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Intoplicine

Development stage: Phase 1
Lead developer: Sanofi
Modality: Small Molecules
Administration: Intravenous

Overview

Intoplicine is a pyrido[4,3-b]indole derivative that acts as a dual inhibitor of DNA topoisomerase I and II. It was developed as an antitumor agent and has shown activity against various solid tumors in preclinical models. Intoplicine works by inhibiting DNA nicking and closing reactions, stabilizing the cleavable complex formed during the religation reaction involving topoisomerase I and II and DNA. It was initially developed by Rhone-Poulenc Sante (now part of Sanofi) but its clinical development was discontinued.

Other names: RP-60475RP60475RP 60475NSC 645008NSC645008NSC-645008

Targets

DNATOP2A (DNA topoisomerase II)TOP1MT (Mitochondrial topoisomerase I)

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