Drug intelligence / Profile preview

5-fluorouracil + hydroxyurea + levofolinic acid

Development stage
Unknown
Modality
Small Molecules
Administration
Intravenous, Oral
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 leading to cell death in rapidly dividing tumor cells. - **Hydroxyurea:** A ribonucleotide reductase inhibitor that impedes DNA synthesis by preventing the conversion of ribonucleotides to deoxyribonucleotides. It also acts as a radiosensitizer and can enhance the cytotoxic effects of other chemotherapeutic agents. - **Levofolinic acid (levoleucovorin):** The pharmacologically active enantiomer of folinic acid; it stabilizes the binding of 5-FU to thymidylate synthase, thereby enhancing its antitumor activity. This combination has been investigated primarily for advanced gastrointestinal cancers such as metastatic colorectal cancer and pancreatic adenocarcinoma. Clinical studies have shown moderate efficacy with manageable toxicity profiles. Levofolinic acid potentiates the effect of 5-FU, while hydroxyurea may further modulate this activity without significantly increasing toxicity at standard doses[1][2][4][10].

Other names
5-FU + hydroxyurea + levofolinic acidfluorouracil + hydroxyurea + levoleucovorin5-fluorouracil/levofolinic acid/hydroxyurea
02

Targets

RNR (Ribonucleotide reductase)TS (Thymidylate synthase)

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