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Chemistry

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Also known as: 1015787-98-0, Af-219, Mk-7264, Gefapixant [usan], Ro4926219, Rg-1646
Molecular Formula
C14H19N5O4S
Molecular Weight
353.40  g/mol
InChI Key
HLWURFKMDLAKOD-UHFFFAOYSA-N
FDA UNII
6K6L7E3F1L

Gefapixant Citrate
Gefapixant is under investigation in clinical trial NCT02397460 (Effect of Gefapixant (AF-219/MK-7264) on Cough Reflex Sensitivity).
1 2D Structure

Gefapixant Citrate

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
5-(2,4-diaminopyrimidin-5-yl)oxy-2-methoxy-4-propan-2-ylbenzenesulfonamide
2.1.2 InChI
InChI=1S/C14H19N5O4S/c1-7(2)8-4-10(22-3)12(24(17,20)21)5-9(8)23-11-6-18-14(16)19-13(11)15/h4-7H,1-3H3,(H2,17,20,21)(H4,15,16,18,19)
2.1.3 InChI Key
HLWURFKMDLAKOD-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CC(C)C1=CC(=C(C=C1OC2=CN=C(N=C2N)N)S(=O)(=O)N)OC
2.2 Other Identifiers
2.2.1 UNII
6K6L7E3F1L
2.3 Synonyms
2.3.1 MeSH Synonyms

1. 5-((2,4-diamino-5-pyrimidinyl)oxy)-4-isopropyl-2-methoxybenzenesulfonamide

2. Af-219

3. Benzenesulfonamide, 5-((2,4-diamino-5-pyrimidinyl)oxy)-2-methoxy-4-(1-methylethyl)-

4. Mk-7264

2.3.2 Depositor-Supplied Synonyms

1. 1015787-98-0

2. Af-219

3. Mk-7264

4. Gefapixant [usan]

5. Ro4926219

6. Rg-1646

7. Ro-4926219

8. Benzenesulfonamide, 5-[(2,4-diamino-5-pyrimidinyl)oxy]-2-methoxy-4-(1-methylethyl)-

9. 6k6l7e3f1l

10. R-1646

11. Af219

12. Rg1646

13. Mk-7264;af-219

14. R1646

15. 5-[(2,4-diaminopyrimidin-5-yl)oxy]-2-methoxy-4-(propan-2-yl)benzene-1-sulfonamide

16. C14h19n5o4s

17. 5-((2,4-diaminopyrimidin-5-yl)oxy)-4-isopropyl-2-methoxybenzenesulfonamide

18. 5-(2,4-diaminopyrimidin-5-yl)oxy-2-methoxy-4-propan-2-ylbenzenesulfonamide

19. 5-[(2,4-diamino-5-pyrimidinyl)oxy]-4-isopropyl-2-methoxybenzenesulfonamide

20. 5-((2,4-diaminopyrimidin-5-yl)oxy)-2-methoxy-4-(propan-2-yl)benzenesulfonamide

21. 5-[2,4-bis(azanyl)pyrimidin-5-yl]oxy-2-methoxy-4-propan-2-yl-benzenesulfonamide

22. Benzenesulfonamide, 5-((2,4-diamino-5-pyrimidinyl)oxy)-2-methoxy-4-(1-methylethyl)-

23. 5-((2,4-diamino-5-pyrimidinyl)oxy)-4-isopropyl-2-methoxybenzenesulfonamide

24. Gefapixant [inn]

25. Gefapixant (usan/inn)

26. Gefapixant [who-dd]

27. Unii-6k6l7e3f1l

28. Gtpl9540

29. Schembl1493905

30. Chembl3716057

31. Dtxsid401337212

32. Amy27911

33. Bcp26079

34. Ex-a2788

35. Gefapixant(af-219,mk-7264)

36. Bdbm50533006

37. Mfcd24539325

38. S6664

39. Akos037515637

40. Zinc116342482

41. Db15097

42. Af-219; Mk-7264

43. Ac-35643

44. As-78086

45. Bm170818

46. Sy282739

47. Hy-101588

48. Cs-0021727

49. Ro 4926219

50. J3.556.891c

51. D11349

52. A934898

53. 2-methoxy-4-isopropyl-5-(2,4-diamino-5-pyrimidinyloxy)benzenesulfonamide

54. 5-(2,4-diamino-pyrimidin-5-yloxy)-4-isopropyl-2-methoxy-benzenesulfonamide

55. Af9

2.4 Create Date
2008-04-21
3 Chemical and Physical Properties
Molecular Weight 353.40 g/mol
Molecular Formula C14H19N5O4S
XLogP30.7
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count9
Rotatable Bond Count5
Exact Mass353.11577528 g/mol
Monoisotopic Mass353.11577528 g/mol
Topological Polar Surface Area165 Ų
Heavy Atom Count24
Formal Charge0
Complexity512
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Pharmacology and Biochemistry
4.1 ATC Code

R - Respiratory system

R05 - Cough and cold preparations

R05D - Cough suppressants, excl. combinations with expectorants

R05DB - Other cough suppressants

R05DB29 - Gefapixant


API SUPPLIERS

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01

Metrochem API Private Limited

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

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BIO Partnering at JPM
Not Confirmed
  • fda
  • EDQM
  • WHO-GMP

Virtual BoothMetrochem has been delivering customized volume & quality products to customers across the world, taking utmost care of their needs.

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USDMF CEP/COS JDMF EU-WC NDC KDMF VMF Others AUDIT
Metrochem

02

Jinan Tantu Chemicals

China

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothJinan Tantu Chemicals offers customized R&D services & production of small molecule APIs & pharmaceutical intermediates.

