FDA approves Lipfendra, first oral PCSK9 inhibitor, to lower LDL cholesterol in adults

The U.S. Food and Drug Administration has approved Lipfendra (enlicitide), the first oral inhibitor of the PCSK9 protein, for use as an adjunct to diet and exercise in adults with high cholesterol, including those with heterozygous familial hypercholesterolemia.

Lipfendra is taken as a once‑daily tablet, marking the first oral option in a class that has previously been limited to injectable drugs. The new formulation provides an additional pathway for patients who need further LDL‑C reduction beyond existing therapies.

Michael Davis, M.D., Ph.D., Acting Director of the FDA’s Center for Drug Evaluation and Research, highlighted that cardiovascular disease remains the leading cause of death in the United States and that lowering LDL‑C is a key modifiable risk factor. He said the approval reflects the agency’s commitment to expanding patient access to innovative treatments.

Hypercholesterolemia, characterized by elevated LDL‑C, can lead to plaque buildup in arteries and increase the risk of heart disease. The oral PCSK9 inhibitor offers clinicians a new tool to manage this risk in a broader patient population.