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Also known as: Etc-1002, 738606-46-7, 8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid, Nexletol, Esp-55016, Nilemdo
Molecular Formula
C19H36O5
Molecular Weight
344.5  g/mol
InChI Key
HYHMLYSLQUKXKP-UHFFFAOYSA-N
FDA UNII
1EJ6Z6Q368

Bempedoic Acid
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. 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. 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. 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.
Bempedoic acid is an Adenosine Triphosphate-Citrate Lyase Inhibitor. The mechanism of action of bempedoic acid is as an Adenosine Triphosphate-Citrate Lyase Inhibitor.
1 2D Structure

Bempedoic Acid

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid
2.1.2 InChI
InChI=1S/C19H36O5/c1-18(2,16(21)22)13-9-5-7-11-15(20)12-8-6-10-14-19(3,4)17(23)24/h15,20H,5-14H2,1-4H3,(H,21,22)(H,23,24)
2.1.3 InChI Key
HYHMLYSLQUKXKP-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CC(C)(CCCCCC(CCCCCC(C)(C)C(=O)O)O)C(=O)O
2.2 Other Identifiers
2.2.1 UNII
1EJ6Z6Q368
2.3 Synonyms
2.3.1 MeSH Synonyms

1. 8-hydroxy-2,2,14,14-tetramethylpentadecanedioic Acid

2. Esp-55016

3. Esp55016

4. Etc-1002

5. Nexletol

6. Nilemdo

2.3.2 Depositor-Supplied Synonyms

1. Etc-1002

2. 738606-46-7

3. 8-hydroxy-2,2,14,14-tetramethylpentadecanedioic Acid

4. Nexletol

5. Esp-55016

6. Nilemdo

7. Etc1002

8. Etc 1002

9. Esp 55016

10. 1ej6z6q368

11. Mfcd18800820

12. Etc-1002;esp-55016

13. Pentadecanedioic Acid, 8-hydroxy-2,2,14,14-tetramethyl-

14. Bempedoate

15. Unii-1ej6z6q368

16. Bempedoic Acid [usan:inn]

17. Bempedoic-acid

18. Bempedoic Acid

19. Esp-55016

20. Acido Bempedoico

21. Acide Bempedoique

22. Acidum Bempedoicum

23. Nexletol (tn)

24. Bempedoic Acid (usan/inn)

25. Bempedoic Acid [inn]

26. Bempedoic Acid [jan]

27. Bempedoic Acid [usan]

28. Schembl185768

29. Gtpl8321

30. Bempedoic Acid [who-dd]

31. Chembl3545313

32. Chebi:149601

33. Dtxsid401027952

34. Amy31933

35. Bcp16083

36. Esp55016

37. Ex-a1243

38. Zinc3948738

39. Bempedoic Acid [orange Book]

40. S7953

41. Akos027439916

42. Ccg-267969

43. Cs-3952

44. Db11936

45. Nexlizet Component Bempedoic Acid

46. Ac-29040

47. As-49804

48. Hy-12357

49. Sy244715

50. Bempedoic Acid Component Of Nexlizet

51. Bempedoic Acid(etc-1002;esp-55016)

52. Db-108321

53. D10691

54. N10681

55. A905695

56. Q27075007

57. 8-hydroxy-2,2,14,14-tetramethylpentadecanedioic Acid;etc-1002

2.4 Create Date
2006-10-25
3 Chemical and Physical Properties
Molecular Weight 344.5 g/mol
Molecular Formula C19H36O5
XLogP34.8
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count5
Rotatable Bond Count14
Exact Mass344.25627424 g/mol
Monoisotopic Mass344.25627424 g/mol
Topological Polar Surface Area94.8 Ų
Heavy Atom Count24
Formal Charge0
Complexity351
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Indication

Bempedoic acid is indicated as an adjunct to diet and maximally tolerated statin therapy for adults with heterozygous familial hypercholesterolemia or existing atherosclerotic cardiovascular disease that warrants additional lowering of LDL-C. The combination of bempedoic and ezetimibe is also indicated with diet management and maximally tolerated statin therapy to treat elevated LDL-C levels in adults with heterozygous familial hypercholesterolemia or existing atherosclerotic cardiovascular disease who require further lowering of LDL-C.


FDA Label


Nilemdo is indicated in adults with primary hypercholesterolaemia (heterozygous familial and non familial) or mixed dyslipidaemia, as an adjunct to diet:

- in combination with a statin or statin with other lipid-lowering therapies in patients unable to reach LDL C goals with the maximum tolerated dose of a statin (see sections 4. 2, 4. 3, and 4. 4) or,

- alone or in combination with other lipid-lowering therapies in patients who are statin intolerant, or for whom a statin is contraindicated.