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USDMF CEP/COS JDMF EU-WC NDC KDMF VMF Others AUDIT
Jinan Tantu Chemicals

03

Shandong Loncom Pharmaceutical

China

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

arrow
BIO Partnering at JPM
Not Confirmed
  • fda
  • EDQM
  • WHO-GMP

Virtual BoothShandong Loncom is an R&D-focused manufacturer of Anti-cancer APIs.

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Digital Content Digital Content
USDMF CEP/COS JDMF EU-WC NDC KDMF VMF Others AUDIT
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04

Beijing Mesochem Technology

China

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

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BIO Partnering at JPM
Not Confirmed
  • fda
  • EDQM
  • WHO-GMP

Virtual BoothMesochem is focused on incessant innovation along with the R&D of new APIs.

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USDMF CEP/COS JDMF EU-WC NDC KDMF VMF Others AUDIT
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05

Glixx Laboratories

U.S.A

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

BIO Partnering at JPM
Not Confirmed
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Glixx Laboratories

U.S.A

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

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BIO Partnering at JPM
Not Confirmed
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Drugs in Development

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Details:

Lyfnua (gefapixant) is an investigational, non-narcotic, oral selective P2X3 receptor antagonist, under development for the treatment of refractory chronic cough or unexplained chronic cough in adults.


Lead Product(s): Gefapixant Citrate

Therapeutic Area: Pulmonary/Respiratory Diseases Brand Name: Lyfnua

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable December 20, 2023

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01

Merck & Co

U.S.A
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BIO Partnering at JPM
Not Confirmed

Merck & Co

U.S.A
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BIO Partnering at JPM
Not Confirmed

Details : Lyfnua (gefapixant) is an investigational, non-narcotic, oral selective P2X3 receptor antagonist, under development for the treatment of refractory chronic cough or unexplained chronic cough in adults.

Brand Name : Lyfnua

Molecule Type : Small molecule

Upfront Cash : Not Applicable

December 20, 2023

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Details:

MK-7264 (gefapixant), an investigational, orally administered, selective P2X3 receptor antagonist, is being developed for the potential treatment of refractory or unexplained chronic cough and was approved in Japan and Switzerland under the brand name Lyfnua®.


Lead Product(s): Gefapixant Citrate

Therapeutic Area: Pulmonary/Respiratory Diseases Brand Name: MK-7264

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable July 21, 2023

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02

Merck & Co

U.S.A
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BIO Partnering at JPM
Not Confirmed

Merck & Co

U.S.A
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BIO Partnering at JPM
Not Confirmed

Details : MK-7264 (gefapixant), an investigational, orally administered, selective P2X3 receptor antagonist, is being developed for the potential treatment of refractory or unexplained chronic cough and was approved in Japan and Switzerland under the brand name Ly...

Brand Name : MK-7264

Molecule Type : Small molecule

Upfront Cash : Not Applicable

July 21, 2023

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Details:

Last week, the Japan Ministry of Health, Labor and Welfare (MHLW) approved LYFNUA® (gefapixant) Tablets 45 mg for adults with refractory or unexplained chronic cough.


Lead Product(s): Gefapixant Citrate

Therapeutic Area: Pulmonary/Respiratory Diseases Brand Name: Lyfnua

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable January 24, 2022

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03

Merck & Co

U.S.A
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BIO Partnering at JPM
Not Confirmed

Merck & Co

U.S.A
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BIO Partnering at JPM
Not Confirmed

Details : Last week, the Japan Ministry of Health, Labor and Welfare (MHLW) approved LYFNUA® (gefapixant) Tablets 45 mg for adults with refractory or unexplained chronic cough.

Brand Name : Lyfnua

Molecule Type : Small molecule

Upfront Cash : Not Applicable

January 24, 2022

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Details:

COUGH-1 and COUGH-2 are international Phase 3, randomized, double-blind, placebo-controlled, studies to evaluate the efficacy and safety of gefapixant in reducing cough frequency in adult participants with refractory or unexplained chronic cough.


Lead Product(s): Gefapixant Citrate

Therapeutic Area: Pulmonary/Respiratory Diseases Brand Name: MK-7264

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable September 08, 2020

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04

Merck & Co

U.S.A
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BIO Partnering at JPM
Not Confirmed

Merck & Co

U.S.A
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BIO Partnering at JPM
Not Confirmed

Details : COUGH-1 and COUGH-2 are international Phase 3, randomized, double-blind, placebo-controlled, studies to evaluate the efficacy and safety of gefapixant in reducing cough frequency in adult participants with refractory or unexplained chronic cough.

Brand Name : MK-7264

Molecule Type : Small molecule

Upfront Cash : Not Applicable

September 08, 2020

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FDF Dossiers

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Merck & Co

U.S.A
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Not Confirmed
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Merck & Co

U.S.A
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Gefapiksantsitrat

Brand Name : Lyfnua

Dosage Form : Tablet, film-coated

Dosage Strength : 45 mg

Packaging : Blisterpakning 56item

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Norway

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Europe

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BIO Partnering at JPM
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BIO Partnering at JPM
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Gefapiksantsitrat

Brand Name : Lyfnua

Dosage Form : Tablet, film-coated

Dosage Strength : 45 mg

Packaging : Blisterpakning 56item

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Norway

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ABOUT THIS PAGE

Gefapixant Citrate Manufacturers

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

Gefapixant Citrate Suppliers

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

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

Gefapixant Citrate GMP

Gefapixant Citrate 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 Gefapixant Citrate 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 Gefapixant Citrate GMP manufacturer or Gefapixant Citrate GMP API supplier for your needs.

Gefapixant Citrate CoA

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

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

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