Sartan drugs are angiotensin II receptor antagonists that can selectively block the binding of angiotensin II to the angiotensin II-1 receptor (AT1 receptor), thereby inhibiting vasoconstriction, reducing water and sodium retention, improving vascular elasticity, and lowering blood pressure. This class of drugs was first introduced into clinical practice in the 1990s and has now developed into one of the important first-line drugs in hypertension treatment guidelines.
The sartan family includes:
Losartan: The first-generation sartan drug, which laid the foundation for ARBs.
Valsartan, Irbesartan, Telmisartan: The new generation of sartan drugs, which have improved efficacy due to their longer half-life and stronger receptor binding.
Azilsartan: The newest member, considered to be the most effective and longest-acting member of the sartan drug family.
In 2011, azilsartan potassium was first approved by the U.S. FDA for the treatment of primary hypertension. Japan and other regions have also successively approved this drug, and in 2021, it was approved for marketing in China.
Advantages of Azilsartan
Highly Selective AT1 Antagonism
Azilsartan potassium completely and irreversibly blocks the activity of AT1 receptors, inhibiting angiotensin II-induced vasoconstriction and aldosterone release, thereby lowering blood pressure and improving cardiovascular function. Compared to other sartans, azilsartan has a higher affinity for AT1 receptors and achieves more complete receptor blockade. Studies show that azilsartan's affinity for AT1 receptors is approximately 10 times that of losartan and twice that of valsartan. Additionally, azilsartan maintains vasodilatory effects during receptor desensitization, demonstrating a "host effect" that supports its position columnar title as the "most potent sartan".
Most Potent and Long-Lasting Antihypertensive Effect
Azilsartan's unique molecular structure and pharmacokinetic properties provide significant blood pressure-lowering advantages.
Significant Reduction in Systolic and Diastolic Blood Pressure: In a pivotal clinical trial involving 1,291 patients randomly assigned to azilsartan (40 mg or 80 mg), valsartan (320 mg), or olmesartan (40 mg), the azilsartan 80 mg group showed a significantly greater reduction in systolic blood pressure (-14.3 mmHg) compared to valsartan (-10.0 mmHg) and olmesartan (-11.3 mmHg). In another randomized controlled trial, azilsartan 100 mg achieved a blood pressure control rate of 95%, compared to 84% for valsartan.
Long-Lasting Effect: In an ambulatory blood pressure monitoring (ABPM) study, azilsartan 80 mg consistently reduced 24-hour systolic and diastolic blood pressure, with superior control of nighttime blood pressure compared to valsartan and irbesartan.
Morning Surge Hypertension: Azilsartan significantly reduces morning surge blood pressure (-8.7 mmHg), providing additional protection for patients with morning hypertension, which is critical for preventing stroke and myocardial infarction.
Multifaceted Cardiovascular Protection
Azilsartan is not only an antihypertensive drug but also offers extensive cardiovascular and metabolic benefits.
Left Ventricular Hypertrophy: Studies show azilsartan significantly improves left ventricular mass index (LVMI), outperforming valsartan.
Renal Protection: In a study of chronic kidney disease (CKD) patients, azilsartan reduced urinary protein levels by 47% and slowed the decline in glomerular filtration rate (eGFR).
Anti-Inflammatory and Antioxidant Effects: Azilsartan reduces inflammatory factors (e.g., CRP, IL-6) and oxidative stress, slowing the progression of atherosclerosis.
Metabolic Benefits: In patients with metabolic syndrome, azilsartan improved insulin sensitivity (HOMA-IR index decreased by 15%) and reduced the risk of diabetic complications.
These benefits make azilsartan a highly effective and versatile option for hypertension management and cardiovascular health.
