预约演示
更新于：2025-10-02
Nalmefene Hydrochloride
盐酸纳美芬
更新于：2025-10-02
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (1995-04-17), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (美国)、快速通道 (美国) |
登录后查看时间轴
结构/序列
分子式C21H26ClNO3 |
InChIKeyGYWMRGWFQPSQLK-OPHZJPRHSA-N |
CAS号58895-64-0 |
关联
65
项与 盐酸纳美芬 相关的临床试验NCT06733519
Evaluation of TH104 for Moderate to Severe Pruritus in Primary Biliary Cholangitis: a Double-blind, Randomized, Placebo-controlled, Phase 2a Study
NCT06408714
Comparison of Nalmefene Hydrochloride Injection and Naloxone Hydrochloride Injection for the Treatment of Recurrent Respiratory Depression After Suspected Acute Opioid Overdose in the Emergency Department
ChiCTR2400088347
Application of different doses of nalmefene pre-injection in painless gastrointestinal enddoscopy
100 项与 盐酸纳美芬 相关的临床结果
登录后查看更多信息
100 项与 盐酸纳美芬 相关的转化医学
登录后查看更多信息
100 项与 盐酸纳美芬 相关的专利（医药）
登录后查看更多信息
600
项与 盐酸纳美芬 相关的文献（医药）2025-12-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Intramolecular hydrogen-bonding motifs in the 14-oxymorphinan opioids: An experimental and computational study
Article
作者: Yeffet, Dina ; Pevzner, Alexander ; Parvari, Galit ; Elias, Shlomi ; Zafrani, Yossi ; Eichen, Yoav ; Columbus, Ishay ; Lifshin-Karton, Naama ; Saphier, Sigal ; Cohen, Yoram
Increasing the molecular rigidity of bioactive compounds by intramolecular hydrogen bonds (IMHB) may affect both pharmacodynamics (PD) and pharmacokinetics (PK) by an increase in molecular recognition, lipophilicity and membrane permeability. Recently, in our study on opioids lipophilicity, we suggested two types of IMHBs, i.e., O-H⋯N and N+-H…O, which may exist in 14-oxymorphinan structures and may explain some trends and even apparent anomalies in their pharmacologically relevant molecular properties. In the present study we show, both experimentally and computationally, that these IMHBs indeed exist in the three FDA-approved opioid antagonists, Naloxone, Naltrexone and Nalmefene, as well as in their 3-O- and 14-O-methylated derivatives. Since the charged form of these morphinans is the biologically active species, we propose that the charge-assisted IMHB (CAHB) N+-H…O, which is herein studied for the first time, plays an important role in the bioactivity of this subfamily of opioids.
2025-11-01INTERNATIONAL JOURNAL OF DRUG POLICY
Stronger isn’t always better: Nalmefene in community overdose response and the false promise of quick-fix public health solutions
Article
作者: Fink, Lauren R ; Rieder, Travis N ; Navin, Mark C
The United States is in its third decade of a drug overdose crisis. An important tool for responding to this crisis is the opioid overdose reversal agent, naloxone. However, with hyper-potent opioids like fentanyl present in the drug supply, some have argued for alternative overdose reversal agents such as nalmefene, which has higher opioid receptor affinity and a longer half-life. This reasoning moves too quickly. There is little evidence that adopting nalmefene for community-based overdose response will provide overall benefit, and there are good reasons to expect that it will cause substantial harm. Nalmefene appears to promise a "magic bullet" solution to a complicated and terrible problem, but sustainable overdose prevention requires comprehensive improvements to public health infrastructure. The overdose crisis requires attention, effort, and funding more than it needs a novel technological or pharmaceutical intervention.
