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Chemistry

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Also known as: 1103522-45-7, Act-132577, Aprocitentan [usan], Macitentan metabolite m6, Mzi81hv01p, 5-(4-bromophenyl)-4-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-6-(sulfamoylamino)pyrimidine
Molecular Formula
C16H14Br2N6O4S
Molecular Weight
546.2  g/mol
InChI Key
DKULOVKANLVDEA-UHFFFAOYSA-N
FDA UNII
MZI81HV01P

Aprocitentan
Aprocitentan is under investigation in clinical trial NCT03541174 (A Research Study to Show the Effect of Aprocitentan in the Treatment of Difficult to Control (Resistant) High Blood Pressure (Hypertension) and Find Out More About Its Safety).
1 2D Structure

Aprocitentan

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
5-(4-bromophenyl)-4-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-6-(sulfamoylamino)pyrimidine
2.1.2 InChI
InChI=1S/C16H14Br2N6O4S/c17-11-3-1-10(2-4-11)13-14(24-29(19,25)26)22-9-23-15(13)27-5-6-28-16-20-7-12(18)8-21-16/h1-4,7-9H,5-6H2,(H2,19,25,26)(H,22,23,24)
2.1.3 InChI Key
DKULOVKANLVDEA-UHFFFAOYSA-N
2.1.4 Canonical SMILES
C1=CC(=CC=C1C2=C(N=CN=C2OCCOC3=NC=C(C=N3)Br)NS(=O)(=O)N)Br
2.2 Other Identifiers
2.2.1 UNII
MZI81HV01P
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Act-132577

2. N-(5-(4-bromophenyl)-6-(2-((5-bromo-2-pyrimidinyl)oxy)ethoxy)-4-pyrimidinyl)sulfuric Diamide

3. Sulfamide, N-(5-(4-bromophenyl)-6-(2-((5-bromo-2-pyrimidinyl)oxy)ethoxy)-4-pyrimidinyl)-

2.3.2 Depositor-Supplied Synonyms

1. 1103522-45-7

2. Act-132577

3. Aprocitentan [usan]

4. Macitentan Metabolite M6

5. Mzi81hv01p

6. 5-(4-bromophenyl)-4-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-6-(sulfamoylamino)pyrimidine

7. Chembl2165326

8. Chebi:76609

9. N-[5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl]sulfuric Diamide

10. N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]sulfamide

11. Sulfamide, N-(5-(4-bromophenyl)-6-(2-((5-bromo-2-pyrimidinyl)oxy)ethoxy)-4-pyrimidinyl)-

12. Despropyl Macitentan

13. N-despropyl-macitentan

14. Unii-mzi81hv01p

15. N-(5-(4-bromophenyl)-6-(2-((5-bromo-2-pyrimidinyl)oxy)ethoxy)-4-pyrimidinyl)sulfamide

16. N-(5-(4-bromophenyl)-6-(2-((5-bromopyrimidin-2-yl)oxy)ethoxy)pyrimidin-4-yl)sulfuric Diamide

17. Act 132577

18. Aprocitentan (usan/inn)

19. Aprocitentan [inn]

20. Schembl3646065

21. Aprocitentan (act-132577)

22. Gtpl10070

23. Amy39078

24. Bcp28125

25. Ex-a4419

26. Bdbm50395672

27. Who 10552

28. Zinc95553608

29. Db15059

30. Ncgc00378592-01

31. Ac-36529

32. As-82256

33. Hy-15895

34. Db-130379

35. D11441

36. D87138

37. A922313

38. Q27146161

39. Act-132577; Act 132577; Act132577

40. 5-(4-bromophenyl)-4-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-6-(sulfamoylamino)pyrimidine.

41. N-(5-(4-bromophenyl)-6-(2-((5-bromo-2-pyrimidinyl)oxy)ethoxy)-4-pyrimidinyl)-sulfamide

42. N-(5-(4-bromophenyl)-6-(2-((5-bromo-2-pyrimidinyl)oxy)ethoxy)-4-pyrimidinyl)sulfuric Diamide

43. N-(5-(4-bromophenyl)-6-(2-((5-bromopyrimidin-2-yl)oxy)ethoxy)pyrimidin-4-yl)sulfamide

2.4 Create Date
2008-12-15
3 Chemical and Physical Properties
Molecular Weight 546.2 g/mol
Molecular Formula C16H14Br2N6O4S
XLogP32.4
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count10
Rotatable Bond Count8
Exact Mass545.91435 g/mol
Monoisotopic Mass543.91640 g/mol
Topological Polar Surface Area151 Ų
Heavy Atom Count29
Formal Charge0
Complexity597
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

Treatment of hypertension


Drugs in Development

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Details:

Jeraygo (aprocitentan), the first endothelin receptor antagonist, treats hypertension in adults by combining it with other antihypertensives to reduce blood pressure.


