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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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
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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.