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 reports 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 after the FDA approval.
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.