PCSK9 Inhibitors for Statin-Intolerant Patients: Is the Jury In?

PCSK9 Inhibitors for Statin-Intolerant Patients: Is the Jury In?

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By Elyse Grusky, MAReviewed by Nihar Desai, MD, MPH Assistant Professor of Medicine (Cardiology), Yale School of Medicine, New Haven, Connecticut


Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors have the potential to provide an additional avenue for low-density lipoprotein cholesterol (LDL-C) reduction in the


statin-intolerant patient.  According to the recent GAUSS-3 (Goal Achievement After Utilizing an Anti-PCSK9 Antibody in Statin Intolerant Subjects 3 trial results),1 the use of a PCSK9


inhibitor (evolocumab) resulted in a significantly greater reduction in LDL-C levels and other atherogenic lipoproteins in patients intolerant to statins due to muscle symptoms than another


LDL-C lowering option (ezetimibe).


GAUSS-3 was a blinded, two-stage crossover study involving placebo and statin rechallenge with atorvastatin.1 In Phase A, 491 patients (mean age, 60.7 years; 246 women, 246 men) received 24


weeks of placebo or atorvastatin to identify patients having muscle symptoms with atorvastatin. At least 80% of patients had a history of intolerance to 3 or more statins at baseline. After


a 2-week washout, 218 patients were randomized in Phase B: 73 patients received ezetimibe plus subcutaneous placebo and 145 patients received evolocumab plus oral placebo. The patient


population studied had either preexisting cardiovascular (CV) disease or multiple risk factors with very high baseline LDL-C levels (mean, >210 mg/dL).


After 24 weeks of therapy, evolocumab (PCSK9) was associated with a >50% reduction in LDL-C (54.5% mean reduction) versus 16.7% mean reduction with ezetimibe.  The LDL-C goal of