Peringatan Keamanan

LD50 information for bempedoic acid is not readily available in the literature. In the case of an overdose with bempedoic acid, contact the local poison control center. To this date, there is no experience with bempedoic acid overdoses. Employ general supportive measures.L12144

Bempedoic acid

DB11936

small molecule approved investigational

Deskripsi

High levels of LDL cholesterol (LDL-C) are a major risk factor for cardiovascular events. Caused by genetic mutations or lifestyle factors, hypercholesterolemia can significantly reduce quality of life and increase the risk of mortality from cardiovascular disease.L12153 About 1 in 4 patients, or 15 million Americans with elevated LDL-C, are insufficiently managed with maximally tolerated statin therapy alone, requiring additional treatment for hypercholesterolemia.L12180

Bempedoic acid is first-in-class adenosine triphosphate-citrate lyase (ACL) inhibitor used once a day for reducing LDL cholesterol levels in statin-refractory patients.L12144,L12147 It was developed by Esperion Therapeutics Inc. and approved by the FDA on February 21, 2020. A combination product of bempedoic acid and ezetimibe was approved on February 26, 2020 for increased control of LDL cholesterol levels in patients experiencing refractory elevations despite previous statin treatment.L12144,L12150

Struktur Molekul 2D

Berat 344.492
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of bempedoic acid ranges between 15 and 24 hours.[A191877] Prescribing information indicates a clearance of 21 hours +/- 11 hours.[L12144]
Volume Distribusi The apparent volume of distribution of bempedoic acid is about 18L.[L12144]
Klirens (Clearance) The clearance (CL/F) of bempedoic acid at steady state was estimated at 11.2 mL/min during clinical trials.[L12144]

Absorpsi

Bempedoic acid is rapidly absorbed in the small intestine.A191877,A191904 The Tmax of the 180mg tablet is estimated at 3.5 hours.L12144

Metabolisme

The two main metabolites of bempedoic metabolism are ETC-1002-CoAA191907 and ESP15228. Bempedoic acid is primarily eliminated via the metabolism of its acyl glucuronide. This drug is reversibly converted to an active metabolite (ESP15228) based on observations during in vitro studies. Both compounds resulting from the metabolism of bempedoic acid are metabolized to become inactive glucuronide conjugates by the enzyme UGT2B7.L12144

Rute Eliminasi

Bempedoic acid's conjugates are primarily eliminated via the urine (70%) and the feces (30%). A total of 5% of the unchanged drug is excreted in the urine and feces, combined.L12144

