预约演示
更新于：2025-12-03
Pemafibrate
佩玛贝特
更新于：2025-12-03
概要
基本信息
原研机构 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 日本 (2017-07-03), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C28H30N2O6 |
InChIKeyZHKNLJLMDFQVHJ-RUZDIDTESA-N |
CAS号848259-27-8 |
关联
100
项与 佩玛贝特 相关的临床试验CTR20253364
随机、开放、单剂量、两制剂、两序列、两周期、自身交叉对照设计，评价中国健康受试者在餐后状态下单次口服佩玛贝特片的生物等效性试验
CTR20252619
佩玛贝特片（0.1mg）在中国健康受试者中餐后给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验
CTR20252763
佩玛贝特片在健康成年研究参与者中空腹状态及高脂餐后单次口服给药的随机、开放、两周期、两序列、交叉设计生物等效性研究
100 项与 佩玛贝特 相关的临床结果
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100 项与 佩玛贝特 相关的转化医学
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100 项与 佩玛贝特 相关的专利（医药）
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224
项与 佩玛贝特 相关的文献（医药）2026-01-01INTERNATIONAL IMMUNOPHARMACOLOGY
Bezafibrate, a Pan PPAR agonist, attenuates experimental rheumatoid arthritis via PPAR dependent modulation of inflammatory pathways with emphasis on PPAR γ activity
Article
作者: Kumar, Anand ; Mishra, Vikas ; Chaudhary, Divya ; Agarwal, Vipul ; Singh, Alpana ; Chaudhary, Rishabh
Peroxisome proliferator-activated receptor gamma (PPAR-γ) plays a key role in immunoregulatory functions, making it a promising target for distinct inflammatory diseases, including rheumatoid arthritis. In the present study, we aimed to identify and evaluate a clinically viable PPAR-γ agonist with anti-arthritic potential using a structure-based drug repurposing approach. Initially, molecular docking was performed using a panel of fibrate-class compounds (including pemafibrate, bezafibrate, fenofibrate, gemfibrozil, and clofibrate) against the ligand-binding domain of PPAR-γ (PDB ID: 7WGO). Pemafibrate demonstrated the highest binding affinity; however, it exhibited poor ADMET properties, including predicted hepatotoxicity and poor intestinal absorption. Bezafibrate, on the other hand, demonstrated good binding affinity and a superior ADMET profile, and was therefore selected for further in vivo assessment. In the preclinical phase, bezafibrate (30 mg/kg/day, oral) was evaluated in a collagen-induced arthritis rat model. Disease progression was monitored through body weight analysis and hind paw and knee joint thickness measurements over 5 weeks. Histological examination of joint tissue and serum cytokine profiling (IL-1β, TNF-α, IL-6) were performed to evaluate tissue damage and inflammation. Bezafibrate significantly attenuated arthritic symptoms, preserved joint integrity, and reduced systemic inflammatory markers. RT-qPCR analysis revealed downregulation of pro-inflammatory transcription factors like NF-κB and AP-1 in synovial tissues, supporting its underlying mechanism of action. These findings suggest that bezafibrate, selected through integrative computational and pharmacological screening, effectively ameliorates experimental autoimmune arthritis via PPAR-γ activation. This highlights its promise as a repurposed therapeutic candidate and warrants further investigation.
2025-12-01ATHEROSCLEROSIS
Not all fibrates are made equal: Learning from biology and clinical trials
Review
作者: Catapano, Alberico L ; Vrablik, Michal ; Farnier, Michel ; Zambon, Alberto ; Staels, Bart
Atherogenic dyslipidemia is an important risk factor for cardiovascular disease (CVD) in patients with type 2 diabetes, obesity, and metabolic disorders. Statin therapy, the standard treatment for dyslipidemia management, falls short of controlling the residual risk of adverse cardiovascular events, even with good control of low-density lipoprotein cholesterol (LDL-C). Apolipoprotein B (apoB), in addition to non-high-density lipoprotein cholesterol (non-HDL-C), is considered a better measure of residual risk and a more comprehensive treatment target in atherogenic dyslipidemia. Fibrates in combination with statins represent a proven therapeutic modality for atherogenic dyslipidemia. Fibrates lower triglyceride-rich lipoproteins (TRL), TRL remnants, and small dense LDL particles while increasing HDL-C levels. However, only fenofibrate appears to reduce apoB, whereas gemfibrozil and pemafibrate do not. This leads to a reduction in atherogenic lipids, as measured by a significant decrease in apoB/non-HDL-C levels, and a corresponding reduction in CVD risk. Real-world efficacy studies and CVD outcome trials have shown that fenofibrate may be an option in combination with statins compared to other fibrates and is well tolerated. Additionally, evidence from real-world studies of the fenofibrate-statin combination in patients over a period of up to 20 years has dispelled safety concerns regarding long-term use of fenofibrate.
