Drug intelligence / Profile preview

5-fluorouracil + apatinib

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination therapy consisting of 5-fluorouracil (5-FU), a pyrimidine analog antimetabolite chemotherapeutic agent, and apatinib, an oral small molecule tyrosine kinase inhibitor that selectively inhibits vascular endothelial growth factor receptor-2 (VEGFR-2). 5-fluorouracil interferes with DNA synthesis by inhibiting thymidylate synthase, leading to cytotoxicity in rapidly dividing tumor cells. Apatinib blocks angiogenesis by inhibiting VEGFR-2 signaling pathways, thereby reducing tumor blood supply and enhancing the efficacy of chemotherapy. This combination has been investigated primarily for metastatic colorectal cancer as a third-line or subsequent treatment option and is also being studied in other advanced solid tumors such as gastric cancer and hepatocellular carcinoma[1][4][7]. The regimen aims to exploit the synergistic effects between antiangiogenic therapy and cytotoxic chemotherapy.

Brand names
AiTan
Other names
5-FU + apatinibapatinib + 5-fluorouracil
02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)TS (Thymidylate synthase)

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