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Laroprovstat + ezetimibe is a fixed-dose combination (FDC) therapy being developed by AstraZeneca for the treatment of hypercholesterolemia. It combines laroprovstat (AZD0780), an oral small molecule inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9), with ezetimibe, a cholesterol absorption inhibitor that targets the Niemann-Pick C1-like 1 (NPC1L1) protein. Laroprovstat works by preventing PCSK9-mediated degradation of LDL receptors, thereby increasing LDL-C clearance from the blood, while ezetimibe reduces the absorption of biliary and dietary cholesterol in the small intestine. This dual mechanism is intended to provide robust reductions in LDL-C levels. The combination is currently in Phase I clinical development to assess bioavailability and food effects.
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