Bempedoic acid

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Cat Number

INT738606467

CAS Number

738606-46-7

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Product Detail Description Scientific Support Customer Q&A

CAS Number

738606-46-7

Storage

2-8℃

Molecular Formula

C19H36O5

Molecular Weight

344.49

Smiles

C(O)(=O)C(C)(C)CCCCCC(O)CCCCCC(C)(C)C(O)=O

Appearance

White to off-white powder

Melting Point

87-92℃

Boiling Point

507℃

Relative Density

1.04

pKa

4.55

General Description

Bempedoic acid is a synthetic small-molecule drug that acts as an inhibitor of ATP-citrate lyase (ACL), an enzyme in the hepatic cholesterol biosynthesis pathway upstream of HMG-CoA reductase (the target of statins). It is a prodrug activated by very long-chain acyl-CoA synthetase 1 (ACSVL1) in the liver, which converts it to the active-CoA thioester, ensuring liver-specific target engagement with minimal extrahepatic effects.

Mechanism of Action

Bempedoic acid, after conversion to its active CoA thioester form in hepatocytes, inhibits ATP-citrate lyase (ACL), the enzyme that catalyzes the cleavage of citrate to acetyl-CoA and oxaloacetate in the cholesterol synthesis pathway. By inhibiting ACL, bempedoic acid reduces hepatic acetyl-CoA flux into cholesterol biosynthesis, leading to upregulation of LDL receptor (LDLR) expression on hepatocyte surfaces and increased clearance of LDL-cholesterol from the bloodstream.

Application

Bempedoic acid is indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of heterozygous familial hypercholesterolemia or established atherosclerotic cardiovascular disease in adults who require additional LDL-cholesterol lowering.

Bempedoic acid (ETC-1002) is an oral prodrug that inhibits ATP-citrate lyase (ACL), an enzyme upstream of HMG-CoA reductase in cholesterol synthesis. It is activated by very long-chain acyl-CoA synthetase 1 (ACSVL1), which is highly expressed in liver but absent in skeletal muscle, potentially reducing muscle-related adverse effects compared to statins. In Phase 2 trials, bempedoic acid (120-180 mg daily) reduced LDL-C by 26-30% as monotherapy and by up to 48% when combined with ezetimibe. It also lowered hsCRP by 25-40% and non-HDL-C, apoB, and LDL particle number. Bempedoic acid was effective in patients with hypercholesterolemia, type 2 diabetes, statin intolerance, and hypertension. Bempedoic acid offers a promising oral add-on option for patients not at LDL-C goal on statins.

Fig. 1 Bempedoic acid (ETC-1002) is converted to ETC-1002-CoA by ACSVL1. (Penson P.; et al. 2017)

References

Penson P, et al. Evaluating bempedoic acid for the treatment of hyperlipidaemia. Expert Opinion on Investigational Drugs, 2017, 26(2): 251-259.

What is the recommended storage condition for Bempedoic acid?

It should be stored at 2-8°C in a well-sealed container, protected from moisture and direct light, to maintain its chemical integrity throughout the shelf life.

What documentation is provided with each batch of Bempedoic acid?

Each batch is accompanied by a Certificate of Analysis (COA) covering identity, potency, and relevant purity tests. Safety Data Sheets (SDS) are available upon request.

Can Bempedoic acid be provided with custom specifications for synthetic applications?

Custom specifications including adjusted particle size, solvent residue limits, or additional purity testing can be arranged for qualified customers with defined requirements.

Is Bempedoic acid available in high-chemical-purity grade for pharmaceutical synthesis?

Yes, it is supplied in high chemical purity grades suitable for demanding pharmaceutical intermediate applications. Specifications and analytical data are available upon request.

Is Bempedoic acid manufactured under GMP conditions?

It is produced in facilities operating under applicable GMP or equivalent quality standards, ensuring consistent product quality and compliance with pharmaceutical industry requirements.