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Placebo、5-Fluorouracil、Leucovorin

Jiangsu HengRui Medicine Co., Ltd. · Phase 3 active Small molecule

5-Fluorouracil is a pyrimidine antimetabolite that inhibits thymidylate synthase and gets incorporated into RNA, disrupting nucleotide synthesis and cancer cell division, while leucovorin enhances its efficacy by stabilizing the drug-enzyme complex.

5-Fluorouracil is a pyrimidine antimetabolite that inhibits thymidylate synthase and gets incorporated into RNA, disrupting nucleotide synthesis and cancer cell division, while leucovorin enhances its efficacy by stabilizing the drug-enzyme complex. Used for Colorectal cancer (adjuvant or metastatic), Gastric cancer, Breast cancer.

At a glance

Generic namePlacebo、5-Fluorouracil、Leucovorin
SponsorJiangsu HengRui Medicine Co., Ltd.
Drug classAntimetabolite chemotherapy
TargetThymidylate synthase
ModalitySmall molecule
Therapeutic areaOncology
PhasePhase 3

Mechanism of action

5-Fluorouracil (5-FU) acts as a prodrug that is converted intracellularly to active metabolites, primarily inhibiting thymidylate synthase to block dTMP synthesis and DNA replication. Leucovorin (folinic acid) provides reduced folate cofactors that increase the stability and potency of the 5-FU-thymidylate synthase inhibitory complex, thereby enhancing cytotoxic effects. This combination is a standard chemotherapy regimen used across multiple cancer types.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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