盐皮质激素受体(MR)在全身广泛表达,过度的激活被认为与心肾及其他血管系统的纤维化有关,因此,阻断该受体是临床工作中重要的治疗靶点。根据药物结构可分为第1代甾体类盐皮质激素受体拮抗剂如螺内酯、第2代甾体类盐皮质激素受体拮抗剂...盐皮质激素受体(MR)在全身广泛表达,过度的激活被认为与心肾及其他血管系统的纤维化有关,因此,阻断该受体是临床工作中重要的治疗靶点。根据药物结构可分为第1代甾体类盐皮质激素受体拮抗剂如螺内酯、第2代甾体类盐皮质激素受体拮抗剂依普利酮以及第3代非甾体盐皮质激素受体拮抗剂。非奈利酮作为人工合成的非甾体类盐皮质激素受体拮抗剂,已经有大量临床试验证明,其对糖尿病肾脏疾病患者及心力衰竭患者的治疗有效性及安全性;考虑到MR在全身的广泛表达,非奈利酮也在降低血压、干预房颤方面发挥了治疗效果,以及部分临床前试验中也证实了非奈利酮对心肌代谢及骨代谢的作用。本综述将重点总结第3代MRA非奈利酮在目前临床中的应用进展。Mineralocorticoid receptors (MR) are widely expressed in the body and their overactivation is thought to be associated with the fibrosis of the heart, kidney and other vascular systems. Therefore, blocking this receptor is an important therapeutic target in our clinical work. According to the structure features, the mineralocorticoid receptor antagonist (MRA) include the first generation of MRAs such as spironolactone, the second generation of MRAs eplenone and the third generation of non-steroidal mineralocorticoid receptor antagonists. As a synthetic nonsteroidal mineralocorticoid receptor antagonist, a large number of clinical trials have proved finerenone’s efficacy and safety in the treatment of diabetic kidney disease and heart failure patients. Considering the widespread expression of MR throughout the body, finerenone has also played a therapeutic effect in lowering blood pressure and intervening in atrial fibrillation, and some preclinical trials have also confirmed the effects of finerenone on myocardial metabolism and bone metabolism. This review will focus on the current clinical application of the third generation MRA finerenone.展开更多
文摘盐皮质激素受体(MR)在全身广泛表达,过度的激活被认为与心肾及其他血管系统的纤维化有关,因此,阻断该受体是临床工作中重要的治疗靶点。根据药物结构可分为第1代甾体类盐皮质激素受体拮抗剂如螺内酯、第2代甾体类盐皮质激素受体拮抗剂依普利酮以及第3代非甾体盐皮质激素受体拮抗剂。非奈利酮作为人工合成的非甾体类盐皮质激素受体拮抗剂,已经有大量临床试验证明,其对糖尿病肾脏疾病患者及心力衰竭患者的治疗有效性及安全性;考虑到MR在全身的广泛表达,非奈利酮也在降低血压、干预房颤方面发挥了治疗效果,以及部分临床前试验中也证实了非奈利酮对心肌代谢及骨代谢的作用。本综述将重点总结第3代MRA非奈利酮在目前临床中的应用进展。Mineralocorticoid receptors (MR) are widely expressed in the body and their overactivation is thought to be associated with the fibrosis of the heart, kidney and other vascular systems. Therefore, blocking this receptor is an important therapeutic target in our clinical work. According to the structure features, the mineralocorticoid receptor antagonist (MRA) include the first generation of MRAs such as spironolactone, the second generation of MRAs eplenone and the third generation of non-steroidal mineralocorticoid receptor antagonists. As a synthetic nonsteroidal mineralocorticoid receptor antagonist, a large number of clinical trials have proved finerenone’s efficacy and safety in the treatment of diabetic kidney disease and heart failure patients. Considering the widespread expression of MR throughout the body, finerenone has also played a therapeutic effect in lowering blood pressure and intervening in atrial fibrillation, and some preclinical trials have also confirmed the effects of finerenone on myocardial metabolism and bone metabolism. This review will focus on the current clinical application of the third generation MRA finerenone.
