Evolocumab: First Global Approval.
Evolocumab (Repatha™) is a fully human monoclonal antibody developed by Amgen that has been approved as a treatment for hypercholesterolaemia in the EU, and is awaiting approval in the USA and Japan. It specifically binds proprotein convertase subtilisin/kexin type 9 (PCSK9)-a negative regulator of low-density lipoprotein (LDL)-receptors-thereby improving the ability of the liver to bind LDL-cholesterol (LDL-C), leading to reduced LDL-C blood levels. The drug reduces LDL-C levels in patients with hypercholesterolaemia when used as monotherapy or in conjunction with a statin. This article summarizes the milestones in the development of evolocumab leading to this approval for the treatment of adults with primary hypercholesterolaemia (heterozygous familial and non-familial) or mixed dyslipidaemia as an adjunct to diet with or without a statin and/or other lipid lowering therapies, and in adults and adolescents aged ≥12 years with homozygous familial hypercholesterolaemia in combination with other lipid lowering therapies.
Springer, Private Bag 65901, Mairangi Bay 0754, Auckland, New Zealand, dru@adis.com.
Anthony
A
Markham
D000293:Adolescent; D000328:Adult; D000911:Antibodies, Monoclonal / Q000494:pharmacology / Q000627:therapeutic use*; D061067:Antibodies, Monoclonal, Humanized; D000924:Anticholesteremic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D008078:Cholesterol, LDL / Q000097:blood; D017277:Drug Approval; D006801:Humans; D006937:Hypercholesterolemia / Q000188:drug therapy*; D000071449:Proprotein Convertase 9; D043484:Proprotein Convertases / Q000378:metabolism; D012697:Serine Endopeptidases / Q000378:metabolism
D000911:Antibodies, Monoclonal; D061067:Antibodies, Monoclonal, Humanized; D000924:Anticholesteremic Agents; D008078:Cholesterol, LDL; C472125:PCSK9 protein, human; D000071449:Proprotein Convertase 9; D043484:Proprotein Convertases; D012697:Serine Endopeptidases; C577155:evolocumab