Health Canada, the Canadian equivalent of the FDA, recently issued a public advisory about postmarketing reports of myalgia, rhabdomyolysis, hepatitis, pancreatitis and thrombocytopenia associated with use of ezetimibe (Zetia in the US; Ezetrol in Canada). Ezetimibe is often added to a statin to increase LDL cholesterol lowering (Drugs for Lipids, Treat Guidel Med Lett 2005; 3:15). The advisory did not specify whether these patients were also taking a statin, but according to the Canadian manufacturer Merck Frosst/Schering (Merck/Schering-Plough in the US), some of the patients who developed...

Combining a statin with another drug that lowers low-density lipoprotein cholesterol (LDL-C), such as colesevelam (Welchol), niacin (Niaspan, and others), or ezetimibe (Zetia), can reduce LDL-C levels more than a statin alone, but studies convincingly demonstrating that such combinations improve clinical outcomes have been lacking. The results of a long-term randomized, double-blind clinical trial (IMPROVE-IT) recently presented at the American Heart Association's Scientific Sessions 2014 indicate that addition of ezetimibe to simvastatin in high-risk patients reduces cardiovascular...

The FDA has approved a fixed-dose combination of the cholesterol absorption inhibitor ezetimibe and the HMG-CoA reductase inhibitor (statin) atorvastatin as Liptruzet (Merck) for treatment of hyperlipidemia. Ezetimibe is also available in a fixed-dose combination with simvastatin (Vytorin).

Since our initial review of the oral lipid-lowering adenosine triphosphate-citrate lyase (ACL) inhibitor bempedoic acid (Nexletol – Esperion) in 2020, cardiovascular outcomes data in statin-intolerant patients have become available.

The results of the recently published FOURIER trial have shown a reduction in cardiovascular events with addition of the PCSK9 inhibitor evolocumab (Repatha) to statin therapy in patients with atherosclerotic cardiovascular disease (ASCVD).

In recent months, both the lay media and some medical experts have raised concerns about the effectiveness and safety of ezetimibe, a widely used drug that prevents absorption of cholesterol from the GI tract. Ezetimibe is available alone as Zetia and in combination with 10, 20, 40 and 80 mg of simvastatin (Zocor, and others) as Vytorin.

The FDA has approved evinacumab-dgnb (Evkeeza – Regeneron), an angiopoietin-like 3 (ANGPTL3) inhibitor, for adjunctive IV treatment of homozygous familial hypercholesterolemia (HoFH) in patients ≥12 years old. Evinacumab is the first ANGPTL3 inhibitor to be approved in the US.

The oral adenosine triphosphate-citrate lyase (ACL) inhibitor bempedoic acid was approved by the FDA in 2020 for use alone (Nexletol – Esperion) and in a fixed-dose combination with the cholesterol absorption inhibitor ezetimibe (Nexlizet) as an adjunct to maximally tolerated statin therapy in adults with heterozygous familial hypercholesterolemia (HeFH) or established atherosclerotic cardiovascular disease (ASCVD) who require additional LDL-cholesterol (LDL-C) lowering. The indication has now been expanded to include reducing the risk of myocardial infarction (MI) and coronary...

The FDA has approved the subcutaneously injected PCSK9 (proprotein convertase subtilisin kexin type 9) inhibitor alirocumab (Praluent – Sanofi/Regeneron) as an adjunct to diet and maximally tolerated statin therapy for adults with heterozygous familial hypercholesterolemia (HeFH) or clinical atherosclerotic cardiovascular disease who require additional lowering of LDL-cholesterol (LDL-C). It was not approved for general use in statin-intolerant patients. Alirocumab is the first PCSK9 inhibitor to be approved in the US. Evolocumab (Repatha – Amgen), another PCSK9 inhibitor, was...

The FDA has approved inclisiran (Leqvio – Novartis), a small interfering RNA (siRNA) directed to proprotein convertase subtilisin/kexin type 9 (PCSK9) mRNA, as an adjunct to diet and maximally tolerated statin therapy for subcutaneous (SC) treatment of adults with heterozygous familial hypercholesterolemia (HeFH) or clinical atherosclerotic cardiovascular disease (ASCVD) who require additional lowering of low-density lipoprotein cholesterol (LDL-C). Inclisiran is the first FDA-approved PCSK9-directed siRNA therapeutic agent.