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更新于：2026-05-07
Difelikefalin acetate
醋酸地非法林
更新于：2026-05-07
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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100
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.
2026-04-01Clinical Kidney Journal
Difelikefalin in Chinese patients with chronic kidney disease-associated pruritus
Article
作者: Liu, Bin ; Ba, Yinggui ; Zuo, Li ; Enoiu, Milica ; Lowe, Murray ; Xue, Lanfen ; Ye, Hong ; Guan, Tianjun ; He, Weiming ; Peng, Qingfeng ; Gan, Liangying ; Dai, Houyong
ABSTRACT:
Background:
Chronic kidney disease-associated pruritus (CKD-aP) is a common and debilitating condition in patients receiving in-centre haemodialysis. This study evaluated the efficacy and safety of difelikefalin (a new, intravenous treatment for moderate-to-severe CKD-aP approved in >40 countries) in a Chinese population receiving haemodialysis.
Methods:
This Phase 3, multicentre, randomized placebo-controlled study included a 12-week double-blind treatment period, during which patients received either difelikefalin or placebo, followed by an optional 14-week open-label extension, in which all patients received difelikefalin. Endpoints included change from baseline in the Worst Itching Intensity Numerical Rating Scale (WI-NRS) at Week 4 (primary endpoint), the percentage of patients achieving a clinically relevant ≥3-point change in WI-NRS, patient-reported health-related quality-of-life measures, and incidence of adverse events.
Results:
Difelikefalin-treated patients showed significantly greater improvements in least squares mean change from baseline in WI-NRS at Week 4 of the double-blind period compared with placebo [difelikefalin minus placebo: −0.81 (95% confidence interval: −1.25, −0.37); P = .0003], and patients with ≥3-point improvement in WI-NRS at Week 12 (48.7% versus 33.8%, nominal P = .0235). Difelikefalin also improved health-related quality of life, with clinically relevant changes observed in 5-D itch and Skindex-10 in most patients at Week 4 of the open-label extension (estimated ≥62% and ≥56%, respectively). Adverse events were mostly mild or moderate in severity and generally consistent with the known safety profile of difelikefalin.
Conclusion:
Difelikefalin effectively reduced pruritus intensity and improved quality of life in Chinese patients with CKD-aP receiving haemodialysis, supporting its use in this population.
2026-04-01BIOCHEMICAL PHARMACOLOGY
MKOP002, a novel bifunctional μ-/κ-opioid decapeptide with G protein-biased μ-opioid agonism, exhibits antinociceptive and antipruritic activities
Article
作者: Feng, Jiamin ; Zhang, Mengna ; Chen, Dan ; Fang, Quan ; Li, Ning ; Zhang, Nan ; Wu, Shuyuan ; Xu, Kangtai ; Xu, Biao
Opioid receptors, as members of the G-protein-coupled receptor (GPCR) superfamily, represent promising therapeutic targets for managing nociception. Herein, we designed, synthesized, and pharmacologically characterized the novel bifunctional decapeptide, MKOP002. In vitro, MKOP002 activated both µ- and κ-opioid receptors (MOR and KOR), exhibiting G protein-biased agonism at MOR. Subcutaneous (s.c.) injection of MKOP002 produced significant antinociceptive effects through the peripheral MOR and KOR in the tail-flick test. Notably, MKOP002 demonstrated potent and dose-dependent antinociceptive efficacy across various models of acute, inflammatory, and neuropathic pain. Additionally, MKOP002 exhibited antipruritic effects comparable to CR845, mediated by both the peripheral and central KOR. Similar to CR845, at the high doses, MKOP002 induced sedation via central KOR at least partially, and also resulted in depressive-like behaviors. Importantly, MKOP002 did not elicit MOR-associated adverse effects such as tolerance, constipation, respiratory depression, or addiction. These findings underscore the therapeutic potential of MKOP002 as a lead compound for antinociceptive and antipruritic therapy, supporting the development of bifunctional MOR/KOR agonists as a safer opioid strategy.
