RAS/MAPK通路

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Erasca Announces IND Clearance for Potential First-in-Class and Best-in-Class Pan-KRAS Inhibitor ERAS-4001
Globenewswire· 2025-06-02 12:00
Core Insights - Erasca, Inc. has received IND clearance from the FDA for ERAS-4001, a potential first-in-class pan-KRAS inhibitor, and ERAS-0015, a pan-RAS molecular glue, ahead of company guidance [1][2] - Initial Phase 1 monotherapy data for both RAS-targeting programs is expected in 2026 [1] Company Overview - Erasca is a clinical-stage precision oncology company focused on therapies for RAS/MAPK pathway-driven cancers [5] - The company aims to develop novel therapies to comprehensively shut down the RAS/MAPK pathway [5] Product Details - **ERAS-4001**: - A selective pan-KRAS inhibitor targeting multiple KRAS mutations and wildtype KRAS, with no activity against HRAS or NRAS [4] - Demonstrated potent activity against both active and inactive states of KRAS with single-digit nanomolar IC50s [4] - Induced tumor regression in multiple KRASm models during preclinical studies [4] - **ERAS-0015**: - An oral pan-RAS molecular glue with significantly higher binding affinity and potency compared to existing treatments [3] - Designed to prevent resistance against mutant-selective inhibitors by inhibiting RAS wildtype variants [3] - Showed favorable pharmacokinetic properties in preclinical studies [3] Clinical Trials - The BOREALIS-1 Phase 1 trial will assess the safety, tolerability, pharmacokinetics, pharmacodynamics, and preliminary efficacy of ERAS-4001 in KRASm solid tumors [2] - ERAS-0015 is being evaluated in the AURORAS-1 Phase 1 trial for RAS-mutant solid tumors [2]