The purpose of this study is to investigate the efficacy, safety, tolerability and pharmacokinetics of multiple oral administration of MT-3995 in patients with NASH.

开始日期2016-09-01

申办/合作机构

Mitsubishi Tanabe Pharma Corp.

NCT02900235

/ Completed临床1期

An Open-label, Mass Balance Study to Investigate the Absorption, Metabolism and Excretion of [14C]-MT-3995 After a Single Oral Dose to Healthy Male Subjects

The purpose of this study is to investigate the absorption, metabolism and excretion of MT-3995 in healthy subjects.

开始日期2016-08-01

申办/合作机构

Mitsubishi Tanabe Pharma Corp.

NCT02676401

/ Completed临床2期

An Extended Treatment Study of MT-3995 in Patients With Diabetic Nephropathy

This study aims to evaluate the safety and efficacy of MT-3995 administered over the longer term, following MT-3995-J05 study.

开始日期2016-02-01

申办/合作机构

Mitsubishi Tanabe Pharma Corp.

100 项与阿帕利酮相关的临床结果

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100 项与阿帕利酮相关的转化医学

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100 项与阿帕利酮相关的专利（医药）

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项与阿帕利酮相关的文献（医药）

2025-03-01·Nefrologia

Evidence for the use of a nonsteroidal mineralocorticoid receptor antagonist for the treatment of chronic kidney disease

Review

作者: Avito Fernandes de Almeida, Edgar ; Marques da Silva, Bernardo ; Morais David Pliças, Mariana

INTRODUCTION AND OBJECTIVES:

Chronic kidney disease morbimortality drives the development of new drugs. This work summarizes the evidence on the use of non-steroidal mineralocorticoid receptor antagonists on chronic kidney disease.

MATERIALS AND METHODS:

A search was performed on PubMed and ClinicalTrials.gov using relevant keywords for clinical trials and observational studies, finished or ongoing, from 2019 to 2023.

RESULTS:

Finerenone is currently approved for diabetic kidney disease with albuminuria, with results from two phase three trials, presenting satisfactory results on renal and cardiovascular outcomes and an appropriate safety profile, namely regarding potassium balance. Regarding nondiabetic kidney disease, combining sodium glucose transport protein-2 inhibitors and finerenone points toward reliable results, although these came from non-placebo-controlled trials. An ongoing phase three trial is assessing finerenone efficacy and safety on nondiabetic chronic kidney disease. Esaxerenone is approved for diabetic nephropathies and hypertension in Japan, based on two phase three clinical trials. These trials' external validity is compromised, as they were only developed in Japan. Ocedurenone presents results from a phase two trial on managing refractory hypertension on chronic kidney disease. Apararenone is being investigated for diabetic kidney disease, with results from a phase two study, limited for only including Japanese patients.

CONCLUSIONS:

With this review we provide a global perspective on the available clinical results for these drugs to improve its evidence-based use.

2024-06-01·Drug Metabolism and Pharmacokinetics

Insights into drug development with quantitative systems pharmacology: A prospective case study of uncovering hyperkalemia risk in diabetic nephropathy with virtual clinical trials

Review

作者: Saito, Ryuta ; Nakada, Tomohisa

The quantitative systems pharmacology (QSP) approach is widely applied to address various essential questions in drug discovery and development, such as identification of the mechanism of action of a therapeutic agent, patient stratification, and the mechanistic understanding of the progression of disease. In this review article, we show the current landscape of the application of QSP modeling using a survey of QSP publications over 10 years from 2013 to 2022. We also present a use case for the risk assessment of hyperkalemia in patients with diabetic nephropathy treated with mineralocorticoid receptor antagonists (MRAs, renin-angiotensin-aldosterone system inhibitors), as a prospective simulation of late clinical development. A QSP model for generating virtual patients with diabetic nephropathy was used to quantitatively assess that the nonsteroidal MRAs, finerenone and apararenone, have a lower risk of hyperkalemia than the steroidal MRA, eplerenone. Prospective simulation studies using a QSP model are useful to prioritize pharmaceutical candidates in clinical development and validate mechanism-based pharmacological concepts related to the risk-benefit, before conducting large-scale clinical trials.

