Aprocitentan
Chemical compound
From Wikipedia, the free encyclopedia
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]
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| Clinical data | |
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| Trade names | Tryvio |
| Other names | ACT-132577 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a624023 |
| Routes of administration | By mouth |
| Drug class | Antihypertensive |
| ATC code | |
| Legal status | |
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| Identifiers | |
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| CAS Number | |
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| DrugBank | |
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| ChEMBL | |
| ECHA InfoCard | 100.282.677 |
| Chemical and physical data | |
| Formula | C16H14Br2N6O4S |
| Molar mass | 546.19 g·mol−1 |
| 3D model (JSmol) | |
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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] The FDA considers it to be a first-in-class medication.[8]
Medical uses
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 antagonist that inhibits the protein endothelin-1 from binding to endothelin A and endothelin B receptors.[1][6] 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.[9]
Legal status
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.[2][10] The applicant for this medicinal product is Idorsia Pharmaceuticals Deutschland GmbH.[2] Aprocitentan was approved for medical use in the European Union in June 2024.[2][3]
