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Drug intelligence / Profile preview
VRTX171
- Development stage
- Preclinical
- Lead developer
- VRise Therapeutics
- Modality
- Small Molecules
01
Overview
VRTX171 (also known as VRTX-171) is a preclinical, selective small molecule inhibitor of the KRAS G12V mutant protein. Developed by VRise Therapeutics, VRTX171 was designed using a de novo drug design approach to selectively target and inhibit KRAS G12V with high potency while sparing wild-type KRAS and other KRAS mutant isoforms. In preclinical studies, VRTX171 demonstrated target engagement and downstream inhibition of the Raf/mitogen-activated protein kinase (MAPK) pathway in KRAS G12V-mutated cancer cell lines. It is being evaluated in preclinical xenograft models of KRAS G12V-mutated cancers, such as pancreatic, colorectal, and non-small cell lung cancers, both as a monotherapy and in combination with other targeted therapies.
02
Targets
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