2024-06-01·Journal of Diabetes

Renal effects and safety between Asian and non‐Asian chronic kidney disease and type 2 diabetes treated with nonsteroidal mineralocorticoid antagonists

Article

作者: Liao, Lin ; Feng, Jing ; Cui, Yuying ; Dong, Jianjun ; Xu, Xiaoming ; Li, Pingjiang

Abstract:

Background:

Asians bear a heavier burden of chronic kidney disease (CKD), a common comorbidity of type 2 diabetes mellitus (T2DM), than non‐Asians. Nonsteroidal mineralocorticoid receptor antagonists (MRAs) have garnered attention for their potential advantages in renal outcomes. Nevertheless, the impact on diverse ethnic groups remains unknown.

Methods:

The PubMed, Embase, Cochrane Library, China National Knowledge Infrastructure (CNKI), Wanfang database, and clinical trial registries were searched through August 2023 with the following keywords: nonsteroidal MRAs (finerenone, apararenone, esaxerenone, AZD9977, KBP‐5074), CKD, T2DM, and randomized controlled trial (RCT). A random effects model was used to calculate overall effect sizes.

Results:

Seven RCTs with 14 997 participants were enrolled. Nonsteroidal MRAs reduced urinary albumin to creatinine ratio (UACR) significantly more in Asians than non‐Asians: (weighted mean difference [WMD], −0.59, 95% CI, −0.73 to −0.45, p < .01) vs (WMD, −0.29, 95% CI, −0.32 to −0.27, p < .01), respectively. The average decline of estimated glomerular filtration rate (eGFR) was similar in Asians and non‐Asians (p > .05). Regarding systolic blood pressure (SBP), nonsteroidal MRAs had a better antihypertension performance in Asians (WMD, −5.12, 95% CI, −5.84 to −4.41, p < .01) compared to non‐Asians (WMD, −3.64, 95% CI, −4.38 to −2.89, p < .01). A higher incidence of hyperkalemia and eGFR decrease ≥30% was found in Asians than non‐Asians (p < .01).

Conclusions:

Nonsteroidal MRAs exhibited significant renal benefits by decreasing UACR and lowering SBP in Asian than that of non‐Asian patients with CKD and T2DM, without increase of adverse events except hyperkalemia and eGFR decrease ≥30%.image

项与阿帕利酮相关的新闻（医药）

2022-12-12

·PRNewswire

Propulsion of Nonalcoholic Steatohepatitis Pipeline as Novel and Extensive 150+ Therapies Likely to Enter in the Treatment Domain | DelveInsight

