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GenSciP166
- Development stage
- Preclinical
- Lead developer
- Changchun GeneScience Pharmaceutical
- Modality
- PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
GenSciP166 is an oral small-molecule proteolysis-targeting chimera (PROTAC) designed to degrade signal transducer and activator of transcription 6 (STAT6). Developed by GeneScience Pharmaceuticals (GenSci) as the originator, GenSciP166 recruits the cereblon (CRBN) E3 ubiquitin ligase to target STAT6 for proteasomal degradation, thereby blocking downstream interleukin-4 (IL-4) and interleukin-13 (IL-13) signaling. The drug is currently in preclinical development, with its lead indication being atopic dermatitis, and is also positioned for other Th2/type 2 inflammatory and allergic diseases. In preclinical studies, GenSciP166 demonstrated picomolar potency in degrading STAT6 across human, mouse, dog, and monkey blood cells, showing high selectivity over other phosphorylated STATs and superior efficacy compared to reference compounds.
02
Targets
CRBN (Cereblon)STAT6 (Signal Transducer and Activator of Transcription 6)
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