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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)-
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
| Molecular Weight | 546.2 g/mol |
|---|---|
| Molecular Formula | C16H14Br2N6O4S |
| XLogP3 | 2.4 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 10 |
| Rotatable Bond Count | 8 |
| Exact Mass | 545.91435 g/mol |
| Monoisotopic Mass | 543.91640 g/mol |
| Topological Polar Surface Area | 151 Ų |
| Heavy Atom Count | 29 |
| Formal Charge | 0 |
| Complexity | 597 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 1 |
Treatment of hypertension
Drugs in Development
Details:
Tryvio (aprocitentan) is a first and only endothelin receptor antagonist, which is indicated for the treatment of hypertension in adult patients, in combination with other antihypertensive drugs.
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 November 15, 2024
Lead Product(s) : Aprocitentan
Therapeutic Area : Cardiology/Vascular Diseases
Highest Development Status : Approved
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Idorsia Launches TRYVIO™ in the U.S. for Hard-to-Control Hypertension
Details : Tryvio (aprocitentan) is a first and only endothelin receptor antagonist, which is indicated for the treatment of hypertension in adult patients, in combination with other antihypertensive drugs.
Brand Name : Tryvio
Molecule Type : Small molecule
Upfront Cash : Not Applicable
November 15, 2024
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
Lead Product(s) : Aprocitentan
Therapeutic Area : Cardiology/Vascular Diseases
Highest Development Status : Approved
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
JERAYGO Recommended for Approval in Europe for Resistant Hypertension Treatment
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
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
Lead Product(s) : Aprocitentan
Therapeutic Area : Cardiology/Vascular Diseases
Highest Development Status : Approved
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
US FDA Approves Idorsia's TRYVIO As First Endothelin Antagonist for High Blood Pressure
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
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
Lead Product(s) : Aprocitentan
Therapeutic Area : Cardiology/Vascular Diseases
Highest Development Status : Phase III
Partner/Sponsor/Collaborator : Idorsia Pharmaceuticals
Deal Size : $343.0 million
Deal Type : Licensing Agreement
Idorsia Reacquires the World-Wide Rights to Aprocitentan
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
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
Lead Product(s) : Aprocitentan
Therapeutic Area : Cardiology/Vascular Diseases
Highest Development Status : Phase III
Partner/Sponsor/Collaborator : Johnson & Johnson Innovative Medicine
Deal Size : Not Applicable
Deal Type : Not Applicable
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
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
Lead Product(s) : Aprocitentan
Therapeutic Area : Cardiology/Vascular Diseases
Highest Development Status : Phase III
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
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
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
Lead Product(s) : Aprocitentan
Therapeutic Area : Cardiology/Vascular Diseases
Highest Development Status : Phase III
Partner/Sponsor/Collaborator : Idorsia Pharmaceuticals
Deal Size : Not Applicable
Deal Type : Not Applicable
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
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
Lead Product(s) : Aprocitentan
Therapeutic Area : Cardiology/Vascular Diseases
Highest Development Status : Phase III
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
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
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
Lead Product(s) : Aprocitentan
Therapeutic Area : Cardiology/Vascular Diseases
Highest Development Status : Phase III
Partner/Sponsor/Collaborator : Undisclosed
Deal Size : $341.0 million
Deal Type : Public Offering
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
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]INTERMEDIATE SUPPLIERS
5-(4-Bromophenyl)-4,6-dichloropyrimidine
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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Patents & EXCLUSIVITIES
US Patents
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]US Exclusivities
Exclusivity Code : NCE
Exclusivity Expiration Date : 2029-03-22
Application Number : 217686
Product Number : 1
Exclusivity Details :
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]ABOUT THIS PAGE
A Aprocitentan manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Aprocitentan, including repackagers and relabelers. The FDA regulates Aprocitentan manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Aprocitentan API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.
A Aprocitentan supplier is an individual or a company that provides Aprocitentan active pharmaceutical ingredient (API) or Aprocitentan finished formulations upon request. The Aprocitentan suppliers may include Aprocitentan API manufacturers, exporters, distributors and traders.
Aprocitentan 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 Aprocitentan 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 Aprocitentan GMP manufacturer or Aprocitentan GMP API supplier for your needs.
A Aprocitentan CoA (Certificate of Analysis) is a formal document that attests to Aprocitentan's compliance with Aprocitentan specifications and serves as a tool for batch-level quality control.
Aprocitentan CoA mostly includes findings from lab analyses of a specific batch. For each Aprocitentan 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.
Aprocitentan may be tested according to a variety of international standards, such as European Pharmacopoeia (Aprocitentan EP), Aprocitentan JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Aprocitentan USP).
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