Drug intelligence / Profile preview

indimitecan

Development stage
Phase 1
Lead developer
Gibson Oncology
Modality
Small Molecules
Administration
Intravenous
01

Overview

Indimitecan (DC-105, LMP776) is a small molecule indenoisoquinoline that acts as a non-camptothecin inhibitor of DNA topoisomerase I (TOP1). Developed by Gibson Oncology through a license from the National Cancer Institute (NCI) and Purdue University, indimitecan is designed to address the clinical limitations of traditional camptothecin-based drugs, such as chemical instability and susceptibility to efflux-mediated resistance (e.g., via the ABCG2/BCRP transporter). The drug works by stabilizing the covalent cleavage complexes formed between TOP1 and DNA, which prevents DNA religation and results in lethal double-strand breaks during replication, ultimately leading to apoptosis. Indimitecan is currently being evaluated in clinical trials for the treatment of relapsed solid tumors and various lymphomas.

Other names
indimitecanindenoisoquinoline LMP776
02

Targets

TOP1 (DNA Topoisomerase I)

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