Aprocitentan

Aprocitentan
Clinical data
Trade namesTryvio
Other namesACT-132577
Routes of
administration		By mouth
Drug classAntihypertensive
ATC code
Legal status
Legal status
Identifiers
IUPAC name
  • 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)
SMILES
  • C1=CC(=CC=C1C2=C(N=CN=C2OCCOC3=NC=C(C=N3)Br)NS(=O)(=O)N)Br
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)
  • Key:DKULOVKANLVDEA-UHFFFAOYSA-N

Aprocitentan, sold under the brand name Tryvio, is a medication used for the treatment of hypertension (high blood pressure).[1] It is an endothelin receptor antagonist active at both endothelin A and endothelin B receptors.[2] It is developed for resistant hypertension by Idorsia, which sold it to Janssen but purchased the rights back in 2023 for $343 million.[3]

Aprocitentan is an active metabolite of macitentan.[4]

Aprocitentan was approved for medical use in the United States in March 2024.[1]

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 drugs.[1]

References

  1. 1 2 3 4 https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/217686s000lbl.pdf
  2. ↑ 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.
  3. ↑ Deswal, Phalguni (6 September 2023). "Idorsia reacquires aprocitentan rights from Janssen for $343m". Pharmaceutical Technology. Archived from the original on 8 November 2023. Retrieved 8 November 2023.
  4. ↑ CID 25099191 from PubChem


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