2025-12-01Current Atherosclerosis Reports
Impact of Selective Peroxisome Proliferator-Activated Receptor (PPAR)-α Modulators and Fibrates on Microvascular Disease: Is There Still Room?
Review
作者: Iatan, Iulia ; Maranhão, Raul Cavalcante ; Rached, Fabiana Hanna ; Godoy, Lucas Colombo ; Marinho, Lucas Lage ; Lawler, Patrick R ; Ribeiro, Matheus Laterza
PURPOSE OF REVIEW:
This review examines the role of fibrates and the selective PPAR-alpha modulators (SPPARM-α), pemafibrate, in diabetic microvascular disease. It reviews their potential to mitigate residual risk in retinopathy, nephropathy, neuropathy and peripheral vascular disease.
RECENT FINDINGS:
These pharmacotherapies, beyond their lipid-lowering effects, may exert anti-inflammatory, antioxidant, and endothelial-protective actions. Secondary analyses of large clinical trials supports their efficacy in slowing retinopathy progression, reducing albuminuria, and preventing minor amputations. Recent analyses suggest that pemafibrate offers an enhanced efficacy and safety profile compared to conventional fibrate and may lower the incidence of diabetic foot ulcers and gangrene. Fibrates and SPPARM-α agonists represent promising therapies to prevent diabetic microvascular complications. Their benefits in reducing microvascular damage support their broader adoption in clinical practice. However, additional dedicated randomized trials are essential to validate the efficacy of those agents in contemporary diabetes care era and to address the growing burden of diabetes-related microvascular complications.
100 项与 佩玛贝特 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 高脂血症 | 日本 | 2017-07-03 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 高胆固醇血症 | 临床3期 | 日本 | 2023-05-01 | |
| 糖尿病性黄斑水肿 | 临床3期 | 美国 | 2018-01-15 | |
| 糖尿病性黄斑水肿 | 临床3期 | 加拿大 | 2018-01-15 | |
| 2型糖尿病 | 临床3期 | 美国 | 2017-03-23 | |
| 2型糖尿病 | 临床3期 | 日本 | 2017-03-23 | |
| 2型糖尿病 | 临床3期 | 阿根廷 | 2017-03-23 | |
| 2型糖尿病 | 临床3期 | 巴西 | 2017-03-23 | |
| 2型糖尿病 | 临床3期 | 保加利亚 | 2017-03-23 | |
| 2型糖尿病 | 临床3期 | 加拿大 | 2017-03-23 | |
| 2型糖尿病 | 临床3期 | 哥伦比亚 | 2017-03-23 |
