alirocumab   Click here for help

GtoPdb Ligand ID: 6744

Synonyms: Praluent® | REGN727 | SAR-236553 | SAR236553
Approved drug
alirocumab is an approved drug (EMA & FDA (2015))
Compound class: Antibody
Comment: Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record. Based on peptide sequence matches we presume alirocumab is H1H316P in the patent document [4].
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No information available.
Summary of Clinical Use Click here for help
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 3 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]. EMA approval followed a few months later.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
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.