圖注：Finerenone作用機(jī)制

 

　　Finerenone III期臨床項(xiàng)目是迄今為止最大的CKD III期臨床項(xiàng)目。該項(xiàng)目由兩項(xiàng)研究組成，入組了全球各地1.3萬例伴有廣泛嚴(yán)重程度CKD疾病的T2D患者，包括早期腎損害和更晚期腎病的患者。該項(xiàng)目旨在評(píng)估Finerenone與安慰劑分別聯(lián)合標(biāo)準(zhǔn)護(hù)理對腎臟和心血管（CV）預(yù)后的影響。

 

　　FIDELIO-DKD（Finerenone降低糖尿病腎病腎衰竭和疾病進(jìn)展）是一項(xiàng)隨機(jī)、雙盲、安慰劑對照、平行組、多中心、事件驅(qū)動(dòng)的III期研究，入組了來自全球48個(gè)國家1000多個(gè)地點(diǎn)的約5700例伴有CKD的T2D患者。研究中，這些患者被隨機(jī)分配，接受每天一次口服10mg或20mg的Finerenone或安慰劑，同時(shí)接受標(biāo)準(zhǔn)護(hù)理，包括降糖治療和最大耐受劑量的腎素-血管緊張素系統(tǒng)（RAS）阻斷劑，如血管緊張素轉(zhuǎn)換酶（ACE）抑制劑或血管緊張素II受體阻滯劑（ARB）。該研究已經(jīng)達(dá)到了主要終點(diǎn)。

 

　　FIGARO-DKD（Finerenone降低糖尿病腎病心血管病發(fā)病率和死亡）研究仍在進(jìn)行中，該研究在歐洲、日本、中國、美國等48個(gè)國家入組了約7400例伴有CKD的T2D患者。

 

　　拜耳最近宣布啟動(dòng)FINEARTS-HF研究，這是一項(xiàng)多中心、隨機(jī)、雙盲、安慰劑對照III期研究，將在超過5500例左心室射血分?jǐn)?shù)≥40%的有癥狀心力衰竭（HF）患者（紐約心臟協(xié)會(huì)II-IV級(jí)）中調(diào)查Finerenone與安慰劑。

 

　　參考文獻(xiàn)

 

　　[1].Lowe Jeovanna;Kolkhof Peter;Haupt Michael J;Peczkowski Kyra K;Rastogi Neha;Hauck J Spencer;Kadakia Feni K;Zins Jonathan G;Ciccone Pierce C;Smart Suzanne;Sandner Peter;Raman Subha V;Janssen Paul M L;RafaelFortney Jill A.Mineralocorticoid receptor antagonism by finerenone is sufficient to improve function in preclinical muscular dystrophy.[J].ESC heart failure.2020

 

　　[2].RicoMesa Juan Simon;White Averi;AhmadianTehrani Ashkan;Anderson Allen S.Mineralocorticoid Receptor Antagonists:a Comprehensive Review of Finerenone.[J].Current cardiology reports.2020

 

　　[3].Vincenzo Marzolla;Alessandra Feraco;Stefania Gorini;Caterina Mammi;Carmen Marrese;Valentina Mularoni;Carla Boitani;Marc Lombès;Peter Kolkhof;Maria Rosa Ciriolo;Andrea Armani;Massimiliano Caprio.The novel non‐steroidal MR antagonist finerenone improves metabolic parameters in high‐fat diet‐fed mice and activates brown adipose tissue via AMPK‐ATGL pathway.[J].The FASEB Journal.2020

 

　　[3].Roland Heinig;Michael Gerisch;Michaela Bairlein;Johannes Nagelschmitz;Stephanie Loewen.Results from Drug–Drug Interaction Studies In Vitro and In Vivo Investigating the Effect of Finerenone on the Pharmacokinetics of Comedications.[J].European Journal of Drug Metabolism and Pharmacokinetics.2020

 

　　[4].Nelleke Snelder;Roland Heinig;Henk-Jan Drenth;Amer Joseph;Peter Kolkhof;Jörg Lippert;Dirk Garmann;Bart Ploeger;Thomas Eissing.Population Pharmacokinetic and Exposure–Response Analysis of Finerenone:Insights Based on Phase IIb Data and Simulations to Support Dose Selection for Pivotal Trials in Type 2 Diabetes with Chronic Kidney Disease.[J].Clinical Pharmacokinetics.2020

 

　　[5].Snelder Nelleke;Heinig Roland;Drenth Henk-Jan;Joseph Amer;Kolkhof Peter;Lippert Jörg;Garmann Dirk;Ploeger Bart;Eissing Thomas.Population Pharmacokinetic and Exposure-Response Analysis of Finerenone:Insights Based on Phase IIb Data and Simulations to Support Dose Selection for Pivotal Trials in Type 2 Diabetes with Chronic Kidney Disease.[J].Clinical pharmacokinetics.2020

 

　　[6].Gil-Ortega Marta;Vega-Martín Elena;Martín-Ramos Miriam;González-Blázquez Raquel;Pulido-Olmo Helena;Ruiz-Hurtado Gema;Schulz Angela;Ruilope Luis M;Kolkhof Peter;Somoza Beatriz;Kreutz Reinhold;Fernández-Alfonso Maria S.Finerenone Reduces Intrinsic Arterial Stiffness in Munich Wistar Frömter Rats,a Genetic Model of Chronic Kidney Disease.[J].American journal of nephrology.2020

 

　　[7].Daniel Lavall;Nadine Jacobs;Felix Mahfoud;Peter Kolkhof;Michael Böhm;Ulrich Laufs.The non-steroidal mineralocorticoid receptor antagonist finerenone prevents cardiac fibrotic remodeling.[J].Biochemical Pharmacology.2020

 

　　[8].Bakris George L;Agarwal Rajiv;Anker Stefan D;Pitt Bertram;Ruilope Luis M;Nowack Christina;Kolkhof Peter;Ferreira Anna C;Schloemer Patrick;Filippatos Gerasimos.Design and Baseline Characteristics of the Finerenone in Reducing Kidney Failure and Disease Progression in Diabetic Kidney Disease Trial.[J].American journal of nephrology.2020

 

　　[9].Ruilope Luis M;Agarwal Rajiv;Anker Stefan D;Bakris George L;Filippatos Gerasimos;Nowack Christina;Kolkhof Peter;Joseph Amer;Mentenich Nicole;Pitt Bertram.Design and Baseline Characteristics of the Finerenone in Reducing Cardiovascular Mortality and Morbidity in Diabetic Kidney Disease Trial.[J].American journal of nephrology.2020

 

　　[10].Gerisch Michael;Heinig Roland;Engelen Anna;Lang Dieter;Kolkhof Peter;Radke Martin;Platzek Johannes;Lovis Kai;Rohde Gabriele;Schwarz Thomas.Biotransformation of Finerenone,a Novel Nonsteroidal Mineralocorticoid Receptor Antagonist,in Dogs,Rats,and Humans,In Vivo and In Vitro.[J].Drug metabolism and disposition:the biological fate of chemicals.2020

 

　　注：本文為載，僅做分享之用，對文章觀點(diǎn)保持中立，侵權(quán)即刪。