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Azilsartan medoxomil

Generic Name
Azilsartan medoxomil
Brand Names
Edarbyclor, Edarbi
Drug Type
Small Molecule
Chemical Formula
C30H24N4O8
CAS Number
863031-21-4
Unique Ingredient Identifier
LL0G25K7I2

Overview

Azilsartan medoxomil is a prodrug that is broken down to azilsartan, which belongs in the angiotensin-receptor blocking (ARB) drug class. It is a selective AT1 subtype angiotensin II receptor antagonist. Azilsartan medoxomil is a relatively recently-developed antihypertensive drug that was first approved by the FDA in February 2011. Many guidelines recommend the use of ARBs as first-line therapy when initiating antihypertensive therapy and indicate that the clinical efficacy of ARBs is comparable to angiotensin-converting enzyme (ACE) inhibitors that are also used as first-line treatment for hypertension. Azilsartan medoxomil is marketed under the brand name Edarbi. It is used to treat hypertension as monotherapy or in combination with other antihypertensive drugs. It is also available in a combination product with chlorthalidone. As hypertension is a major risk factor for cardiovascular disease, early management of hypertension has several implications on patients' survival rate and quality of life in the future. Lowering blood pressure is associated with a reduced risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. Azilsartan medoxomil is thus speculated to lower mortality rates and the onset of cardiovascular disease. Although there is no clinical significance yet determined, azilsartan medoxomil may have potential off-label uses in patients with a history of myocardial infarction or heart failure.

Background

Azilsartan medoxomil is a prodrug that is broken down to azilsartan, which belongs in the angiotensin-receptor blocking (ARB) drug class. It is a selective AT1 subtype angiotensin II receptor antagonist. Azilsartan medoxomil is a relatively recently-developed antihypertensive drug that was first approved by the FDA in February 2011. Many guidelines recommend the use of ARBs as first-line therapy when initiating antihypertensive therapy and indicate that the clinical efficacy of ARBs is comparable to angiotensin-converting enzyme (ACE) inhibitors that are also used as first-line treatment for hypertension. Azilsartan medoxomil is marketed under the brand name Edarbi. It is used to treat hypertension as monotherapy or in combination with other antihypertensive drugs. It is also available in a combination product with chlorthalidone. As hypertension is a major risk factor for cardiovascular disease, early management of hypertension has several implications on patients' survival rate and quality of life in the future. Lowering blood pressure is associated with a reduced risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. Azilsartan medoxomil is thus speculated to lower mortality rates and the onset of cardiovascular disease. Although there is no clinical significance yet determined, azilsartan medoxomil may have potential off-label uses in patients with a history of myocardial infarction or heart failure.

Indication

Azilsartan medoxomil is indicated for the treatment of hypertension to lower blood pressure in patients over 18 years of age. It may be used either alone or in combination with other antihypertensive agents. Some antihypertensive drugs have lesser effects on blood pressure in black patients. Azilsartan medoxomil is available as a fixed-dose combination product with chlorthalidone, which is indicated for the treatment of hypertension in patients whose hose blood pressure is not adequately controlled on monotherapy. It may be used as initial therapy if a patient is likely to need multiple drugs to achieve blood pressure goals. Azilsartan medoxomil belongs to the angiotensin-receptor blocking (ARB) class of drugs, which are used to decrease the progression of moderate-to-severe albuminuria and prevent the recurrence of atrial fibrillation as off-label uses in patients with diabetes mellitus and hypertension.

Associated Conditions

  • Albuminuria
  • Hypertension
  • Atrial Fibrillation

Research Report

Published: May 16, 2025

Azilsartan Medoxomil: A Comprehensive Pharmacological and Clinical Review

1. Introduction to Azilsartan Medoxomil

1.1. Overview, Chemical Identity, and Brand Names

Azilsartan medoxomil is an orally administered angiotensin II receptor blocker (ARB) that functions as a prodrug. It undergoes hydrolysis in the gastrointestinal tract to its pharmacologically active metabolite, azilsartan.[1] This small molecule drug, identified by DrugBank ID DB08822 and CAS Number 863031-21-4, plays a significant role in the management of hypertension.[1]

The chemical name for azilsartan medoxomil is (5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-1-[[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylate.[2] Its molecular formula is C30​H24​N4​O8​, and it has a molecular weight of approximately 568.53 g/mol.[4] The potassium salt, azilsartan kamedoxomil, is often used in pharmaceutical formulations.[3] Azilsartan medoxomil is marketed under various brand names, most notably Edarbi® for the monotherapy formulation and Edarbyclor® for the fixed-dose combination product with the diuretic chlorthalidone.[1]

Continue reading the full research report

FDA Approved Products

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