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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.
New PCSK9 inhibitors, alirocumab and evolocumab, effectively lower LDL-C by 50-60% when added to statins. These well-tolerated therapies offer a new option for high-risk patients.
Area of Science:
- Cardiovascular Medicine
- Pharmacology
Background:
- Elevated low-density lipoprotein cholesterol (LDL-C) is a major cardiovascular risk factor.
- Statins and ezetimibe are standard lipid-lowering therapies, but some patients require additional treatment.
- Proprotein convertase subtilisin-kexin type 9 (PCSK9) inhibitors represent a novel therapeutic class.
Purpose of the Study:
- To evaluate the efficacy and safety of subcutaneous PCSK9 inhibitors (alirocumab and evolocumab).
- To assess the role of PCSK9 inhibition in patients with refractory hypercholesterolemia.
- To identify patient populations who may benefit most from PCSK9 inhibitor therapy.
Main Methods:
- Subcutaneous administration of alirocumab or evolocumab every 2 or 4 weeks.
- Addition of PCSK9 inhibitors to maximally tolerated statin and/or ezetimibe therapy.
- Assessment of LDL-C reduction and safety profile compared to placebo.
Main Results:
- PCSK9 inhibitors reduced LDL-C by 50-60% in addition to existing therapies.
- The therapies were well-tolerated, with a safety profile comparable to placebo in published studies.
- Long-term outcome data and cardiovascular event information are pending from ongoing trials.
Conclusions:
- PCSK9 inhibitors are a safe and effective option for selected high-cardiovascular-risk patients with persistently high LDL-C.
- Ideal candidates include patients with familial hypercholesterolemia and those experiencing statin-associated muscle symptoms (SAMS).
- Further data on long-term safety and cardiovascular outcomes are anticipated.
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