Drug intelligence / Profile preview

5-fluorouracil + carboplatin + folinic acid

Development stage
Phase 3
Lead developer
Johnson Matthey
Modality
DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of three agents: - **5-fluorouracil (5-FU):** An antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis and repair. It is incorporated into RNA and DNA, interfering with their function and leading to cell death. - **Carboplatin:** A platinum-based chemotherapeutic agent that forms DNA crosslinks, inhibiting DNA replication and transcription. - **Folinic acid (leucovorin):** A reduced form of folic acid that enhances the binding of 5-FU’s active metabolite to thymidylate synthase, increasing its cytotoxicity. This combination has been studied primarily in advanced or recurrent squamous carcinoma of the head and neck. The regimen typically involves intravenous administration over two days every three weeks. The main toxicity observed is hematological; non-hematological toxicities are generally mild[2][4][6].

Other names
5-FU + carboplatin + folinic acidfluorouracil + carboplatin + leucovorin5-fluorouracil/carboplatin/folinic acid
02

Targets

DNATS (Thymidylate synthase)

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