Drug intelligence / Profile preview

cyclophosphamide + fluorouracil + folinic acid + gemcitabine

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of four agents: cyclophosphamide, fluorouracil (5-FU), folinic acid (leucovorin), and gemcitabine. Each component has a distinct mechanism of action: - Cyclophosphamide is an alkylating agent that crosslinks DNA, leading to cell death. - Fluorouracil is an antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis. - Folinic acid enhances the binding of 5-FU to thymidylate synthase, increasing its cytotoxicity. - Gemcitabine is a nucleoside analog that incorporates into DNA and inhibits ribonucleotide reductase, blocking DNA replication. This combination has been studied primarily in metastatic or poor-prognosis breast cancer patients previously treated with anthracyclines and taxanes. It has demonstrated promising response rates (~38–42%) and manageable toxicity profiles when administered with granulocyte colony-stimulating factor support[1][2][3]. The regimen may also be explored in other solid tumors such as pancreatic cancer[4].

Other names
gemcitabine + cyclophosphamide + 5-fluorouracil + folinic acidgemcitabine-CTX-5-FU/LFA
02

Targets

RNR (Ribonucleotide reductase)TS (Thymidylate synthase)DNA

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