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Folinic Acid + 5 FU

Pfizer · Phase 3 active Small molecule

Folinic acid enhances the cytotoxic activity of 5-fluorouracil (5-FU) by stabilizing the ternary complex between 5-FU metabolites and thymidylate synthase, thereby increasing DNA synthesis inhibition and cancer cell death.

Folinic acid enhances the cytotoxic activity of 5-fluorouracil (5-FU) by stabilizing the ternary complex between 5-FU metabolites and thymidylate synthase, thereby increasing DNA synthesis inhibition and cancer cell death. Used for Metastatic colorectal cancer, Adjuvant treatment of stage III colorectal cancer, Advanced gastric cancer.

At a glance

Generic nameFolinic Acid + 5 FU
SponsorPfizer
Drug classAntimetabolite chemotherapy combination
TargetThymidylate synthase
ModalitySmall molecule
Therapeutic areaOncology
PhasePhase 3

Mechanism of action

5-FU is a pyrimidine antimetabolite that inhibits thymidylate synthase, blocking DNA synthesis. Folinic acid (leucovorin) provides reduced folate cofactors that stabilize the binding of fluorodeoxymonophosphate to thymidylate synthase, prolonging enzyme inhibition and enhancing 5-FU cytotoxicity. This combination is a standard chemotherapy regimen used in colorectal and other gastrointestinal cancers.

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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