Esaxerenone

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Esaxerenone


Esaxerenone (INN, USAN) is a nonsteroidal mineralocorticoid receptor antagonist that is marketed in Japan for the treatment of hypertension. It was developed by Daiichi Sankyo and approved for medical use in Japan in January 2019.

Pharmacology[edit | edit source]

Esaxerenone acts as a selective and competitive antagonist of the mineralocorticoid receptor, which is a nuclear receptor that is activated by the hormone aldosterone. By blocking the action of aldosterone, esaxerenone reduces the reabsorption of sodium and the excretion of potassium in the kidneys, which in turn decreases blood volume and lowers blood pressure.

Clinical use[edit | edit source]

Esaxerenone is used in the treatment of hypertension, a common condition in which the force of the blood against the artery walls is too high. It is particularly useful in patients who have not responded adequately to other antihypertensive drugs, such as angiotensin converting enzyme inhibitors (ACE inhibitors), angiotensin II receptor blockers (ARBs), and calcium channel blockers.

Side effects[edit | edit source]

The most common side effects of esaxerenone are hyperkalemia (high potassium levels in the blood), increased blood urea nitrogen, and increased serum creatinine. These side effects are generally mild and reversible upon discontinuation of the drug.

History[edit | edit source]

Esaxerenone was developed by the Japanese pharmaceutical company Daiichi Sankyo. It was approved for medical use in Japan in January 2019, making it the first nonsteroidal mineralocorticoid receptor antagonist to be marketed.

See also[edit | edit source]

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Contributors: Prab R. Tumpati, MD