Drug intelligence / Profile preview

endostatin + capecitabine

Development stage
Unknown
Modality
Recombinant Proteins and Enzymes, Small Molecules
Administration
Intravenous, Oral
01

Overview

A combination therapy consisting of endostatin, an angiogenesis inhibitor that blocks new blood vessel formation in tumors, and capecitabine, an oral chemotherapy prodrug that converts to 5-fluorouracil (5-FU) in tumor cells. This combination has shown efficacy in various cancer types including colorectal, breast, nasopharyngeal, and esophageal cancers. The combination works synergistically as endostatin normalizes tumor vasculature, which can improve the delivery of capecitabine to tumor areas. Endostatin is a naturally occurring 20-kDa C-terminal fragment derived from collagen XVIII that inhibits angiogenesis by multiple mechanisms. It can directly bind to vascular endothelial growth factor receptor-2 (VEGF-R2), blocking the action of VEGF and suppressing vascular endothelial tube formation[1]. It also normalizes tumor vasculature structure and function, which can improve the delivery of cytotoxic agents to tumor areas[1]. Capecitabine is a fluoropyrimidine carbamate that belongs to the antimetabolite class of antineoplastic agents. It's an orally administered systemic prodrug with little pharmacologic activity until converted to 5-fluorouracil (5-FU) by enzymes expressed in higher concentrations in many tumors[7]. This design allows capecitabine to be selectively delivered to tumor tissues through enzymatic conversion preferentially inside tumor cells[7].

Other names
Endostar + capecitabineRecombinant human endostatin + capecitabineEndostar + Xeloda
02

Targets

GPC (Lassa virus glycoprotein complex)VEGFR2 (Vascular endothelial growth factor receptor 2)TS (Thymidylate synthase)ITGA5:ITGB1 (Integrin α5β1)

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