Aprocitentan: First Approval

Drugs. 2024 Jul;84(7):841-847. doi: 10.1007/s40265-024-02053-0. Epub 2024 Jun 4.

Abstract

Aprocitentan (TRYVIO™) is a once-daily oral dual endothelin A (ETA) and B (ETB) receptor antagonist developed by Idorsia Pharmaceuticals for the treatment of hypertension. The endothelin pathway has been implicated in hypertension. Aprocitentan inhibits the binding of endothelin-1 to ETA and ETB receptors, thereby preventing its deleterious effects and lowering blood pressure. In March 2024, aprocitentan received its first approval in the USA 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. This article summarizes the milestones in the development of aprocitentan leading to this first approval for hypertension not adequately controlled on other drugs.

Publication types

  • Review

MeSH terms

  • Antihypertensive Agents* / administration & dosage
  • Antihypertensive Agents* / adverse effects
  • Antihypertensive Agents* / pharmacology
  • Antihypertensive Agents* / therapeutic use
  • Blood Pressure / drug effects
  • Drug Approval*
  • Endothelin Receptor Antagonists / administration & dosage
  • Endothelin Receptor Antagonists / pharmacology
  • Endothelin Receptor Antagonists / therapeutic use
  • Humans
  • Hypertension* / drug therapy
  • Pyrimidines
  • Sulfonamides
  • United States

Substances

  • Antihypertensive Agents
  • aprocitentan
  • Endothelin Receptor Antagonists
  • Pyrimidines
  • Sulfonamides