Drug intelligence / Profile preview

fluorouracil + folinic acid + paclitaxel

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of three agents: - **Fluorouracil (5-FU):** A pyrimidine analog antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis and function, leading to cell death. It is widely used in the treatment of various solid tumors. - **Folinic acid (leucovorin):** A reduced form of folic acid that enhances the cytotoxic effects of fluorouracil by stabilizing the binding of 5-FU’s active metabolite to thymidylate synthase, thereby increasing its efficacy. - **Paclitaxel:** A microtubule-stabilizing agent that promotes tubulin polymerization and prevents microtubule disassembly, inhibiting mitosis and inducing apoptosis in cancer cells. This combination has been investigated for enhanced anti-tumor efficacy through synergistic mechanisms. Folinic acid potentiates 5-FU activity, while paclitaxel targets a different aspect of cell division. The regimen has been studied particularly for breast cancer and other solid tumors[1]. Delivery systems such as folic acid-functionalized exosomes have also been explored to improve targeted delivery and reduce toxicity[1].

02

Targets

TUBB (Tubulin (alpha and beta subunits))TS (Thymidylate synthase)

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