orforglipron + itraconazole

LY3509754 (orforglipron) is an investigational, oral, non-peptide glucagon-like peptide-1 (GLP-1) receptor agonist developed by Eli Lilly for the treatment of type 2 diabetes and obesity. Unlike injectable GLP-1 analogs, orforglipron is a small molecule designed for once-daily oral administration. Itraconazole is a triazole antifungal agent and a potent inhibitor of the cytochrome P450 3A4 (CYP3A4) enzyme. The co-administration of LY3509754 and itraconazole has been evaluated in Phase 1 clinical pharmacology studies to determine the impact of strong CYP3A4 inhibition on the pharmacokinetics of orforglipron, which is a substrate for CYP3A-mediated metabolism. These studies are critical for establishing dosing recommendations and understanding the safety profile of orforglipron when used alongside common medications that inhibit metabolic pathways.

Other names

LY3509754 + itraconazoleorforglipron + itraconazole