laroprovstat

Laroprovstat is an orally bioavailable small-molecule inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) being developed primarily for the treatment of dyslipidemia and atherosclerotic cardiovascular disease. By binding to a non-classical pocket within the C-terminal domain of PCSK9, it induces conformational changes that reduce PCSK9-mediated targeting of low-density lipoprotein receptor (LDLR) to lysosomal degradation, thereby enhancing LDLR recycling and lowering plasma LDL cholesterol levels. Developed by AstraZeneca following early work from Dogma Therapeutics, laroprovstat has demonstrated robust, dose-dependent LDL-C reductions on top of background statin therapy in phase 2 trials and is currently in phase 3 development as a once-daily oral PCSK9 inhibitor for patients with heterozygous familial hypercholesterolemia, clinical atherosclerotic cardiovascular disease, and those at high risk for a first ASCVD event.[1][2][3][4][6][7][9][14]

Other names

laroprovstat