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Chemistry

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Also known as: 934016-19-0, Gonax, Firmagon, Ext215f4zu, Degarelix (as acetate), Degarelix acetate hydrate
Molecular Formula
C84H107ClN18O18
Molecular Weight
1692.3  g/mol
InChI Key
AUTFSFUMNFDPLH-KYMMNHPFSA-N
FDA UNII
EXT215F4ZU

Degarelix Acetate
Degarelix Acetate is the acetate form of a long-acting, synthetic peptide with gonadotrophin-releasing hormone (GnRH) antagonistic properties. Degarelix targets and blocks GnRH receptors located on the surfaces of gonadotroph cells in the anterior pituitary, thereby reducing secretion of luteinizing hormone (LH) by pituitary gonadotroph cells and so decreasing testosterone production by interstitial (Leydig) cells in the testes.
1 2D Structure

Degarelix Acetate

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
(4S)-N-[4-[(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]amino]-3-[[(2R)-1-[[(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]amino]-3-[4-(carbamoylamino)phenyl]-1-oxopropan-2-yl]amino]-3-oxopropyl]phenyl]-2,6-dioxo-1,3-diazinane-4-carboxamide;acetic acid
2.1.2 InChI
InChI=1S/C82H103ClN18O16.C2H4O2/c1-45(2)35-60(72(107)92-59(16-9-10-33-87-46(3)4)80(115)101-34-12-17-68(101)79(114)88-47(5)70(84)105)93-74(109)63(38-51-23-30-58(31-24-51)91-81(85)116)95-76(111)64(39-50-21-28-57(29-22-50)90-71(106)66-42-69(104)100-82(117)99-66)97-78(113)67(44-102)98-77(112)65(41-53-13-11-32-86-43-53)96-75(110)62(37-49-19-26-56(83)27-20-49)94-73(108)61(89-48(6)103)40-52-18-25-54-14-7-8-15-55(54)36-52;1-2(3)4/h7-8,11,13-15,18-32,36,43,45-47,59-68,87,102H,9-10,12,16-17,33-35,37-42,44H2,1-6H3,(H2,84,105)(H,88,114)(H,89,103)(H,90,106)(H,92,107)(H,93,109)(H,94,108)(H,95,111)(H,96,110)(H,97,113)(H,98,112)(H3,85,91,116)(H2,99,100,104,117);1H3,(H,3,4)/t47-,59+,60+,61-,62-,63-,64+,65-,66+,67+,68+;/m1./s1
2.1.3 InChI Key
AUTFSFUMNFDPLH-KYMMNHPFSA-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(CC2=CC=C(C=C2)NC(=O)N)NC(=O)C(CC3=CC=C(C=C3)NC(=O)C4CC(=O)NC(=O)N4)NC(=O)C(CO)NC(=O)C(CC5=CN=CC=C5)NC(=O)C(CC6=CC=C(C=C6)Cl)NC(=O)C(CC7=CC8=CC=CC=C8C=C7)NC(=O)C.CC(=O)O
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](CC2=CC=C(C=C2)NC(=O)N)NC(=O)[C@H](CC3=CC=C(C=C3)NC(=O)[C@@H]4CC(=O)NC(=O)N4)NC(=O)[C@H](CO)NC(=O)[C@@H](CC5=CN=CC=C5)NC(=O)[C@@H](CC6=CC=C(C=C6)Cl)NC(=O)[C@@H](CC7=CC8=CC=CC=C8C=C7)NC(=O)C.CC(=O)O
2.2 Other Identifiers
2.2.1 UNII
EXT215F4ZU
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Ac-2nal-4cpa-3pal-ser-4aph(hydroorotyl)-4aph(carbamoyl)-leu-ilys-pro-ala-nh2

2. Acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ilys-prolyl-alaninamide

3. Degarelix

4. Fe 200486

5. Fe-200486

6. Fe200486

7. Firmagon

8. Gonax

9. Uglypeptide1

2.3.2 Depositor-Supplied Synonyms

1. 934016-19-0

2. Gonax

3. Firmagon

4. Ext215f4zu

5. Degarelix (as Acetate)

6. Degarelix Acetate Hydrate

7. Fe-200486

8. Degarelix Acetate (jan)

9. N-acetyl-3-(2-naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-4-[[[(4s)-hexahydro-2,6-dioxo-4-pyrimidinyl]carbonyl]amino]-l-phenylalanyl-4-[(aminocarbonyl)amino]-d-phenylalanyl-l-leucyl-n6-(1-methylethyl)-l-lysyl-l-prolyl-d-alaninamide,monoacetate

10. Asp3550

11. Fe200486

12. Unii-ext215f4zu

13. Fe200486 (free Base)

14. Firmagon (tn)

15. Degarelix Monoacetate

16. Chembl2028987

17. Degarelix Acetate Anhydrous

18. Dtxsid201027699

19. Asp-3550

20. Mfcd16879085

21. Degarelix Monoacetate Anhydrous

22. Degarelix (acetate) Pound>>fe 200486

23. Degarelix Acetate(214766-78-6 Free Base)

24. D09400

25. Q27277419

26. D-alaninamide, N-acetyl-3-(naphtalen-2-yl)-d-alanyl-4-chloro-d-phenylalanyl-3-(pyridin-3-yl)-d-alanyl-l-seryl-4-((((4s)-2,6-dioxohexahydropyrimidin-4-yl)carbonyl)amino)-l-phenylalanyl-4-(carbamoylamino)-d-phenylalanyl-l-leucyl-n6-(1-methylethyl)-l-lysyl-l-prolyl-, Acetate (1:1)

2.4 Create Date
2007-07-04
3 Chemical and Physical Properties
Molecular Weight 1692.3 g/mol
Molecular Formula C84H107ClN18O18
Hydrogen Bond Donor Count18
Hydrogen Bond Acceptor Count20
Rotatable Bond Count41
Exact Mass1690.7699263 g/mol
Monoisotopic Mass1690.7699263 g/mol
Topological Polar Surface Area550 Ų
Heavy Atom Count121
Formal Charge0
Complexity3420
Isotope Atom Count0
Defined Atom Stereocenter Count11
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count2
4 Drug and Medication Information
4.1 Drug Indication

FIRMAGON is a gonadotrophin releasing hormone (GnRH) antagonist indicated:

- for treatment of adult male patients with advanced hormone-dependent prostate cancer .

- for treatment of high-risk localised and locally advanced hormone dependent prostate cancer in combination with radiotherapy.

- as neo-adjuvant treatment prior to radiotherapy in patients with high-risk localised or locally advanced hormone dependent prostate cancer .


5 Pharmacology and Biochemistry
5.1 ATC Code

L02BX02


API Reference Price

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02-Dec-2021
05-Feb-2022
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FDA Orange Book

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01

FERRING

Switzerland
Duphat
Not Confirmed
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FERRING

Switzerland
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Duphat
Not Confirmed

DEGARELIX ACETATE

Brand Name : FIRMAGON

Dosage Form : POWDER;SUBCUTANEOUS

Dosage Strength : EQ 80MG BASE/VIAL

Approval Date : 2008-12-24

Application Number : 22201

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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02

FERRING

Switzerland
Duphat
Not Confirmed
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FERRING

Switzerland
arrow
Duphat
Not Confirmed

DEGARELIX ACETATE

Brand Name : FIRMAGON

Dosage Form : POWDER;SUBCUTANEOUS

Dosage Strength : EQ 120MG BASE/VIAL

Approval Date : 2008-12-24

Application Number : 22201

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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Europe

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Duphat
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degarelixacetat

Brand Name : FIRMAGON

Dosage Form : POWDER AND SOLVENT FOR SOLUTION FOR INJECTION

Dosage Strength : 80 MG

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Sweden

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02

Duphat
Not Confirmed
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Duphat
Not Confirmed

degarelixacetat

Brand Name : FIRMAGON

Dosage Form : POWDER AND SOLVENT FOR SOLUTION FOR INJECTION

Dosage Strength : 120 MG

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Sweden

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03

Duphat
Not Confirmed
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Duphat
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Degarelix Acetate

