Aprocitentan

Last updated

Aprocitentan
Aprocitentan.svg
Clinical data
Trade names Tryvio
Other namesACT-132577
AHFS/Drugs.com Tryvio
Routes of
administration
By mouth
Drug class Antihypertensive
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
Formula C16H14Br2N6O4S
Molar mass 546.19 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. [2] It is taken by mouth. [1]

Contents

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. [1] [2] It is the first endothelin receptor antagonist to be approved by the US Food and Drug Administration (FDA) to treat systemic hypertension. [2]

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. [1]

Adverse effects

Aprocitentan may cause hepatotoxicity (liver damage), edema (fluid retention), anemia (reduced hemoglobin), and decreased sperm count. [1]

Contraindications

Data from animal reproductive toxicity studies with other endothelin-receptor agonists indicate that use is contraindicated in pregnant women. [1]

Mechanism of action

Aprocitentan is an endothelin receptor agonist that inhibits the protein endothelin-1 from binding to endothelin A and endothelin B receptors. [1] [4] Endothelin-1 mediates various adverse effects via its receptors, such as inflammation, cell proliferation, fibrosis, and vasoconstriction. [1]

Society and culture

Economics

Aprocitentan is developed by Idorsia, which sold it to Janssen and purchased the rights back in 2023, for US$343 million. [5]

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

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. [6] The applicant for this medicinal product is Idorsia Pharmaceuticals Deutschland GmbH. [6]

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References

  1. 1 2 3 4 5 6 7 8 9 10 "Tryvio- aprocitentan tablet, film coated". DailyMed. 29 March 2024. Retrieved 25 April 2024.
  2. 1 2 3 "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. Retrieved 28 April 2024 via PR Newswire.
  3. 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.
  4. 1 2 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.
  5. 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.
  6. 1 2 "Jeraygo EPAR". European Medicines Agency . 25 April 2024. Retrieved 27 April 2024. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.

Further reading