Lipfendra (Enlicitide) is used to reduce low-density lipoprotein cholesterol (LDL-C) in adults with hypercholesterolemia, including heterozygous familial hypercholesterolemia (HeFH), along with diet and exercise.
It is an oral tablet taken once a day.
Enlicitide works by blocking a protein PCSK9 (proprotein convertase subtilisin kexin type 9).
Normally, PCSK9 attaches to LDL receptors on the surface of liver cells and causes them to break down.
These receptors are what the liver uses to clear LDL cholesterol from the blood, so fewer receptors means more LDL cholesterol stays in circulation.
By stopping PCSK9 from attaching to these receptors, Enlicitide leaves more of them available to remove LDL cholesterol, which lowers LDL cholesterol levels.
Enlicitide belongs to the drug class called PCSK9 inhibitors, and is the first oral PCSK9 inhibitor for lowering LDL-C to be approved.
Approval was based on two Phase 3 trials from the CORALreef program.
CORALreef Lipid: LDL-C dropped 56% compared to placebo at week 24.
Th reduction was 60% from the starting level.
CORALreef HeFH: in people with an inherited form of high cholesterol, LDL-C dropped 59% compared to placebo.
Both trials also showed reductions in non-HDL-C and ApoB.
Safety in CORALreef Lipids was similar to placebo; in CORALreef HeFH, the most common side effects were diarrhea (7% vs 2%) and dizziness (9% vs 4%).
It is not known if Enlicitide is safe and effective in children.
Common side effects
In people with high cholesterol, the side effects of Enlicitide are about the same as in people who are not taking Enlicitide.
In people with HeFH, the most common side effects of Enlicitide are diarrhea and dizziness.
Taken as Enlicitide-1 tablet of Lipfendra by mouth each morning on an empty stomach with water, black coffee, or plain tea.
Swallow the tablet whole.
Do not split, crush or chew the tablet.
After taking Enlicitide, wait at least 30 minutes before you eat or drink anything other than water, black coffee, or plain tea.