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 in laboratory rats. The authors stated that 鈥淓SP 55016 reduced serum non-HDL1-cholesterol (non-HDL-C), triglyceride, and nonesterified fatty acid levels while increasing serum HDL-C and 尾-hydroxybutyrate levels in a dose-dependent manner.鈥�
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, 鈥渂empedoic acid added to maximally tolerated statin therapy did not lead to a higher incidence of overall adverse events than placebo and led to .
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 鈥渁mong statin-intolerant patients, treatment with bempedoic acid was associated with a lower risk of major adverse cardiovascular events.鈥�
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聽hazard information*
| Hazard class** | GHS code and hazard statement | |
|---|---|---|
| Acute toxicity, oral, category 4 | H302鈥擧armful if swallowed |  |
Acute toxicity, dermal, category 4 | H312鈥擧armful in contact with skin | |
| Skin corrosion/irritation, category 2 | H315鈥擟auses skin irritation | |
| Serious eye damage/eye irritation, category 2A | H319鈥擟auses serious eye irritation | |
| Acute toxicity, inhalation, category 4 | H332鈥擧armful if inhaled | |
| Specific target organ toxicity, single exposure, respiratory tract irritation, category 3 | H335鈥擬ay cause respiratory irritation | |
| Reproductive toxicity, category 2 | H361鈥擲uspected of damaging fertility or the unborn child |  |
| Specific target organ toxicity. repeated exposure, category 1 | H372鈥擟auses 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. .
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 鈥淪ubstituted tetrahydrofurans as modulators of sodium channels鈥�. 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, 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 to come into the market in more than 20 years.
1. CAS Reg. No. 2649467-58-1.
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Bempedoic acid聽
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鈥�91 潞C |
| Water solubility | <1 g/L |
MOTW update:
March 31, 2025
Bempedoic acid1聽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鈥檚 LDL level significantly. After 6 months of using the combination therapy, however, the patient began to exhibit . When the fenofibrate was discontinued, the patient鈥檚 HDL levels returned to normal.
1. CAS Reg. No. 738606-46-7.
2. CAS Reg. No. 49562-28-9.
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