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

125 Data
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Bempedoic acid.
Valsartan The excretion of Valsartan can be decreased when combined with Bempedoic acid.
Erythromycin The excretion of Erythromycin can be decreased when combined with Bempedoic acid.
Torasemide The excretion of Torasemide can be decreased when combined with Bempedoic acid.
Liothyronine The excretion of Liothyronine can be decreased when combined with Bempedoic acid.
Conjugated estrogens The excretion of Conjugated estrogens can be decreased when combined with Bempedoic acid.
Digoxin The excretion of Digoxin can be decreased when combined with Bempedoic acid.
Cerivastatin The excretion of Cerivastatin can be decreased when combined with Bempedoic acid.
Raloxifene The excretion of Raloxifene can be decreased when combined with Bempedoic acid.
Caspofungin The excretion of Caspofungin can be decreased when combined with Bempedoic acid.
Bosentan The excretion of Bosentan can be decreased when combined with Bempedoic acid.
Methotrexate The excretion of Methotrexate can be decreased when combined with Bempedoic acid.
Enalapril The excretion of Enalapril can be decreased when combined with Bempedoic acid.
Sumatriptan The excretion of Sumatriptan can be decreased when combined with Bempedoic acid.
Mycophenolate mofetil The excretion of Mycophenolate mofetil can be decreased when combined with Bempedoic acid.
Penicillamine The excretion of Penicillamine can be decreased when combined with Bempedoic acid.
Repaglinide The excretion of Repaglinide can be decreased when combined with Bempedoic acid.
Dinoprostone The excretion of Dinoprostone can be decreased when combined with Bempedoic acid.
Fexofenadine The excretion of Fexofenadine can be decreased when combined with Bempedoic acid.
Benzylpenicillin The excretion of Benzylpenicillin can be decreased when combined with Bempedoic acid.
Atorvastatin The excretion of Atorvastatin can be decreased when combined with Bempedoic acid.
Ouabain The excretion of Ouabain can be decreased when combined with Bempedoic acid.
Fluvastatin The excretion of Fluvastatin can be decreased when combined with Bempedoic acid.
Rosuvastatin The excretion of Rosuvastatin can be decreased when combined with Bempedoic acid.
Liotrix The excretion of Liotrix can be decreased when combined with Bempedoic acid.
Cholic Acid The excretion of Cholic Acid can be decreased when combined with Bempedoic acid.
Taurocholic acid The excretion of Taurocholic acid can be decreased when combined with Bempedoic acid.
Cobimetinib The excretion of Bempedoic acid can be decreased when combined with Cobimetinib.
Atrasentan The excretion of Atrasentan can be decreased when combined with Bempedoic acid.
Simeprevir The excretion of Simeprevir can be decreased when combined with Bempedoic acid.
Ambrisentan The excretion of Ambrisentan can be decreased when combined with Bempedoic acid.
Axitinib The excretion of Axitinib can be decreased when combined with Bempedoic acid.
Gimatecan The excretion of Gimatecan can be decreased when combined with Bempedoic acid.
Temocapril The excretion of Temocapril can be decreased when combined with Bempedoic acid.
Cholecystokinin The excretion of Cholecystokinin can be decreased when combined with Bempedoic acid.
Gadoxetic acid The excretion of Gadoxetic acid can be decreased when combined with Bempedoic acid.
Technetium Tc-99m mebrofenin The excretion of Technetium Tc-99m mebrofenin can be decreased when combined with Bempedoic acid.
Fimasartan The excretion of Fimasartan can be decreased when combined with Bempedoic acid.
Paritaprevir The excretion of Paritaprevir can be decreased when combined with Bempedoic acid.
Tenofovir alafenamide The excretion of Tenofovir alafenamide can be decreased when combined with Bempedoic acid.
Selexipag The excretion of Selexipag can be decreased when combined with Bempedoic acid.
Grazoprevir The excretion of Grazoprevir can be decreased when combined with Bempedoic acid.
Asunaprevir The excretion of Asunaprevir can be decreased when combined with Bempedoic acid.
Elagolix The excretion of Elagolix can be decreased when combined with Bempedoic acid.
Voxilaprevir The excretion of Voxilaprevir can be decreased when combined with Bempedoic acid.
Letermovir The excretion of Letermovir can be decreased when combined with Bempedoic acid.
Levosalbutamol The excretion of Levosalbutamol can be decreased when combined with Bempedoic acid.
Glecaprevir The excretion of Glecaprevir can be decreased when combined with Bempedoic acid.
Remdesivir The excretion of Bempedoic acid can be decreased when combined with Remdesivir.
Belantamab mafodotin The excretion of Belantamab mafodotin can be decreased when combined with Bempedoic acid.
Progesterone The excretion of Bempedoic acid can be increased when combined with Progesterone.
Cyclosporine The excretion of Bempedoic acid can be decreased when combined with Cyclosporine.
Nelfinavir The excretion of Bempedoic acid can be decreased when combined with Nelfinavir.
Beclomethasone dipropionate The excretion of Bempedoic acid can be decreased when combined with Beclomethasone dipropionate.
Vincristine The excretion of Bempedoic acid can be decreased when combined with Vincristine.
Ivermectin The excretion of Bempedoic acid can be decreased when combined with Ivermectin.
Nystatin The excretion of Bempedoic acid can be decreased when combined with Nystatin.
Roxithromycin The excretion of Bempedoic acid can be decreased when combined with Roxithromycin.
Sulfasalazine The excretion of Bempedoic acid can be decreased when combined with Sulfasalazine.
Mifepristone The excretion of Bempedoic acid can be decreased when combined with Mifepristone.
Tipranavir The excretion of Bempedoic acid can be decreased when combined with Tipranavir.
Dipyridamole The excretion of Bempedoic acid can be decreased when combined with Dipyridamole.
Telithromycin The excretion of Bempedoic acid can be decreased when combined with Telithromycin.
Novobiocin The excretion of Bempedoic acid can be decreased when combined with Novobiocin.
Atazanavir The excretion of Bempedoic acid can be decreased when combined with Atazanavir.
Nefazodone The excretion of Bempedoic acid can be decreased when combined with Nefazodone.
Gemfibrozil The excretion of Bempedoic acid can be decreased when combined with Gemfibrozil.
Everolimus The excretion of Bempedoic acid can be decreased when combined with Everolimus.
Lopinavir The excretion of Bempedoic acid can be decreased when combined with Lopinavir.
Dronedarone The excretion of Bempedoic acid can be decreased when combined with Dronedarone.
Ataluren The excretion of Bempedoic acid can be decreased when combined with Ataluren.
Ginsenoside Rb1 The excretion of Bempedoic acid can be decreased when combined with Ginsenoside Rb1.
Rilpivirine The excretion of Bempedoic acid can be decreased when combined with Rilpivirine.
Dabrafenib The excretion of Bempedoic acid can be decreased when combined with Dabrafenib.
Idelalisib The excretion of Bempedoic acid can be decreased when combined with Idelalisib.
Cobicistat The excretion of Bempedoic acid can be decreased when combined with Cobicistat.
Daclatasvir The excretion of Bempedoic acid can be decreased when combined with Daclatasvir.
Sacubitril The excretion of Bempedoic acid can be decreased when combined with Sacubitril.
Silibinin The excretion of Bempedoic acid can be decreased when combined with Silibinin.
Velpatasvir The excretion of Bempedoic acid can be decreased when combined with Velpatasvir.
Istradefylline The excretion of Bempedoic acid can be decreased when combined with Istradefylline.
Valspodar The excretion of Bempedoic acid can be decreased when combined with Valspodar.
Testosterone The excretion of Testosterone can be decreased when combined with Bempedoic acid.
Paclitaxel The excretion of Paclitaxel can be decreased when combined with Bempedoic acid.
Docetaxel The excretion of Docetaxel can be decreased when combined with Bempedoic acid.
Sincalide The excretion of Sincalide can be decreased when combined with Bempedoic acid.
Selinexor The excretion of Bempedoic acid can be decreased when combined with Selinexor.
Fedratinib The excretion of Bempedoic acid can be decreased when combined with Fedratinib.
Pexidartinib The excretion of Bempedoic acid can be decreased when combined with Pexidartinib.
Enasidenib The excretion of Bempedoic acid can be decreased when combined with Enasidenib.
Pibrentasvir The excretion of Bempedoic acid can be decreased when combined with Pibrentasvir.
Elexacaftor The serum concentration of Bempedoic acid can be increased when it is combined with Elexacaftor.
Ritonavir The excretion of Bempedoic acid can be decreased when combined with Ritonavir.
Fostemsavir The excretion of Bempedoic acid can be decreased when combined with Fostemsavir.
Pralsetinib The excretion of Bempedoic acid can be decreased when combined with Pralsetinib.
Clarithromycin The excretion of Bempedoic acid can be decreased when combined with Clarithromycin.
Darolutamide The excretion of Bempedoic acid can be decreased when combined with Darolutamide.
Revefenacin Bempedoic acid may decrease the excretion rate of Revefenacin which could result in a higher serum level.
Dovitinib The excretion of Bempedoic acid can be decreased when combined with Dovitinib.
Indomethacin The metabolism of Bempedoic acid can be decreased when combined with Indomethacin.

