What molecule am I?
Bempedoic acid is a hydroxyalkane diacid and the active ingredient in hypercholesteremia medication. Under the name ESP 55016, it was first described in 2004 by Michael E. Pape and co-workers at Esperion Therapeutics (Ann Arbor, MI) as a dual lipid synthesis inhibitor in laboratory rats. The authors stated that “ESP 55016 reduced serum non-HDL1-cholesterol (non-HDL-C), triglyceride, and nonesterified fatty acid levels while increasing serum HDL-C and β-hydroxybutyrate levels in a dose-dependent manner.”
Bempedoic acid was developed for use in patients who do not tolerate statins for reducing LDL1-C or are already using the maximum tolerated dose of a statin. In 2019, Kausik K. Ray and colleagues in the CLEAR Harmony Trial2 team reported on the long-term safety, tolerability, and efficacy of bempedoic acid in high cardiovascular-risk patients with LDL-C of >1.8 mmol/L who were already on maximally tolerated statins. The team found that in the 52-week trial on 1488 patients, “bempedoic acid added to maximally tolerated statin therapy did not lead to a higher incidence of overall adverse events than placebo and led to significantly lower LDL cholesterol levels.
The following year, the US Food and Drug Administration approved bempedoic acid (trade name Nexletol) for lowering LDL-C in adults with family-related hypercholesteremia and those with established cardiovascular disease. Three years later, FDA expanded the label to include the broader treatment of primary hyperlipidemia with bempedoic acid alone or in combination with ezetimibe3, another nonstatin and a previous Molecule of the Future.
In 2023, Steven E. Nissen at the Cleveland Clinic and members of what was by then called the CLEAR Outcomes Investigators reported on the effects of bempedoic acid on cardiovascular outcomes in statin-intolerant patients; the effects were uncertain at the time. The authors concluded that “among statin-intolerant patients, treatment with bempedoic acid was associated with a lower risk of major adverse cardiovascular events.”
1. HDL stands for high-density lipoprotein; non-HDL is often referred to as low-density lipoprotein, or LDL.
2. The CLEAR Harmony clinical trial was funded by Esperion and included researchers at multiple drug companies and government institutions.
3. CAS Reg. No. 163222-33-1.
Bempedoic acid hazard information*
| Hazard class** | GHS code and hazard statement | |
|---|---|---|
| Acute toxicity, oral, category 4 | H302—Harmful if swallowed |  |
Acute toxicity, dermal, category 4 | H312—Harmful in contact with skin | |
| Skin corrosion/irritation, category 2 | H315—Causes skin irritation | |
| Serious eye damage/eye irritation, category 2A | H319—Causes serious eye irritation | |
| Acute toxicity, inhalation, category 4 | H332—Harmful if inhaled | |
| Specific target organ toxicity, single exposure, respiratory tract irritation, category 3 | H335—May cause respiratory irritation | |
| Reproductive toxicity, category 2 | H361—Suspected of damaging fertility or the unborn child |  |
| Specific target organ toxicity. repeated exposure, category 1 | H372—Causes damage to organs through prolonged or repeated exposure | |
*Compilation of multiple safety data sheets; considerable variation among published SDSs.
**Globally Harmonized System (GHS) of Classification and Labeling of Chemicals. Explanation of pictograms.
Suzetrigine1 is a newly registered nonopioid pain medication. It was first described in world patent application WO2021113627 (2021) to inventor Steven Durrant at Vertex Pharmaceuticals (Boston) under the title “Substituted tetrahydrofurans as modulators of sodium channels”. Vertex filed three additional patent applications in 2022.
In 2023, Stephen G. Waxman at the Yale School of Medicine (New Haven, CT) wrote that suzetrigine, then called VX-548, inhibits sodium channel NaV1.8 to control pain. NaV1.8 has been shown to be resistant to earlier analgesics.
On January 30, the US Food and Drug Administration approved suzetrigine (trade name Journavx) as the first new type of pain reliever to come into the market in more than 20 years.
1. CAS Reg. No. 2649467-58-1.
Molecule of the Future
Once a month we bring you a newly discovered or developed molecule that has important implications for the future of chemistry or society in general. Look for it the third week of each month. Learn more about this month's Molecule of the Future.
We're looking for more molecules of the future!
Do you have a suggestion for the next molecule of the future? Send your idea to MOTW.
This molecule was suggested by a reader. We present almost all of the molecules suggested by our readers. If you have a molecule you would like us to consider, please send us a message. And thank you for your interest in Molecule of the Week! —Ed.
Bempedoic acid
fast facts
| CAS Reg. No. | 738606-46-7 |
| SciFindern name | Pentadecanedioic acid, 8-hydroxy-2,2,14,14-tetramethyl- |
| Empirical formula | C19H36O5 |
| Molar mass | 344.49 |
| Appearance | White to off-white crystalline powder |
| Melting point | 88–91 ºC |
| Water solubility | <1 g/L |
MOTW update:
March 31, 2025
Bempedoic acid1 is a drug used by hypercholesteremic patients who do not tolerate statins for reducing low-density lipoprotein (LDL) or are already using the maximum-tolerated dose of a statin.
Last week, Francesco Sbrana*, Federico Bigazzi, and Beatrice Dal Pino at Fondazione Toscana Gabriele Monasterio (Pisa, Italy) reported that adding fenofibrate2, another cholesterol-lowering drug, to bempedoic acid decreased an obese patient’s LDL level significantly. After 6 months of using the combination therapy, however, the patient began to exhibit greatly reduced high-density lipoprotein (HDL) levels. When the fenofibrate was discontinued, the patient’s HDL levels returned to normal.
1. CAS Reg. No. 738606-46-7.
2. CAS Reg. No. 49562-28-9.
Learn more about this molecule from CAS, the most authoritative and comprehensive source for chemical information.
Molecule of the Week needs your suggestions!
If your favorite molecule is not in our archive, please send us a message. The molecule can be notable for its current or historical importance or for any quirky reason. Thank you!
Stay Ahead of the Chemistry Curve
Learn how ACS can help you stay ahead in the world of chemistry.
