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GS-0201
- Development stage
- Phase 1
- Lead developer
- Gilead Sciences
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
GS-0201 is an investigational, orally administered small molecule that acts as a selective inhibitor of poly (ADP-ribose) polymerase 1 (PARP1). By binding to and inhibiting PARP1, GS-0201 prevents the repair of damaged DNA via the base excision repair pathway, leading to accumulation of DNA strand breaks, genomic instability, and ultimately apoptosis in cancer cells. It is being developed by Gilead Sciences for the treatment of advanced solid tumors including triple negative breast cancer and HR-positive or HER2-negative breast cancer. The drug is currently in Phase 1 clinical trials as monotherapy and in combination with sacituzumab govitecan[1][2][3][4][5].
02
Targets
PARP1 (Poly (adp-ribose) polymerase 1)
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