Drug intelligence / Profile preview

azidothymidine + fluorouracil + leucovorin

Development stage
Unknown
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination chemotherapy regimen consisting of azidothymidine (also known as zidovudine or AZT), fluorouracil (5-FU), and leucovorin. Azidothymidine is a thymidine nucleoside analog that incorporates into DNA and disrupts DNA synthesis. Fluorouracil is a pyrimidine analog antimetabolite that inhibits thymidylate synthase, blocking the conversion of deoxyuridylic acid to thymidylic acid and thereby interfering with DNA synthesis. Leucovorin (folinic acid) enhances the cytotoxicity of fluorouracil by stabilizing the binding of its active metabolite to thymidylate synthase, further inhibiting DNA synthesis. This combination has been studied for use in metastatic colorectal cancer, where it has shown promising activity with acceptable toxicity profiles[1][2]. The regimen exploits synergistic effects between 5-FU and AZT; 5-FU depletes normal thymidine nucleotides, increasing incorporation of AZT into nucleic acids[2].

Other names
AZT + 5-FU + leucovorinzidovudine + fluorouracil + leucovorinAZT/5-FU/leucovorin
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseTS (Thymidylate synthase)DHFR (Dihydrofolate reductase)

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