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LV5FU2 or capecitabine

Federation Francophone de Cancerologie Digestive · Phase 3 active Small molecule

LV5FU2/capecitabine is a fluoropyrimidine prodrug that inhibits thymidylate synthase and gets incorporated into DNA/RNA, disrupting cancer cell replication.

LV5FU2/capecitabine is a fluoropyrimidine prodrug that inhibits thymidylate synthase and gets incorporated into DNA/RNA, disrupting cancer cell replication. Used for Colorectal cancer (metastatic and adjuvant settings), Gastric cancer, Breast cancer.

At a glance

Generic nameLV5FU2 or capecitabine
SponsorFederation Francophone de Cancerologie Digestive
Drug classFluoropyrimidine antimetabolite
TargetThymidylate synthase
ModalitySmall molecule
Therapeutic areaOncology
PhasePhase 3

Mechanism of action

Capecitabine is an oral prodrug of 5-fluorouracil (5-FU) that is preferentially activated in tumor tissue by thymidine phosphorylase. Once activated, it inhibits thymidylate synthase, blocking dTMP synthesis and preventing DNA replication, while also incorporating into RNA to disrupt protein synthesis. LV5FU2 refers to the combination of leucovorin (folinic acid) with 5-FU, where leucovorin enhances 5-FU efficacy by stabilizing the thymidylate synthase-FdUMP complex.

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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