Lead Product(s): Aprocitentan

Therapeutic Area: Cardiology/Vascular Diseases Brand Name: Jeraygo

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable April 26, 2024

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01

Medlab Asia & Asia Health
Not Confirmed
Medlab Asia & Asia Health
Not Confirmed

Details : Jeraygo (aprocitentan), the first endothelin receptor antagonist, treats hypertension in adults by combining it with other antihypertensives to reduce blood pressure.

Brand Name : Jeraygo

Molecule Type : Small molecule

Upfront Cash : Not Applicable

April 26, 2024

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Details:

Tryvio (aprocitentan), an endothelin receptor antagonist, is indicated for treating hypertension when combined with other antihypertensives to lower blood pressure in adults.


Lead Product(s): Aprocitentan

Therapeutic Area: Cardiology/Vascular Diseases Brand Name: Tryvio

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable March 20, 2024

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Medlab Asia & Asia Health
Not Confirmed
Medlab Asia & Asia Health
Not Confirmed

Details : Tryvio (aprocitentan), an endothelin receptor antagonist, is indicated for treating hypertension when combined with other antihypertensives to lower blood pressure in adults.

Brand Name : Tryvio

Molecule Type : Small molecule

Upfront Cash : Not Applicable

March 20, 2024

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Details:

Idorsia will reacquire the development and commercialization rights for aprocitentan, a potential novel, effective, once-daily, orally active, dual endothelin A and B receptor antagonist and well-tolerated treatment for resistant hypertension, from Janssen.


Lead Product(s): Aprocitentan

Therapeutic Area: Cardiology/Vascular Diseases Brand Name: ACT-132577

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Idorsia Pharmaceuticals

Deal Size: $343.0 million Upfront Cash: Undisclosed

Deal Type: Licensing Agreement September 05, 2023

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Medlab Asia & Asia Health
Not Confirmed
Medlab Asia & Asia Health
Not Confirmed

Details : Idorsia will reacquire the development and commercialization rights for aprocitentan, a potential novel, effective, once-daily, orally active, dual endothelin A and B receptor antagonist and well-tolerated treatment for resistant hypertension, from Janss...

Brand Name : ACT-132577

Molecule Type : Small molecule

Upfront Cash : Undisclosed

September 05, 2023

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Details:

ACT-132577 (aprocitentan) is a dual endothelin receptor antagonist, which potently inhibits the binding of ET-1 to ETA and ETB receptors. It has a mechanism of action that is ideally suited for the pathophysiology of resistant hypertension.


Lead Product(s): Aprocitentan

Therapeutic Area: Cardiology/Vascular Diseases Brand Name: ACT-132577

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Johnson & Johnson Innovative Medicine

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable January 31, 2023

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04

Medlab Asia & Asia Health
Not Confirmed
Medlab Asia & Asia Health
Not Confirmed

Details : ACT-132577 (aprocitentan) is a dual endothelin receptor antagonist, which potently inhibits the binding of ET-1 to ETA and ETB receptors. It has a mechanism of action that is ideally suited for the pathophysiology of resistant hypertension.

Brand Name : ACT-132577

Molecule Type : Small molecule

Upfront Cash : Not Applicable

January 31, 2023

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Details:

ACT-132577 (aprocitentan), is an investigational, novel, oral, dual endothelin receptor antagonist (ERA), which potently inhibits the binding of ET-1 to ETA and ETB receptors.


Lead Product(s): Aprocitentan

Therapeutic Area: Cardiology/Vascular Diseases Brand Name: ACT-132577

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable December 20, 2022

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05

Medlab Asia & Asia Health
Not Confirmed
Medlab Asia & Asia Health
Not Confirmed

Details : ACT-132577 (aprocitentan), is an investigational, novel, oral, dual endothelin receptor antagonist (ERA), which potently inhibits the binding of ET-1 to ETA and ETB receptors.

Brand Name : ACT-132577

Molecule Type : Small molecule

Upfront Cash : Not Applicable

December 20, 2022

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Details:

Aprocitentan (ACT-132577), a novel, dual ERA, which potently inhibits the binding of ET-1 to ETA and ETB receptors. Aprocitentan has a low potential for drug-drug interaction and a mechanism of action that is intended to address the pathophysiology of difficult-to-control HTN.


Lead Product(s): Aprocitentan

Therapeutic Area: Cardiology/Vascular Diseases Brand Name: ACT-132577

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Idorsia Pharmaceuticals

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable November 07, 2022

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06

Medlab Asia & Asia Health
Not Confirmed
Medlab Asia & Asia Health
Not Confirmed

Details : Aprocitentan (ACT-132577), a novel, dual ERA, which potently inhibits the binding of ET-1 to ETA and ETB receptors. Aprocitentan has a low potential for drug-drug interaction and a mechanism of action that is intended to address the pathophysiology of di...

Brand Name : ACT-132577

Molecule Type : Small molecule

Upfront Cash : Not Applicable

November 07, 2022

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Details:

ACT-132577 (aprocitentan) reduces blood pressure compared to placebo by week 4 of treatment, the effect is maintained and confirmed over a period of 48 weeks, and is generally well tolerated with no major safety concerns.


Lead Product(s): Aprocitentan

Therapeutic Area: Cardiology/Vascular Diseases Brand Name: ACT-132577

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable May 23, 2022

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07

Medlab Asia & Asia Health
Not Confirmed
Medlab Asia & Asia Health
Not Confirmed

Details : ACT-132577 (aprocitentan) reduces blood pressure compared to placebo by week 4 of treatment, the effect is maintained and confirmed over a period of 48 weeks, and is generally well tolerated with no major safety concerns.

Brand Name : ACT-132577

Molecule Type : Small molecule

Upfront Cash : Not Applicable

May 23, 2022

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Details:

The net proceeds from this offering will help Idorsia to prepare to launch its first commercial product and continue to fund the development of its pipeline candidates including aprocitentan, clazosentan and lucerastat, as well as its early-stage and preclinical pipeline.


Lead Product(s): Aprocitentan

Therapeutic Area: Cardiology/Vascular Diseases Brand Name: Undisclosed

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Undisclosed

Deal Size: $341.0 million Upfront Cash: Undisclosed

Deal Type: Public Offering May 20, 2020

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08

Medlab Asia & Asia Health
Not Confirmed
Medlab Asia & Asia Health
Not Confirmed

Details : The net proceeds from this offering will help Idorsia to prepare to launch its first commercial product and continue to fund the development of its pipeline candidates including aprocitentan, clazosentan and lucerastat, as well as its early-stage and pre...

Brand Name : Undisclosed

Molecule Type : Small molecule

Upfront Cash : Undisclosed

May 20, 2020

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INTERMEDIATES SUPPLIERS

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Cosmoprof India
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Cosmoprof India
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CAS Number : 146533-41-7

End Use API : Aprocitentan

About The Company : Glenfin Chemicals, a trusted provider of high-quality chemical solutions tailored to meet the diverse needs of industries worldwide. Based in the heart of inno...

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FDF Dossiers

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Cosmoprof India
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APROCITENTAN

Brand Name : TRYVIO

Dosage Form : TABLET;ORAL

Dosage Strength : 12.5MG

Packaging :

Approval Date : 2024-03-19

Application Number : 217686

Regulatory Info : RX

Registration Country : USA

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FDA Orange Book

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IDORSIA

Switzerland
Medlab Asia & Asia Health
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IDORSIA

Switzerland
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APROCITENTAN

Brand Name : TRYVIO

Dosage Form : TABLET;ORAL

Dosage Strength : 12.5MG

Approval Date : 2024-03-19

Application Number : 217686

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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Patents & EXCLUSIVITIES

Check the patents & exclusivity for this product

US Patents

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Medlab Asia & Asia Health
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IDORSIA

Switzerland
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Medlab Asia & Asia Health
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APROCITENTAN

US Patent Number : 11787782

Drug Substance Claim :

Drug Product Claim :

Application Number : 217686

Patent Use Code : U-3877

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2038-03-02

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Medlab Asia & Asia Health
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IDORSIA

Switzerland
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Medlab Asia & Asia Health
Not Confirmed

APROCITENTAN

US Patent Number : 11680058

Drug Substance Claim :

Drug Product Claim :

Application Number : 217686

Patent Use Code : U-3878

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2038-07-26

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Medlab Asia & Asia Health
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IDORSIA

Switzerland
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Medlab Asia & Asia Health
Not Confirmed

APROCITENTAN

US Patent Number : 11174247

Drug Substance Claim :

Drug Product Claim :

Application Number : 217686

Patent Use Code : U-3879

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2037-11-06

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Medlab Asia & Asia Health
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IDORSIA

Switzerland
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Medlab Asia & Asia Health
Not Confirmed

APROCITENTAN

US Patent Number : 8324232

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 217686

Patent Use Code : U-3878

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2029-09-21

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Medlab Asia & Asia Health
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IDORSIA

Switzerland
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Medlab Asia & Asia Health
Not Confirmed

APROCITENTAN

US Patent Number : 10919881

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 217686

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2038-02-26

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US Exclusivities

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Cosmoprof India
Not Confirmed

IDORSIA

Switzerland
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Cosmoprof India
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APROCITENTAN

Exclusivity Code : NCE

Exclusivity Expiration Date : 2029-03-22

Application Number : 217686

Product Number : 1

Exclusivity Details :

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