5 Pharmacology and Biochemistry
5.1 Pharmacology

Bempedoic acid inhibits the synthesis of cholesterol in the liver, reducing LDL-C levels. This reduces the development of atherosclerotic plaques that may increase the risk of cardiovascular events. Earlier clinical trials studying the effects of bempedoic acid showed a dosedependent reduction of LDLC levels in addition to decreased LDL particle number, and reduced levels of apolipoprotein B, nonHDL cholesterol, and highsensitivity Creactive protein. Due to its unique mechanism of action, bempedoic acid is not associated with myositis, an adverse effect that frequently accompanies statin therapy. More recent trials have supported that this drug significantly decreases LDL-C levels after 12 weeks of therapy and provides additional lowering of LDL-C when combined with ezetimibe and statin therapy. The effects of bempedoic acid on mortality are currently unknown.


5.2 MeSH Pharmacological Classification

Enzyme Inhibitors

Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. (See all compounds classified as Enzyme Inhibitors.)


Hypoglycemic Agents

Substances which lower blood glucose levels. (See all compounds classified as Hypoglycemic Agents.)


Hypolipidemic Agents

Substances that lower the levels of certain LIPIDS in the BLOOD. They are used to treat HYPERLIPIDEMIAS. (See all compounds classified as Hypolipidemic Agents.)


5.3 FDA Pharmacological Classification
5.3.1 Active Moiety
BEMPEDOIC ACID
5.3.2 FDA UNII
1EJ6Z6Q368
5.3.3 Pharmacological Classes
Adenosine Triphosphate-Citrate Lyase Inhibitors [MoA]; Adenosine Triphosphate-Citrate Lyase Inhibitor [EPC]
5.4 ATC Code

C10AX


C - Cardiovascular system

C10 - Lipid modifying agents

C10A - Lipid modifying agents, plain

C10AX - Other lipid modifying agents

C10AX15 - Bempedoic acid


5.5 Absorption, Distribution and Excretion

Absorption

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


Route of Elimination

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.


Volume of Distribution

The apparent volume of distribution of bempedoic acid is about 18L.


Clearance

The clearance (CL/F) of bempedoic acid at steady state was estimated at 11.2 mL/min during clinical trials.


5.6 Metabolism/Metabolites

The two main metabolites of bempedoic metabolism are ETC-1002-CoA 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.


5.7 Biological Half-Life

The half-life of bempedoic acid ranges between 15 and 24 hours. Prescribing information indicates a clearance of 21 hours +/- 11 hours.


5.8 Mechanism of Action

Normally, LDL cholesterol is produced in the liver and circulates in the blood. When the blood becomes saturated, excess LDL deposits in blood vessels including the coronary arteries, increasing the risk of cardiovascular events. Bempedoic acid is a prodrug that requires activation in the liver. The very-long-chain acyl-CoA synthetase-1 (ACSVL1) enzyme is responsible for its activation to ETC-1002-CoA, the pharmacologically active metabolite. ATP lyase (also known as ATP synthase) plays an important part of cholesterol synthesis. BETC-1002-CoA directly inhibits this enzyme after the parent drug is activated in the liver by coenzyme A (CoA). This inhibition leads to upregulation of the LDL cholesterol receptor, reducing serum LDL-C via increased uptake and LDL clearance in the liver. By the above mechanisms, bempedoic acid causes a total decrease of circulating LDL-C that normally damages blood vessels and leads to atherosclerosis. Lastly, ETC-1002 activates AMP-activated protein kinase (AMPK) in rodents, which inhibits the synthesis of cholesterol via the inhibition of HMG-CoA reductase. The relevance of this to humans is unknown.


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Looking for 738606-46-7 / Bempedoic Acid API manufacturers, exporters & distributors?

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PharmaCompass offers a list of Bempedoic Acid API manufacturers, exporters & distributors, which can be sorted by GMP, USDMF, JDMF, KDMF, CEP (COS), WC, Price,and more, enabling you to easily find the right Bempedoic Acid manufacturer or Bempedoic Acid supplier for your needs.

Send us enquiries for free, and we will assist you in establishing a direct connection with your preferred Bempedoic Acid manufacturer or Bempedoic Acid supplier.

PharmaCompass also assists you with knowing the Bempedoic Acid API Price utilized in the formulation of products. Bempedoic Acid API Price is not always fixed or binding as the Bempedoic Acid Price is obtained through a variety of data sources. The Bempedoic Acid Price can also vary due to multiple factors, including market conditions, regulatory modifications, or negotiated pricing deals.

API | Excipient name

Bempedoic Acid

Synonyms

Etc-1002, 738606-46-7, 8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid, Nexletol, Esp-55016, Nilemdo

Cas Number

738606-46-7

Unique Ingredient Identifier (UNII)

1EJ6Z6Q368

About Bempedoic Acid

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. 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. 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. 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.

Bempedoic acid|ESP-55016 Manufacturers

A Bempedoic acid|ESP-55016 manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Bempedoic acid|ESP-55016, including repackagers and relabelers. The FDA regulates Bempedoic acid|ESP-55016 manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Bempedoic acid|ESP-55016 API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.

