Heart Health

First Oral PCSK9 Inhibitor Cuts LDL Cholesterol by 80% in Phase 1 Trial

For the first time, researchers have demonstrated that a PCSK9 inhibitor can be taken as a pill rather than an injection. Laroprovstat (AZD0780), developed by AstraZeneca, works through a novel mechanism — stabilizing a region of the PCSK9 protein to prevent it from destroying LDL receptors. In a Phase 1 trial, treatment-naive patients with hypercholesterolemia who took laroprovstat 30 mg alongside the statin rosuvastatin achieved an approximately 80% reduction in LDL cholesterol from baseline. The drug was well tolerated, showed predictable once-daily pharmacokinetics, and could be taken with or without food. These early results suggest laroprovstat could eventually offer patients a convenient oral alternative to injectable PCSK9 drugs like evolocumab and alirocumab.