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brostallicin
- Development stage
- Phase 2
- Lead developer
- Sobi
- Modality
- Classical Binding Small Molecules → Small Molecules, Recombinant Proteins and Enzymes, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Prodrugs/Conditional Activator Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
Brostallicin is a synthetic second-generation DNA minor groove binder and alkylating agent developed for the treatment of cancer. It is an α-bromoacryloyl derivative of distamycin A and acts by binding to the DNA minor groove after forming a reactive glutathione-brostallicin complex in the presence of glutathione S-transferase (GST), which is often overexpressed in cancer cells. This interaction inhibits DNA replication and cell division, leading to tumor cell death. Brostallicin has shown potent cytotoxic activity against various tumor types in preclinical studies, including those resistant to other alkylating agents and camptothecins. It was investigated primarily for soft tissue sarcoma, triple-negative breast cancer, and colorectal cancer but did not demonstrate superiority over standard treatments in clinical trials[1][3][4][5][6][7].
- Other names
- brostallicin
02
Targets
DNA minor groove
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