Pharmacology and Therapeutic Potential of Finerenone: A Novel Third-Generation Nonsteroidal Mineralocorticoid Receptor Antagonist

非奈利酮的药理学和治疗潜力:一种新型第三代非甾体盐皮质激素受体拮抗剂

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Abstract

Finerenone is a novel third-generation nonsteroidal mineralocorticoid receptor antagonist (MRA) that has demonstrated efficacy in treating chronic kidney disease (CKD) and heart failure with reduced ejection fraction (HFrEF). Unlike traditional steroidal MRAs such as Spironolactone and Eplerenone, Finerenone offers high selectivity for MR, resulting in reduced off-target effects, including hyperkalemia and antiandrogenic side effects. It exerts renoprotective and cardioprotective effects through its anti-inflammatory and antifibrotic actions, making it a good therapeutic option for patients with CKD and HFrEF. The pharmacokinetic profile of Finerenone demonstrates rapid absorption, satisfactory oral bioavailability, and predictable systemic clearance, contributing to its efficacy and tolerability. Clinical trials, including advanced Phase III studies, have established Finerenone's ability to delay CKD progression, reduce proteinuria, and improve cardiovascular (CV) outcomes (such as hospitalization for heart failure and CV death) in patients with diabetes mellitus and CKD. Compared to other MRAs, Finerenone demonstrates improved tolerability; however, clinically significant risks such as hyperkalemia necessitate proactive monitoring and protocol-driven management. Additionally, its unique molecular structure and mechanism of action make it a safer alternative for long-term use in diverse populations. While initial results are promising, further research is necessary to evaluate the long-term outcomes and explore its full therapeutic potential, including novel applications in high-risk patients and biomarker-driven treatments. These findings position finerenone as a valuable addition to current therapies for CKD and HFrEF, though broader adoption awaits real-world validation of its safety and cost-effectiveness.

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