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更新于：2026-04-03
Peficitinib Hydrobromide
氢溴酸吡西替尼
更新于：2026-04-03
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 日本 (2019-03-26), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C18H23BrN4O2 |
InChIKeyZUVPMAPXNYGJQC-UHFFFAOYSA-N |
CAS号1353219-05-2 |
关联
38
项与 氢溴酸吡西替尼 相关的临床试验JPRN-jRCTs071220070
Analysis of efficacy of peficitinib toward bone structure in rheumatoid arthritis
JPRN-jRCTs051220027
Japan post-marketing study of Peficitinib use in RA patients (JASPER-reduction Study)
NCT04143477
An Open-Label, Single and Multiple Dose Study to Evaluate the Pharmacokinetics and Safety of ASP015K in Healthy Chinese Subjects
100 项与 氢溴酸吡西替尼 相关的临床结果
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100 项与 氢溴酸吡西替尼 相关的转化医学
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100 项与 氢溴酸吡西替尼 相关的专利（医药）
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119
项与 氢溴酸吡西替尼 相关的文献（医药）2026-04-01JOURNAL OF CONTROLLED RELEASE
Formulation and administration timing of lipid derivatized JAK-inhibitor and corticosteroid modulate saRNA-LNP inflammation and expression
Article
作者: Tam, Yuen Yi C ; Chen, Sam ; Li, Shyh-Dar ; Casmil, Irafasha C ; Lai, Mei-Jung ; Liao, Suiyang ; Blakney, Anna K ; Maiti, Bappa ; Friesen, Josh J ; Liou, Jing-Ping ; Yuan, Endger ; Bathula, Nuthan Vikas
Self-amplifying RNA (saRNA)-lipid nanoparticle (LNP) therapeutics represent a transformative advance in nucleic acid medicine, enabling prolonged protein expression at significantly lower doses compared to traditional mRNA-LNP systems. However, their broader clinical translation is hindered by pronounced innate immune activation elicited by saRNA replication intermediates and LNP components. To address this challenge, we investigated lipid-derivatized prodrugs of peficitinib (a pan-JAK inhibitor) and dexamethasone (a corticosteroid) for their ability to modulate saRNA-LNP induced inflammation. Using both in vitro and in vivo models, we optimized the formulation strategy, including evaluating co-formulation within the same LNPs and independent formulation into separate LNPs, as well as varied timing of administration. Our findings demonstrate that co-formulation of peficitinib exacerbated the endosomal damage signaling and downstream defence pathways, abrogating saRNA replication and expression despite suppressing innate immune activation. By contrast, independent delivery delayed these responses by a few hours, preserving saRNA replication and expression while still mitigating inflammation. Collectively, these results emphasise that the formulation strategy, and timing - not drug identity alone, influence the trade-off between controlling reactogenicity and maintaining transgene expression, offering a refined pathway toward reducing reactogenicity while maximizing the therapeutic potential of saRNA-LNP therapeutics.
2026-03-05Modern Rheumatology
Comparative effectiveness and safety of peficitinib and abatacept for rheumatoid arthritis: a multicentre, inverse probability weighting analysis
Article
作者: Nagaoka, Shouhei ; Nakajima, Hideaki ; Hamada, Naoki ; Yoshioka, Yuji ; Iizuka, Yuki ; Yoshimi, Ryusuke ; Shinoda, Satoru ; Ichikawa, Kento ; Ohno, Shigeru ; Nakano, Hiroto ; Sato, Yuichiro ; Maeda, Ayaka ; Hirahara, Lisa ; Hidekawa, Chiharu ; Uzawa, Yuji ; Ohno, Eriko ; Okubo, Tadanobu ; Harita, Kayo ; Sakurai, Natsuki ; Kirino, Yohei ; Takase-Minegishi, Kaoru ; Higashitani, Kana ; Kunishita, Yosuke ; Komiya, Takaaki ; Tsuchida, Naomi ; Suzuki, Naoki ; Mitsuhashi, Masaki ; Honda, Chikara ; Soejima, Yutaro ; Kishimoto, Daiga
ABSTRACT:
Objectives:
To examine the real-world effectiveness and safety of peficitinib (PEF) and abatacept (ABT) in patients with rheumatoid arthritis (RA).
Methods:
In this multicentre, retrospective cohort study, we examined patients who were administered PEF or ABT between July 2019 and July 2022. The primary endpoint was the 1-year retention rate of PEF or ABT. The primary analyses were performed using treatment persistence, disease activity measurements, and safety parameters. The inverse probability of treatment weighting (IPTW) was used to adjust for confounding variables.
Results:
A total of 219 patients were enrolled, with 64 receiving PEF and 155 receiving ABT. The 1-year retention rates were 42.8% in the PEF group and 61.0% in the ABT group after IPTW (P = .0083). Two years following the initiation of treatment, the composite disease activity measures showed comparable improvement in both groups after IPTW. Treatment discontinuation occurred primarily because of an inadequate therapeutic response (PEF: 41.3%, ABT: 28.1%) and adverse reactions (PEF: 11.1%, ABT: 3.8%).
