General Information

Nexlizet is an oral, once-daily bempedoic acid 180 mg/ezetimibe 10 mg combination tablet. The combination tablet inhibits 2 key enzymes—ACL and NPC1L1.

Nexlizet is specifically indicated with diet and maximally tolerated statins for adults with heterozygous familial hypercholesterolemia (HeFH) or established atherosclerotic cardiovascular disease (ASCVD) who need additional help lowering LDL-C.

Nexlizet is supplied as a tablet for once daily, oral administration.

Mechanism of Action

Nexlizet is an oral, once-daily bempedoic acid 180 mg/ezetimibe 10 mg combination tablet. Nexlizet inhibits 2 key enzymes—ACL and NPC1L1—and is designed to have two complementary mechanisms of action: Bempedoic acid inhibits cholesterol synthesis via ACL inhibition in the liver. Ezetimibe blocks gastrointestinal cholesterol absorption via NPC1L1 (Niemann-Pick C1-Like 1) inhibition, reducing cholesterol delivery to the liver. These complementary mechanisms are designed to result in LDL receptor upregulation and increased LDL-C clearance from the bloodstream.

Side Effects

Adverse effects associated with the use of Nexlizet may include, but are not limited to, the following:

upper respiratory tract infection

muscle spasms

hyperuricemia

back pain

abdominal pain or discomfort

bronchitis

pain in the extremities

anemia

elevated liver enzymes

diarrhea

arthralgia

sinusitis

fatigue

influenza

Clinical Trial Results

The FDA approval of Nexlizet was based on a single, pivotal, Phase 3 bridging study (1002-053) evaluating bempedoic acid 180 mg/ezetimibe 10 mg combination tablet in 382 patients with ASCVD, or at high risk for ASCVD, taking maximally tolerated statin therapy. Safety data was also gathered from the Nexletol tablet global pivotal Phase III LDL-C lowering program and the existing safety profile of ezetimibe. In the trials, Nexlizet decreased LDL-C by a mean of 38% compared to placebo when added to the maximum tolerated dose of statins. The drug was generally well-tolerated.