738606-46-7

Product Details:

CasNo： 738606-46-7

Molecular Formula： C19H36O5

Appearance： White to off-white Powder

Packing： Aluminium bag

Throughput： 100KG/Month

Purity： 99%

Brief Summary

Bempedoic acid (CAS 738606-46-7) is an oral, first-in-class ATP-citrate lyase (ACL) inhibitor for lipid management. It reduces hepatic cholesterol synthesis upstream of statins and lowers LDL‑C, non‑HDL‑C and apolipoprotein B. Originally developed by Esperion under the brand name Nexletol®, it is indicated for heterozygous familial hypercholesterolemia (HeFH) and atherosclerotic cardiovascular disease (ASCVD) in patients requiring additional LDL‑C reduction. This API is supplied for generic formulation development, CMC studies and preclinical lipid metabolism research.

Product Overview

Bempedoic acid is a novel oral lipid-lowering agent with a unique mechanism distinct from statins, ezetimibe and PCSK9 inhibitors. It is a prodrug activated selectively in the liver by very long-chain acyl-CoA synthetase 1 (ACSVL1), which is minimally expressed in skeletal muscle. This liver-selective activation profile largely avoids the myalgia and myopathy risks commonly associated with statin therapy. Marketed as Nexletol®, it is used as monotherapy or in combination with other lipid-lowering therapies for patients who cannot tolerate statins or fail to reach LDL‑C targets on existing regimens. Bempedoic acid is the free acid form used directly in the commercial tablet formulation and serves as the reference API for generic development worldwide.

Mechanism of Action

ATP-citrate lyase (ACL) catalyses the conversion of cytosolic citrate to acetyl-CoA, a fundamental precursor for de novo cholesterol and fatty acid biosynthesis in the liver. Bempedoic acid is converted in hepatocytes to its active CoA-thioester metabolite, which competitively inhibits ACL. Suppression of ACL activity reduces the hepatic pool of acetyl-CoA, downregulates HMG-CoA reductase expression and diminishes endogenous cholesterol synthesis. This leads to upregulation of hepatic LDL receptors, increased clearance of circulating LDL particles and sustained reduction in plasma LDL‑C, non‑HDL‑C and apoB. Since activation occurs mainly within hepatocytes, peripheral muscle tissue is spared from drug exposure, separating its lipid-lowering effect from statin-like muscular adverse events.

Research & Clinical Background

Bempedoic acid received its first FDA approval in 2020, followed by authorisation in the EU and other regions. Key phase 3 programmes including CLEAR Harmony, CLEAR Wisdom and CLEAR Outcomes validated its lipid-lowering efficacy and cardiovascular safety profile. Core approved indications:

• Adjunct to diet and maximally tolerated statin therapy for reduction of elevated LDL‑C in adults with heterozygous familial hypercholesterolemia (HeFH) or established atherosclerotic cardiovascular disease (ASCVD);
• For patients with statin intolerance who require LDL‑C lowering. The CLEAR Outcomes trial demonstrated that bempedoic acid reduces major adverse cardiovascular events (MACE) including cardiovascular death, non‑fatal myocardial infarction and non‑fatal stroke. Fixed-dose combinations with ezetimibe are also available for simplified lipid control. Ongoing research evaluates its metabolic effects on NAFLD, diabetes and high-risk primary prevention populations.

Research & Commercial Applications

Our Bempedoic Acid API is offered for generic drug development and preclinical metabolic research:

• Nexletol® generic formulation development, process optimisation and CMC dossier preparation
• Polymorph control, impurity profiling, residual solvent testing and stability evaluation
• In vitro ACL enzyme inhibition, hepatocyte lipid biosynthesis and LDL receptor regulation assays
• In vivo rodent models of hypercholesterolemia, atherosclerosis and metabolic dysfunction
• Mechanism studies of hepatic lipogenesis and cross-talk between cholesterol and glucose metabolism
• Combination strategy research with statins, ezetimibe, PCSK9 inhibitors and SGLT‑2 agents

Product Statement & Disclaimer

This product is Bempedoic Acid API for pharmaceutical R&D and generic formulation use. Material produced under full GMP compliance may be used for clinical trial material manufacturing. It is not a finished dosage form. End users shall comply with local pharmaceutical regulations and complete required quality audits and registrations prior to clinical application. All technical data is provided for reference only.