The US FDA has approved enlicitide (Lipfendra), the first oral PCSK9 inhibitor, as an adjunct to diet and exercise to reduce low-density lipoprotein cholesterol (LDL-C) in adults with hypercholesterolemia, including heterozygous familial hypercholesterolemia (HeFH). Mechanism of Action PCSK9 binds to low-density lipoprotein receptors (LDLRs) on hepatocytes, promoting their degradation. Enlicitide blocks the interaction between PCSK9 and LDLRs, increasing the number of available LDL receptors and enhancing LDL-C clearance from the bloodstream.
Clinical Evidence In a clinical trial involving 2,904 adults with hypercholesterolemia, enlicitide reduced LDL-C levels by 56% versus placebo at week 24. In a separate trial of 303 adults with HeFH, enlicitide achieved a 59% greater reduction in LDL-C levels compared with placebo. Dosage and Administration 20 mg orally once daily Take on an empty…
