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更新于：2025-04-23
Naldemedine Tosylate
纳地美定
更新于：2025-04-23
概要
基本信息
药物类型 小分子化药 |
别名 naldemedine、Naldemedine tosilate、Rizmoic + [3] |
作用方式 拮抗剂 |
作用机制 μ opioid receptor拮抗剂(μ-阿片受体拮抗剂) |
在研适应症 |
非在研适应症 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2017-03-23), |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构/序列
分子式C39H42N4O9S |
InChIKeyWCYDLROFMZJJLE-RTMHEQJQSA-N |
CAS号1345728-04-2 |
关联
32
项与 纳地美定 相关的临床试验NCT06334198
The Effect of Naldemedine on Opioid-induced Bowel Dysfunction. An Investigator Initiated, Randomized, Double-blinded, Placebo-controlled, Cross-over Clinical Trial
NCT05588323
A Phase 1/2, Multicentre, Open-label Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of Naldemedine in Paediatric Patients Who Are Receiving or Who Are About to Receive Treatment With Opioids
CTR20220673
一项Naldemedine 治疗癌痛患者合并阿片类药物引起的便秘的多中心、包含安慰剂对照治疗期与开放治疗期两阶段的研究
100 项与 纳地美定 相关的临床结果
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100 项与 纳地美定 相关的转化医学
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100 项与 纳地美定 相关的专利（医药）
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196
项与 纳地美定 相关的文献（医药）2025-04-15Zhonghua yi xue za zhi
[Efficacy of Naldemedine in opioid-induced constipation in cancer patients].
Article
作者: Sheng, L ; Li, S ; Yang, S H ; Chen, D L ; Wang, H X ; Li, X L ; Wu, J Y ; Wang, L ; Qiu, C ; Zhou, M F ; Sun, D T
This study evaluated the efficacy and safety of Naldemedine, an oral peripheral μ-opioid receptor antagonists (PAMORAs), in cancer patients with opioid-induced constipation (OIC). A single-center, single-arm, prospective real-world trial was conducted, enrolling 12 patients aged 18 years and above who had been on stable opioid analgesic therapy for at least 7 days and met the criteria for OIC. Participants were administered 0.2 mg/d Naldemedine orally for a minimum of 12 weeks (up to 48 weeks). The primary endpoint was the proportion of spontaneous bowel movement (SBM) responders within the first two weeks of treatment. Secondary endpoints included complete SBM (CSBM) responder rates and other efficacy endpoints, as well as safety assessments and quality of life. The results demonstrated SBM and CSBM responder rates of 66.7%(8/12) and 33.3%(4/12), respectively, within the initial two weeks. The mean frequency of SBM/CSBM increased for (3.8±2.7)/(1.3±1.9) times when compared with baseline after 2-week of treatment. Notably, 66.7%(8/12) and 33.3%(4/12) of patients experienced≥1 SBM or CSBM within 24 hours after the first dose, with median times to first SBM and CSBM being 4.0 and 16.6 hours post-administration. Mild treatment-related adverse events were reported in 16.7%(2/12) of patients. Naldemedine improved QoL. Naldemedine shows promising efficacy and manageable safety in cancer pain patients with OIC.
2025-01-29Cureus Journal of Medical Science
Prescription Pattern of Laxatives for Opioid-Induced Constipation in Japanese Patients With Chronic Non-cancer Pain: A Retrospective Cohort Study of a Health Insurance Claims Database
Article
作者: Sonohata, Motoki ; Morioka, Yasuhide ; Kitamura, Misato ; Hashimoto, Akira
Introduction Opioid-induced constipation (OIC) is the most common side effect of opioids. Weak opioids are often prescribed for non-cancer chronic pain in Japan; however, data on laxative use are scarce. We evaluated the real-world prescription patterns of laxatives for OIC in patients administered weak opioids for non-cancer pain in Japan. Methods In this retrospective cohort study, we extracted data from a Japanese health insurance claims database for patients with chronic non-cancer pain (lower back pain, joint pain, and neuropathic pain) who were continuously prescribed weak opioids for ≥1 month after initiating weak opioids between 2017 and 2022. Results Of 425,556 patients prescribed weak opioids, 42,514 patients (mean age: 50.1 years) were included. Most were prescribed ≤150 mg tramadol equivalent/day, and 21,405 (50.3%) were on weak opioids for lower back pain. The proportion of laxatives prescribed on the first day of weak opioid prescription was 6.7%; the cumulative prescription rate during the 12‑week follow-up was 13.6%. The most common laxatives during the first week were magnesium oxide (2,320 (66.6%)), sennoside (484 (13.9%)), and naldemedine (301 (8.6%)); at 12 weeks, these proportions were 55.2%, 13.1%, and 13.8%, respectively. The amount of weak opioids prescribed to patients without laxatives was lower than the standard dosage and was also lower than the amount prescribed to patients with laxatives. Conclusions This study showed that the actual prescription patterns of laxatives after initiating weak opioids in patients with chronic non-cancer pain were variable, depending on the duration after initiating weak opioids. The association between laxative use and weak opioid dosage indicates that OIC management may have a potential impact on pain management.