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Bempedoic acid|ESP-55016 Suppliers

A Bempedoic acid|ESP-55016 supplier is an individual or a company that provides Bempedoic acid|ESP-55016 active pharmaceutical ingredient (API) or Bempedoic acid|ESP-55016 finished formulations upon request. The Bempedoic acid|ESP-55016 suppliers may include Bempedoic acid|ESP-55016 API manufacturers, exporters, distributors and traders.

click here to find a list of Bempedoic acid|ESP-55016 suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.

Bempedoic acid|ESP-55016 USDMF

A Bempedoic acid|ESP-55016 DMF (Drug Master File) is a document detailing the whole manufacturing process of Bempedoic acid|ESP-55016 active pharmaceutical ingredient (API) in detail. Different forms of Bempedoic acid|ESP-55016 DMFs exist exist since differing nations have different regulations, such as Bempedoic acid|ESP-55016 USDMF, ASMF (EDMF), JDMF, CDMF, etc.

A Bempedoic acid|ESP-55016 DMF submitted to regulatory agencies in the US is known as a USDMF. Bempedoic acid|ESP-55016 USDMF includes data on Bempedoic acid|ESP-55016's chemical properties, information on the facilities and procedures used, and details about packaging and storage. The Bempedoic acid|ESP-55016 USDMF is kept confidential to protect the manufacturer’s intellectual property.

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Bempedoic acid|ESP-55016 WC

A Bempedoic acid|ESP-55016 written confirmation (Bempedoic acid|ESP-55016 WC) is an official document issued by a regulatory agency to a Bempedoic acid|ESP-55016 manufacturer, verifying that the manufacturing facility of a Bempedoic acid|ESP-55016 active pharmaceutical ingredient (API) adheres to the Good Manufacturing Practices (GMP) regulations of the importing country. When exporting Bempedoic acid|ESP-55016 APIs or Bempedoic acid|ESP-55016 finished pharmaceutical products to another nation, regulatory agencies frequently require a Bempedoic acid|ESP-55016 WC (written confirmation) as part of the regulatory process.

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Bempedoic acid|ESP-55016 NDC

National Drug Code is a comprehensive database maintained by the FDA that contains information on all drugs marketed in the US. This directory includes information about finished drug products, unfinished drug products, and compounded drug products, including those containing Bempedoic acid|ESP-55016 as an active pharmaceutical ingredient (API).

Finished drug products

The FDA updates the NDC directory daily. The NDC numbers for Bempedoic acid|ESP-55016 API and other APIs are published in this directory by the FDA.

Unfinished drugs

The NDC unfinished drugs database includes product listing information submitted for all unfinished drugs, such as active pharmaceutical ingredients (APIs), drugs intended for further processing and bulk drug substances for compounding.

Pharmaceutical companies that manufacture Bempedoic acid|ESP-55016 as an active pharmaceutical ingredient (API) must furnish the FDA with an updated record of all drugs that they produce, prepare, propagate, compound, or process for commercial distribution in the US at their facilities.

Compounded drug products

The NDC directory also contains data on finished compounded human drug products that contain Bempedoic acid|ESP-55016 and are produced by outsourcing facilities. While these outsourcing facilities are not mandated to assign a Bempedoic acid|ESP-55016 NDC to their finished compounded human drug products, they may choose to do so.

click here to find a list of Bempedoic acid|ESP-55016 suppliers with NDC on PharmaCompass.

Bempedoic acid|ESP-55016 GMP

Bempedoic acid|ESP-55016 Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.

GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).

PharmaCompass offers a list of Bempedoic acid|ESP-55016 GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, API price, and more, enabling you to easily find the right Bempedoic acid|ESP-55016 GMP manufacturer or Bempedoic acid|ESP-55016 GMP API supplier for your needs.

Bempedoic acid|ESP-55016 CoA

A Bempedoic acid|ESP-55016 CoA (Certificate of Analysis) is a formal document that attests to Bempedoic acid|ESP-55016's compliance with Bempedoic acid|ESP-55016 specifications and serves as a tool for batch-level quality control.

Bempedoic acid|ESP-55016 CoA mostly includes findings from lab analyses of a specific batch. For each Bempedoic acid|ESP-55016 CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.

Bempedoic acid|ESP-55016 may be tested according to a variety of international standards, such as European Pharmacopoeia (Bempedoic acid|ESP-55016 EP), Bempedoic acid|ESP-55016 JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Bempedoic acid|ESP-55016 USP).

Inform the supplier about your product requirements, specifying if you need a product with particular monograph like EP (Ph. Eur.), USP, JP, BP, or any other quality. In addition, clarify whether you need hydrochloride (HCl), anhydricum, base, micronisatum or a specific level of purity. To find reputable suppliers, utilize the filters and select those certified by GMP, FDA, or any other certification as per your requirement.
For your convenience, we have listed synonyms and CAS numbers to help you find the best supplier. The use of synonyms and CAS numbers can be helpful in identifying potential suppliers, but it is crucial to note that they might not always indicate the exact same product. It is important to confirm the product details with the supplier before making a purchase to ensure that it meets your requirements.
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