Target Protein

ATP-citrate synthase ACLY

Referensi & Sumber

Synthesis reference: David M Paton. Bempedoic Acid: ATP-citrate lyase inhibitor.(2017). Drugs of the Future. 42(4):201-208
Artikel (PubMed)
  • PMID: 29609755
    Saeed A, Ballantyne CM: Bempedoic Acid (ETC-1002): A Current Review. Cardiol Clin. 2018 May;36(2):257-264. doi: 10.1016/j.ccl.2017.12.007. Epub 2018 Feb 21.
  • PMID: 27663902
    Bilen O, Ballantyne CM: Bempedoic Acid (ETC-1002): an Investigational Inhibitor of ATP Citrate Lyase. Curr Atheroscler Rep. 2016 Oct;18(10):61. doi: 10.1007/s11883-016-0611-4.
  • PMID: 29939848
    Zagelbaum NK, Yandrapalli S, Nabors C, Frishman WH: Bempedoic Acid (ETC-1002): ATP Citrate Lyase Inhibitor: Review of a First-in-Class Medication with Potential Benefit in Statin-Refractory Cases. Cardiol Rev. 2019 Jan/Feb;27(1):49-56. doi: 10.1097/CRD.0000000000000218.
  • PMID: 30922156
    Jia X, Virani SS: CLEAR Serenity Trial: More Clarity for the Future of Bempedoic Acid in Patients Unable to Take Statins? J Am Heart Assoc. 2019 Apr 2;8(7):e012352. doi: 10.1161/JAHA.119.012352.
  • PMID: 30865796
    Ray KK, Bays HE, Catapano AL, Lalwani ND, Bloedon LT, Sterling LR, Robinson PL, Ballantyne CM: Safety and Efficacy of Bempedoic Acid to Reduce LDL Cholesterol. N Engl J Med. 2019 Mar 14;380(11):1022-1032. doi: 10.1056/NEJMoa1803917.

Contoh Produk & Brand

Produk: 24 • International brands: 0
Produk
  • Nexletol
    Tablet, film coated • 180 mg/1 • Oral • US • Approved
  • Nexlizet
    Tablet, film coated • - • Oral • US • Approved
  • Nilemdo
    Tablet, film coated • 180 mg • Oral • EU • Approved
  • Nilemdo
    Tablet, film coated • 180 mg • Oral • EU • Approved
  • Nilemdo
    Tablet, film coated • 180 mg • Oral • EU • Approved
  • Nilemdo
    Tablet, film coated • 180 mg • Oral • EU • Approved
  • Nilemdo
    Tablet, film coated • 180 mg • Oral • EU • Approved
  • Nilemdo
    Tablet, film coated • 180 mg • Oral • EU • Approved
Menampilkan 8 dari 24 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul