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Synopsis

Synopsis

ACTIVE PHARMA INGREDIENTS

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USDMF

US DMFs Filed

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CEP/COS

CEP/COS Certifications

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JDMF

JDMFs Filed

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EU WC

EU WC

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KDMF

KDMF

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NDC API

NDC API

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VMF

NDC API

API REF. PRICE (USD/KG)

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$ 0

MARKET PLACE

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API

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FDF

0INTERMEDIATES

FINISHED DOSAGE FORMULATIONS

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Europe

Europe

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Canada

Canada

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Australia

Australia

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South Africa

South Africa

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Listed Dossiers

Listed Dossiers

0 DRUGS IN DEVELOPMENT

FDF Dossiers

DRUG PRODUCT COMPOSITIONS

REF. STANDARDS OR IMPURITIES

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EDQM

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USP

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JP

PATENTS & EXCLUSIVITIES

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US Patents

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US Exclusivities

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Health Canada Patents

DIGITAL CONTENT

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Data Compilation #PharmaFlow

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News #PharmaBuzz

GLOBAL SALES INFORMATION

US Medicaid

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Annual Reports

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Finished Drug Prices

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0RELATED EXCIPIENT COMPANIES

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Chemistry

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Also known as: Plenaxis, 183552-38-7, Ppi-149, Ppi 149, R 3827, R3827
Molecular Formula
C72H95ClN14O14
Molecular Weight
1416.1  g/mol
InChI Key
AIWRTTMUVOZGPW-HSPKUQOVSA-N

Abarelix
Abarelix is a synthetic decapeptide and antagonist of naturally occurring gonadotropin-releasing hormone (GnRH). Abarelix directly and competitively binds to and blocks the gonadotropin releasing hormone receptor in the anterior pituitary gland, thereby inhibiting the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. As a result, this may relieve symptoms associated with prostate hypertrophy or prostate cancer, since testosterone is required to sustain prostate growth.
1 2D Structure

Abarelix

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
(2R)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]-methylamino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[(2S)-1-[[(2S)-1-[(2S)-2-[[(2R)-1-amino-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxo-6-(propan-2-ylamino)hexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]butanediamide
2.1.2 InChI
InChI=1S/C72H95ClN14O14/c1-41(2)32-54(64(93)80-53(17-10-11-30-77-42(3)4)72(101)87-31-13-18-60(87)69(98)78-43(5)63(75)92)81-68(97)58(38-62(74)91)84-70(99)61(37-46-22-27-52(90)28-23-46)86(7)71(100)59(40-88)85-67(96)57(36-48-14-12-29-76-39-48)83-66(95)56(34-45-20-25-51(73)26-21-45)82-65(94)55(79-44(6)89)35-47-19-24-49-15-8-9-16-50(49)33-47/h8-9,12,14-16,19-29,33,39,41-43,53-61,77,88,90H,10-11,13,17-18,30-32,34-38,40H2,1-7H3,(H2,74,91)(H2,75,92)(H,78,98)(H,79,89)(H,80,93)(H,81,97)(H,82,94)(H,83,95)(H,84,99)(H,85,96)/t43-,53+,54+,55-,56-,57-,58-,59+,60+,61+/m1/s1
2.1.3 InChI Key
AIWRTTMUVOZGPW-HSPKUQOVSA-N
2.1.4 Canonical SMILES
CC(C)CC(C(=O)NC(CCCCNC(C)C)C(=O)N1CCCC1C(=O)NC(C)C(=O)N)NC(=O)C(CC(=O)N)NC(=O)C(CC2=CC=C(C=C2)O)N(C)C(=O)C(CO)NC(=O)C(CC3=CN=CC=C3)NC(=O)C(CC4=CC=C(C=C4)Cl)NC(=O)C(CC5=CC6=CC=CC=C6C=C5)NC(=O)C
2.1.5 Isomeric SMILES
C[C@H](C(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(=O)N)NC(=O)[C@H](CC2=CC=C(C=C2)O)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](CC3=CN=CC=C3)NC(=O)[C@@H](CC4=CC=C(C=C4)Cl)NC(=O)[C@@H](CC5=CC6=CC=CC=C6C=C5)NC(=O)C
2.2 Synonyms
2.2.1 MeSH Synonyms

1. Plenaxis

2. Ppi-149

2.2.2 Depositor-Supplied Synonyms

1. Plenaxis

2. 183552-38-7

3. Ppi-149

4. Ppi 149

5. R 3827

6. R3827

7. R-3827

8. Chembl1252

9. Plenaxis Depot

10. Chebi:337298

11. D-alaninamide, N-acetyl-3-(2-naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-n-methyl-l-tyrosyl-d-asparaginyl-l-leucyl-n6-(1-methylethyl)-l-lysyl-l-prolyl-

12. Abarelix-depot-m

13. Plenaxis (tn)

14. Abarelix (usan/inn)

15. Abarelix [usan:inn]

16. Unii-w486sj5824

17. N-acetyl-3-(2-naphthyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridyl)-d-alanyl-l-seryl-n-methyl-l-tyrosyl-d-asparginyl-l-leucyl-n6-isopropyl-l-lysyl-l-prolyl-d-alaninamide

18. Schembl9533

19. Gtpl1188

20. Ppi149

21. Schembl19712245

22. Dtxsid20171443

23. Bdbm50102442

24. Ppi 149r3827

25. R3827;ppi 149

26. Cs-5873

27. Db00106

28. D-alaninamide, N-acetyl-3-(2-naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-n-methyl-l-tyrosyl-d-asparaginyl-l-leucyl-n6-(1-methylethyl)-l-lysyl-l-prolyl- 10

29. Hy-13534

30. N-acetyl-3-(2-naphthyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(pyridin-3-yl)-d-alanyl-l-seryl-n-methyl-l-tyrosyl-d-asparginyl-l-leucyl-n(6)-isopropyl-l-lysyl-l-prolyl-d-alaninamide

31. A12613

32. D02738

33. 552a387

34. Q305555

35. Ac-d-nal-[d-(pcl)phe]-d-pal-ser-[nalpha-me-tyr]-d-asn-leu-ilys-pro-dala-nh2

36. N-acetyl-3-(2-naphthyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridyl)-d-alanyl-l-seryl-n-methyl-l-tyrosyl-d-asparagyl-l-leucyl-n6-isopropyl-l-lysyl-l-prolyl-d-alaninamide

2.3 Create Date
2007-07-03
3 Chemical and Physical Properties
Molecular Weight 1416.1 g/mol
Molecular Formula C72H95ClN14O14
XLogP33.7
Hydrogen Bond Donor Count13
Hydrogen Bond Acceptor Count16
Rotatable Bond Count38
Exact Mass1414.6840715 g/mol
Monoisotopic Mass1414.6840715 g/mol
Topological Polar Surface Area425 Ų
Heavy Atom Count101
Formal Charge0
Complexity2770
Isotope Atom Count0
Defined Atom Stereocenter Count10
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

For palliative treatment of advanced prostate cancer.


FDA Label


5 Pharmacology and Biochemistry
5.1 Pharmacology

Used in the palliative treatment of advanced prostate cancer. Abarelix is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis.


5.2 MeSH Pharmacological Classification

Hormone Antagonists

Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites. (See all compounds classified as Hormone Antagonists.)


5.3 ATC Code

L - Antineoplastic and immunomodulating agents

L02 - Endocrine therapy

L02B - Hormone antagonists and related agents

L02BX - Other hormone antagonists and related agents

L02BX01 - Abarelix


5.4 Absorption, Distribution and Excretion

Absorption

Following IM administration of 100 mg, abarelix is absorbed slowly with a mean peak concentration of 43.4 ng/mL observed approximately 3 days after the injection.


5.5 Metabolism/Metabolites

In vitro hepatocyte (rat, monkey, human) studies and in vivo studies in rats and monkeys showed that the major metabolites of abarelix were formed via hydrolysis of peptide bonds. No significant oxidative or conjugated metabolites of abarelix were found either in vitro or in vivo. There is no evidence of cytochrome P-450 involvement in the metabolism of abarelix.


5.6 Biological Half-Life

13.2 ± 3.2 days


5.7 Mechanism of Action

Abarelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion.


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Looking for 183552-38-7 / Abarelix API manufacturers, exporters & distributors?

Abarelix manufacturers, exporters & distributors 1

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PharmaCompass offers a list of Abarelix 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 Abarelix manufacturer or Abarelix supplier for your needs.

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

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

API | Excipient name

Abarelix

Synonyms

Plenaxis, 183552-38-7, Ppi-149, Ppi 149, R 3827, R3827

Cas Number

183552-38-7

About Abarelix

Abarelix is a synthetic decapeptide and antagonist of naturally occurring gonadotropin-releasing hormone (GnRH). Abarelix directly and competitively binds to and blocks the gonadotropin releasing hormone receptor in the anterior pituitary gland, thereby inhibiting the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. As a result, this may relieve symptoms associated with prostate hypertrophy or prostate cancer, since testosterone is required to sustain prostate growth.

Abarelix Manufacturers

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

click here to find a list of Abarelix manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.

Abarelix Suppliers

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

click here to find a list of Abarelix suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.

Abarelix GMP

Abarelix 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 Abarelix 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 Abarelix GMP manufacturer or Abarelix GMP API supplier for your needs.

Abarelix CoA

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

Abarelix CoA mostly includes findings from lab analyses of a specific batch. For each Abarelix 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.

Abarelix may be tested according to a variety of international standards, such as European Pharmacopoeia (Abarelix EP), Abarelix JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Abarelix 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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