Drug intelligence / Profile preview

VRTX-126

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

Overview

VRTX-126 is a highly selective, potent, and orally available small molecule inhibitor targeting the KRAS G12C mutation. It is being developed by VRise Therapeutics for the treatment of solid tumors, specifically non-small cell lung cancer (NSCLC) and colorectal cancer. The drug acts as a covalent inhibitor of the mutant KRAS protein (KRAS G12C), which plays a key role in driving tumor growth through activation of downstream signaling pathways such as MAPK and PI3K-AKT-mTOR. Preclinical studies have shown that VRTX-126 significantly reduces tumor burden with favorable safety margins. Combination studies are ongoing to evaluate its efficacy alongside other inhibitors targeting related pathways[1][2][5].

Other names
KRAS G12C inhibitor - VRise Therapeutics
02

Targets

KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)

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