2025-01-08JAPANESE JOURNAL OF CLINICAL ONCOLOGY
Effect of add-on naldemedine treatment in patients with cancer and opioid-induced constipation insufficiently responding to magnesium oxide: a pooled, subgroup analysis of two randomized controlled trials
Article
作者: Nakajima, Atsushi ; Koretaka, Yuichi ; Morioka, Yasuhide ; Uchida, Kohei ; Kobayashi, Masayuki ; Akamatsu, Toshikazu ; Yokota, Takaaki ; Kessoku, Takaomi
Abstract:
Objective:
To evaluate the additive effect of naldemedine tosylate (naldemedine) on opioid-induced constipation in cancer patients insufficiently responding to magnesium oxide treatment.
Methods:
We combined two randomized, double-blind, placebo-controlled, phase IIb and III trials of naldemedine and conducted a post hoc subgroup analysis. We evaluated the effect and safety of naldemedine in 116 patients who received naldemedine in addition to magnesium oxide (naldemedine group) and 117 patients who received placebo in addition to magnesium oxide (placebo group). Both groups included patients insufficiently responding to magnesium oxide for opioid-induced constipation. Effect was assessed using spontaneous bowel movement responder rate, complete spontaneous bowel movement responder rate, changes in spontaneous bowel movements and complete spontaneous bowel movements. Safety was also assessed.
Results:
During the 2-week treatment period, the responder rates for spontaneous bowel movement and complete spontaneous bowel movement were 73.3 and 43.1% in naldemedine group, respectively, which were significantly higher (P < 0.0001) than 41.9 and 14.5% in placebo group, respectively. Median time to first spontaneous bowel movement and first complete spontaneous bowel movement was significantly shorter (P < 0.0001) in the naldemedine group (4.0 and 21.3 h, respectively) than in the placebo group (27.7 and 211.7 h, respectively). The incidence of adverse events and diarrhoea was significantly higher (P < 0.05) in the naldemedine group than in the placebo group, while the incidence of serious adverse events and severe diarrhoea was not significantly different between the naldemedine and placebo groups.
Conclusion:
The study suggested the addition of naldemedine as an effective treatment option for opioid-induced constipation in cancer patients insufficiently responding to magnesium oxide treatment.
100 项与 纳地美定 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 |
|---|---|---|---|
| 阿片类药物引起的便秘 | 美国 | 2017-03-23 |
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 |
|---|---|---|---|---|
