Merck Secures FDA Approval for First Oral PCSK9 Inhibitor LIPFENDRA to Treat High LDL Cholesterol
Merck has received approval from the US Food and Drug Administration (FDA) for LIPFENDRA® (enlicitide) 20 mg, making it the first oral PCSK9 inhibitor authorised in the United States.
For reducing low-density lipoprotein cholesterol (LDL-C) in adults with hypercholesterolaemia, including patients with heterozygous familial hypercholesterolaemia (HeFH).
The medicine is approved for use alongside a healthy diet and regular exercise to help manage elevated cholesterol levels.
LIPFENDRA is a once-daily tablet developed using macrocyclic peptide technology. It works by blocking the interaction between PCSK9 proteins and LDL receptors, enabling the liver to remove more LDL cholesterol from the bloodstream.
The oral formulation offers an alternative to injectable PCSK9 inhibitors for eligible patients.
The FDA approval is supported by results from the Phase III CORALreef Lipids and CORALreef HeFH clinical trials.
In these studies, patients treated with LIPFENDRA achieved LDL-C reductions of 56% and 59%, respectively, after 24 weeks compared with placebo.
The treatment also lowered non-HDL cholesterol and apolipoprotein B, both recognised markers linked to cardiovascular disease risk.
Clinical findings showed that LIPFENDRA had a safety profile comparable to placebo. In the HeFH study, diarrhoea and dizziness were the most frequently reported adverse events.
Merck is continuing to evaluate the therapy through the ongoing CORALreef Outcomes trial to determine its long-term impact on cardiovascular events and mortality in patients at increased cardiovascular risk.