Brand Name : Firmagon

Dosage Form : Degarelix 120Mg 2 Units Parenteral Use

Dosage Strength : 2 vials groun 120 mg + 2 Syringes solv 3 ml

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Italy

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04

Duphat
Not Confirmed
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Duphat
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Degarelix Acetate

Brand Name : Firmagon

Dosage Form : Degarelix 80Mg 1 Unit Parenteral Use

Dosage Strength : 1 vial 80 mg groun + 1 syringe solv 4,2 ml

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Italy

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05

Ferring Solvay A/S

Switzerland
Duphat
Not Confirmed
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Ferring Solvay A/S

Switzerland
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Duphat
Not Confirmed

Degarelix Acetate

Brand Name : Firm Agon

Dosage Form : Powder and liquid to the injection fluid, resolution

Dosage Strength : 120 mg

Packaging : Hood glass

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Norway

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06

Ferring Solvay A/S

Switzerland
Duphat
Not Confirmed
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Ferring Solvay A/S

Switzerland
arrow
Duphat
Not Confirmed

Degarelix Acetate

Brand Name : Firm Agon

Dosage Form : Powder and liquid to the injection fluid, resolution

Dosage Strength : 80 mg

Packaging : Hood glass

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Norway

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07

Ferring AG

Switzerland
Duphat
Not Confirmed
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Ferring AG

Switzerland
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Duphat
Not Confirmed

Degarelixum

Brand Name : Firmagon

Dosage Form : Trockensub

Dosage Strength : 120mg

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Switzerland

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08

Ferring AG

Switzerland
Duphat
Not Confirmed
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Ferring AG

Switzerland
arrow
Duphat
Not Confirmed

Degarelixum

Brand Name : Firmagon

Dosage Form : Trockensub

Dosage Strength : 80mg

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Switzerland

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ABOUT THIS PAGE

Degarelix Acetate Manufacturers

A Degarelix Acetate manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Degarelix Acetate, including repackagers and relabelers. The FDA regulates Degarelix Acetate manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Degarelix Acetate 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 Degarelix Acetate manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.

Degarelix Acetate Suppliers

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

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

Degarelix Acetate USDMF

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

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

click here to find a list of Degarelix Acetate suppliers with USDMF on PharmaCompass.

Degarelix Acetate KDMF

In Korea, the Ministry of Food and Drug Safety (MFDS) is in charge of regulating pharmaceutical products and services.

Pharmaceutical companies submit a Degarelix Acetate Drug Master File in Korea (Degarelix Acetate KDMF) to the MFDS, which includes comprehensive information about the production, processing, facilities, materials, packaging, and testing of Degarelix Acetate. The MFDS reviews the Degarelix Acetate KDMF as part of the drug registration process and uses the information provided in the Degarelix Acetate KDMF to evaluate the safety and efficacy of the drug.

After submitting a Degarelix Acetate KDMF to the MFDS, the registered manufacturer can provide importers or distributors with the registration number without revealing confidential information to Korean business partners. Applicants seeking to register their Degarelix Acetate API can apply through the Korea Drug Master File (KDMF).

click here to find a list of Degarelix Acetate suppliers with KDMF on PharmaCompass.

Degarelix Acetate 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 Degarelix Acetate as an active pharmaceutical ingredient (API).

Finished drug products

The FDA updates the NDC directory daily. The NDC numbers for Degarelix Acetate 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 Degarelix Acetate 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 Degarelix Acetate and are produced by outsourcing facilities. While these outsourcing facilities are not mandated to assign a Degarelix Acetate NDC to their finished compounded human drug products, they may choose to do so.

click here to find a list of Degarelix Acetate suppliers with NDC on PharmaCompass.

Degarelix Acetate GMP

Degarelix Acetate 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 Degarelix Acetate 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 Degarelix Acetate GMP manufacturer or Degarelix Acetate GMP API supplier for your needs.

Degarelix Acetate CoA

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

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

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