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更新于：2026-08-26
Difelikefalin acetate
醋酸地非法林
更新于：2026-08-26
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 新加坡 () |
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C36H53N7O6.C2H4O2 |
InChIKeyMZWHRPKAHCWTOI-KGURMGBCSA-N |
CAS号1024829-44-4 |
Sequence Code 319389768
关联
37
项与 醋酸地非法林 相关的临床试验NCT06593392
KOR-PED-202 An Open-label, Single-arm Study to Evaluate the Safety and Tolerability of Intravenous Difelikefalin in Adolescents Aged 12 to 17 Years on Haemodialysis With Moderate-to-Severe Pruritus
NCT07526324
Effect of Difelikefalin on CKD-Associated Pruritus in Patients on Maintenance Hemodialysis: A Randomized, Placebo-Controlled Trial
ChiCTR2500109843
An Open-label, Single-arm Study to Evaluate the Safety and Tolerability of Intravenous Difelikefalin in Adolescents Aged 12 to 17 Years on Haemodialysis with Moderate-to-Severe Pruritus
100 项与 醋酸地非法林 相关的临床结果
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100 项与 醋酸地非法林 相关的转化医学
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100 项与 醋酸地非法林 相关的专利（医药）
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112
项与 醋酸地非法林 相关的文献（医药）2026-12-31RENAL FAILURE
Association of pruritus with comorbidities and survival in chronic kidney disease: a narrative review of the pre-difelikefalin era literature
Review
作者: Misery, Laurent ; Rostoker, Guy ; Saucereau, Justine ; Brenaut, Emilie ; Le Gall-Ianotto, Christelle ; Ficheux, Anne-Sophie
Pruritus is a frequent and distressing symptom in chronic kidney disease (CKD). This study aimed to evaluate the association between pruritus and comorbidities or survival in CKD before the approval of difelikefalin (DFK), a novel treatment for CKD-associated pruritus (CKD-aP). A systematic literature review was conducted using PubMed and Embase, including studies published between January 2000 and August 2022 that examined the link between CKD-aP and morbidity or survival in CKD. We analyzed 5,867 title/abstracts (3,541 from Pubmed, 2,313 from Embase, and nine additional articles) and excluded 5,721 references. Thirty-seven of the 146 articles that were eligible for full reading were included in the analysis. Thus, 18 identified a statistically significant association between CKD-aP and mortality. However, this association lost significance in 3 studies after adjusting for sleep. Two additional studies found no association between CKD-aP and mortality. In terms of sleep disturbance, 14 out of 15 studies reported a significant link with CKD-aP. Moreover, six studies demonstrated relationship between CKD-aP and cardiovascular events, which remained robust even after adjusting for diabetes. The connection between CKD-aP and mental health and depressive symptoms was investigated in 20 studies, with 18 confirming a significant association between the outcomes. Finally, six studies indicated that healthcare costs were higher in CKD-aP compared to those without. Pruritus appears to be associated with increased mortality, cardiovascular events, depressive symptoms, and healthcare costs in CKD patients. Early detection and treatment, particularly with new drugs like DFK, may improve patients' quality of life and reduce CKD-aP related.
2026-08-01JOURNAL OF PHARMACEUTICAL SCIENCES
Development of a SMEDDS for oral delivery of hydrophilic peptide difelikefalin acetate: Preparation, characterization, and PK/PD evaluation
Article
作者: Ming, Congmei ; Zhou, Wu ; Li, Zhongyuan
Difelikefalin acetate (DF) is indicated for the treatment of moderate-to-severe pruritus associated with chronic kidney disease in adult patients undergoing hemodialysis. The marketed formulation is an injectable, while this study aims to develop an oral formulation to improve patient compliance. DF is designed to incorporated into lipid nanoparticles with 1,2-dipalmitoyl-rac-glycerol-3-phosphocholine (DPPC), 1,2-distearoyl-sn‑glycero-3-phospho-rac-(1-glycerol) sodium salt (DSPG), and cholesterol (CHOL) (at a ratio of 8:2:6), which are mixed with 20% oleic acid, 20% medium-chain triglycerides (MCT), 24% PEG-40 hydrogenated castor oil (RH40), and 36% transcutol to prepare a self-microemulsifying concentrate. The concentrate can achieve self-emulsification in purified water, pH 1.2(HCl solution), pH 4.5(acetate buffer), and pH 6.8(phosphate buffer) media, with a droplet size of 53-59 nm, polydispersity index (PDI) of 0.09-0.27, zeta potential of -36.39 to -6.1 mV, and drug loading of 90.3%. In vitro release results showed that the DF solution was almost completely released at 8 h in pH 6.8 medium, while the DF self-microemulsion only achieved approximately 20% release at 24 h. Enzymatic degradation experiments demonstrated that trypsin, elastase, and α-chymotrypsin could not effectively degrade DF. The rat pharmacokinetic study showed that, relative to intravenous administration, the oral bioavailability of the DF solution was 0.656%, whereas that of DF self-microemulsifying drug delivery systems (SMEDDS) was 2.04%, representing a 3-fold increase. In the mouse pharmacodynamic test, the scratching episodes inhibition of orally administered DF SMEDDS at a dose of 5 mg/kg was comparable to that of DF injection at 0.3 mg/kg.
