Drug intelligence / Profile preview

SP09253

Development stage
Preclinical
Lead developer
Essoras
Modality
Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules
Administration
Oral
01

Overview

SP09253 is an orally bioavailable, highly potent pan-RAS molecular glue inhibitor developed by Hefei Shengpu Pharmaceutical. It specifically targets the active ON state of multiple oncogenic RAS variants, including KRAS G12C, G12D, G12V, and G13D, while maintaining high selectivity over wild-type KRAS. By acting as a molecular glue, SP09253 facilitates the formation of a complex that inhibits RAS signaling, leading to the potent suppression of ERK phosphorylation and reduced cellular viability in KRAS-mutant cancer cells. In preclinical studies, it has demonstrated robust anti-tumor activity in various KRAS-mutant xenograft models and exhibits favorable ADME and pharmacokinetic profiles, showing superiority in efficacy compared to first-in-class pan-RAS molecular glues in clinical development.

02

Targets

HRAS (H-Ras protein)NRAS (Neuroblastoma RAS viral oncogene homolog)KRAS (Kirsten rat sarcoma viral oncogene homolog)

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