The prevalence of nonalcoholic steatohepatitis has been rising since the past few years, which prompts the growing demand for treatment options. The increasing prevalence of Nonalcoholic Steatohepatitis and the growing research and development activities drive the market. The Companies developing the potential therapies in the last stage of development include Madrigal Pharmaceuticals, Inventiva, Boehringer Ingelheim, and several others. LAS VEGAS, Dec. 12, 2022 /PRNewswire/ -- DelveInsight's ' Nonalcoholic Steatohepatitis Pipeline Insight – 2022 ' report provides comprehensive global coverage of available, marketed, and pipeline nonalcoholic steatohepatitis therapies in various stages of clinical development, major pharmaceutical companies are working to advance the pipeline space and future growth potential of the nonalcoholic steatohepatitis pipeline domain. Key Takeaways from the Nonalcoholic Steatohepatitis Pipeline Report DelveInsight's nonalcoholic steatohepatitis pipeline report depicts a robust space with 130+ active players working to develop 150+ pipeline therapies for nonalcoholic steatohepatitis treatment. Key nonalcoholic steatohepatitis companies such as Madrigal Pharmaceuticals, Intercept Pharmaceuticals, Cirius Therapeutics, Novo Nordisk, Galmed Pharmaceuticals, AstraZeneca, Galectin Therapeutics, Viking Therapeutics, Eli Lilly and Company, Terns Pharmaceuticals, Sinew Pharma, Novartis Pharmaceuticals, Poxel SA, AngioLab, Pfizer, Lipocine, Inc., CytoDyn, Inc., Alnylam Pharmaceuticals, Inc., Mitsubishi Tanabe Pharma, Chemomab Therapeutics, NuSirt Biopharma, HK inno. N, Kowa Pharmaceutical, Ionis Pharmaceuticals, NorthSea Therapeutics, Rivus Pharmaceuticals, Hanmi Pharmaceutical, Hepagene Therapeutics, HighTide Biopharma, Akero Therapeutics, Merck Sharp & Dohme LLC, Cascade Pharmaceuticals, Hepion Pharmaceuticals, Chipscreen Biosciences, Boston Pharmaceuticals, Bristol-Myers Squibb, Sunshine Lake Pharma, GSK plc., Future Medicine, Gilead Sciences, ENYO Pharma, Histogen, and others are evaluating nonalcoholic steatohepatitis drugs to improve the treatment landscape. Promising nonalcoholic steatohepatitis pipeline therapies in various stages of development include TERN-101, SNP-610, LJN452 (tropifexor + licogliflozin), PXL065, ALS-L1023, PF-06865571 + PF-05221304, PF-06835919, PF-06865571, ORMD-0801, Norucholic acid, NNC0194-0499, MN-001, MK-3655, MET642, MET409, LPCN 1144, LIK066, Leronlimab, ALN-HSD, MT-3995, CM101, Leu-Mit-Sil (NS-0200), IN-A010, Efruxifermin (EFX), Efinopegdutide, EDP-305, JKB-122, CS0159 (Linafexor), CRV431, Chiglitazar sodium, BOS-580, BMS-986263, HEC96719, GSK4532990, FM101, Firsocostat, EPY001a, Emricasan, BMS-986036, BIO89-100, BI 456906, BFKB8488A, AXA1125, ASC 41, GS-9674 (Cilofexor), ZSP1601, and others. In November 2022, Sagimet Biosciences announced positive interim data from its Phase IIb clinical trial (FASCINATE-2) with denifanstat, a fatty acid synthase (FASN) inhibitor, in non-alcoholic steatohepatitis patients. Data showed statistically significant improvements across key markers of NASH, reinforcing results observed in earlier studies, including statistically significant reductions in markers of liver fat, inflammation, and fibrosis. There were no treatment-related serious adverse events, with the majority of adverse events mild to moderate in nature (Grade 1 and 2). Additional interim data are expected in early 2023. In November 2022, Inventiva announced that the United States Patent and Trademark Office granted a patent (U.S. Patent No. 11,504,380) that protects the use of lanifibranor for the treatment of cirrhotic patients at risk of progressing from compensated stage to decompensated stage. This patent will expire on November 8, 2039. This patent further expands the intellectual property protection of lanifibranor in the United States for use in patients with cirrhotic NASH. In October 2022, Galectin Therapeutics, Inc. reported the positive outcome of its second data and safety monitoring board (DSMB) meeting for NAVIGATE, its seamless, adaptive, phase IIb/III study of belapectin in patients with liver cirrhosis caused by non-alcoholic steatohepatitis (NASH). The objective of this second independent DSMB was further to review the emerging tolerance and safety profiles of belapectin. Based on its deliberation, the DSMB concluded that NAVIGATE could continue as designed, without modifications. In September 2022, Inventiva and