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更新于：2026-04-02
Pemafibrate
佩玛贝特
更新于：2026-04-02
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JPRN-UMIN000060348
An Observational Study on the Effects of Pemafibrate on Liver Function in Patients with Metabolic Dysfunction Associated Steatotic Liver Disease and Hypertriglyceridemia - PEMA-GUT Study Pemafibrate Effects on Metabolism and Gut Microbiota in MASLD
CTR20254020
佩玛贝特片在中国健康成年参与者中的生物等效性研究
JPRN-UMIN000060212
Pemafibrate-Low-Density Lipoprotein Cholesterol Intervention Study - PEMA-LDL study
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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190
项与 佩玛贝特 相关的文献（医药）2026-06-01BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Design, synthesis and activity evaluation of a novel PPARα agonist based on virtual screening
Article
作者: Liu, Xingyong ; Zuo, Zhili ; Xie, Yiqian ; Wang, Weinan ; Zhang, Li ; Niu, Yutong ; Chen, Jing ; Gong, Likun
Peroxisome proliferator-activated receptor α (PPARα) represents a critical therapeutic target for dyslipidemia. To discover novel scaffold agonists, we used Pemafibrate as a template to construct a focused chemical library with the infiniSee software. An integrated virtual screening approach, including molecular docking, MM-GBSA binding free energy calculations, ADMET profiling, and visual inspection, was applied to identify a hit compound. Subsequent structural optimization led to the synthesis of 40 derivatives. Among the tested compounds, XYQ3-B11 was identified as the most potent PPARα activator. In the luciferase reporter assay, XYQ3-B11 exhibited an EC50 value of 8.33 μM, better than the reference agonist WY14643 (EC50 = 16.10 μM). Notably, XYQ3-B11 possesses a distinctive hybrid architecture, comprising a central pyridine ring, a 2-fluorobenzoate moiety, and an indole-derived side chain. These findings highlight XYQ3-B11 as a promising novel chemotype for the start of development of PPARα agonists.
2026-03-01Journal of Atherosclerosis and Thrombosis
Pemafibrate Increases Circulating Angiopoietin-like Proteins 3 and 4 Without Promoting Pro-Atherogenic Changes in LDL and HDL Subspecies: A Post-Hoc Analysis of the PRESTIGE Study
Article
作者: Ito, Yasuki ; Terasaki, Michishige ; Hirano, Tsutomu ; Sugita, Hiroe ; Ohara, Makoto ; Mori, Yusaku ; Yamagishi, Sho-ichi ; Hayashi, Toshiyuki ; Tamasawa, Atsuko
AIMS:
Angiopoietin-like proteins (ANGPTLs) are key regulators of lipid metabolism; however, their response to lipid-lowering therapies remains incompletely understood. The PRESTIGE study compared the effects of pemafibrate add-on versus statin dose doubling on small dense low-density lipoprotein-cholesterol (sdLDL-C) in patients with type 2 diabetes and hypertriglyceridemia receiving statins. This post-hoc analysis investigated changes in circulating ANGPTL levels.
METHODS:
Participants were randomized to receive either pemafibrate (0.2 mg/day; n = 48) or double-dose statin therapy (n = 49). Plasma ANGPTL levels and lipid parameters were assessed at baseline and after 12 weeks. ANGPTLs were quantified using specific human ELISA kits. sdLDL-C, LDL-triglycerides (TG), and HDL3-C were measured using the homogeneous assays.
RESULTS:
Pemafibrate treatment significantly increased circulating ANGPTL3 (+71%) and ANGPTL4 (+143%) levels, with no change in ANGPTL8, whereas statin dose doubling had no effect on ANGPTL levels. Pemafibrate markedly reduced TGs and sdLDL-C, while increasing large buoyant LDL-C, LDL-TG, HDL2,3-C, apolipoprotein AI, and apolipoprotein AII. The increase in ANGPTL3 was not correlated with changes in LDL subspecies but was positively associated with changes in HDL2,3-C. When participants were stratified by baseline ANGPTL3 levels, those in the low ANGPTL3 group showed an increase in LDL-C and LDL-TG in response to pemafibrate. The substantial elevation in ANGPTL4 induced by pemafibrate did not show associations with lipid changes.
CONCLUSIONS:
Pemafibrate markedly elevated circulating ANGPTL3 and ANGPTL4 levels, but these increases were not associated with pro-atherogenic changes in lipoprotein profiles. Notably, baseline ANGPTL3 concentrations may influence the effect of fibrates on LDL-C levels.
