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Irinotecan, 5FU, leucovorin

Asan Medical Center · FDA-approved active Small molecule

This combination chemotherapy regimen inhibits DNA synthesis and cell division through topoisomerase I inhibition and fluoropyrimidine-mediated nucleotide antagonism.

This combination chemotherapy regimen inhibits DNA synthesis and cell division through topoisomerase I inhibition and fluoropyrimidine-mediated nucleotide antagonism. Used for Metastatic colorectal cancer, Advanced gastric cancer, Pancreatic cancer.

At a glance

Generic nameIrinotecan, 5FU, leucovorin
Also known asCAMPTO (CAMPOSAR)
SponsorAsan Medical Center
Drug classChemotherapy combination (topoisomerase I inhibitor + antimetabolite)
TargetTopoisomerase I; thymidylate synthase
ModalitySmall molecule
Therapeutic areaOncology
PhaseFDA-approved

Mechanism of action

Irinotecan is a topoisomerase I inhibitor that prevents DNA religation, leading to DNA damage and cell death. 5-Fluorouracil (5FU) is a nucleotide analog that inhibits thymidylate synthase and incorporates into RNA/DNA, disrupting synthesis. Leucovorin (folinic acid) enhances 5FU efficacy by stabilizing the 5FU-thymidylate synthase complex, increasing cytotoxicity.

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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