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GS-2426
- Development stage
- Phase 1
- Lead developer
- Gilead Sciences
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
GS-2426 is an orally bioavailable small molecule inhibitor of Protein Arginine Methyltransferase 5 (PRMT5) developed by Gilead Sciences. It is specifically designed to treat advanced solid tumors characterized by the deletion of the methylthioadenosine phosphorylase (MTAP) gene. MTAP deletion leads to the accumulation of the metabolite methylthioadenosine (MTA), which binds to PRMT5 and creates a unique vulnerability in cancer cells. GS-2426 acts as an MTA-cooperative inhibitor, meaning it preferentially binds to the PRMT5-MTA complex, thereby selectively inhibiting PRMT5 activity in MTAP-deleted tumor cells while minimizing effects on healthy tissues. It is currently being evaluated in Phase 1 clinical trials to determine its safety, tolerability, and recommended dose for further development.
02
Targets
PRMT5 (Protein arginine N-methyltransferase 5)
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