Chia Tai-Tianqing Pharmaceutical Group entered into a licensing and collaboration agreement to develop and commercialize lanifibranor, if approved, for the treatment of nonalcoholic steatohepatitis and potentially other metabolic diseases in mainland China, Hong Kong, Macau, and Taiwan. In June 2022, Poxel SA announced that the U.S. Patent and Trademark Office (PTO) has issued to Poxel US Patent No. 11319313, which represents a new patent for PXL065, a novel, proprietary deuterium-stabilized R-stereoisomer of pioglitazone which is being investigated in Phase II stage of clinical trial evaluation for the treatment of Nonalcoholic steatohepatitis (NASH). In May 2022, Pfizer Inc. announced the U.S. Food and Drug Administration (FDA) had granted Fast Track designation to Pfizer's investigational combination therapy for the treatment of non-alcoholic steatohepatitis (NASH) with liver fibrosis: ervogastat (PF-06865571, a diacylglycerol O-acyltransferase 2 inhibitor, or DGAT2i) and clesacostat (PF-05221304, an acetyl-CoA carboxylase inhibitor, or ACCi). In May 2022, Hepion Pharmaceuticals, Inc. announced that it has entered into a clinical collaboration with HepQuant, a Denver-based, privately held company with novel, proprietary investigational technology for evaluating liver function and health in patients with chronic liver diseases. Hepion will incorporate the HepQuant 'SHUNT' test into a dedicated Phase IIb clinical trial in presumed NASH F3 subjects. In February 2022, the US Food and Drug Administration (FDA) granted a Fast-Track Designation to Axcella Therapeutics' AXA1125 to treat non-alcoholic steatohepatitis (NASH) with liver fibrosis. In January 2022, LISCure Biosciences announced that it had executed a research collaboration agreement with Mayo Clinic for new drug development for rare liver diseases. LISCure Biosciences Inc. has executed a research collaboration agreement with US based-Mayo Clinic for new drug development for rare liver diseases. Request a sample and discover the nash drugs in development 2022 @ Nonalcoholic Steatohepatitis Pipeline 2022 Report The nonalcoholic steatohepatitis pipeline report provides detailed profiles of pipeline assets, a comparative analysis of clinical and non-clinical stage nonalcoholic steatohepatitis drugs, inactive and dormant assets, a comprehensive assessment of driving and restraining factors, and an assessment of opportunities and risks in the nonalcoholic steatohepatitis clinical trial landscape. Nonalcoholic Steatohepatitis Overview Nonalcoholic steatohepatitis (NASH) is a type of liver inflammation and damage caused by fat buildup. It is one of several conditions known as nonalcoholic fatty liver disease. Nonalcoholic fatty liver disease is classified into two types: isolated fatty liver, in which only fat accumulates, and nonalcoholic steatohepatitis, in which fat, inflammation, and liver cell damage occur. NASH does not usually cause symptoms. Most people with NASH feel fine and are unaware that they have it. As NASH progresses and liver damage worsens, a patient may experience fatigue, weight loss, general weakness, and acne in the upper right part of the belly. Screening for nonalcoholic fatty liver disease in the general population is not advised. It is usually considered after discovering unexplained liver enzyme levels, or imaging reveals hepatic steatosis. A patient's medical history, a physical exam, and tests for nonalcoholic steatohepatitis are used by doctors. Want to discover how the Nash treatment pipeline will look like? Request for sample @ NASH Drug Pipeline 2022 A snapshot of the Nonalcoholic Steatohepatitis Pipeline Drugs mentioned in the report: Want to know how nash dash the pipeline race is for new agents? Download the sample page @ NASH Clinical Trials Nonalcoholic Steatohepatitis Therapeutics Assessment The nonalcoholic steatohepatitis pipeline report proffers an integral view of nonalcoholic steatohepatitis emerging novel therapies segmented by stage, product type, molecule type, mechanism of action, and route of administration. Scope of the Nonalcoholic Steatohepatitis Pipeline Report Coverage: Global Therapeutic Assessment By Product Type: Mono, Combination, Mono/Combination Therapeutic Assessment By Clinical Stages: Discovery, Pre-clinical, Phase I, Phase II, Phase III Therapeutics Assessment By Route of Administration: Intravenous, Parenteral, Oral, Subcutaneous Therapeutics Assessment By Molecule