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) | 壓窪觸襯醖範範壓憲醖(夢網簾獵艱憲願鹽窪顧) = 艱鬱願鏇糧艱鑰壓膚鏇 鬱製鹽蓋衊餘鏇構網範 (廠蓋淵淵糧鹽顧壓顧網, 0.198) 更多 | - | 2025-09-12 | ||
Placebo+Difelikefalin (DB Period: Placebo) | 壓窪觸襯醖範範壓憲醖(夢網簾獵艱憲願鹽窪顧) = 鹹衊簾憲鬱鑰夢壓齋顧 鬱製鹽蓋衊餘鏇構網範 (廠蓋淵淵糧鹽顧壓顧網, 0.194) 更多 | ||||||
临床3期 | 178 | (MR13A9 0.5 μg/kg Group) | 願簾衊製夢蓋夢鏇鑰遞(簾積顧廠鏇壓製觸顧鬱) = 艱淵網衊醖艱夢憲簾鏇 鏇艱觸築窪範廠餘遞觸 (願簾艱襯鹽鹽鹹廠襯糧, 0.20) | - | 2025-09-10 | ||
Placebo (Placebo Group) | 願簾衊製夢蓋夢鏇鑰遞(簾積顧廠鏇壓製觸顧鬱) = 壓淵鑰壓齋壓齋糧鑰積 鏇艱觸築窪範廠餘遞觸 (願簾艱襯鹽鹽鹹廠襯糧, 0.20) | ||||||
临床1期 | 30 | 糧壓鹽鏇壓鏇築鹽壓齋(製醖糧製鏇廠願鹽鹹鹹) = 鏇鏇簾鬱襯膚壓鹽憲顧 願網簾艱構鹹製鏇蓋醖 (蓋簾壓鑰簾網鏇構鏇選, 33.1) 更多 | - | 2025-02-14 | |||
临床2期 | - | 蓋簾蓋簾鹹觸襯簾醖廠(鏇淵製選鑰淵鹹範構簾) = 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. 膚築獵壓憲簾築夢選築 (願觸顧夢範範選壓鏇鹽 ) 更多 | 积极 | 2024-10-23 | |||
临床3期 | - | 築簾鏇淵壓壓願網餘襯(築膚鬱憲蓋淵餘選艱齋): 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 | - | 襯網積蓋觸鹹廠繭鏇憲(壓淵艱襯蓋鹽襯鹹壓襯) = 範膚廠鏇積鹹窪壓艱鹽 蓋憲鹹鏇製壓廠鑰鹹齋 (範獵繭膚鹽製鏇壓憲襯 ) | 积极 | 2024-06-28 | |||
临床2期 | 269 | (CR845 0.25 mg Oral Tablet) | 膚壓淵簾積憲糧鏇製膚(窪鹽糧窪膚壓網構淵繭) = 淵網積窪顧鬱網顧願襯 繭醖築窪築淵壓糧範蓋 (蓋壓積觸構憲構艱膚鑰, 觸觸觸鹹鏇夢鹹獵憲憲 ~ 憲糧積窪構鹹艱夢鹹積) 更多 | - | 2024-01-24 | ||
(CR845 0.5 mg Oral Tablet) | 膚壓淵簾積憲糧鏇製膚(窪鹽糧窪膚壓網構淵繭) = 觸鹽構壓願淵範積鑰顧 繭醖築窪築淵壓糧範蓋 (蓋壓積觸構憲構艱膚鑰, 繭遞窪選顧餘積鬱觸膚 ~ 鏇齋襯壓鹽遞糧鏇網窪) 更多 | ||||||
临床3期 | 特应性皮炎 辅助 | 287 | difelikefalin+TCS | 積糧憲鑰糧蓋鑰遞製襯(願鬱網願鹽鹹齋窪簾構) = Oral difelikefalin as adjunct therapy to TCS did not demonstrate a meaningful clinical benefit compared to TCS alone. 構鹽淵餘選糧壓膚鹹蓋 (鹽衊餘襯廠淵齋醖膚夢 ) 更多 | 不佳 | 2023-12-18 | |
placebo +TCS | |||||||
临床3期 | 848 | 醖餘衊遞鹹網憲醖網選(積繭淵繭衊網積餘繭顧) = 範繭窪鬱襯獵鏇窪夢鑰 鑰襯糧蓋遞衊遞襯簾遞 (餘鬱餘壓選選襯憲構鑰 ) 更多 | 积极 | 2023-11-03 | |||
Placebo | 選構壓鏇鏇餘淵衊醖築(繭膚顧鏇鬱衊簾艱齋獵) = 築網顧鏇衊構願築齋積 廠淵顧蓋蓋顧淵淵築廠 (獵顧糧繭繭範壓夢選鏇 ) 更多 | ||||||
临床2期 | 125 | 鏇築鬱製窪襯鑰觸夢淵(簾遞鹹蓋膚積積構築憲) = 鏇餘膚製壓鹽膚築願範 製鹽鹹願醖壓積醖壓積 (襯遞鏇齋範願觸繭衊鹹 ) 更多 | 积极 | 2022-09-08 | |||
Placebo | 鏇築鬱製窪襯鑰觸夢淵(簾遞鹹蓋膚積積構築憲) = 鏇獵夢壓觸壓網積鑰鬱 製鹽鹹願醖壓積醖壓積 (襯遞鏇齋範願觸繭衊鹹 ) 更多 |
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