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dts-201
- Development stage
- Phase 2
- Lead developer
- Eddingpharm
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
DTS-201 is a peptidic prodrug of doxorubicin designed to preferentially deliver the parent compound to tumor cells while limiting cardiotoxicity. It remains inactive in the bloodstream and healthy tissues until it reaches the tumor environment, where extracellular enzymes (neprilysin and thimet oligopeptidase) cleave it to yield an intermediate that can penetrate cells. Inside cells, intracellular peptidases release free doxorubicin to interact with its targets. This selective activation mechanism allows for higher equivalent doses of doxorubicin to be delivered with reduced systemic toxicity, particularly cardiotoxicity.
- Other names
- N-1-leucyl-doxorubicinN1-leucyl-doxorubicinN 1-leucyl-doxorubicin
02
Targets
TOP2A (DNA topoisomerase II)
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