New Tablets for Lowering Cholesterol Granted FDA Approval

Officials with the FDA have approved Esperion’s bempedoic acid and ezetimibe (Nexlizet) tablet for lowering nonstatin LDL-Cholesterol (LDL-C). The oral, once-daily medication is indicated 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) that require additional lowering of LDL-C.¹

Bempedoic acid and ezetimibe combined is the first non-statin, LDL-C lowering combination medicine ever approved, according to Esperion.¹ The approval of the combination drug follows the February 21, 2020 approval of bempedoic acid (Nexletol) tablet for LDL-C by reducing cholesterol biosynthesis and up-regulating the LDL receptors.²

Both approved medications will be available only by prescription. The bempedoic acid and ezetimibe combined tablet will be commercially available in July 2020 for patients in the United States. The bempedoic acid tablet will be commercially available in the US patients on March 30, 2020, according to Esperion.¹

LDL-C is a waxy, fat-like substance found in the body. Elevated LDL-C contributes to a buildup of this fat in the arteries, and can lead to cardiovascular events, such as heart attack, and stroke. It is estimated that nearly 15 million patients with ASCVD or HeFH on maximally tolerated statins in the US cannot achieve guideline recommended LDL-C levels.^1-2 Bempedoic acid and ezetimibe combined lowers elevated LDL-C through complementary mechanisms of action by inhibiting cholesterol synthesis in the liver and absorption in the intestine.¹

The approval of the bempedoic acid and ezetimibe combination tablet is supported by the phase 3 Fixed Combination Drug Product LDL-C Lowering program, as well as safety data from the bempedoic acid tablet global pivotal phase 3 LDL-C lowering program, and the existing ezetimibe safety profile. The bempedoic acid and ezetimibe combination lowered LDL-C by a mean of 38% compared to placebo when added on to maximally tolerated statins.¹

The bempedoic acid and ezetimibe combination was generally well-tolerated in a pivotal phase 3 study, according to Esperion. Label warnings and precautions include hyperuricemia, with the development of gout in a small percentage of patients, as well as an increased risk of tendon rupture or injury.¹

The most common adverse events reported in the development program (incidence ≥ 2% and greater than placebo) were generally reported at similar rates in patients who received placebo. These adverse events included 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. The majority of adverse events reported with bempedoic acid and ezetimibe were mild to moderate in severity.¹

The effect on cardiovascular morbidity and mortality has not been determined in the bempedoic acid and ezetimibe combination,¹ nor in bempedoic acid alone.²

According to Esperion, the company is working with health insurance providers to help ensure broad insurance coverage, and patient access to its medicines. Eligible patients with commercial drug insurance coverage for these medicines may pay as little as $10 per fill, for up to a 3-month supply. Both the bempedoic acid and ezetimibe combination tablet and the bempedoic acid tablet will be priced at parity. Additionally, Esperion will provide resources to patients whose physician recommends treatment these newly approved medications. These resources include educational materials, a dedicated call center, as well as a co-pay program for eligible patients.^1-2

REFERENCES

• Esperion Announces FDA Approval of the NEXLIZET™ (bempedoic acid and ezetimibe) Tablet, an Oral, Once-Daily, Non-Statin LDL-Cholesterol Lowering Medicine [news release]. Ann Arbor, MI; February 26, 2020. Esperion website. https://www.esperion.com/investors-media/press-releases/. Accessed February 27, 2020.
• Esperion Announces FDA Approval of NEXLETOL™ (bempedoic acid) Tablet, an Oral, Once-Daily, Non-Statin LDL-Cholesterol Lowering Medicine [news release]. Ann Arbor, MI; February 21, 2020. Esperion website. https://www.esperion.com/investors-media/press-releases/. Accessed February 27, 2020.