Aprecitentan: Effective effects and clinical data of new antihypertensive drugs

Aprocitentan, a dual endothelin receptor antagonist, is becoming a breakthrough drug in the treatment of resistant hypertension. It controls hypertension from the fundamental mechanism by blocking endothelin A (ETA) and B (ETB) receptors and inhibiting the activity of the powerful vasoconstrictor factor ET-1. It is especially suitable for patients who are ineffective with traditional treatments or have difficulty controlling blood pressure. Its effect is not limited to lowering blood pressure, but may also improve cardiovascular remodeling and reduce complications of chronic hypertension such as organ damage.

Key clinical data come fromPRECISION clinical trial (The Phase III Study of Resistant Hypertension with Aprocitentan). The study included more than 730 patients with hypertension who were refractory to three or more antihypertensive drugs and were randomly divided into aprecitentan 10mg group, 25mg group and placebo group. The results showed that during the four-week treatment, the systolic blood pressure of the aprecitentan 10 mg group was reduced by about 15 mmHg on average compared with the placebo group, while the systolic blood pressure of the 25 mg group was greater. More importantly, during the 48-week extended study phase, the blood pressure control effect continued to be stable, and no obvious drug resistance occurred.

The antihypertensive effect of aprecitentan is also significant in patients with salt-sensitive hypertension, elderly hypertension, and hypertensive patients with multiple metabolic disorders. When used in combination withRAAS inhibitors, calcium channel blockers, diuretics, etc., it shows a synergistic antihypertensive effect and significantly improves the blood pressure compliance rate. The drug has no significant effect on heart rate. The main adverse reactions are mild headache, fatigue, edema, etc. The incidence rate is controllable, indicating that it is generally well tolerated.

In addition, aprecitentan also shows potential in improving vascular endothelial function, anti-inflammatory effects, and reducing left ventricular hypertrophy. The study found that its long-term protective effect on cardiovascular events deserves further attention, which is particularly important for hypertensive patients with high cardiovascular risk.

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