Bempedoic acid
NEXLETOL
Pronunciation: bem-pe-DOE-ik AS-id (NEX-le-tol)
“Necks let all Blimps peddle”
What it isATP-citrate lyase inhibitor acting upstream of HMG-CoA reductase; hyperlipidemia and ASCVD risk reduction.
Why this oneLiver-only activation spares muscle, and it reduces cardiovascular events in statin-intolerant patients.
What limits itHyperuricemia, gout, and tendon rupture can end treatment; it also raises exposure to some statins.
Pearls
- Modest LDL lowering alone; additive with ezetimibe (fixed combination exists).
- Can raise creatinine; cholelithiasis reported.
Bempedoic acid prescription history
Animated chart of estimated U.S. prescriptions per year, Lipid-lowering meds (1955–2026). Bempedoic acid enters in 2020 (estimated).
FDA-approved for
- hyperlipidemia / ASCVD risk reduction (2020)
Principal riskHyperuricemia and gout; tendon rupture
Classes and tags
Clinical profile
Legacy pregnancy categoryNot assigned — PLLR-era drug
Defining liabilityMyopathy/rhabdomyolysis and hepatotoxicity; interaction burden varies by agent.
FDA label
Read the full label on DailyMed ↗
NO BOXED WARNINGS
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Reduce risk of major adverse cardiovascular events (CV death, MI, stroke, coronary revascularization) in adults at increased risk unable to take recommended statin therapy | Adult | 180 mg QD | 180 mg QD | 180 mg QD |
| Hypercholesterolemia incl. HeFH — adjunct to diet/exercise, with other LDL-C-lowering therapy or alone when concomitant therapy not possible | Adult | 180 mg QD | 180 mg QD | 180 mg QD |
Renal Undefined
Hepatic No adjustment for mild or moderate impairment (Child-Pugh A or B); severe (Child-Pugh C) not studied
Instructions
- Take once daily with or without food
- Analyze lipid levels within 8-12 weeks after initiation
- Missed dose: take as soon as possible; do not double next dose
Available strengths
- tab 180 mg
Cautions
- Hyperuricemia — inhibits renal OAT2; may precipitate gout (gout 3.2% vs 2.2% placebo in CV outcomes trial); assess uric acid as indicated and treat with urate-lowering drugs as appropriate
- Tendon rupture (rotator cuff, biceps, Achilles; 0.5-1.2%) — discontinue immediately at first sign of rupture; consider discontinuing for joint pain/swelling/inflammation; consider alternatives in patients with tendon-disorder history; risk higher >60 yr, with corticosteroids/fluoroquinolones, renal failure
Adverse reactions
- Upper respiratory tract infection
- Muscle spasms
- Hyperuricemia, gout
- Back pain, abdominal pain, pain in extremity
- Bronchitis
- Anemia
- Elevated liver enzymes
- Renal impairment, cholelithiasis (CV outcomes trial)
Pregnancy Discontinue when pregnancy recognized unless benefits outweigh risks; may cause fetal harm based on mechanism (decreases cholesterol synthesis); insufficient human data
Lactation Detected in human breast milk (mean RID ~0.5%); may cause harm to breastfed infant; weigh benefits of breastfeeding against need and risk
Cost
| Strength | #/mo | generic $/mo | brand $/mo | CostPlus | |
|---|---|---|---|---|---|
| 180 mg | tab | 30 qd | — | $414.31 | not offered |
Generic entry2040 est.
Open Bempedoic acid in the interactive console ↗
Self-check
- Where is bempedoic acid activated rather than skeletal muscle?
Liver. - Which tendon complication can end bempedoic acid treatment?
Tendon rupture.