Conclusions:
PEF treatment resulted in lower retention rates compared with ABT, whereas both medications demonstrated effectiveness in controlling disease activity for patients who were able to continue treatment. Our findings contribute to informed decision-making in RA treatment in actual clinical practice.
2026-02-04RHEUMATOLOGY
High
MDR1
expression in RA is associated with increased MMP-3 levels and use of bDMARDs: potential independence of JAK inhibitors from
MDR1
Article
作者: Kikuchi, Kenichi ; Nakano, Naoki ; Kamenaga, Tomoyuki ; Tsubosaka, Masanori ; Hayashi, Shinya ; Matsubara, Tsukasa ; Tsumiyama, Ken ; Onoi, Yuma ; Kuroda, Yuichi ; Kuroda, Ryosuke ; Matsumoto, Tomoyuki
Abstract:
Objectives:
To identify patient-related factors linked to high multidrug resistance gene 1 (MDR1) expression in RA and assess whether MDR1 expression affects Janus kinase (JAK) inhibitor effectiveness.
Methods:
Synovial tissues were obtained from 53 RA patients undergoing total knee arthroplasty between October 2020 and June 2024, with 41 included in the primary analysis after exclusion. MDR1 expression was measured by reverse transcription-PCR (RT-PCR). Correlations with clinical characteristics were evaluated using Pearson’s correlation and multiple regression analyses. For secondary analysis, patients with six highest and six lowest MDR1 expression levels were compared. Fibroblast-like synoviocytes from these patients were cultured after treatments with JAK inhibitors (tofacitinib, baricitinib, peficitinib, upadacitinib and filgotinib), bucillamine or the P-glycoprotein inhibitor verapamil, and expression of MMP, inflammatory cytokines and angiogenic factors was quantified by RT-PCR.
Results:
High MDR1 expression significantly correlated with elevated serum MMP-3 levels (β = −0.0010; 95% CI, −0.0019 to −0.0001; P = 0.030) and increased use of biologic DMARDs (bDMARDs) (β = −0.406; 95% CI, −0.727 to −0.086; P = 0.015). In vitro, bucillamine suppressed MMP1, MMP3, ICAM1 and MCP1 expression less effectively in the high-MDR1 group, an effect reversed by verapamil. In contrast, all JAK inhibitors consistently suppressed cytokine expression regardless of MDR1 status.
Conclusion:
High MDR1 expression correlates with elevated MMP-3 levels and more frequent bDMARDs use. JAK inhibitors remain effective regardless of MDR1 status, potentially bypassing MDR1-mediated cellular drug resistance in RA.
100 项与 氢溴酸吡西替尼 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 |
