Azilsartan medoxomil tablets (Edarbi): Tablets for the treatment of hypertension alone or in combination with other antihypertensive agents

May 1, 2011

New molecular entity: Azilsartan medoxomil tablets are selective AT1 subtype angiotensin receptor antagonists that were approved by FDA to lower blood pressure.

Hypertension impacts approximately 74.5 million Americans, or nearly 1 in 3 adults. Recent estimates from the American Heart Association suggest that the cost of hypertension in the United States, including both direct and indirect costs, exceeded $76 billion in 2010. Azilsartan medoxomil 40 mg and 80 mg tablets were approved by FDA for the treatment of hypertension, either alone or in combination with other antihypertensive agents. Azilsartan is a selective AT1 subtype angiotensin II receptor antagonist that lowers blood pressure by blocking the action of angiotensin II, a vasopressor hormone that constricts blood vessels.

Efficacy. The antihypertensive efficacy of azilsartan was evaluated in a total of 7 randomized, double-blind trials. Of note, two 6-week, randomized, double-blind trials compared azilsartan 40 mg and 80 mg to placebo, olmesartan 40 mg, and valsartan 320 mg. Compared to placebo, azilsartan lowered systolic and diastolic blood pressure by up to 15.5 mmHg and 8.6 mmHg, respectively, when measured during clinic visits, and by as much as 14.3 mmHg and 9.4 mmHg, respectively, upon use of 24-hour ambulatory blood pressure monitoring. Most of the antihypertensive effect seen with azilsartan occurred within the first 2 weeks of treatment. When compared to active controls, azilsartan 80 mg daily was found to be statistically superior to the highest FDA-approved doses of olmesartan and valsartan upon both clinic and 24-hour ambulatory blood pressure monitoring.

Safety. Nearly 5,000 patients taking azilsartan (at doses between 20 mg and 80 mg) were evaluated for safety end points during clinical trials. This included 1,704 patients treated for at least 6 months and 588 for a minimum of 1 year on azilsartan. Diarrhea (2%) was the most common adverse effect seen in patients during clinical trials. Other adverse effects (occurring in ≥0.3% of patients and more often than placebo) included: dizziness, cough, asthenia, fatigue, and muscle spasm. As with all approved angiotensin receptor antagonists and other medications that act directly on the renin-angiotensin system, use during pregnancy can result in fetal injury and death and is contraindicated.