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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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