Drug intelligence / Profile preview

RM-055

Development stage
Preclinical
Lead developer
REVOLUTION Medicines
Modality
Small Molecules
Administration
Oral
01

Overview

RM-055 is an innovative oral small molecule RAS inactivator being developed by Revolution Medicines for the treatment of RAS-addicted cancers, including pancreatic ductal adenocarcinoma, non-small cell lung cancer, and colorectal cancer. The drug utilizes a unique mechanism of action by forming a binary complex with the intracellular chaperone cyclophilin A (CypA). This complex then binds to mutant RAS proteins in their active, GTP-bound state (RAS(ON)), accelerating the hydrolysis of RAS-GTP to the inactive RAS-GDP state (RAS(OFF)). By effectively switching the oncogenic protein to its inactive form, RM-055 inhibits downstream RAS signaling and tumor cell proliferation. Preclinical studies have demonstrated deep and durable antitumor activity across multiple cancer models and the potential to overcome resistance to prior RAS inhibitor treatments. A Phase 1 clinical study is anticipated to commence in 2026.

02

Targets

PPIA (Peptidyl-prolyl cis-trans isomerase A)NRAS (Neuroblastoma RAS viral oncogene homolog)

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