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CPT-11 (Irinotecan)

Epidemiological and Clinical Research Information Network · Phase 3 active Small molecule

CPT-11 (irinotecan) is a topoisomerase I inhibitor that prevents DNA unwinding and repair, leading to DNA damage and cancer cell death.

CPT-11 (irinotecan) is a topoisomerase I inhibitor that prevents DNA unwinding and repair, leading to DNA damage and cancer cell death. Used for Metastatic colorectal cancer (first-line and second-line), Small cell lung cancer, Ovarian cancer.

At a glance

Generic nameCPT-11 (Irinotecan)
Also known asIrinotecan
SponsorEpidemiological and Clinical Research Information Network
Drug classTopoisomerase I inhibitor
TargetTopoisomerase I
ModalitySmall molecule
Therapeutic areaOncology
PhasePhase 3

Mechanism of action

Irinotecan is a semisynthetic derivative of camptothecin that inhibits topoisomerase I, an enzyme essential for DNA replication and transcription. By stabilizing the topoisomerase I-DNA complex, the drug prevents religation of DNA strands, causing double-strand breaks during S-phase and triggering apoptosis in rapidly dividing cancer cells. The active metabolite SN-38 is responsible for most of the drug's cytotoxic activity.

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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