Type: Antibody, Biologic, Cell therapy, Peptide, Protein, Small molecule Therapeutics Assessment By Mechanism of Action: Adiponutrin inhibitor, Diacylglycerol O acyltransferase inhibitor, Adiponutrin modulator, RNA interference, Glucagon like peptide 1 receptor agonist, Ornithine decarboxylase stimulant, Farnesoid X-activated receptor agonist, Thyroid hormone receptor beta agonist, Mitochondrial membrane transport protein modulator, Thyroid hormone receptor beta agonists, Peroxisome proliferator-activated receptor alpha agonist Key Nonalcoholic Steatohepatitis Companies:Madrigal Pharmaceuticals, Intercept Pharmaceuticals, Cirius Therapeutics, Novo Nordisk, Galmed Pharmaceuticals, AstraZeneca, Galectin Therapeutics, Viking Therapeutics, Eli Lilly and Company, Terns Pharmaceuticals, Sinew Pharma, Novartis Pharmaceuticals, Poxel SA, AngioLab, Pfizer, Lipocine, Inc., CytoDyn, Inc., Alnylam Pharmaceuticals, Inc., Mitsubishi Tanabe Pharma, Chemomab Therapeutics, NuSirt Biopharma, HK inno. N, Kowa Pharmaceutical, Ionis Pharmaceuticals, NorthSea Therapeutics, Rivus Pharmaceuticals, Hanmi Pharmaceutical, Hepagene Therapeutics, HighTide Biopharma, Akero Therapeutics, Merck Sharp & Dohme LLC, Cascade Pharmaceuticals, Hepion Pharmaceuticals, Chipscreen Biosciences, Boston Pharmaceuticals, Bristol-Myers Squibb, Sunshine Lake Pharma, GSK plc., Future Medicine, Gilead Sciences, ENYO Pharma, Histogen, and others. Key Nonalcoholic Steatohepatitis Pipeline Therapies: TERN-101, SNP-610, LJN452(tropifexor + licogliflozin), PXL065, ALS-L1023, PF-06865571 + PF-05221304, PF-06835919, PF-06865571, ORMD-0801, Norucholic acid, NNC0194-0499, MN-001, MK-3655, MET642, MET409, LPCN 1144, LIK066, Leronlimab, ALN-HSD, MT-3995, CM101, Leu-Mit-Sil (NS-0200), IN-A010, Efruxifermin (EFX), Efinopegdutide, EDP-305, JKB-122, CS0159 (Linafexor), CRV431, Chiglitazar sodium, BOS-580, BMS-986263, HEC96719, GSK4532990, FM101, Firsocostat, EPY001a, Emricasan, BMS-986036, BIO89-100, BI 456906, BFKB8488A, AXA1125, ASC 41, GS-9674 (Cilofexor), ZSP1601, and others. Dive deep into rich insights for nonalcoholic steatohepatitis research; visit @ NASH Treatment Pipeline Table of Contents For further information on the most promising nash drugs, reach out @ NASH Medication Pipeline Related Reports Nonalcoholic Steatohepatitis Epidemiology Nonalcoholic Steatohepatitis Epidemiology Forecast – 2032 report delivers an in-depth understanding of the disease, historical, and forecasted nonalcoholic steatohepatitis epidemiology in the 7MM. Nonalcoholic Steatohepatitis Market Nonalcoholic Steatohepatitis Market Insight, Epidemiology, and Market Forecast – 2032 report delivers an in-depth understanding of the market trends, market drivers, market barriers, and key nonalcoholic steatohepatitis companies, including Boehringer Ingelheim, Oramed Pharmaceuticals, ENYO Pharma, Terns Pharmaceuticals, Cirius Therapeutics, among others. Non-Alcoholic Fatty Liver Disease Market Non-Alcoholic Fatty Liver Disease Market Insights, Epidemiology, and Market Forecast – 2032 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key non-alcoholic fatty liver disease companies including AstraZeneca, Novartis, Pfizer, Roche, among others. Non-Alcoholic Fatty Liver Disease Pipeline Non-Alcoholic Fatty Liver Disease Pipeline Insight – 2022 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key advanced non-alcoholic fatty liver disease companies, including AstraZeneca, Novartis, Pfizer, Roche, among others. Non-Alcoholic Fatty Liver Disease Epidemiology Non-Alcoholic Fatty Liver Disease Epidemiology Forecast – 2032 report delivers an in-depth understanding of the disease, historical, and forecasted non-alcoholic fatty liver disease epidemiology in the 7MM. Other Trending Reports Alcohol Use Disorder Market | Liver Cancer Market | Alcoholic Hepatitis - Market | Acute Liver Failure - Market | Liver Angiosarcoma - Market | Liver Cirrhosis - Market | Chronic Liver Disease - Market | Advanced Liver Cancer - Market | Acute On Chronic Liver Failure (ACLF) Market Related Healthcare Services Healthcare Business Consulting Healthcare Competitive Intelligence Services Healthcare Asset Prioritization Services About DelveInsight DelveInsight is a leading Business Consultant and Market Research firm focused exclusively on life sciences. Connect with us at LinkedIn Contact Us Shruti Thakur [email protected] +1(919)321-6187 Logo: SOURCE DelveInsight Business Research LLP

