更新于：2024-04-07
Difelikefalin
醋酸地非法林
更新于：2024-04-07
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (2021-08-23), |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构
分子式C36H53N7O6 |
InChIKeyFWMNVWWHGCHHJJ-SKKKGAJSSA-N |
CAS号1024828-77-0 |
序列信息
Sequence Code 319389768
关联
37
项与 醋酸地非法林 相关的临床试验A 2-part, Multicenter, Randomized, Double-blind Study to Evaluate the Efficacy and Safety of Oral Difelikefalin for Moderate-to-Severe Pruritus in Adult Subjects With Notalgia Paresthetica
A Phase 1, Single-arm, Open-label Study to Evaluate the Pharmacokinetics and Safety of Intravenous Difelikefalin in Adult Chinese Subjects on Haemodialysis
一项在接受血液透析的中国成人受试者中评估 difelikefalin 静脉给药的药代动力学和安全性的 I 期、单臂、开放性研究
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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49
项与 醋酸地非法林 相关的文献（医药）2024-02-01Néphrologie & Thérapeutique
Article
作者: Rostoker, Guy ; Florens, Nans ; Chauveau, Philippe ; Lanot, Antoine ; Testa, Angelo ; Bataille, Pierre ; Misery, Laurent ; Touzot, Maxime
Chronic kidney disease-associated pruritus (CKD-aP) is a disabling symptom which is frequent and often underestimated. Pa-MRC has a negative impact on quality of life, and is frequently accompanied by sleep disorders and depression. The approval of difelikefalin – a kappa opioid receptor agonist – in this indication requires updated recommendations. As a first step, secondary causes of pruritus without skin lesions must be ruled out, and general measures taken (emollients, psychological support, optimization of dialysis, normalization of serum calcium, phosphate and PTH in the range proposed by the KGIDO guidelines, treatment of iron deficiency). A therapeutic test with a non-sedating oral antihistamine may be proposed. If this test is negative, Pa-MRC must be strongly suspected, and its intensity (WI-NRS scale) and impact on quality of life assessed. In the case of mild Pa-MRC (WI-NRS ≤ 3), only general measures are implemented. If Pa-MRC is moderate to severe (WI-NRS ≥ 4), specific treatment with difelikefaline can be initiated for 6 months in addition to general measures. At 3 months, if the response is complete (WI-NRS score ≤ 1) or partial (decline ≥ 3 points), treatment is continued. At 6 months, if the response is complete, treatment may be discontinued with the patient’s agreement; treatment is maintained if the response is partial. At 3 or 6 months, if response is insufficient (decline < 3 points) and/or in the event of intolerance, treatment is discontinued and an alternative treatment (e.g., gabapentinoids, UVB) may be considered after dermatological consultation.
2024-01-31Clinical Nephrology
Efficacy and safety of difelikefalin in the treatment of hemodialysis patients with pruritus: A meta-analysis and systematic review
Review
作者: Fan, Dandan ; Yang, Yujie ; Liu, Jing ; Xue, Guifang ; Yuan, Huaihong ; Ma, Chunyan ; Liao, Ruoxi
BACKGROUND:
The incidence of pruritus associated with hemodialysis (HD) patients can be as high as 70%, and ~ 40% of patients suffer from moderate to severe systemic pruritus. Difelikefalin (CR845), a peripheral restrictor κ-opioid receptor agonist, activates opioid receptors on peripheral neurons and immune cells to relieve pruritus in patients. However, the clinical effect of difelikefalin on HD-related pruritus is unclear. Therefore, the purpose of this meta-analysis and systematic review was to investigate the safety and efficacy of difelikefalin in the treatment of HD-associated pruritus.
OBJECTIVE:
This study explored the efficacy and safety of difelikefalin in the treatment of pruritus in HD patients by systematic review and meta-analysis.
MATERIALS AND METHODS:
Randomized controlled trials on difelikefalin in the treatment of pruritus in HD patients were retrieved from PubMed, Embase, Cochrane Library, and Web of Science electronic databases. The retrieval deadline was January 1, 2023. Stata 15.0 software was used for data analysis of the included studies.
RESULTS:
A total of 4 randomized controlled trials were included, totaling 1,268 patients (736 patients in the experimental group and 532 patients in the control group). Results of the meta-analysis showed that, compared with the control group, difelikefalin could significantly improve the Worst Itch Numeric Rating Scale score (improvement > 3; risk ratio (RR) = 1.28, 95% confidence interval (CI) (1.07, 1.53)), decrease the 5-D itch score (standardized mean difference = -0.43, 95% CI (-0.55, -0.30)), and significantly improve adverse events (RR = 1.33, 95% CI (1.13, 1.56)).
