Drug intelligence / Profile preview

ERAS-0015

Development stage
Phase 2
Lead developer
Erasca
Modality
Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules
Administration
Oral
01

Overview

ERAS-0015 is an orally bioavailable, highly potent pan-RAS molecular glue small molecule designed to inhibit RAS signaling in cancer. It acts as a tricomplex inhibitor by binding to cyclophilin A (CypA) and forming a high-affinity complex that targets active (GTP-bound) RAS proteins, thereby shutting down both mutant and wildtype RAS-driven oncogenic signaling. Preclinical studies have shown that ERAS-0015 has 8–21 times higher binding affinity for CypA compared to leading competitors, approximately fivefold greater potency in inhibiting RAS, and superior antitumor activity at lower doses. The drug is intended to overcome resistance mechanisms associated with mutant-selective inhibitors by also targeting wildtype RAS variants. Favorable pharmacokinetic properties have been demonstrated across multiple animal species. ERAS-0015 is currently being evaluated in the AURORAS-1 Phase 1 clinical trial for patients with advanced or metastatic solid tumors harboring certain RAS mutations[1][3][5][6][7].

Other names
ERAS-0015ERAS0015ERAS 0015
02

Targets

HRAS (H-Ras protein)PPIA (Peptidyl-prolyl cis-trans isomerase A)

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