临床2期引进/卖出快速通道

2022-07-01

·CPhI制药在线

新药 | 正式上市！非奈利酮拉动糖尿病肾病靶向药物“三驾马车”

点击关注，星标CPhI制药在线近日，非奈利酮（finerenone，图一）被我国国家药品监督管理局正式批准上市，用于2型糖尿病相关的慢性肾脏病成人患者的治疗。此前，非奈利酮（finerenone）在2021年已经被提前列入我国糖尿病肾病（DKD）诊疗指南，与RASi和SGLT-2i一同成为糖尿病肾病（DKD）治疗的"三驾马车"。此次正式上市，意味着非奈利酮这驾"马车"在我国正式启动。图一非奈利酮（finerenone）结构式一．关于糖尿病肾病（diabetic kidney disease，DKD）非奈利酮的适应症为糖尿病肾病，该疾病是一种由糖尿病引起的慢性肾病，发病机制复杂，临床表现为持续性白蛋白尿排泄升高、肾小球滤过率进行性下降，最终可发展为终末期肾脏疾病。糖尿病肾病是引起终末期肾脏疾病的主要原因。糖尿病肾病患者的主要死因是心血管并发症，研究显示，糖尿病肾病患者合并心血管疾病的死亡风险是单纯糖尿病患者的3倍，是糖尿病肾病患者的2倍。由此，《KDIGO临床实践指南：慢性肾脏疾病患者的糖尿病管理》和中华医学会制订《糖尿病肾脏疾病临床诊疗中国指南》均强调在糖尿病肾病的治疗过程中要兼顾延缓肾脏疾病进展和降低心血管并发症风险。二．关于盐皮质激素受体拮抗剂（MRA）非奈利酮属于盐皮质激素受体拮抗剂。盐皮质激素受体拮抗剂主要分为甾体和非甾体两类。甾体类代表药物为第一代拮抗剂螺内酯，以及第二代拮抗剂依普利酮。螺内酯是非特异性盐皮质激素受体拮抗剂，对射血分数降低型心衰、难治性高血压、醛固酮增多症等疾病疗效显著，同时还可减少慢性肾病患者的蛋白尿，延缓慢性肾病进展。但由于螺内酯的选择性低，存在抗雄激素和孕激素相关副作用。相比而言，第二代盐皮质激素受体拮抗剂--依普利酮的选择性高，不良反应也大大降低，但其阻断盐皮质激素受体的作用低于螺内酯40倍。第三代盐皮质激素受体拮抗剂（包括非奈利酮、埃沙西林酮、阿帕利酮等）正是在第一代和第二代拮抗剂存在相应不足的大背景下产生。他们具有选择性高于螺内酯，而抗盐皮质激素受体的作用高于依普利酮的特点。因此，第三代盐皮质激素受体拮抗剂的临床应用前景被普遍看好。三．关于非奈利酮（Finerenone，Kerendia）非奈利酮是拜耳（Bayer）公司旗下一款"first-in-class"非甾体选择性盐皮质激素受体拮抗剂，2021年7月，美国食品药品管理局（FDA）批准非奈利酮在美国上市，用于治疗伴有慢性肾病（CKD）的Ⅱ型糖尿病患者。非奈利酮的Ⅲ期临床试验（FIDELIO-DKD）证实非奈利酮可为Ⅱ型糖尿病肾病患者带来心、肾双重获益，且具有良好的安全性。基于此，我国在2021年发布的《糖尿病肾脏疾病临床诊疗中国指南》中已推荐非奈利酮作为糖尿病肾病患者降低尿白蛋白以及合并心血管病并发症的治疗药物。这是该指南继肾素-血管紧张素系统阻断剂（renin-angiotensin system inhibitor，RASi）和钠-葡萄糖协同转运蛋白2抑制剂（sodium glucose cotransporter 2 inhibitor，SGLT2i）之后的推荐的糖尿病肾病治疗的最新药物。四．非奈利酮的合成图二非奈利酮（Finerenone）专利合成路线非奈利酮（Finerenone）的专利合成路线如图二所示，该工艺以4-溴-2-羟基苯甲酸为起始原料，经醚化-酯化反应、Red-Al还原反应得到4-溴-2-甲氧基苯甲醛；再经过Ullman氰化反应、Knoevenagel缩合反应，得到Z-型及E-型不饱和酰胺；该酰胺与4-氨基-5-甲基吡啶-2-酮环合构建1，4-二氢吡啶结构，然后经O-烷基化反应，得到非奈利酮（Finerenone）的外消旋体；非奈利酮（Finerenone）消旋体经动力学拆分，得到4S-型光学异构体--非奈利酮（Finerenone）。参考资料： 1. 程宽.非奈利酮的研究应用新进展[J].中国临床药理学与治疗学, 2022, 27(04): 450-456. 2. 万瑾瑾,刁倩,徐菲,陶泽颖,敖检根,林环玉,张卫芳.治疗糖尿病肾病的新型醛固酮受体拮抗剂--非奈利酮[J/OL].医药导报: 1-12 [2022-07-01]. http://kns.cnki.net/kcms/detail/42.1293.R.20220615.1838.002.html. 3. 丁雪婷,许佑君.非奈利酮(Finerenone,Kerendia)[J].中国药物化学杂志,2022,32(05):418. 4. 米未,马鑫,金玉洁.非甾体类盐皮质激素受体拮抗剂finerenone[J].现代药物与临床,2016,31(01):111-115. 作者简介：云天，药物化学博士，主要从事小分子药物研究，尤其擅长小分子药物的合成工艺及后期药物开发研究，已完成多个抗癌药物分子的合成和活性评估。扫码领取小程序福利速来投稿参与金笔奖征文活动！来源：CPhI制药在线声明：本文仅代表作者观点，并不代表制药在线立场。本网站内容仅出于传递更多信息之目的。如需转载，请务必注明文章来源和作者。投稿邮箱：Kelly.Xiao@imsinoexpo.com▼更多制药资讯，请关注CPhI制药在线▼点击阅读原文，进入智药研习社~

