Enlicitide is an oral medication that works by inhibiting the PCSK9 protein to lower bad (LDL) cholesterol, a potential first-in-class oral PCSK9 inhibitor.
It has shown significant LDL-C reduction in Phase 3 trials, with a safety profile comparable to a placebo.
Enlicitide is a small molecule that inhibits the PCSK9 protein, which is the same mechanism as current injectable PCSK9 inhibitors.
By binding to PCSK9, enlicitide prevents it from binding to LDL receptors on liver cells, allowing more LDL cholesterol to be cleared from the blood.
Cholesterol reduction: In clinical trials, enlicitide significantly lowered LDL-C, by up to nearly 60%.
It also reduced other lipids like non-HDL cholesterol and apolipoprotein B.
Its safety profile in trials has been comparable to a placebo.
A full effect requires taking the medication on an empty stomach.
It is an oral alternative to injectable PCSK9 inhibitors, which may improve treatment options and adherence.
Phase 3 clinical trials have been completed with positive results.
Ongoing trials are expected to determine enlicitide’s impact on preventing major cardiovascular events.
Among adults with heterozygous familial, hypercholesterolemia, treatment withenlicitide was well tolerated and significantly reduced levels of LDL – apoliporotein B, non-HDL – C and lipoprotein (a) A.
Among participants with the history of or were at risk for first atherosclerotic disease event, treatment with the oral PCSK9 inhibitor enlicitide resulted in significant lower LDL cholesterol levels than placebo at 24 weeks.