Bempedoic Acid/Ezetimibe Combination Tablet
Partners in LDL-C Lowering: Bempedoic Acid/Ezetimibe
Combination Tablet
ESPERION is developing a once-daily, oral bempedoic acid 180 mg/ezetimibe 10 mg combination tablet that is designed to lower LDL-C.1  

This non-statin, combination oral investigational therapy is designed to be used in combination with other lipid-lowering therapies for patients with primary hyperlipidemia who need additional LDL-C lowering.1

LDL-C=low-density lipoprotein cholesterol.
 
Complementary Mechanisms of Action
Bempedoic acid/ezetimibe combination tablet inhibits 2 key enzymes–ACL and NPC1L1, and is designed to have two complementary mechanisms of action:
1 Bempedoic acid inhibits cholesterol synthesis via ACL inhibition in the liver.
2 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.  

Based on feedback received from the FDA, Esperion completed 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. This trial was completed in 2018. The Phase 3 bridging study is intended to support approval for an LDL-C lowering indication in both the US and Europe.1

Development Timeline for Bempedoic Acid 180 mg/ezetimibe 10 mg combination tablet1,2
Bempedoic Acid/Ezetimibe
Oral, small molecule in fixed-dose combination
 
Lowering
elevated LDL-C
PHASE 1
PHASE 2
PHASE 3
NDA filed 
Feb 26, 2019
MAA filed 
Feb 11, 2019
In tandem with a New Drug Application (NDA) submission for bempedoic acid, ESPERION submitted an NDA for an LDL-C lowering indication for bempedoic acid 180 mg/ezetimibe 10 mg combination tablet through the abbreviated 505(b)(2) pathway on Feb. 26, 2019.  

Also, on Feb. 11, 2019, Esperion submitted a Marketing Authorization Application (MAA) for an LDL-C lowering indication for bempedoic acid 180 mg/ezetimibe 10 mg combination tablet consistent with the European Medicines Agency’s “Guideline on Clinical Development of Fixed Combination Medicinal Products.”

Get updates about ESPERION and the bempedoic acid/ ezetimibe
combination tablet
References: 1. Data on file. Esperion Therapeutics, Inc. 2019. 2. A study evaluating the safety and efficacy of bempedoic acid plus ezetimibe fixed-dose combination compared to bempedoic acid, ezetimibe, and placebo in patients treated with maximally tolerated statin therapy. ClinicalTrials.gov. https://clinicaltrials.gov/ct2/show/NCT03337308. Accessed February 8, 2019.