Drug intelligence / Profile preview

PSTA-2413

Development stage
Preclinical
Lead developer
Prospect Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

**PSTA-2413** is an investigational oral small molecule developed by Prospect Therapeutics as a pan-RAS inhibitor with selectivity for mutant over wild-type KRAS. It disrupts the RAS/BRAF interaction by forming a tri-complex with RAS(ON) and cyclophilin A (CypA), demonstrating nanomolar potency in vitro against various RAS mutants, activity in AMG510-resistant cells, and robust in vivo antitumor efficacy with tumor regression in preclinical models of colorectal cancer, non-small cell lung cancer, and other solid tumors. The compound exhibits favorable pharmacokinetics, a 10-fold safety margin in rat toxicity studies, and advantages over competitors like RMC-6236 and ERAS-0015 in potency and wild-type selectivity, positioning it as a potential best-in-class candidate for RAS-driven cancers.[1][3][5]

02

Targets

PPIA (Peptidyl-prolyl cis-trans isomerase A)HRAS (H-Ras protein)NRAS (Neuroblastoma RAS viral oncogene homolog)KRAS (Kirsten rat sarcoma viral oncogene homolog)

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