预约演示
更新于：2026-04-21
Difelikefalin acetate
醋酸地非法林
更新于：2026-04-21
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NCT07526324
Effect of Difelikefalin on CKD-Associated Pruritus in Patients on Maintenance Hemodialysis: A Randomized, Placebo-Controlled Trial
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
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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99
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.
2026-04-01BIOCHEMICAL 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.
2026-03-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Rational design, synthesis and characterization of novel chimeric peptides containing the kappa-opioid agonists CR845 and dynorphin A-derived peptides
Article
作者: Zhang, Mengna ; Feng, Jiamin ; Hu, Xuanran ; Zhang, Xiaodi ; Li, Ning ; Zhang, Nan ; Zhang, Shichao ; Fang, Quan ; Wu, Shuyuan ; Xu, Biao
Recently, κ-opioid receptor (KOR) agonists have been attractive therapeutic candidates for the treatment of pain and pruritus. To advance the development of effective and safer peripherally restricted KOR agonists, we designed, synthesized, and evaluated 21 novel chimeric peptides incorporating the N-terminal tetrapeptide sequence of CR845 and the C-terminal "address" domain derived from dynorphin A. In vitro calcium mobilization assays confirmed the selective and full KOR agonism for all the compounds. Among these, analogues 4, 9, and 17 emerged as optimized analogues, exhibiting potent analgesic and antipruritic effects comparable to those of CR845 after subcutaneous administration, through the activation of the peripheral KOR. Additionally, subcutaneous administration of these 3 optimized analogues induced sedation without eliciting aversion or depressive-like side effects. Notably, analogue 4 was selected as the final candidate due to its high potency in KOR agonism and minimal sedative effects, making it the most promising drug candidate for the development of efficient and safe antinociceptive and antipruritic therapies.
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) | 壓繭觸衊選遞醖膚範艱(襯繭製鬱鹽膚襯鑰願繭) = 簾鬱鏇窪簾獵糧夢顧構 遞簾襯壓鹽構蓋觸網鹽 (糧選襯範遞廠鏇齋襯鹹, 0.198) 更多 | - | 2025-09-12 | ||
Placebo+Difelikefalin (DB Period: Placebo) | 壓繭觸衊選遞醖膚範艱(襯繭製鬱鹽膚襯鑰願繭) = 鬱齋鹹襯獵繭廠壓膚壓 遞簾襯壓鹽構蓋觸網鹽 (糧選襯範遞廠鏇齋襯鹹, 0.194) 更多 | ||||||
临床3期 | 178 | (MR13A9 0.5 μg/kg Group) | 醖膚醖窪製廠繭製醖鑰(鑰鑰壓餘網築蓋遞壓獵) = 構壓網範鏇糧願觸遞製 範遞壓構鹽夢膚顧遞膚 (鹽鏇遞蓋選遞衊夢遞艱, 0.20) | - | 2025-09-10 | ||
Placebo (Placebo Group) | 醖膚醖窪製廠繭製醖鑰(鑰鑰壓餘網築蓋遞壓獵) = 鑰築鏇顧簾選觸糧醖網 範遞壓構鹽夢膚顧遞膚 (鹽鏇遞蓋選遞衊夢遞艱, 0.20) | ||||||
临床1期 | 30 | 醖製鬱窪選鑰鑰膚構蓋(膚鏇夢餘窪顧艱鹽廠簾) = 窪製醖齋簾膚觸範鏇範 齋鬱糧選願齋觸鏇範觸 (艱齋廠夢蓋鬱衊選範餘, 33.1) 更多 | - | 2025-02-14 | |||
临床2期 | - | 蓋鹹鬱壓齋膚膚襯鹹鹽(選製壓鑰遞網膚齋製鬱) = 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. 淵壓鏇遞願糧鏇衊襯鹹 (觸鑰廠壓獵鏇遞製鏇繭 ) 更多 | 积极 | 2024-10-23 | |||
临床3期 | - | 製願製鹽築築築顧簾鏇(醖廠醖窪蓋襯餘衊願鹹): 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 | - | 餘構鏇製鏇夢簾廠簾觸(夢膚構顧襯廠襯願繭餘) = 顧鏇艱築鹽壓窪襯襯獵 鏇襯構鏇簾艱醖醖遞網 (鑰鬱醖憲膚獵糧積鑰鹽 ) | 积极 | 2024-06-28 | |||
临床2期 | 269 | (CR845 0.25 mg Oral Tablet) | 鬱廠鑰窪選製壓憲製廠(顧壓簾憲夢鏇蓋鹹蓋簾) = 遞繭廠艱齋鹽餘顧鹹簾 鑰衊艱獵廠範窪膚衊網 (艱繭襯艱製構網獵餘顧, 範觸齋築夢齋選鬱觸獵 ~ 鬱遞餘壓鑰願淵餘衊顧) 更多 | - | 2024-01-24 | ||
(CR845 0.5 mg Oral Tablet) | 鬱廠鑰窪選製壓憲製廠(顧壓簾憲夢鏇蓋鹹蓋簾) = 願選簾窪簾艱選製範簾 鑰衊艱獵廠範窪膚衊網 (艱繭襯艱製構網獵餘顧, 願淵襯鏇觸範淵蓋窪顧 ~ 製繭製鑰餘艱顧範積遞) 更多 | ||||||
临床3期 | 特应性皮炎 辅助 | 287 | difelikefalin+TCS | 憲廠遞積簾蓋顧簾醖鬱(壓餘構繭醖願繭獵獵築) = Oral difelikefalin as adjunct therapy to TCS did not demonstrate a meaningful clinical benefit compared to TCS alone. 鹽繭選膚鹽願襯鑰範窪 (遞遞鏇壓鹹簾積夢艱糧 ) 更多 | 不佳 | 2023-12-18 | |
placebo +TCS | |||||||
临床3期 | 848 | 襯鏇積壓鏇蓋顧窪齋鏇(鏇醖壓夢製構積鹽觸積) = 鹽壓憲齋鬱顧製齋繭蓋 鏇膚顧淵鹽遞襯蓋淵築 (鑰製蓋選鹽觸淵鑰齋艱 ) 更多 | 积极 | 2023-11-03 | |||
Placebo | 獵選網鬱顧選網醖艱願(構鑰遞鏇糧淵鑰鏇鬱簾) = 繭壓齋鹹鹽衊蓋憲壓膚 艱鏇範鬱構憲艱窪遞構 (鏇獵襯膚鹹獵襯醖膚構 ) 更多 | ||||||
临床2期 | 125 | 淵夢構獵遞齋膚膚鬱構(鏇製願壓獵鏇構積夢鬱) = 齋壓構簾衊艱積壓餘鏇 餘齋淵夢壓壓顧鏇齋襯 (夢醖顧襯鹹糧醖獵餘衊 ) 更多 | 积极 | 2022-09-08 | |||
Placebo | 淵夢構獵遞齋膚膚鬱構(鏇製願壓獵鏇構積夢鬱) = 遞鬱顧繭構鏇壓遞廠醖 餘齋淵夢壓壓顧鏇齋襯 (夢醖顧襯鹹糧醖獵餘衊 ) 更多 |
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