Aprocitentan

Aprocitentan
Clinical data
Trade names	Tryvio
Other names	ACT-132577
AHFS/Drugs.com	Tryvio
Routes of; administration	By mouth
Drug class	Antihypertensive
ATC code	C02KN01 (WHO) ;
Legal status
Legal status	US: ℞-only;
Identifiers
	IUPAC name 5-(4-Bromophenyl)-4-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-6-(sulfamoylamino)pyrimidine;
CAS Number	1103522-45-7;
PubChem CID	25099191;
IUPHAR/BPS	10070;
DrugBank	DB15059;
ChemSpider	25027753;
UNII	MZI81HV01P;
KEGG	D11441;
ChEBI	CHEBI:76609;
ChEMBL	ChEMBL2165326;
Chemical and physical data
Formula	C16H14Br2N6O4S
Molar mass	546.19 g·mol−1
3D model (JSmol)	Interactive image;
	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 by Idorsia.

Aprocitentan is an active metabolite of macitentan.^[3]

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]

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.^[4]

Legal status

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.^[5] The applicant for this medicinal product is Idorsia Pharmaceuticals Deutschland GmbH.^[5]

References

^ ^a ^b ^c ^d "Tryvio- aprocitentan tablet, film coated". DailyMed. 29 March 2024. Retrieved 25 April 2024.
^ 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.
^ CID 25099191 from PubChem
^ 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.
^ ^a ^b "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.

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[Tryvio_FDA_label-1] "Tryvio- aprocitentan tablet, film coated". DailyMed. 29 March 2024. Retrieved 25 April 2024.

[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] CID 25099191 from PubChem

[4] 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.

[Jeraygo_EPAR-5] "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.

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