Aprocitentan

{{Short description|Chemical compound}}

{{Use dmy dates|date=March 2024}}

{{cs1 config |display-authors=6}}

{{Infobox drug

| image = Aprocitentan.svg

| alt =

| caption =

| pronounce =

| tradename = Tryvio

| Drugs.com = {{drugs.com|monograph|aprocitentan}}

| MedlinePlus =

| pregnancy_AU =

| pregnancy_AU_comment =

| pregnancy_category=

| routes_of_administration = By mouth

| class = Antihypertensive

| ATC_prefix = C02

| ATC_suffix = KN01

| ATC_supplemental =

| legal_AU =

| legal_AU_comment =

| legal_BR =

| legal_BR_comment =

| legal_CA =

| legal_CA_comment =

| legal_DE =

| legal_DE_comment =

| legal_NZ =

| legal_NZ_comment =

| legal_UK =

| legal_UK_comment =

| legal_US = Rx-only

| legal_US_comment = {{cite web | title=Tryvio- aprocitentan tablet, film coated | website=DailyMed | date=29 March 2024 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=dfe7a2ee-612c-4aba-834a-d68e6b59a0a6 | access-date=25 April 2024 | archive-date=25 April 2024 | archive-url=https://web.archive.org/web/20240425054923/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=dfe7a2ee-612c-4aba-834a-d68e6b59a0a6 | url-status=live }}

| legal_EU = Rx-only

| legal_EU_comment =

| legal_UN =

| legal_UN_comment =

| legal_status =

| bioavailability =

| protein_bound =

| metabolism =

| metabolites =

| onset =

| elimination_half-life =

| duration_of_action=

| excretion =

| 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.{{cite press release | title=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 | publisher=Idorsia | via=PR Newswire | date=20 March 2024 | url=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 | access-date=28 April 2024 | archive-date=28 April 2024 | archive-url=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 | url-status=live }} It is taken by mouth.

Aprocitentan is a receptor antagonist that targets both endothelin A and endothelin B receptors.{{cite journal |last1=Ojha |first1=Utkarsh |last2=Ruddaraju |first2=Sanjay |last3=Sabapathy |first3=Navukkarasu |last4=Ravindran |first4=Varun |last5=Worapongsatitaya |first5=Pitchaya |last6=Haq |first6=Jeesanul |last7=Mohammed |first7=Raihan |last8=Patel |first8=Vinod |title=Current and Emerging Classes of Pharmacological Agents for the Management of Hypertension |journal=American Journal of Cardiovascular Drugs |date=2022 |volume=22 |issue=3 |pages=271–285 |doi=10.1007/s40256-021-00510-9 |pmid=34878631 |pmc=8651502 }}{{cite journal | last=Xu | first=Jingjing |last2=Jiang | first2=Xiaohua | last3=Xu | first3=Suowen | title = Aprocitentan, a dual endothelin-1 (ET-1) antagonist for treating resistant hypertension: Mechanism of action and therapeutic potential | journal = Drug Discovery Today | volume = 28 | issue = 11 | pages = 103788 | date = November 2023 | pmid = 37742911 | doi = 10.1016/j.drudis.2023.103788 }}

Aprocitentan was approved for medical use in the United States in March 2024.{{cite web | title=Novel Drug Approvals for 2024 | website=U.S. Food and Drug Administration (FDA) | date=29 April 2024 | url=https://www.fda.gov/drugs/novel-drug-approvals-fda/novel-drug-approvals-2024 | access-date=30 April 2024 | archive-date=30 April 2024 | archive-url=https://web.archive.org/web/20240430031024/https://www.fda.gov/drugs/novel-drug-approvals-fda/novel-drug-approvals-2024 | url-status=live }} It is the first endothelin receptor antagonist to be approved by the US Food and Drug Administration (FDA) to treat systemic hypertension. The FDA considers it to be a first-in-class medication.{{cite report | title=New Drug Therapy Approvals 2024 | website=U.S. Food and Drug Administration (FDA) | date=January 2025 | url=https://www.fda.gov/media/184967/download | format=PDF | access-date=21 January 2025 | archive-url=https://web.archive.org/web/20250121045744/https://www.fda.gov/media/184967/download | archive-date=21 January 2025 | url-status=live }}