Current Project under Consideration for Partnership

The current project centers on PKCβ as a critical regulator of obesity and fatty liver disease, with knockout studies confirming its role in diet‑induced obesity through increased energy expenditure without affecting food intake. In‑vitro screening identified three potent and selective small‑molecule PKCβ inhibitors, including the lead compound INST‑3399, which exhibits a favorable pharmacokinetic profile, no observed toxicity, and reduced ALT levels. In vivo studies in diet‑induced obesity mouse models demonstrated that INST‑3399 significantly reduces obesity, liver lipid accumulation, and hypercholesterolemia, supporting its promise as a therapeutic for metabolic disorders. INST‑3399 is now ready to enter clinical trials for fatty liver disease and lipid disorders, and INST‑3579 is prepared for clinical evaluation for obesity. A partnership at this stage offers substantial benefits, including early access to two novel, first‑in‑class metabolic therapeutics, the opportunity to co‑develop and commercialize assets with strong preclinical validation, and the ability to leverage complementary expertise to accelerate clinical development and expand future indications.

Scientific Strategy and Progress

  • Identified β as a key regulator of diet-induced obesity and fatty liver disease.

  • Demonstrated the role of PKCβ in diet-induced obesity using PKCβ knockout models, showing increased energy expenditure without changes in food intake.

  • Completed in-vitro screening to identify potent and selective next-generation PKCβ inhibitor.

  • Identified three small-molecule PKCβ inhibitors, including the lead compound INST-3399.

  • Determined INST3399 pharmacokinetics (half-life via mass spectrometry) with no observed toxicity and any effect on liver function.

  • Completed in-vivo efficacy studies of of INST3399 in a DIO (diet-induced obesity) mouse model.

  • Demonstrated that INST3399 treatment reduces diet-induced obesity, liver lipid accumulation and hypercholesterolemia.

  • INST3399 treatment is also therapeutically effective in reducing pre-existed obesity and related disorders.

    Planned Clinical Trials

Our team brings extensive expertise in PKCβ biology, metabolic disease models, medicinal chemistry, and small‑molecule development. We are well positioned to collaborate on IND‑directed PK/PD and toxicity studies, NHP efficacy studies, and Phase I IND preparation. The program may also benefit from the FDA Animal Rule and the potential for Priority Review Vouchers for obesity and fatty liver indications.INST-3399 is ready to enter clinical trials for the treatment of obesity either alone or in combination with GLP-1 receptor agonist.

I am confident that together we can accelerate the development of a first‑in‑class therapeutic with the potential to address major unmet needs in obesity and metabolic disease. I hope we can explore this opportunity soon and look forward to the possibility of working together.

  • INST3399 is ready to enter preclinical studies for the treatment of Obesity either alone or in combination with GLP_1 receptor agonist.