文摘
Evolocumab (Repatha®) is a monoclonal antibody targeting proprotein convertase subtilisin/kexin type 9 (PCSK9) that is administered subcutaneously at a dosage of 140 mg every 2 weeks or 420 mg once monthly. Across 12-week phase III trials in patients with primary hypercholesterolemia or mixed dyslipidemia, evolocumab was more effective than placebo (treatment difference −54.8 to −76.3 %) and/or ezetimibe (treatment difference −36.9 to −47.2 %) at reducing low-density lipoprotein cholesterol (LDL-C) levels, including when added to statin therapy, when administered to statin-intolerant patients, when administered as monotherapy, and in patients with heterozygous familial hypercholesterolemia who were receiving statins with or without other lipid-lowering drugs. Evolocumab also significantly lowered LDL-C levels (treatment difference of ≈30 % vs. placebo) in patients with homozygous familial hypercholesterolemia when added to statins with or without ezetimibe in a 12-week phase III trial. The efficacy of evolocumab was maintained in the longer term, and it was well tolerated. In conclusion, subcutaneous evolocumab is a valuable new treatment for use in primary hypercholesterolemia or mixed dyslipidemia and homozygous familial hypercholesterolemia, particularly in patients unable to reach LDL-C goals despite treatment with statins with or without other lipid-lowering therapies and in patients who do not tolerate or are not able to receive statins. The manuscript was reviewed by: A. Hirayama, Division of Cardiology, Department of Medicine, Nihon University School of Medicine, Tokyo, Japan; G. K. Hovingh, Department of Vascular Medicine, Academic Medical Center, Amsterdam, the Netherlands; J. Mansourati, Department of Cardiology, University Hospital of Brest, Hôpital de la Cavale Blanche, Brest, France; A. G. Olsson, Department of Medical and Health Sciences, Linköping University, Linköping, Sweden; K. G. Parhofer, Medizinische Klinik II—Grosshadern, Klinikum der Universität München, Munich, Germany; G. F. Watts, School of Medicine and Pharmacology, University of Western Australia, Western Australia, Australia.