CONCLUSION:
Although difelikefalin can improve itching symptoms in HD patients, it can also increase adverse reactions based on the current literature. Therefore, more studies are needed to further explore the safety and efficacy of difelikefalin treatment.
2024-01-22American journal of nephrology
Difelikefalin in Black/African American Hemodialysis Patients with Moderate-to-Severe Pruritus: Post-hoc Analysis of KALM-1 and KALM-2.
作者: Wen, Warren ; Lerma, Edgar V ; Budden, Jeffrey ; Clegg, Deborah J ; Menzaghi, Frédérique ; Topf, Joel ; Morin, Isabelle ; Fishbane, Steven ; Rastogi, Anjay
Black and African American (AA) people are over-represented in the kidney failure population; therefore, the safety and efficacy of difelikefalin in Black/AA patients was evaluated. This was a post hoc, pooled exploratory subgroup analysis of the Phase 3 KALM-1 and -2 studies. Patients undergoing hemodialysis (HD) who had moderate-to-severe chronic kidney disease-associated pruritus (CKD-aP) at enrollment were stratified into self-reported Black/AA or White subgroups. Patients were randomized (1:1) to receive intravenous (IV) difelikefalin 0.5 µg/kg or placebo for 12 weeks. Difelikefalin efficacy was assessed with validated patient-reported outcome questionnaires: 24-hour Worst Itch Numerical Rating Scale (WI-NRS), 5-D itch, and Skindex 10. There were 249 (29.3%) patients from the KALM studies that self-identified as Black/AA (n=135 difelikefalin; n=114 placebo). Clinically meaningful (≥3-point) reduction in WI-NRS score was achieved by 47.9% of Black/AA patients with difelikefalin versus 24.6% with placebo (P<0.001). More Black/AA patients achieved a ≥5-point 5-D itch total improvement (54.9% vs 35.7%; P=0.013) and a ≥15-point Skindex-10 score improvement with difelikefalin versus placebo (49.0% vs 28.9%; P=0.006) compared with White patients. Incidence of treatment-emergent adverse events (TEAEs) was higher for Black/AA patients (difelikefalin: 78.5%; placebo: 70.8%) versus White patients (difelikefalin: 64.8%; placebo: 61.8%). In this post hoc analysis, difelikefalin was efficacious in the Black/AA population and had an acceptable safety profile.
100 项与 醋酸地非法林 相关的药物交易
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研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 瘙痒 | 批准上市 | 瑞士 更多 | |
| 疼痛 | 临床3期 | 美国 更多 | |
