Aprocitentan Explained

Tradename:Tryvio
Routes Of Administration:By mouth
Class:Antihypertensive
Atc Prefix:C02
Atc Suffix:KN01
Legal Us:Rx-only
Legal Us Comment:[1]
Legal Eu:Rx-only
Cas Number:1103522-45-7
Pubchem:25099191
Iuphar Ligand:10070
Drugbank:DB15059
Chemspiderid:25027753
Unii:MZI81HV01P
Kegg:D11441
Chebi:76609
Chembl:2165326
Synonyms:ACT-132577
Iupac Name:5-(4-Bromophenyl)-4-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-6-(sulfamoylamino)pyrimidine
C:16
H:14
Br:2
N:6
O:4
S:1
Smiles:C1=CC(=CC=C1C2=C(N=CN=C2OCCOC3=NC=C(C=N3)Br)NS(=O)(=O)N)Br
Stdinchi: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)
Stdinchikey:DKULOVKANLVDEA-UHFFFAOYSA-N

Aprocitentan, sold under the brand name Tryvio, is a medication used to treat hypertension (high blood pressure). It is developed by Idorsia.[2] It is taken by mouth.

Aprocitentan is a dual endothelin-1 antagonist that targets both endothelin A and endothelin B receptors.[3] [4]

Aprocitentan was approved for medical use in the United States in March 2024.[5] It is the first endothelin receptor antagonist to be approved by the US Food and Drug Administration (FDA) to treat systemic hypertension.

Medical uses

Aprocitentan is indicated for the treatment of hypertension in combination with other antihypertensive drugs, to lower blood pressure in adults who are not adequately controlled on other medications.

Adverse effects

Aprocitentan may cause hepatotoxicity (liver damage), edema (fluid retention), anemia (reduced hemoglobin), and decreased sperm count.

Contraindications

Data from animal reproductive toxicity studies with other endothelin-receptor agonists indicate that use is contraindicated in pregnant women.

Mechanism of action

Aprocitentan is an endothelin receptor antagonist that inhibits the protein endothelin-1 from binding to endothelin A and endothelin B receptors. Endothelin-1 mediates various adverse effects via its receptors, such as inflammation, cell proliferation, fibrosis, and vasoconstriction.

Society and culture

Economics

Aprocitentan is developed by Idorsia, which sold it to Janssen and purchased the rights back in 2023, for .[6]

Legal status

Aprocitentan was approved for medical use in the United States in March 2024.

In April 2024, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Jeraygo, intended for the treatment of resistant hypertension in adults.[7] The applicant for this medicinal product is Idorsia Pharmaceuticals Deutschland GmbH.[8] Aprocitentan was approved for medical use in the European Union in June 2024.[9]

Further reading

Notes and References

  1. Web site: Tryvio- aprocitentan tablet, film coated . DailyMed . 29 March 2024 . 25 April 2024 . 25 April 2024 . https://web.archive.org/web/20240425054923/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=dfe7a2ee-612c-4aba-834a-d68e6b59a0a6 . live .
  2. US FDA approves Idorsia's once-daily Tryvio (aprocitentan) - the first and only endothelin receptor antagonist for the treatment of high blood pressure not adequately controlled in combination with other antihypertensives . Idorsia . PR Newswire . 20 March 2024 . 28 April 2024 . 28 April 2024 . https://web.archive.org/web/20240428041218/https://www.prnewswire.com/news-releases/us-fda-approves-idorsias-once-daily-tryvio-aprocitentan--the-first-and-only-endothelin-receptor-antagonist-for-the-treatment-of-high-blood-pressure-not-adequately-controlled-in-combination-with-other-antihypertensives-302094474.html . live .
  3. Ojha . Utkarsh . Ruddaraju . Sanjay . Sabapathy . Navukkarasu . Ravindran . Varun . Worapongsatitaya . Pitchaya . Haq . Jeesanul . Mohammed . Raihan . Patel . Vinod . Current and Emerging Classes of Pharmacological Agents for the Management of Hypertension . American Journal of Cardiovascular Drugs . 2022 . 22 . 3 . 271–285 . 10.1007/s40256-021-00510-9 . 34878631 . 8651502 .
  4. Xu . Jingjing . Jiang . Xiaohua . Xu . Suowen . Aprocitentan, a dual endothelin-1 (ET-1) antagonist for treating resistant hypertension: Mechanism of action and therapeutic potential . Drug Discovery Today . 28 . 11 . 103788 . November 2023 . 37742911 . 10.1016/j.drudis.2023.103788 .
  5. Web site: Novel Drug Approvals for 2024 . U.S. Food and Drug Administration (FDA) . 29 April 2024 . 30 April 2024 . 30 April 2024 . https://web.archive.org/web/20240430031024/https://www.fda.gov/drugs/novel-drug-approvals-fda/novel-drug-approvals-2024 . live .
  6. News: Deswal . Phalguni . Idorsia reacquires aprocitentan rights from Janssen for $343m . 8 November 2023 . Pharmaceutical Technology . 6 September 2023 . 8 November 2023 . https://web.archive.org/web/20231108014011/https://www.pharmaceutical-technology.com/news/idorsia-reacquires-aprocitentan-rights-from-janssen-for-343m/ . live .
  7. Meeting highlights from the Committee for Medicinal Products for Human Use (CHMP) 22-25 April 2024 . European Medicines Agency . 26 April 2024 . 13 June 2024 . 5 July 2024 . https://web.archive.org/web/20240705192841/https://www.ema.europa.eu/en/news/meeting-highlights-committee-medicinal-products-human-use-chmp-22-25-april-2024 . live .
  8. Web site: Jeraygo EPAR . . 25 April 2024 . 13 June 2024 . 13 June 2024 . https://web.archive.org/web/20240613055805/https://www.ema.europa.eu/en/medicines/human/EPAR/jeraygo . live . Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  9. Web site: Jeraygo PI . Union Register of medicinal products . 28 June 2024 . 5 July 2024.

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