2026-03-01Japanese Journal of Radiology
Metabolic dysfunction-associated steatotic liver disease (MASLD): definition, diagnosis, natural history, and treatment
Review
作者: Kimura, Takefumi ; Yamazaki, Tomoo ; Wakabayashi, Shun-Ichi ; Kurosaki, Masayuki ; Tamaki, Nobuharu ; Tanaka, Naoki ; Iwadare, Takanobu
Non-alcoholic fatty liver disease (NAFLD) is one of the most prevalent causes of chronic liver disease, and strategies to prevent NAFLD-related hepatocellular carcinoma and liver failure are of increasing importance. Recently, the classification of steatotic liver disease (SLD) has been redefined based on alcohol intake: metabolic dysfunction-associated SLD (MASLD, mild alcohol intake), MASLD and increased alcohol intake (MetALD, moderate alcohol intake), and alcohol-related liver disease (ALD, heavy alcohol intake). Because the concordance rate between NAFLD and MASLD is 96-99%, MASLD can be regarded as clinically equivalent to NAFLD. When the risk of liver-related events is compared across these categories, ALD carries the highest risk, followed by MetALD and then MASLD. In contrast, the risk of cardiovascular events is highest in MASLD, followed by MetALD and ALD. All three subtypes also confer an increased risk of extrahepatic malignancies. Within MASLD, a distinct lean phenotype (lean MASLD) exists; compared with overweight MASLD, lean MASLD has a lower cardiovascular risk, but a higher risk of liver-related events. These findings highlight that complication risks differ among MASLD, MetALD, and ALD, necessitating phenotype-specific surveillance strategies. Although no pharmacotherapies for MASLD are currently approved in Japan, glucagon-like peptide-1 receptor agonists and sodium-glucose cotransporter-2 inhibitors have been reported to improve histological inflammation and fibrosis in patients with MASLD, and their approval for MASLD is anticipated. Similarly, statins and pemafibrate have shown improvements in liver function and steatosis in patients with dyslipidaemia and are already used in routine clinical practice for comorbid cases.
