Related Experiment Video
Updated: May 29, 2025
Improved Renal Denervation Mitigated Hypertension Induced by Angiotensin II Infusion
Published on: May 26, 2022
A Game Changer for Resistant Hypertension: The Rise of Aprocitentan
1Department of Basic Medical Sciences, College of Medicine, QU Health, Qatar University, Doha, Qatar.
Insights
A new drug, aprocitentan, offers hope for resistant hypertension (rHTN) patients. This dual endothelin receptor antagonist effectively lowers blood pressure, even when other treatments fail.
Area of Science:
- Cardiovascular Medicine
- Pharmacology
- Nephrology
Background:
- Resistant hypertension (rHTN) poses a significant therapeutic challenge, often unresponsive to conventional treatments.
- Elevated blood pressure is a leading cause of global morbidity and mortality, necessitating novel management strategies.
- Endothelin receptors play a crucial role in regulating vascular tone.
Purpose of the Study:
- To review the novel dual endothelin receptor antagonist, aprocitentan, for treating resistant hypertension.
- To highlight aprocitentan's mechanism of action in blocking endothelin A (ETA) and endothelin B (ETB) receptors.
- To discuss the clinical efficacy and recent FDA approval of aprocitentan.
Main Methods:
- Review of preclinical and clinical data on aprocitentan.
- Analysis of the PRECISION clinical trial results.
- Examination of the drug's pharmacological profile as a dual endothelin receptor antagonist.
Main Results:
- Aprocitentan demonstrated superior and sustained blood pressure reduction in patients with rHTN.
- The dual blockade of ETA and ETB receptors by aprocitentan is associated with significant antihypertensive effects.
- The PRECISION trial confirmed the efficacy of aprocitentan in a resistant hypertension population.
Conclusions:
- Aprocitentan represents a significant advancement in pharmacotherapy for resistant hypertension.
- The FDA approval of aprocitentan provides a new, effective option for patients with difficult-to-treat hypertension.
- Targeting the endothelin system with aprocitentan offers a promising approach to managing complex hypertension cases.
Abstract:
Hypertension is a major risk factor for cardiovascular disease, and a major contributor to global morbidity and mortality. In particular, resistant hypertension (rHTN), defined as blood pressure that remains elevated despite treatment with at least three antihypertensive agents including a diuretic, continues to be a major pharmacotherapeutic challenge. Traditional antihypertensive drugs often fail in patients with rHTN, underscoring the need for novel therapies. This is a brief mini-review of aprocitentan, a new drug that promises a glimmer of hope for patients with rHTN. This drug is a dual endothelin (ET) receptor antagonist that blocks both ET A and ET B receptors. Given that these two receptors are critical players in vasotone regulation, antagonizing them, such as by aprocitentan, would be expected to significantly reduce blood pressure in patients with rHTN. Indeed, the PRECISION clinical trial demonstrated aprocitentan's superior effectiveness in reducing blood pressure in resistant patients, and the effects were sustained. Aprocitentan has been recently FDA-approved, marking a major milestone in hypertension management, offering hope for patients with difficult-to-treat hypertension.
Related Concept Videos
01:18Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme...
01:26Heart Failure Drugs: Inhibitors of Renin-Angiotensin System
01:25Antihypertensive Drugs: Direct Renin Inhibitors
01:30Antihypertensive Drugs: Angiotensin II Receptor Blockers
01:30Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors
01:23Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...