2026-06-01Small
Innovative Microneedle Patches for Psoriasis Treatment: A Dual Approach With Methotrexate‐Zinc and Difelikefalin for Enhanced Therapeutic Outcomes
Article
作者: Long, Chunhao ; Xu, Xiaolong ; Zhou, Youyou ; Zhou, Yuze ; Fei, Lujing ; Qi, Min
ABSTRACT:
Psoriasis is a chronic inflammatory skin disease often accompanied by pruritus and a high risk of secondary infection. To address the limitations of current therapies, we developed a dual‐layer microneedle (MN) system that integrates methotrexate‐zinc (MTX‐Zn) for sustained anti‐inflammatory and antibacterial effects with difelikefalin (DFK) for rapid antipruritic action. MTX‐Zn was successfully synthesized through coordination chemistry and exhibited enhanced stability, preserved antiproliferative activity, and strong antibacterial effects. The GelMA/PVA‐based microneedles showed excellent mechanical strength, efficient skin penetration, and distinct spatial drug compartmentalization. In an IMQ‐induced psoriasis model, MTX‐Zn/DFK MNs markedly improved clinical symptoms, reduced epidermal hyperplasia, restored immune‐cell homeostasis, and decreased Th17/Th1‐mediated inflammation. DFK‐loaded MNs rapidly alleviated pruritus, reduced epidermal nerve‐fiber density, and inhibited Schwann cell migration. Transcriptomic analysis further revealed that DFK suppressed Schwann cell EMT pathways. Together, this dual‐functional microneedle platform provides a synergistic therapeutic strategy that combines rapid itch relief with long‐term anti‐psoriatic and antibacterial effects, representing a promising approach for improving psoriasis management.
100 项与 醋酸地非法林 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 |
|---|---|---|---|
| 瘙痒 | 日本 | 2023-09-25 | |
| 慢性肾病相关瘙痒 | 美国 | 2021-08-23 |
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 |
|---|---|---|---|---|
| 特应性皮炎 | 临床3期 | 美国 | 2022-08-16 | |
| 慢性肾病 | 临床3期 | 美国 | 2022-05-17 | |
| 终末期肾脏病 | 临床3期 | 美国 | 2022-05-17 | |
| 疼痛 | 临床3期 | 美国 | 2022-01-30 | |
| 疼痛 | 临床3期 | 韩国 | 2022-01-30 | |
| 尿毒症瘙痒 | 临床3期 | 美国 | 2017-08-14 | |
| 术后疼痛 | 临床3期 | 美国 | 2015-09-01 | |
| 背痛 | 临床2期 | 美国 | 2021-01-11 | |
