemic oral apatinib.

02

Targets

DNAEGFR (Epidermal growth factor receptor)FGFR (Fibroblast growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)RET (Rearranged during transfection receptor tyrosine kinase)TS (Thymidylate synthase)VEGFR2 (Vascular endothelial growth factor receptor 2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)SRC (Proto-oncogene tyrosine-protein kinase Src)

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