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Clinical data | |
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Trade names | Tryvio |
Other names | ACT-132577 |
AHFS/Drugs.com | Monograph |
Routes of administration | By mouth |
Drug class | Antihypertensive |
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Chemical and physical data | |
Formula | C16H14Br2N6O4S |
Molar mass | 546.19 g·mol−1 |
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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]
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]
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]
Aprocitentan may cause hepatotoxicity (liver damage), edema (fluid retention), anemia (reduced hemoglobin), and decreased sperm count. [1]
Data from animal reproductive toxicity studies with other endothelin-receptor agonists indicate that use is contraindicated in pregnant women. [1]
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]
Aprocitentan is developed by Idorsia, which sold it to Janssen and purchased the rights back in 2023, for US$343 million. [9]
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]