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bizelesin
- Development stage
- Phase 1
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
Bizelesin is a synthetic cyclopropylpyrroloindole antineoplastic antibiotic and small molecule that acts as a bifunctional DNA alkylating agent. It binds to the minor groove of DNA, inducing interstrand cross-linking, which inhibits both DNA replication and RNA synthesis. This leads to cell cycle arrest at the G2/M phase and can result in cellular senescence without apoptosis. Bizelesin was initially developed by Pfizer for use in cancer therapy, particularly for advanced solid tumors, but its clinical development was discontinued after early-phase trials[1][3][4][5].
- Other names
- Bizelesina
02
Targets
dsDNA-specific BCR (Double-stranded DNA-specific B-cell receptor)DNA
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