Detailed explanation of the efficacy and side effects of aprecitentan

Aprocitentan is a new endothelin receptor antagonist (ERA) approved in recent years for the treatment of resistant hypertension. It is an oral preparation that dually antagonizes ET-A and ET-B receptors. Its main mechanism is to block the action of the vasoconstrictor factor endothelin-1 (ET-1), thereby dilating blood vessels, reducing peripheral vascular resistance, and reducing blood pressure. Clinical studies such as the PRECISION trial have shown that aprecitentan has a significant effect on patients whose blood pressure cannot be controlled even after using three antihypertensive drugs (usually ACEI/ARB + u200bu200bdiuretics + calcium channel blockers). The average systolic blood pressure can be reduced by 5 to 15 mmHg, and the effect remains stable during long-term follow-up.

In addition to its antihypertensive effect, aprecitentan has also been observed to have a certain protective effect against target organ damage such as left ventricular hypertrophy and worsening renal function, thanks to its properties of improving microvascular function and reducing endothelin-mediated inflammation. However, because its mechanism also acts on kidneys and vascular permeability, aprecitentan also has certain side effects, the most common of which are fluid retention and peripheral edema, especially in the elderly or patients with chronic kidney disease. In addition, some patients may experience headache, nasal congestion, anemia, mild liver function abnormalities, etc. Aprecitentan carries a lower risk of hepatotoxicity and pulmonary hypertension than other endothelin antagonists, but blood pressure, weight, renal function, and electrolytes, especially sodium and potassium levels, still need to be monitored regularly.

It should be noted that aprecitentan has a good safety profile when used in combination with other antihypertensive drugs, and it is currently used clinically in combination with conventional triple drug regimens. Because of its slow onset of action, it may take several weeks for patients to feel a steady drop in blood pressure in the early stages, so they should be patient and insist on taking the medication.

In general, aprecitentan brings a new option for the treatment of resistant hypertension. Its efficacy is clear, but doctors still need to strictly control the dosage and monitor side effects during use to ensure maximum benefit from treatment while minimizing adverse effects.

Reference materials:https://go.drugbank.com/drugs/DB15059