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Ocedurenone is a **novel, orally administered, nonsteroidal mineralocorticoid receptor antagonist (nsMRA)** developed primarily for the treatment of uncontrolled hypertension in patients with advanced chronic kidney disease (CKD, stages 3b/4)[1][2][3]. It specifically binds and antagonizes the human mineralocorticoid receptor (MR), with much less affinity for glucocorticoid, progesterone, or androgen receptors[1]. Ocedurenone is characterized as a third-generation nsMRA, engineered to improve efficacy and safety compared to steroidal MRAs (like spironolactone and eplerenone) and reduce side effects such as hyperkalemia. Its mechanism of action is MR antagonism, which lowers blood pressure and may reduce cardiovascular risk in CKD patients. The drug displays low systemic clearance, a long half-life, is highly protein bound (>99.7%), and is mainly excreted via feces. It is primarily metabolized by CYP3A4 and is a substrate for P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP)[1][3]. Clinical trials, including BLOCK-CKD, have shown it to be effective and well-tolerated in its target populations.
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