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更新于：2025-05-24
MK-0249
更新于：2025-05-24
概要
基本信息
在研机构- |
权益机构- |
最高研发阶段终止临床2期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
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结构/序列
分子式C23H24F3N3O2 |
InChIKeyDDDZBLNULGDPGA-UHFFFAOYSA-N |
CAS号862309-06-6 |
关联
5
项与 MK-0249 相关的临床试验NCT00874939
A Randomized Clinical Trial To Evaluate the Single Dose Acute Effects of MK-0249 and Donepezil On Cognitive Function In Adult Patients With Alzheimer's Disease
NCT00620659
Phase IIa, Randomized, Double-blind, Placebo-controlled, 3-period Crossover, Adaptive Dose Design, Clinical Trial to Evaluate Safety & Efficacy of MK0249 in Treating Refractory Excessive Daytime Sleepiness in Patients With Obstructive Sleep Apnea/Hypopnea Syndrome Appropriately Using nCPAP Therapy.
NCT00506077
A Phase IIa, Randomized, Double-Blind, Placebo-Controlled, 2-Period, Cross-Over Clinical Trial to Study the Safety and Efficacy of MK0249 for the Treatment of Cognitive Impairment in Patients With Schizophrenia
100 项与 MK-0249 相关的临床结果
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100 项与 MK-0249 相关的转化医学
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100 项与 MK-0249 相关的专利（医药）
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16
项与 MK-0249 相关的文献（医药）2014-01-01Journal of nuclear medicine : official publication, Society of Nuclear Medicine1区 · 医学
11C-MK-8278 PET as a Tool for Pharmacodynamic Brain Occupancy of Histamine 3 Receptor Inverse Agonists
1区 · 医学
Article
作者: Iannone, Robert ; Bormans, Guy ; Cerchio, Kristine ; Plalcza, John ; Koole, Michel ; Burns, Donald H. ; Han, Lingling ; Renger, John ; Van Hecken, Anne ; De Lepeleire, Inge ; de Hoon, Jan ; Hamill, Terence G. ; Sanabria-Bohrquez, Sandra M. ; Depre, Marleen ; Mozley, David P. ; Van Laere, Koenraad J. ; Hargreaves, Richard J.
METHODS:
Using PET and a novel high-affinity and selective radioligand (11)C-MK-8278, we studied the tracer biodistribution, quantification, and brain H3 receptor occupancy (RO) of MK-0249 and MK-3134, 2 potential IA drugs targeting cerebral H3 receptors, in 6 healthy male subjects (age, 19-40 y). The relationship among H3 IA dose, time on target, and peripheral pharmacokinetics was further investigated in 15 healthy male volunteers (age, 18-40 y) with up to 3 PET scans and 3 subjects per dose level.
RESULTS:
The mean effective dose for (11)C-MK-8278 was 5.4 ± 1.1 μSv/MBq. Human brain kinetics showed rapid high uptake and fast washout. Binding potential values can be assessed using the pons as a reference region, with a test-retest repeatability of 7%. Drug RO data showed low interindividual variability per dose (mean RO SD, 2.1%), and a targeted 90% RO can be reached for both IAs at clinically feasible doses.
CONCLUSION:
(11)C-MK-8278 is a useful novel PET radioligand for determination of human cerebral H3 receptor binding and allows highly reproducible in vivo brain occupancy of H3-targeting drugs, hereby enabling the evaluation of novel compounds in early development to select doses and schedules.
2013-10-01Sleep medicine3区 · 医学
Alertness and psychomotor performance effects of the histamine-3 inverse agonist MK-0249 in obstructive sleep apnea patients on continuous positive airway pressure therapy with excessive daytime sleepiness: a randomized adaptive crossover study
3区 · 医学
Article
作者: Duane Snavely ; Thomas Roth ; Christopher Lines ; David Michelson ; Paulette Ceesay ; Ellen Snyder ; Jill Hutzelmann ; Kenneth Liu ; W. Joseph Herring
OBJECTIVES:
We aimed to evaluate the efficacy of the selective H3 receptor inverse agonist MK-0249 to treat excessive daytime sleepiness (EDS).
