The Food and Drug Administration (FDA) has approved Nexlizet (bempedoic acid and ezetimibe; Esperion) as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia (HeFH) or established atherosclerotic cardiovascular disease (ASCVD) who require additional lowering of low-density lipoprotein cholesterol (LDL-C). Recently, the Agency approved Nexletol (bempedoic acid) tablet for the same indication.
Nexlizet is a combination of an adenosine triphosphate-citrate lyase (ACL) inhibitor, bempedoic acid, and ezetimibe, a cholesterol absorption inhibitor. The approval was based on data from the phase 3 trial that assessed the efficacy of Nexlizet in 301 adult patients randomized 2:2:2:1 to receive either Nexlizet (180mg bempedoic acid, 10mg ezetimibe) (N=86), bempedoic acid 180mg (n=88), ezetimibe 10mg (n=86), or placebo (n=41) once daily as add-on to maximally tolerated statin therapy. The primary end point was the percent change from baseline to week 12 in LDL-C.
Findings from the study showed that patients treated with Nexlizet achieved greater improvements to LDL-C at week 12 than placebo (adjusted difference -38%; 95% CI: -47, -30; P <.001), ezetimibe alone (-23.2%; P <.001) or bempedoic acid alone (-17.2%; P <.001). Additional exploratory end points evaluated the effects of Nexlizet on high-density lipoprotein (HDL) and triglycerides (TG), which included a placebo-adjusted mean change from baseline to week 12 of -5% for HDL and median change of -11% for TG.
With regard to safety, Nexlizet is supported by data from the Nexletol phase 3 program and the existing ezetimibe safety profile. The most common adverse reactions include upper respiratory tract infection, muscle spasms, hyperuricemia, back pain, abdominal pain or discomfort, bronchitis, pain in extremity, anemia, elevated liver enzymes, diarrhea, arthralgia, sinusitis, fatigue and influenza. Additionally, bempedoic acid has been associated with an increased risk of tendon rupture (0.5% of bempedoic acid-treated patients vs 0% of placebo-treated patients).
“Nexlizet provides significant additional LDL-C lowering for adult patients with ASCVD or HeFH when added to maximally tolerated statin medicine, including those patients for whom maximally tolerated statin may be no statin at all,” said Christie M. Ballantyne, MD, chairman of Esperion’s phase 3 Executive Committee and professor and chief of cardiology at Baylor College of Medicine in Houston. “[…] It also has the conventional, oral, once-daily administration which can prove beneficial to patients struggling to meet their cholesterol goals with the currently available statin options in their daily regimen.”
Nexlizet will be available as 180mg bempedoic acid/10mg ezetimibe tablets in 30- and 90-count bottles in July 2020. Nexletol will be available on March 30, 2020.
For more information visit esperion.com.