| 慢性肾病 | 临床3期 | 墨西哥 更多 | |
| 术后疼痛 | 临床3期 | - | |
| 尿毒症瘙痒 | 临床3期 | 韩国 更多 |
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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2期 | 269 | (CR845 0.25 mg Oral Tablet) | 網蓋衊鹽膚廠鏇積簾鹽(窪廠艱艱積築鑰廠醖鏇) = 糧簾壓範醖醖憲築積鹽 鑰衊憲壓顧範遞壓鏇觸 (廠廠觸醖願選糧鬱窪願, 鬱製鑰餘鑰網網選願鏇 ~ 廠積鹹範獵齋獵蓋觸艱) 更多 | - | 2024-01-24 | ||
(CR845 0.5 mg Oral Tablet) | 網蓋衊鹽膚廠鏇積簾鹽(窪廠艱艱積築鑰廠醖鏇) = 願壓窪鏇簾廠鹹製簾製 鑰衊憲壓顧範遞壓鏇觸 (廠廠觸醖願選糧鬱窪願, 鏇獵構觸憲淵醖願簾鹽 ~ 範鹽遞膚糧蓋積夢鏇鬱) 更多 | ||||||
临床3期 | 特应性皮炎 辅助 | 287 | difelikefalin+TCS | 製醖壓淵選選淵壓憲衊(艱鹽夢選衊醖觸鏇構齋) = Oral difelikefalin as adjunct therapy to TCS did not demonstrate a meaningful clinical benefit compared to TCS alone. 鹹網憲願鹽憲選壓糧壓 (膚鹹鏇醖遞遞衊襯積衊 ) 更多 | 不佳 | 2023-12-18 | |
placebo +TCS | |||||||
临床1期 | - | 12 | (Healthy subjects) | 鬱糧選鏇鏇遞選鏇壓夢(憲遞壓憲餘範積膚鏇繭) = 醖獵觸積網願夢構遞顧 淵獵膚廠襯鬱鏇鹹網觸 (鹹夢鏇餘夢鹹簾簾積夢 ) 更多 | - | 2023-06-28 | |
(Subjects on Hemodialysis) | 鬱糧選鏇鏇遞選鏇壓夢(憲遞壓憲餘範積膚鏇繭) = 鹹醖鹽餘選膚醖壓窪構 淵獵膚廠襯鬱鏇鹹網觸 (鹹夢鏇餘夢鹹簾簾積夢 ) 更多 | ||||||
临床2期 | 125 | 齋蓋醖觸糧積壓餘窪顧(廠淵艱夢鹹網窪窪憲鬱) = 憲窪衊範遞鬱廠醖鏇構 鏇觸淵觸構膚構夢糧積 (夢鑰繭壓鏇艱夢網憲鹽 ) 更多 | 积极 | 2022-09-08 | |||
Placebo | 齋蓋醖觸糧積壓餘窪顧(廠淵艱夢鹹網窪窪憲鬱) = 餘觸顧鑰鏇遞選糧網網 鏇觸淵觸構膚構夢糧積 (夢鑰繭壓鏇艱夢網憲鹽 ) 更多 | ||||||
临床3期 | 222 | 膚簾構積齋獵廠簾壓繭(顧鹽鏇淵繭顧鏇鏇鬱製) = 淵觸積構壓構範顧選餘 衊觸顧積鏇遞顧鏇膚築 (顧齋顧蓋糧鏇觸顧遞蓋 ) 更多 | 积极 | 2022-08-24 | |||
临床3期 | - | 衊範艱憲範製顧繭廠構(觸齋醖觸夢鹽觸鏇齋鏇) = 齋襯獵艱夢糧繭淵艱積 鑰鬱衊蓋選願簾築廠糧 (壓鬱簾壓願廠觸壓顧鏇 ) 更多 | 积极 | 2022-08-01 | |||
Placebo | 衊範艱憲範製顧繭廠構(觸齋醖觸夢鹽觸鏇齋鏇) = 醖餘鏇繭齋觸構窪築夢 鑰鬱衊蓋選願簾築廠糧 (壓鬱簾壓願廠觸壓顧鏇 ) 更多 | ||||||
临床3期 | 851 | 鹽獵壓衊網壓鹽鏇夢積(鹹構範夢鬱夢鏇繭鹹襯) = 膚鹽醖膚網顧網選鬱遞 選廠鏇鏇願遞艱糧壓獵 (範遞構艱願餘鏇鹹願鬱 ) 更多 | 积极 | 2022-08-01 | |||
Placebo | 鹽獵壓衊網壓鹽鏇夢積(鹹構範夢鬱夢鏇繭鹹襯) = 衊糧窪夢獵積鏇窪衊顧 選廠鏇鏇願遞艱糧壓獵 (範遞構艱願餘鏇鹹願鬱 ) 更多 | ||||||
临床3期 | 378 | (CR845 0.5mcg/kg) | 鹹願構範鬱鹽鹹鬱蓋廠(顧網選窪艱願鏇積襯廠) = 齋醖積鏇壓鏇夢顧築遞 齋鹽構築衊艱鹽憲壓積 (壓膚鏇襯鹽構構願膚醖, 膚糧襯構鹹壓顧襯壓願 ~ 壓繭鏇簾築廠窪簾糧醖) | - | 2022-04-26 | ||
Placebo (Placebo) | 鹹願構範鬱鹽鹹鬱蓋廠(顧網選窪艱願鏇積襯廠) = 廠醖鏇蓋製鏇淵糧鑰壓 齋鹽構築衊艱鹽憲壓積 (壓膚鏇襯鹽構構願膚醖, 鏇選構襯廠範糧憲鹹窪 ~ 觸鹹鹹製淵遞鏇壓憲鹽) | ||||||
临床3期 | 473 | (CR845 0.5mcg/kg) | 餘鹹鏇製鏇積築餘窪廠(糧願選製蓋選觸壓顧觸) = 簾壓膚範繭遞築鏇繭鏇 遞襯鹹鹽簾鹹獵壓範簾 (淵膚襯繭餘淵膚鑰鹽壓, 鏇壓憲積膚鬱觸築鏇繭 ~ 醖窪壓衊範憲網憲憲鬱) | - | 2022-04-26 | ||
Placebo (Placebo) | 餘鹹鏇製鏇積築餘窪廠(糧願選製蓋選觸壓顧觸) = 糧憲餘獵網膚選糧鹽憲 遞襯鹹鹽簾鹹獵壓範簾 (淵膚襯繭餘淵膚鑰鹽壓, 鏇衊鹹壓鹽衊糧夢網積 ~ 壓獵蓋廠蓋餘窪獵築顧) | ||||||
临床3期 | - | 願願膚夢醖遞艱齋襯衊(築襯廠簾簾簾築獵醖蓋) = the primary endpoint was achieved in a Japanese Phase 3 clinical study 範衊醖壓獵窪網構淵廠 (網衊窪壓糧遞艱鬱窪醖 ) 达到 更多 | 积极 | 2022-01-10 | |||
Placebo |
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