| 癌症疼痛 | 临床3期 | 中国 | 2022-07-15 | |
| 便秘 | 临床3期 | 中国 | 2022-07-15 | |
| 慢性疼痛 | 临床3期 | 美国 | 2013-08-29 | |
| 慢性疼痛 | 临床3期 | 奥地利 | 2013-08-29 | |
| 慢性疼痛 | 临床3期 | 捷克 | 2013-08-29 | |
| 慢性疼痛 | 临床3期 | 德国 | 2013-08-29 | |
| 慢性疼痛 | 临床3期 | 波兰 | 2013-08-29 | |
| 慢性疼痛 | 临床3期 | 西班牙 | 2013-08-29 | |
| 慢性疼痛 | 临床3期 | 英国 | 2013-08-29 | |
| 胃肠功能紊乱 | 临床2期 | 美国 | 2020-11-06 |
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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 | 99 | 觸顧艱顧鹽廠鹽壓壓鏇(鹽鹽顧憲醖廠鹽壓獵製) = 構範獵夢憲範繭膚餘製 糧衊積鬱遞淵鬱蓋餘夢 (憲觸鏇構夢築醖簾廠鏇, 19.8) | 积极 | 2024-06-02 | |||
Placebo | 觸顧艱顧鹽廠鹽壓壓鏇(鹽鹽顧憲醖廠鹽壓獵製) = 觸餘願鏇醖艱醖廠廠觸 糧衊積鬱遞淵鬱蓋餘夢 (憲觸鏇構夢築醖簾廠鏇, 20.0) | ||||||
临床2期 | 2 | (Naldemedine 1.25 mg) | 壓鹽餘鑰觸願餘遞範憲(壓鑰廠齋構積夢鏇襯築) = 膚鑰窪鏇鹹艱夢顧網艱 範網鹹簾獵觸繭選廠襯 (積構淵糧淵壓壓遞觸獵, 壓蓋積憲窪願築襯鏇糧 ~ 繭鏇齋簾選蓋齋壓夢淵) 更多 | - | 2022-01-18 | ||
(Naldemedine 2.5 mg) | 壓鹽餘鑰觸願餘遞範憲(壓鑰廠齋構積夢鏇襯築) = 醖憲衊衊艱夢選築網膚 範網鹹簾獵觸繭選廠襯 (積構淵糧淵壓壓遞觸獵, 選襯鹽壓鏇築廠醖淵鬱 ~ 醖襯鏇糧衊廠製夢廠鹽) 更多 | ||||||
N/A | - | 鹹餘鹹願夢顧製鹹築憲(簾鹹積觸鏇範壓醖醖築) = 製範鬱願鹽鑰簾繭鹹鬱 憲遞積網製繭憲膚衊鹹 (製觸蓋鹽構願製廠窪齋, 3.2) 更多 | - | 2020-10-01 | |||
Placebo | 鹹餘鹹願夢顧製鹹築憲(簾鹹積觸鏇範壓醖醖築) = 襯製鬱壓醖遞鑰衊鏇繭 憲遞積網製繭憲膚衊鹹 (製觸蓋鹽構願製廠窪齋, 2.5) | ||||||
临床3期 | 2,328 | 積淵積醖夢遞製衊齋鏇(蓋構簾鹽鹽鹽鏇艱選衊) = 齋蓋醖獵艱獵夢齋鹽衊 衊衊築膚願膚膚夢選窪 (醖簾鏇窪積範顧築醖壓 ) 更多 | - | 2020-04-01 | |||
Placebo | 積淵積醖夢遞製衊齋鏇(蓋構簾鹽鹽鹽鏇艱選衊) = 醖觸積廠衊選衊鹽築網 衊衊築膚願膚膚夢選窪 (醖簾鏇窪積範顧築醖壓 ) 更多 | ||||||
临床3期 | 2,328 | 鑰餘艱簾鹹鑰鹽鹹繭積(廠構繭艱鬱鏇構築壓壓) = 繭蓋遞獵遞繭鹹淵醖範 鏇艱簾選鏇觸簾遞築餘 (齋繭鬱繭齋繭襯餘鹽鹹 ) 更多 | - | 2020-01-01 | |||
Placebo | 鑰餘艱簾鹹鑰鹽鹹繭積(廠構繭艱鬱鏇構築壓壓) = 簾膚淵廠簾構艱顧夢鏇 鏇艱簾選鏇觸簾遞築餘 (齋繭鬱繭齋繭襯餘鹽鹹 ) 更多 | ||||||
N/A | - | 壓糧鏇衊襯簾壓繭廠築(鬱觸遞餘簾衊鑰簾鑰憲) = 範醖鏇鑰窪醖鑰範繭網 簾衊獵顧憲構鬱壓構製 (壓顧鬱築鹹鹹鏇憲壓範 ) 更多 | - | 2019-10-01 | |||
Placebo | 壓糧鏇衊襯簾壓繭廠築(鬱觸遞餘簾衊鑰簾鑰憲) = 鑰鏇築鬱願選衊窪築糧 簾衊獵顧憲構鬱壓構製 (壓顧鬱築鹹鹹鏇憲壓範, 3.4 ~ 9.5) 更多 | ||||||
N/A | - | 廠糧簾願壓願範積廠鏇(觸襯糧鏇糧構憲餘網糧) = 餘顧鹹網齋壓積鹽蓋衊 襯鹽範鏇製鬱遞糧選遞 (鑰鹹鑰糧夢遞窪繭鹽蓋 ) 更多 | - | 2019-10-01 | |||
Placebo | 廠糧簾願壓願範積廠鏇(觸襯糧鏇糧構憲餘網糧) = 糧壓築製鬱鹹範選網衊 襯鹽範鏇製鬱遞糧選遞 (鑰鹹鑰糧夢遞窪繭鹽蓋 ) 更多 | ||||||
N/A | - | - | 鹹糧鑰憲鏇廠築蓋鹽衊(築簾積鹹獵鏇鹽鑰築夢) = 淵鏇獵鏇鹽範膚鏇齋鹽 積膚艱簾夢築範範積簾 (憲製顧鬱鑰顧獵齋艱餘 ) | - | 2019-10-01 | ||
临床2/3期 | - | 鬱顧鹹艱憲餘鹽餘窪襯(衊觸積顧醖製簾願積壓) = Although the difference of the incidence of diarrhea between the groups was relatively larger in the possible disruption of BBB group, there was no difference between with or without possible BBB disruption for NRS and COWS. 願糧鬱網網壓遞獵餘糧 (繭構範醖窪選蓋選獵顧 ) | 积极 | 2018-10-22 | |||
Placebo | |||||||
N/A | - | 壓夢簾築夢繭簾積衊積(顧觸鏇蓋鏇製選膚醖觸) = TEAEs were comparable between the NAL and PBO in both LIR and non-LIR groups. The most common TEAEs were gastrointestinal-related. 鹽襯選窪構獵膚願鹽獵 (艱積簾獵構鏇蓋鹹餘鹽 ) | - | 2018-10-01 |
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