Drug intelligence / Profile preview

ompenaclid

Development stage
Phase 2
Lead developer
Inspirna
Modality
Small Molecules
Administration
Oral
01

Overview

Ompenaclid (RG6286) is an orally bioavailable, small-molecule inhibitor specifically targeting the KRAS G12C mutation. Developed by Roche and Genentech, it works by covalently binding to the cysteine residue of the KRAS G12C protein, locking it in its inactive, GDP-bound state. This prevents the activation of downstream signaling pathways, such as the MAPK/ERK pathway, which drive tumor cell proliferation and survival. It is primarily being investigated for the treatment of advanced solid tumors harboring the KRAS G12C mutation, with a particular focus on colorectal cancer and non-small cell lung cancer.

Other names
ompenaclid
02

Targets

KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)SLC6A8 (Sodium- and chloride-dependent creatine transporter 1)

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