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Bempedoic acid/ezetimibe/rosuvastatin is an oral fixed-dose triple combination therapy developed by Daiichi Sankyo for the treatment of hypercholesterolemia and mixed dyslipidemia. This combination leverages three distinct, complementary mechanisms to lower LDL cholesterol: bempedoic acid inhibits ATP citrate lyase upstream of the statin pathway; ezetimibe inhibits the NPC1L1 transporter to reduce intestinal cholesterol absorption; and rosuvastatin inhibits HMG-CoA reductase to decrease hepatic cholesterol synthesis. The formulation is primarily intended for patients with primary hypercholesterolemia or mixed dyslipidemia who require intensive LDL-C lowering beyond what is achievable with dual therapy or standard statin regimens. It is currently being evaluated in Phase 1 bioequivalence studies comparing the fixed-dose combination tablet against the co-administration of its individual reference components.
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