Aprocitentan

Aprocitentan
Clinical data
Trade namesTryvio
Other namesACT-132577
AHFS/Drugs.comMonograph
Routes of
administration		By mouth
Drug classAntihypertensive
ATC code
Legal status
Legal status
Identifiers
  • 5-(4-Bromophenyl)-4-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-6-(sulfamoylamino)pyrimidine
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC16H14Br2N6O4S
Molar mass546.19 g·mol−1
3D model (JSmol)
  • C1=CC(=CC=C1C2=C(N=CN=C2OCCOC3=NC=C(C=N3)Br)NS(=O)(=O)N)Br
  • 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)
  • Key:DKULOVKANLVDEA-UHFFFAOYSA-N

Aprocitentan, sold under the brand name Tryvio, is a medication used to treat hypertension (high blood pressure).[1] It is developed by Idorsia.[4] It is taken by mouth.[1]

Aprocitentan is a receptor antagonist that targets both endothelin A and endothelin B receptors.[5][6]

Aprocitentan was approved for medical use in the United States in March 2024.[1][4][7] It is the first endothelin receptor antagonist to be approved by the US Food and Drug Administration (FDA) to treat systemic hypertension.[4]

  1. ^ a b c d "Tryvio- aprocitentan tablet, film coated". DailyMed. 29 March 2024. Archived from the original on 25 April 2024. Retrieved 25 April 2024.
  2. ^ Cite error: The named reference Jeraygo EPAR was invoked but never defined (see the help page).
  3. ^ Cite error: The named reference Jeraygo PI was invoked but never defined (see the help page).
  4. ^ a b c "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" (Press release). Idorsia. 20 March 2024. Archived from the original on 28 April 2024. Retrieved 28 April 2024 – via PR Newswire.
  5. ^ Ojha, Utkarsh; Ruddaraju, Sanjay; Sabapathy, Navukkarasu; Ravindran, Varun; Worapongsatitaya, Pitchaya; Haq, Jeesanul; et al. (2022). "Current and Emerging Classes of Pharmacological Agents for the Management of Hypertension". American Journal of Cardiovascular Drugs. 22 (3): 271–285. doi:10.1007/s40256-021-00510-9. PMC 8651502. PMID 34878631.
  6. ^ Xu, Jingjing; Jiang, Xiaohua; Xu, Suowen (November 2023). "Aprocitentan, a dual endothelin-1 (ET-1) antagonist for treating resistant hypertension: Mechanism of action and therapeutic potential". Drug Discovery Today. 28 (11): 103788. doi:10.1016/j.drudis.2023.103788. PMID 37742911.
  7. ^ "Novel Drug Approvals for 2024". U.S. Food and Drug Administration (FDA). 29 April 2024. Archived from the original on 30 April 2024. Retrieved 30 April 2024.