TY - JOUR
T1 - Alirocumab for the treatment of hypercholesterolemia
AU - Tomlinson, Brian
AU - Hu, Miao
AU - Zhang, Yuzhen
AU - Chan, Paul
AU - Liu, Zhong Min
N1 - Publisher Copyright:
© 2017 Informa UK Limited, trading as Taylor & Francis Group.
Copyright:
Copyright 2018 Elsevier B.V., All rights reserved.
PY - 2017/5/4
Y1 - 2017/5/4
N2 - Introduction: Alirocumab is a human monoclonal antibody inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) that is administered by subcutaneous injection every 2 weeks. Area covered: Herein, the authors discuss the background to inhibition of PCSK9 and the pharmacodynamics, pharmacokinetics and clinical trials with alirocumab. Alirocumab produces substantial reductions in low density lipoprotein cholesterol (LDL-C) in patients with and without background statin treatment. The safety profile appears very promising from the relatively short term studies that have been completed but there are some remaining concerns about long term risks of neurocognitive events and developing diabetes. Expert opinion: The profound reduction in LDL-C with alirocumab is most likely to translate into cardiovascular benefits in the ODYSSEY OUTCOMES trial and is unlikely in itself to result in any major adverse effects. The high cost and the current lack of long-term safety and efficacy data will restrict the use of alirocumab to patients who have high cardiovascular risk from established atherosclerotic cardiovascular disease or heterozygous familial hypercholesterolemia and who are unable to achieve LDL-C targets with maximally tolerated dose of statins with or without other lipid-lowering drugs. When further data become available, these indications are likely to be expanded.
AB - Introduction: Alirocumab is a human monoclonal antibody inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) that is administered by subcutaneous injection every 2 weeks. Area covered: Herein, the authors discuss the background to inhibition of PCSK9 and the pharmacodynamics, pharmacokinetics and clinical trials with alirocumab. Alirocumab produces substantial reductions in low density lipoprotein cholesterol (LDL-C) in patients with and without background statin treatment. The safety profile appears very promising from the relatively short term studies that have been completed but there are some remaining concerns about long term risks of neurocognitive events and developing diabetes. Expert opinion: The profound reduction in LDL-C with alirocumab is most likely to translate into cardiovascular benefits in the ODYSSEY OUTCOMES trial and is unlikely in itself to result in any major adverse effects. The high cost and the current lack of long-term safety and efficacy data will restrict the use of alirocumab to patients who have high cardiovascular risk from established atherosclerotic cardiovascular disease or heterozygous familial hypercholesterolemia and who are unable to achieve LDL-C targets with maximally tolerated dose of statins with or without other lipid-lowering drugs. When further data become available, these indications are likely to be expanded.
KW - Alirocumab
KW - atherosclerotic cardiovascular disease
KW - heterozygous familial hypercholesterolemia
KW - low-density lipoprotein cholesterol
KW - proprotein convertase subtilisin/kexin type 9
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U2 - 10.1080/14712598.2017.1305354
DO - 10.1080/14712598.2017.1305354
M3 - Article
C2 - 28277798
AN - SCOPUS:85015612086
SN - 1471-2598
VL - 17
SP - 633
EP - 643
JO - Expert Opinion on Biological Therapy
JF - Expert Opinion on Biological Therapy
IS - 5
ER -