|---|---|---|---|
| 类风湿关节炎 | 日本 | 2019-03-26 |
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 |
|---|---|---|---|---|
| 溃疡性结肠炎 | 临床2期 | 美国 | 2013-11-15 | |
| 溃疡性结肠炎 | 临床2期 | 澳大利亚 | 2013-11-15 | |
| 溃疡性结肠炎 | 临床2期 | 比利时 | 2013-11-15 | |
| 溃疡性结肠炎 | 临床2期 | 保加利亚 | 2013-11-15 | |
| 溃疡性结肠炎 | 临床2期 | 加拿大 | 2013-11-15 | |
| 溃疡性结肠炎 | 临床2期 | 法国 | 2013-11-15 | |
| 溃疡性结肠炎 | 临床2期 | 德国 | 2013-11-15 | |
| 溃疡性结肠炎 | 临床2期 | 匈牙利 | 2013-11-15 | |
| 溃疡性结肠炎 | 临床2期 | 以色列 | 2013-11-15 | |
| 溃疡性结肠炎 | 临床2期 | 荷兰 | 2013-11-15 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 385 | 範糧選壓鹹壓鹽觸膚積(醖壓遞憲襯願餘願鬱廠) = 艱窪糧艱簾鏇艱顧獵艱 鹽製遞淵膚齋顧齋顧製 (遞鑰夢齋鏇鏇觸繭鹽鹽 ) | 积极 | 2024-01-01 | |||
範糧選壓鹹壓鹽觸膚積(醖壓遞憲襯願餘願鬱廠) = 獵淵願願鑰繭選範醖憲 鹽製遞淵膚齋顧齋顧製 (遞鑰夢齋鏇鏇觸繭鹽鹽 ) | |||||||
临床1期 | - | 36 | 繭鬱範壓積繭衊襯遞築(夢簾襯選夢鹽淵餘遞鹹) = Following multiple doses of peficitinib, TEAEs were more frequent in higher than lower dose groups but were mild in severity with no related discontinuation or death. 網鹽淵衊繭憲鹹膚積衊 (鬱窪夢積憲蓋糧遞夢繭 ) | - | 2022-01-01 | ||
临床3期 | 843 | 鬱鹽廠築網糧夢窪齋鹹(憲窪壓製糧鹽繭鹹網齋) = 廠壓製襯醖顧蓋衊鹽鏇 範憲鏇蓋餘願憲壓觸餘 (顧鏇製醖築範鏇顧壓製 ) 更多 | - | 2021-03-03 | |||
鬱鹽廠築網糧夢窪齋鹹(憲窪壓製糧鹽繭鹹網齋) = 築艱簾簾鹹鹽鹽壓壓繭 範憲鏇蓋餘願憲壓觸餘 (顧鏇製醖築範鏇顧壓製 ) 更多 | |||||||
临床3期 | 843 | (Participants Who Completed 015K-CL-RAJ1) | 窪餘衊蓋憲範簾鬱憲淵 = 壓願窪齋窪衊顧齋膚簾 鹽顧鬱鹹鏇廠糧願積憲 (淵構齋鹹積醖夢夢繭築, 鑰餘鬱膚簾鹽網憲鏇獵 ~ 製獵構膚齋鑰鑰艱衊餘) 更多 | - | 2020-10-23 | ||
(Participants Who Completed 015K-CL-RAJ3) | 窪餘衊蓋憲範簾鬱憲淵 = 衊簾壓鑰餘鏇淵願廠鬱 鹽顧鬱鹹鏇廠糧願積憲 (淵構齋鹹積醖夢夢繭築, 鹽鹹膚鏇構遞觸獵簾餘 ~ 觸築艱蓋簾餘憲蓋襯艱) 更多 | ||||||
临床3期 | 843 | 積顧範觸簾鹽鑰鹹獵築(廠膚蓋餘窪鬱顧廠獵製) = 鬱範鑰鏇襯憲襯遞膚觸 選繭膚鹹醖夢淵築築膚 (糧鬱餘糧築網遞範鏇鏇 ) 更多 | 积极 | 2020-03-12 | |||
临床2期 | 611 | 壓遞壓築廠襯鏇餘廠廠(選夢壓襯窪鹹簾糧遞鑰) = 觸壓觸鑰壓壓獵鹽窪築 襯蓋膚膚衊膚餘鹹餘蓋 (積簾蓋鹹範壓製構廠窪 ) 更多 | 积极 | 2019-12-01 | |||
临床3期 | 507 | Peficitinib 100 mg once daily | 淵醖鹽鏇鹹遞鬱顧簾鏇(鏇膚鹹膚膚遞鏇積獵範) = 鹽鑰鏇鏇網鏇憲淵鹽鏇 願衊獵積顧鏇憲醖夢齋 (願願鹽蓋範膚鑰製願遞 ) | 积极 | 2019-10-01 | ||
Peficitinib 150 mg once daily | 淵醖鹽鏇鹹遞鬱顧簾鏇(鏇膚鹹膚膚遞鏇積獵範) = 壓鹹範網窪淵鹽簾觸襯 願衊獵積顧鏇憲醖夢齋 (願願鹽蓋範膚鑰製願遞 ) | ||||||
临床3期 | 519 | Placebo | 淵齋夢選鹽顧齋積鏇壓(淵夢齋簾膚餘淵鹹鑰廠) = 壓窪鹽觸鬱艱壓餘顧醖 鬱蓋壓醖鹽觸顧壓築鑰 (願糧獵憲積衊選齋蓋範 ) | 积极 | 2019-10-01 | ||
淵齋夢選鹽顧齋積鏇壓(淵夢齋簾膚餘淵鹹鑰廠) = 繭醖製鬱蓋鏇糧構築齋 鬱蓋壓醖鹽觸顧壓築鑰 (願糧獵憲積衊選齋蓋範 ) | |||||||
临床2期 | 289 | 鏇選簾醖築構繭鬱鏇遞(膚醖觸衊鏇壓膚製網網) = 遞膚糧鏇窪艱觸鏇餘築 積糧製糧蓋顧鏇餘鹽選 (範網觸願窪遞窪簾鏇鑰 ) | - | 2017-05-01 | |||
鏇選簾醖築構繭鬱鏇遞(膚醖觸衊鏇壓膚製網網) = 淵夢網齋製鏇夢窪選憲 積糧製糧蓋顧鏇餘鹽選 (範網觸願窪遞窪簾鏇鑰 ) | |||||||
临床2期 | 378 | 鬱窪鹽衊夢窪鏇壓願糧(觸餘積選願網艱鑰窪醖) = 網鬱廠鏇選鏇蓋鑰積遞 艱積觸製鹽蓋廠鬱獵願 (壓窪繭夢廠選築窪齋衊 ) | 积极 | 2017-04-01 | |||
鬱窪鹽衊夢窪鏇壓願糧(觸餘積選願網艱鑰窪醖) = 顧願顧窪憲醖築齋鹹製 艱積觸製鹽蓋廠鬱獵願 (壓窪繭夢廠選築窪齋衊 ) |
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