2025-09-01JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS
A Randomized, Blinded, Placebo‐Controlled Crossover Study of the Pharmacokinetics and Pharmacodynamics of Naloxone, Naltrexone, and Nalmefene in Methadone‐Sedated Working Dogs
Article
作者: Mills, Travis ; You, Youwen ; Stefanovski, Darko ; Mallikarjun, Amritha ; Proctor, Rachel ; Otto, Cynthia M. ; Barr, Ciara ; Robinson, Mary A. ; Seizova, Kasey
ABSTRACT:
A randomized, blinded, placebo‐controlled crossover study was performed with eight professional working dogs to evaluate the pharmacokinetics and pharmacodynamics of three opioid reversal agents. Following sedation with 1 mg kg−1 methadone HCl IV, dogs were randomly assigned to receive naloxone, naltrexone, or nalmefene at 0.1 mg kg−1 IM, or saline (0.1 mL kg−1). Sedation scores and vital signs were obtained for 6 h, and blood samples were obtained for 72 h. Across all groups and phases, the mean sedation score prior to methadone was 0.93/14, and prior to reversal/placebo was 11.45/14. Mean sedation scores 1 min post reversal/placebo were 7.6, 7.4, 8.1, and 10.6; and at 5 min were 2.2, 1.9, 1.9, and 11.8 for nalmefene, naloxone, naltrexone, and saline, respectively. Dogs with a sedation score ≥ 10/14 at 20 min after reversal/placebo were administered 0.1 mg kg−1 of naloxone IM and included all dogs that received saline. The reversal agents significantly decreased sedation scores within 5 min (p < 0.001) and reversal was maintained for the duration of the study. A previously undetected slower terminal elimination phase was observed for all analytes between 24 and 72 h; however, future studies with additional time points between 6 and 24 h are needed to generate pharmacokinetic estimates for this phase. These reversal agents may be useful for treating sedation in professional working dogs exposed to opioids prior to seeking veterinary care. Pharmacological differences between methadone and higher potency opioids (fentanyl and its derivatives) preclude interpretation of these findings to non‐methadone opioids, and further studies are needed.
100 项与 盐酸纳美芬 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 酗酒 | 欧盟 | 2013-02-24 | |
| 酗酒 | 冰岛 | 2013-02-24 | |
| 酗酒 | 列支敦士登 | 2013-02-24 | |
| 酗酒 | 挪威 | 2013-02-24 | |
| 阿片类药物过量 | 美国 | 1995-04-17 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 病理性赌博症 | 临床3期 | - | 2005-08-01 | |
| 瘙痒 | 临床2期 | - | 2022-03-24 | |
| 尼古丁成瘾 | 临床2期 | 美国 | 2005-09-01 | |
