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Updated: Mar 20, 2026

A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9
Published on: August 28, 2018
[PCSK9 inhibitors : Recommendations for patient selection]
U Laufs1, F Custodis2, C Werner2
1Klinik für Innere Medizin III, Kardiologie, Angiologie und Internistische Intensivmedizin, IMED Geb. 41.1, Universitätsklinikum des Saarlandes, 66421, Homburg/Saar, Deutschland. ulrich.laufs@uks.eu.
Abstract:
The 2 or 4‑week subcutaneous therapy with the recently approved antibodies alirocumab and evolocumab for inhibition of proprotein convertase subtilisin-kexin type 9 (PCSK9) reduces low-density lipoprotein cholesterol (LDL-C) in addition to statins and ezetimibe by 50-60 %. The therapy is well-tolerated. The safety profile in the published studies is comparable to placebo. Outcome data and information on long-term safety and the influence on cardiovascular events are not yet available but the results of several large trials are expected in 2016-2018. At present (spring 2016) PCSK9 inhibitors represent an option for selected patients with a high cardiovascular risk and high LDL-C despite treatment with the maximum tolerated oral lipid-lowering therapy. This group includes selected patients with familial hypercholesterolemia and high-risk individuals with statin-associated muscle symptoms (SAMS).
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