Bempedoic acid

Bempedoic acid May be taken with or without food.

Pregnancy and lactation.

Patient with a history of gout or previous tendon disorders.

Significant: Hyperuricaemia, gout, tendon rupture, increased ALT or AST.
Blood and lymphatic system disorders: Anaemia, leucopenia, thrombocytosis.
Cardiac disorders: Atrial fibrillation.
Gastrointestinal disorders: Abdominal pain, abdominal distress.
Investigations: Increased BUN, serum creatine kinase or serum creatinine.
Musculoskeletal and connective tissue disorders: Pain in extremity, back pain, muscle spasm.
Reproductive system and breast disorders: Benign prostatic hyperplasia.
Respiratory, thoracic and mediastinal disorders: URTI.

PO: Z (Should not be used during pregnancy or contraindicated (manufacturer specific))

Obtain lipid levels within 8-12 weeks of treatment initiation; uric acid levels as necessary. Assess for signs and symptoms of hyperuricaemia, tendinopathy or tendon rupture.

Increased risk of myopathy with statins (e.g. simvastatin, pravastatin). Increases plasma concentration of drugs that are substrates of OATP1B1 or OATP1B3 (e.g. bosentan, fimasartan, asunaprevir, glecaprevir, grazoprevir, voxilaprevir, atorvastatin, simvastatin, rosuvastatin, pravastatin, fluvastatin, pitavastatin). Increased risk of tendon rupture with corticosteroids and fluoroquinolones.

Description:
Mechanism of Action: Bempedoic acid is an adenosine triphosphate-citrate lyase (ACL) inhibitor. It reduces low-density lipoprotein cholesterol (LDL-C) by preventing cholesterol synthesis in the liver. In the cholesterol biosynthesis pathway, ACL is an enzyme upstream of 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase. Bempedoic acid and ESP15228 (active metabolite) require coenzyme A (CoA) activation by very long-chain acyl-CoA synthetase 1 (ACSVL1) into ETC-1002-CoA and ESP15228-CoA, respectively. ETC-1002-CoA inhibits ACL, thereby causing reduced cholesterol synthesis in the liver and decreased LDL-C in the blood through the upregulation of low-density lipoprotein (LDL) receptors.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: 3.5 hours.
Distribution: Volume of distribution: 18 L. Plasma protein binding: 99.3%.
Metabolism: Metabolised in the liver mainly through the metabolism of the acyl glucuronide. Reversibly metabolised by aldo-keto reductase into ESP15228 (active metabolite), which is also converted into a glucuronide conjugate.
Excretion: Via faeces (30%; <5% as unchanged drug); urine (<5% as unchanged drug; approx 70% of total dose as bempedoic acid and metabolites). Elimination half-life: 21 ± 11 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 10472693, Bempedoic Acid. https://pubchem.ncbi.nlm.nih.gov/compound/Bempedoic-Acid. Accessed Apr. 26, 2024.

Store between 15-30°C.

Thuốc trị rối loạn lipid máu

C10AX15 - bempedoic acid ; Belongs to the class of other lipid modifying agents.

Anon. Bempedoic Acid. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 03/04/2024.

Bempedoic Acid. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 15/04/2024.

Bempedoic Acid. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 03/04/2024.

Buckingham R (ed). Bempedoic Acid. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/04/2024.

Joint Formulary Committee. Bempedoic Acid. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/04/2024.

Nexletol Tablet, Film Coated (Esperion Therapeutics, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 03/04/2024.

Nilemdo 180 mg Film-coated Tablets (Daiichi Sankyo UK Ltd). MHRA. https://products.mhra.gov.uk. Accessed 03/04/2024.

Nilemdo Tablets (Daiichi Sankyo Hong Kong Limited). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 03/04/2024.