ARI-2243

ARI-2243 is a highly potent, orally active, small molecule dipeptidyl peptidase-4 (DPP-4) inhibitor developed by Arisaph Pharmaceuticals for the treatment of Type 2 diabetes. The compound is designed as a "smart" DPP-4 inhibitor with a first-in-class "soft drug" feature, meaning it becomes inactive when unbound to the target enzyme. This design is intended to improve the drug's safety profile and therapeutic index by minimizing off-target effects. Arisaph developed ARI-2243 for once-daily administration, emphasizing its functional selectivity and superior preclinical efficacy. In 2008, the FDA accepted an Investigational New Drug (IND) application to evaluate the compound in a Phase 1 clinical trial in healthy volunteers.