Summarized by Masters of Longevity from Longevity Technology.
An article about an AI-designed small-molecule GIPR blocker nominated as a preclinical obesity candidate, outlining its pharmacology, safety profile and development context.
Key Takeaways
- Insilico nominated ISM1354 as a small-molecule GIPR antagonist for obesity and related cardiometabolic indications.
- ISM1354 showed 75–104% oral bioavailability across species and at least 18-fold greater plasma exposure versus a comparator at the same dose.
- Preclinical safety data showed weaker OATP1B1 inhibition, minimal liver cell toxicity up to 200 µM, and a non-GLP monkey safety margin of about 45-fold.