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100 项与阿帕利酮相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	阿帕利酮	-	DB15024

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
非酒精性脂肪性肝炎	临床2期	日本	Mitsubishi Tanabe Pharma Corp.	2016-09-01
糖尿病肾病	临床2期	日本	Mitsubishi Tanabe Pharma Corp.	2015-07-01
白蛋白尿	临床2期	保加利亚	Mitsubishi Tanabe Pharma Corp.	2012-11-01
白蛋白尿	临床2期	匈牙利	Mitsubishi Tanabe Pharma Corp.	2012-11-01
白蛋白尿	临床2期	立陶宛	Mitsubishi Tanabe Pharma Corp.	2012-11-01
白蛋白尿	临床2期	罗马尼亚	Mitsubishi Tanabe Pharma Corp.	2012-11-01
白蛋白尿	临床2期	斯洛伐克	Mitsubishi Tanabe Pharma Corp.	2012-11-01
2型糖尿病肾脏病	临床2期	保加利亚	Mitsubishi Tanabe Pharma Corp.	2012-11-01
2型糖尿病肾脏病	临床2期	匈牙利	Mitsubishi Tanabe Pharma Corp.	2012-11-01
2型糖尿病肾脏病	临床2期	立陶宛	Mitsubishi Tanabe Pharma Corp.	2012-11-01

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT02923154 (Pubmed) 人工标引	临床2期	非酒精性脂肪性肝炎	48	apararenone	鬱鏇網繭鏇鹽餘築積窪(襯範廠憲醖願餘齋淵夢) = 遞繭獵鑰壓獵簾製範範範繭構憲鏇艱製積蓋鹹 (衊窪觸範簾夢網獵遞觸 ) 更多	积极	2021-09-01
				Placebo	鬱鏇網繭鏇鹽餘築積窪(襯範廠憲醖願餘齋淵夢) = 壓醖觸艱夢窪壓鏇範繭範繭構憲鏇艱製積蓋鹹 (衊窪觸範簾夢網獵遞觸 ) 更多
NCT02676401 \| NCT02517320 (Pubmed \| Clin Exp Nephrol)	临床2期	糖尿病肾病	73	Apararenone 2.5 mg	積衊襯餘鏇醖簾繭餘顧(壓醖鏇繭齋衊廠構選繭) = 鬱鬱遞遞窪簾鹽廠襯窪艱醖構顧糧鹽窪簾範遞 (廠構鏇蓋餘鑰鑰願範範 )	-	2021-02-01
				Apararenone 5 mg	積衊襯餘鏇醖簾繭餘顧(壓醖鏇繭齋衊廠構選繭) = 築鬱網構齋醖選憲糧範艱醖構顧糧鹽窪簾範遞 (廠構鏇蓋餘鑰鑰願範範 )