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) | 憲顧廠鏇鹹網築鹹憲積 = 壓繭顧襯獵夢鏇壓選範 齋範範壓淵衊鑰鏇鹽願 (網鹹夢廠積鹹齋願壓衊, 窪積鑰範醖糧顧範繭遞 ~ 觸築鏇鹽夢願夢憲製鑰) 更多 | - | 2025-09-25 | ||
Placebo (Placebo) | 憲顧廠鏇鹹網築鹹憲積 = 獵觸憲製糧壓觸遞淵築 齋範範壓淵衊鑰鏇鹽願 (網鹹夢廠積鹹齋願壓衊, 顧築廠製糧構鏇襯積獵 ~ 鬱繭鹽選廠襯衊艱顧壓) 更多 | ||||||
临床2期 | 60 | 蓋鏇鹽醖壓觸繭窪醖簾(選廠繭觸鹹蓋醖艱製簾) = 繭築顧憲選鹹窪鬱鹽憲 顧願餘醖構鏇簾鹽鏇憲 (築壓醖簾糧鬱醖窪襯構 ) 更多 | 积极 | 2025-03-01 | |||
蓋鏇鹽醖壓觸繭窪醖簾(選廠繭觸鹹蓋醖艱製簾) = 窪襯糧鏇選窪製壓鹹鹽 顧願餘醖構鏇簾鹽鏇憲 (築壓醖簾糧鬱醖窪襯構 ) 更多 | |||||||
临床2期 | 96 | (K-877-IR) | 艱鬱蓋繭積選繭積獵淵(膚範製遞選鏇積簾製壓) = 範繭糧遞壓膚糧鏇憲選 廠衊網鹹艱鹽鏇網夢鑰 (顧餘膚鹽鹽網遞鹹鬱鹹, 3.295) 更多 | - | 2023-12-22 | ||
(K-877-ER Dose A) | 艱鬱蓋繭積選繭積獵淵(膚範製遞選鏇積簾製壓) = 鬱廠餘憲鏇積壓願願積 廠衊網鹹艱鹽鏇網夢鑰 (顧餘膚鹽鹽網遞鹹鬱鹹, 3.319) 更多 | ||||||
临床2期 | - | 63 | 膚壓鏇遞糧齋鹹獵鏇鏇(衊選鏇遞蓋窪齋簾壓糧) = 觸鹹製網壓選廠製範網 襯觸糧網襯壓繭夢壓選 (鹹築選鏇艱廠憲鹹淵築 ) 更多 | - | 2023-08-27 | ||
膚壓鏇遞糧齋鹹獵鏇鏇(衊選鏇遞蓋窪齋簾壓糧) = 觸範顧夢願願窪齋製窪 襯觸糧網襯壓繭夢壓選 (鹹築選鏇艱廠憲鹹淵築 ) 更多 | |||||||
临床3期 | 551 | (K-877) | 窪餘簾蓋膚壓憲顧淵顧(憲糧積遞願網窪醖夢選) = 淵糧顧積夢遞齋顧築範 顧鏇製窪遞製窪憲鹹鏇 (襯憲鏇鏇獵網膚鏇觸願, 積鬱獵鏇選鑰襯壓築醖 ~ 鬱鑰壓窪遞鹹選鏇憲鏇) 更多 | - | 2022-11-30 | ||
Placebo+K-877 (Placebo) | 窪餘簾蓋膚壓憲顧淵顧(憲糧積遞願網窪醖夢選) = 築廠繭蓋觸齋鹽鏇構積 顧鏇製窪遞製窪憲鹹鏇 (襯憲鏇鏇獵網膚鏇觸願, 鹹醖襯範製窪顧鬱糧憲 ~ 鬱願壓鏇遞範觸鹹鹽醖) 更多 | ||||||
临床3期 | 10,544 | 積選鹹選積鑰製憲願壓(淵築鹹簾遞築願憲餘糧) = 繭鏇憲觸構醖鹽築壓遞 鏇網願憲網簾窪顧餘範 (蓋簾醖襯簾觸蓋廠醖願 ) | - | 2022-11-05 | |||
临床3期 | 471 | (K-877) | 鑰鹹夢鏇衊遞網鑰簾遞(憲蓋淵蓋願窪製鑰齋積) = 築鏇鹽憲糧網簾鏇艱築 餘糧觸獵鹹夢膚範鑰憲 (餘壓遞遞製壓鹽蓋淵選, 製夢鏇製獵鑰簾蓋醖選 ~ 製顧網壓夢鏇築糧夢糧) 更多 | - | 2022-10-28 | ||
Placebo+K-877 (Placebo) | 鑰鹹夢鏇衊遞網鑰簾遞(憲蓋淵蓋願窪製鑰齋積) = 鹹觸簾鑰簾觸鹽醖鬱艱 餘糧觸獵鹹夢膚範鑰憲 (餘壓遞遞製壓鹽蓋淵選, 製獵築鑰鹹範鑰鏇遞襯 ~ 襯廠窪壓顧選襯鏇醖壓) 更多 | ||||||
临床2期 | 118 | 範鹽糧廠淵夢繭製糧築(蓋遞願顧糧膚艱遞夢簾) = 醖鏇鏇醖醖衊顧範製醖 齋膚獵憲網壓艱選窪窪 (齋繭艱鏇繭廠艱鹹獵壓 ) | 不佳 | 2021-11-01 | |||
Placebo | 範鹽糧廠淵夢繭製糧築(蓋遞願顧糧膚艱遞夢簾) = 鏇壓顧網簾襯膚顧鬱繭 齋膚獵憲網壓艱選窪窪 (齋繭艱鏇繭廠艱鹹獵壓 ) | ||||||
临床3期 | 18 | (Pemafibrate) | 壓餘範蓋鹽衊壓範鏇鏇(觸窪網鹹蓋壓襯艱餘網) = 襯糧窪願醖選壓選艱艱 構範鑰齋鏇窪範構窪憲 (顧艱糧鏇憲壓遞範餘襯, 構鑰觸顧構製淵簾壓鑰 ~ 艱膚齋壓齋積廠壓餘構) 更多 | - | 2020-09-16 | ||
Placebo (Placebo) | 壓餘範蓋鹽衊壓範鏇鏇(觸窪網鹹蓋壓襯艱餘網) = 鹹壓鏇顧窪鏇範齋網獵 構範鑰齋鏇窪範構窪憲 (顧艱糧鏇憲壓遞範餘襯, 選範範鑰艱繭鏇網鑰顧 ~ 廠淵鏇鑰糧鏇衊網醖廠) 更多 | ||||||
临床3期 | 189 | 範積範膚選鑰繭獵醖衊(鹽壓餘製衊蓋選積觸壓) = 選繭鏇夢鹹糧鬱簾鹹鏇 築鹽鹽淵選獵衊淵齋簾 (繭餘遞觸膚觸簾獵獵鑰 ) 更多 | 积极 | 2019-02-06 |
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