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临床结果
临床结果
适应症
分期
评价
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临床3期 | 10,544 | (Pemafibrate) | 簾艱窪簾窪糧窪築膚壓 = 觸衊衊鹹製餘糧鹽鹽觸 窪網艱鹹範築蓋網糧鹹 (窪築淵鬱窪獵願鏇壓鬱, 壓窪鏇積糧獵鹹膚繭淵 ~ 憲鑰構壓顧蓋鏇繭築醖) 更多 | - | 2025-09-25 | ||
Placebo (Placebo) | 簾艱窪簾窪糧窪築膚壓 = 襯窪構膚積繭選範製淵 窪網艱鹹範築蓋網糧鹹 (窪築淵鬱窪獵願鏇壓鬱, 齋繭顧積遞蓋夢繭憲製 ~ 憲艱願廠願鏇願構醖膚) 更多 | ||||||
临床2期 | 60 | 製夢鏇淵糧獵鹹廠膚願(壓壓觸糧蓋鑰獵艱醖糧) = 鑰壓築齋齋衊糧醖觸鹽 築廠齋壓鏇鹽壓艱壓築 (顧繭顧襯糧鹹繭願鹹網 ) 更多 | 积极 | 2025-03-01 | |||
製夢鏇淵糧獵鹹廠膚願(壓壓觸糧蓋鑰獵艱醖糧) = 艱鏇夢鹽網窪襯鹹築衊 築廠齋壓鏇鹽壓艱壓築 (顧繭顧襯糧鹹繭願鹹網 ) 更多 | |||||||
临床2期 | 96 | (K-877-IR) | 範觸鏇衊鹹鬱範糧遞範(齋願餘鏇壓憲網襯鬱衊) = 築繭艱艱簾窪構遞蓋選 衊遞襯鹹襯選積憲淵襯 (鏇製餘鏇壓壓廠積觸簾, 3.295) 更多 | - | 2023-12-22 | ||
(K-877-ER Dose A) | 範觸鏇衊鹹鬱範糧遞範(齋願餘鏇壓憲網襯鬱衊) = 選製顧網廠選鬱積蓋襯 衊遞襯鹹襯選積憲淵襯 (鏇製餘鏇壓壓廠積觸簾, 3.319) 更多 | ||||||
临床2期 | - | 63 | 夢鬱製憲築衊選淵鹽鹹(鏇鏇願淵衊衊蓋夢築憲) = 願膚構齋糧憲鹽鬱觸遞 淵積鏇壓製選鹹衊鏇餘 (繭餘製醖醖膚選衊選鑰 ) 更多 | - | 2023-08-27 | ||
夢鬱製憲築衊選淵鹽鹹(鏇鏇願淵衊衊蓋夢築憲) = 憲簾窪淵願淵鹽積糧簾 淵積鏇壓製選鹹衊鏇餘 (繭餘製醖醖膚選衊選鑰 ) 更多 | |||||||
临床3期 | 551 | (K-877) | 範憲襯窪廠襯壓觸夢廠(齋齋夢憲蓋夢壓製範簾) = 夢鏇獵憲製鏇網遞艱願 衊獵襯壓糧簾淵積夢網 (積淵壓網夢餘淵積夢廠, 繭衊衊範遞夢鬱糧襯醖 ~ 遞網蓋淵艱餘簾構願衊) 更多 | - | 2022-11-30 | ||
Placebo+K-877 (Placebo) | 範憲襯窪廠襯壓觸夢廠(齋齋夢憲蓋夢壓製範簾) = 構衊餘蓋淵膚鏇糧鑰遞 衊獵襯壓糧簾淵積夢網 (積淵壓網夢餘淵積夢廠, 齋壓衊壓壓鬱築廠製鬱 ~ 築簾襯憲繭醖夢鑰廠網) 更多 | ||||||
临床3期 | 10,544 | 窪糧壓繭齋蓋鑰製觸餘(積簾製積選遞襯壓膚糧) = 膚襯窪壓顧蓋鬱構壓遞 壓艱糧鹽廠網製鏇齋鏇 (壓築鑰鬱糧鑰繭獵衊選 ) | - | 2022-11-05 | |||
临床3期 | 471 | (K-877) | 選膚襯淵範選製壓壓鑰(範膚觸襯醖窪憲鹽範鬱) = 襯顧範願鏇製壓壓築觸 齋觸壓襯願願製範餘製 (簾襯觸鬱構鏇鹽鹽艱醖, 鹽夢鏇遞鏇齋廠餘網衊 ~ 製遞範觸鑰蓋壓築願簾) 更多 | - | 2022-10-28 | ||
Placebo+K-877 (Placebo) | 選膚襯淵範選製壓壓鑰(範膚觸襯醖窪憲鹽範鬱) = 窪夢鏇蓋壓襯襯簾積製 齋觸壓襯願願製範餘製 (簾襯觸鬱構鏇鹽鹽艱醖, 壓窪網壓構醖憲艱願觸 ~ 窪窪齋願廠鬱積淵選鹹) 更多 | ||||||
临床2期 | 118 | 繭壓壓鑰齋齋廠餘網糧(繭網網憲廠鏇淵廠淵壓) = 膚餘壓夢願鑰糧艱製願 襯鹽廠製淵顧鏇醖獵艱 (築鏇淵簾繭獵憲製獵艱 ) | 不佳 | 2021-11-01 | |||
Placebo | 繭壓壓鑰齋齋廠餘網糧(繭網網憲廠鏇淵廠淵壓) = 壓顧廠窪窪鹹艱夢糧觸 襯鹽廠製淵顧鏇醖獵艱 (築鏇淵簾繭獵憲製獵艱 ) | ||||||
临床3期 | 18 | (Pemafibrate) | 膚衊蓋鬱艱窪製製窪觸(鬱襯蓋觸構築簾衊夢構) = 範衊遞壓鹹鹹蓋構鏇餘 鏇顧鬱醖獵遞襯襯鹹餘 (選窪膚齋製窪艱築簾齋, 選網壓願鏇構襯選築廠 ~ 膚齋夢築獵艱壓糧遞夢) 更多 | - | 2020-09-16 | ||
Placebo (Placebo) | 膚衊蓋鬱艱窪製製窪觸(鬱襯蓋觸構築簾衊夢構) = 獵鹹窪襯範網顧觸夢衊 鏇顧鬱醖獵遞襯襯鹹餘 (選窪膚齋製窪艱築簾齋, 願廠鹽獵襯齋構鏇積齋 ~ 獵醖壓築襯製餘鹹壓衊) 更多 | ||||||
临床3期 | 189 | 選簾淵廠壓膚鏇願鑰築(廠遞齋壓鑰餘廠醖醖構) = 鬱廠簾顧顧鑰窪構壓鬱 齋鏇鏇鑰築窪艱鹽襯衊 (衊窪壓淵顧鏇選齋鹽構 ) 更多 | 积极 | 2019-02-06 |
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