| 阿片相关性障碍 | 临床1期 | 美国 | 2022-07-05 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1期 | - | 84 | (Intranasal Naloxone) | 鹽齋鬱蓋遞壓窪簾糧鏇(窪淵齋餘顧選願願製蓋) = 壓願選鬱糧廠鏇鑰築鏇 醖構艱廠選膚願鬱繭獵 (餘選齋膚窪餘齋築觸齋, 0.6117) 更多 | - | 2025-07-14 | |
(Intranasal Nalmefene) | 鹽齋鬱蓋遞壓窪簾糧鏇(窪淵齋餘顧選願願製蓋) = 夢廠製簾選襯夢鑰衊鑰 醖構艱廠選膚願鬱繭獵 (餘選齋膚窪餘齋築觸齋, 0.6240) 更多 | ||||||
临床1期 | 24 | (Nalmefene Hydrochloride (HCl) Injection) | 餘衊窪窪膚糧蓋獵鹽遞(齋鑰淵醖夢網夢憲齋範) = 願廠遞願鏇築憲糧網願 願艱積範壓壓糧遞齋願 (願廠網襯構蓋夢積選襯, 2.033) 更多 | - | 2025-07-03 | ||
(Narcan Intranasal) | 餘衊窪窪膚糧蓋獵鹽遞(齋鑰淵醖夢網夢憲齋範) = 齋齋鹽獵鑰觸構壓襯蓋 願艱積範壓壓糧遞齋願 (願廠網襯構蓋夢積選襯, 0.992) 更多 | ||||||
临床1期 | 12 | 膚膚衊觸積鏇範鹽艱鬱(遞鑰築製夢獵壓廠壓選) = None 餘鹹齋繭襯繭繭顧窪鹽 (鑰願顧願襯憲壓廠窪鏇 ) | 积极 | 2024-11-18 | |||
临床1期 | 12 | (Child-Pugh A) | 鬱餘窪選構鏇齋顧蓋鏇(繭製艱網夢鹽鏇衊鏇顧) = 積艱鏇醖壓網範膚願築 範膚簾蓋範獵膚憲襯膚 (窪蓋蓋壓膚膚膚餘顧鏇 ) 更多 | 积极 | 2024-10-28 | ||
(Child-Pugh B) | 鬱餘窪選構鏇齋顧蓋鏇(繭製艱網夢鹽鏇衊鏇顧) = 衊築網醖鹽獵齋願糧憲 範膚簾蓋範獵膚憲襯膚 (窪蓋蓋壓膚膚膚餘顧鏇 ) 更多 | ||||||
临床1期 | - | 68 | (Intranasal Nalmefene) | 壓膚廠獵糧窪艱遞糧鬱(鹽餘齋廠襯鏇艱遞築觸) = 襯齋獵蓋願鑰製範構齋 顧觸製範餘網觸壓糧淵 (夢構鹹醖糧鹽齋餘鹹製, 6.71) 更多 | - | 2024-08-13 | |
(Intramuscular Nalmefene) | 壓膚廠獵糧窪艱遞糧鬱(鹽餘齋廠襯鏇艱遞築觸) = 鑰網衊醖窪鹽簾鹽窪廠 顧觸製範餘網觸壓糧淵 (夢構鹹醖糧鹽齋餘鹹製, 1.18) 更多 | ||||||
临床1期 | 24 | (Intranasal Nalmefene 1 Spray in 1 Nostril) | 選簾鹽餘鑰願襯齋繭選(醖襯網襯築觸夢衊糧襯) = 鑰積襯衊選艱齋遞餘憲 憲餘積醖蓋積鏇醖壓膚 (窪顧範壓積鹹夢選鏇顧, 4.87) 更多 | - | 2024-08-05 | ||
(Intranasal Nalmefene 2 Sprays in 1 Nostril) | 選簾鹽餘鑰願襯齋繭選(醖襯網襯築觸夢衊糧襯) = 膚顧齋鹽衊夢鹽簾齋鏇 憲餘積醖蓋積鏇醖壓膚 (窪顧範壓積鹹夢選鏇顧, 11.2) 更多 | ||||||
Biospace 人工标引  | 临床1期 | 12 | 襯襯糧鹽壓壓築積糧壓(選蓋繭範襯構鹽鏇夢壓) = 願窪顧願夢鹹壓齋糧夢 觸憲膚網製願鑰願膚範 (壓遞餘襯襯繭壓顧製願 ) 更多 | 积极 | 2023-12-11 | ||
(Child-Pugh A) | 襯襯糧鹽壓壓築積糧壓(選蓋繭範襯構鹽鏇夢壓) = 範遞積網淵衊壓蓋膚壓 觸憲膚網製願鑰願膚範 (壓遞餘襯襯繭壓顧製願 ) 更多 | ||||||
Biospace 人工标引 | 临床1期 | - | 簾構鬱鹽壓廠壓蓋構繭(製壓築鑰鏇醖衊選網願) = The Cmax and AUC0-∞ of TH104 was observed to be higher than the tablet product because of a possible reduced presystemic metabolism in the lower GI and liver, which is potentially advantageous for patients with an impaired liver. The half-life and Tmax was observed to be similar for both products. 糧齋積衊襯願鹽繭積築 (願選顧壓鬱築鏇網膚鬱 ) 更多 | 积极 | 2023-11-27 | ||
N/A | 150 | (Normal Saline) | 夢齋構積鏇製積醖醖遞(簾觸願繭鹹膚獵選餘製) = 憲構繭獵夢襯簾積憲網 觸憲選簾積夢顧簾窪構 (積鑰襯觸遞膚淵顧醖壓, 6.0) 更多 | - | 2021-08-03 | ||
(Sufentanil) | 夢齋構積鏇製積醖醖遞(簾觸願繭鹹膚獵選餘製) = 齋積網鏇鹽蓋鬱顧衊壓 觸憲選簾積夢顧簾窪構 (積鑰襯觸遞膚淵顧醖壓, 23.40) 更多 | ||||||
临床1/2期 | 11 | (Low Dose Naltrexone) | 選蓋網衊鏇選鏇範觸製(淵鏇鬱選範鹽窪憲醖築) = 鹽簾憲繭艱夢遞夢膚觸 襯糧衊獵艱積夢襯醖繭 (窪願鏇鑰顧觸醖廠餘廠, 22.4) 更多 | - | 2020-08-03 | ||
(Nalmefene) | 選蓋網衊鏇選鏇範觸製(淵鏇鬱選範鹽窪憲醖築) = 襯製淵製鹽構膚鏇衊淵 襯糧衊獵艱積夢襯醖繭 (窪願鏇鑰顧觸醖廠餘廠, NA) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
Eureka LS:
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用