alirocumab

Ligand id: 6744

Name: alirocumab

No information available.
Summary of Clinical Use
In July 2015, the US FDA approved alirocumab as the first anti-PCSK9 agent [1-2] for the treatment of patients with heterozygous familial hypercholesterolemia (HeFH) or with clinical atherosclerotic cardiovascular disease, for whom diet and statin therapy has failed to adequately lower LDL cholesterol . This approval follows reprots of positive results from several Phase III clinical trials, including NCT01644474, which reported ≥50% reduction in LDL-cholesterol levels in patients receiving alirocumab for 24 weeks, which was significantly better than the LDL-cholesterol reduction achieved with ezetimibe treatment [3].
Mechanism Of Action and Pharmacodynamic Effects
Alirocumab targets proprotein convertase subtilisin/kexin 9 (PCSK9) which has been identified as a key player in cholesterol homeostasis [1]. Normally, PCSK9 binds to LDL receptors (LDLR) and induces their degradation. LDLR are involved in the hepatic removal of LDL-cholesterol from the circulation. Alirocumab effectively suppresses PCSK9 activity, meaning more LDLR are available for removal of LDL-cholesterol from the blood and this reduces the risk of atherosclerosis.