| 背痛 | 临床2期 | 加拿大 | 2021-01-11 | |
| 胆汁淤积性瘙痒 | 临床2期 | 美国 | 2019-06-25 |
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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 | 260 | (DB Period: Difelikefalin) | 製鹹簾顧範艱構選窪顧(鹹鏇襯顧餘壓餘獵簾製) = 蓋蓋鬱鏇願繭鹽範構遞 齋鹹顧齋憲製遞鹹夢齋 (窪窪窪蓋醖壓廠蓋齋淵, 0.198) 更多 | - | 2025-09-12 | ||
Placebo+Difelikefalin (DB Period: Placebo) | 製鹹簾顧範艱構選窪顧(鹹鏇襯顧餘壓餘獵簾製) = 願窪餘製製積艱願範淵 齋鹹顧齋憲製遞鹹夢齋 (窪窪窪蓋醖壓廠蓋齋淵, 0.194) 更多 | ||||||
临床3期 | 178 | (MR13A9 0.5 μg/kg Group) | 構齋觸蓋齋顧鬱膚鹹窪(廠糧製製觸構齋遞餘糧) = 製遞淵艱構顧艱構製選 遞觸窪顧遞獵艱鏇齋範 (獵糧廠願壓鹽壓簾餘遞, 0.20) | - | 2025-09-10 | ||
Placebo (Placebo Group) | 構齋觸蓋齋顧鬱膚鹹窪(廠糧製製觸構齋遞餘糧) = 網淵選艱範憲遞選夢積 遞觸窪顧遞獵艱鏇齋範 (獵糧廠願壓鹽壓簾餘遞, 0.20) | ||||||
N/A | 28 | 艱製膚衊壓蓋壓範觸築(遞壓製衊遞齋餘衊蓋糧) = After starting DFK, 5D-Itch scores drastically and significantly decreased at 3 months and maintained at 1 year (p = 0.019) 鹹繭顧遞憲壓築夢蓋鏇 (窪窪獵襯鏇鏇製憲衊壓 ) 更多 | 积极 | 2025-06-04 | |||
N/A | 438 | 築窪鬱選遞廠鏇淵顧膚(鹽艱鹽窪齋鏇簾鑰艱憲) = 獵鑰膚壓齋鏇製鹽廠範 餘壓遞蓋築窪艱醖製淵 (獵鑰網窪餘顧網鹽淵廠 ) 更多 | 积极 | 2025-06-04 | |||
临床1期 | 30 | 齋窪積顧鏇齋鹹積齋築(簾鏇襯窪築獵繭艱鏇積) = 憲範顧膚蓋衊憲膚蓋憲 艱衊簾齋糧簾築壓淵簾 (觸簾製獵蓋衊鹹艱夢觸, 33.1) 更多 | - | 2025-02-14 | |||
临床2期 | - | 簾範蓋鑰遞獵鬱艱願積(鬱鬱製簾醖壓遞範齋鹽) = Relative improvement by PGIC category was highly consistent across baseline severity groups, independent of treatment received, with patients reporting their itch having “much improved” seeing a 50% reduction from their baseline WI-NRS value. 夢齋糧選壓壓鏇簾遞憲 (獵觸醖襯憲積鬱選糧選 ) 更多 | 积极 | 2024-10-23 | |||
临床3期 | - | 選鑰齋構淵壓範鑰鬱構(艱鬱製憲憲淵齋壓遞鹹): Difference = -0.81 (95% CI, -1.25 ~ -0.37), P-Value = 0.0003 达到 更多 | 积极 | 2024-09-04 | |||
安慰剂 | |||||||
临床3期 | - | 襯憲襯淵醖願繭獵廠選(齋醖夢壓淵憲鹹醖餘夢) = 艱範鏇願顧顧鬱構鹽壓 鹽醖夢糧艱襯構蓋齋顧 (衊壓範廠鹹製醖鏇憲製 ) | 积极 | 2024-06-28 | |||
N/A | 295 | (Hemodialysis + CKD-associated pruritus) | 憲築網繭觸膚觸簾遞網(鬱窪獵鑰顧艱鹹鹹網獵) = 鹽顧衊觸繭襯鬱夢壓窪 積範鏇鑰膚艱餘襯夢窪 (顧鹽繭鏇艱鏇築範壓鬱 ) 更多 | 积极 | 2024-05-23 | ||
临床2期 | 269 | (CR845 0.25 mg Oral Tablet) | 蓋遞顧構襯遞繭願衊構(艱遞網構艱簾膚壓簾廠) = 鹹選鹹艱築願鬱簾艱願 鹹繭願壓淵網積齋膚蓋 (廠糧網艱鬱鏇夢鬱遞願, 廠構醖網蓋醖蓋糧齋繭 ~ 網糧憲簾遞衊窪壓願網) 更多 | - | 2024-01-24 | ||
(CR845 0.5 mg Oral Tablet) | 蓋遞顧構襯遞繭願衊構(艱遞網構艱簾膚壓簾廠) = 廠築繭遞糧顧醖齋鏇鑰 鹹繭願壓淵網積齋膚蓋 (廠糧網艱鬱鏇夢鬱遞願, 壓窪鹽鹹範築膚鏇築淵 ~ 窪鑰襯夢觸觸鬱膚製淵) 更多 |
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