METHODS:
In this three-period, double-blind, crossover study, 125 patients (100 men, 25 women; mean age, 48.6 years) with obstructive sleep apnea receiving nasal continuous positive airway pressure therapy who had refractory EDS were randomized to 2 weeks each of daily MK-0249 (5, 8, 10, or 12 mg, adaptively assigned), modafinil 200 mg, and placebo. At baseline and after each treatment period, six maintenance of wakefulness tests (MWT) and Psychomotor Vigilance Tasks (PVT) were conducted at 2-h intervals, beginning 1h postdose (∼09:00). The Epworth sleepiness scale (ESS), Clinical Global Impression of Severity (CGIS) and Digit Symbol Substitution Test (DSST) also were assessed. The primary end point was MWT sleep latency averaged over the first four time points (MWT-early).
RESULTS:
MWT-early mean change from baseline sleep latency at week 2 was 1.2 min for placebo, 2.1 min for MK-0249 (top two doses pooled; P>.05 vs. placebo), and 5.9 min for modafinil (P < or = .001 vs. placebo). MK-0249 showed improvements vs placebo on secondary and exploratory end points of ESS, CGIS, PVT, and DSST. Insomnia adverse events (AEs) were greater for MK-0249 (combined doses, 17.5%) than for placebo (0.9%) or modafinil (1.8%).
CONCLUSION:
MK-0249 did not significantly affect MWT sleep latency. However, the pattern of improvement on subjective ratings and psychomotor performance end points suggested that MK-0249 was associated with changes in aspects of cognition and performance not captured by the MWT.
2013-05-01Schizophrenia research2区 · 医学
Randomized crossover study of the histamine H3 inverse agonist MK-0249 for the treatment of cognitive impairment in patients with schizophrenia
2区 · 医学
Article
作者: Ying Zhang ; David Michelson ; Christopher Lines ; Duane Snavely ; Michael F. Egan ; Regina Gottwald ; Xin Zhao ; Lyn Harper-Mozley
BACKGROUND:
Current antipsychotic treatments have little impact on the cognitive deficits associated with schizophrenia. It has been proposed that agents which promote histamine release may enhance cognition. We evaluated whether the H3 inverse agonist MK-0249 might improve cognitive deficits in patients with schizophrenia.
METHODS:
Outpatients (N=55) with schizophrenia between ages 21 and 55 who were clinically stable, experienced no more than mild to moderate overall symptoms (PANSS score total 36-75), and were taking a stable dose of antipsychotic medication were randomized to MK-0249 10mg and placebo in a multi-center, randomized, double-blind, 2-period (4-weeks per period), cross-over study. The primary efficacy endpoint was the mean change from baseline at 4-weeks of treatment in the total cognitive score on the Brief Assessment of Cognition in Schizophrenia (BACS) Battery. Other assessments of cognition were also performed.
RESULTS:
A total of 46 patients completed the study. MK-0249 10mg did not demonstrate a statistically significant difference compared to placebo in the mean change from baseline in the total cognitive score on the BACS battery after 4-weeks of treatment (-0.1, 95% CI: -2.3, 2.1) or with regard to secondary measures of attention/processing speed, episodic memory, or working memory after 4-weeks of treatment. The incidence of adverse events was greater during the MK-0249 treatment period (25/52 patients, 48.1%) compared to the placebo treatment period (15/51 patients, 29.4%).
CONCLUSION:
MK-0249 10mg once daily was not superior to placebo in the treatment of cognitive impairment in patients with schizophrenia after 4-weeks. (Clinicaltrials.gov: NCT00506077).
100 项与 MK-0249 相关的药物交易
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外链
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 白天过度嗜睡 | 临床2期 | - | 2008-02-01 | |
| 低通气综合征 | 临床2期 | - | 2008-02-01 | |
| 阻塞性睡眠呼吸暂停低通气综合征 | 临床2期 | - | 2008-02-01 | |
| 认知功能障碍 | 临床2期 | - | 2007-12-01 | |
| 偏执型精神分裂症 | 临床2期 | - | 2007-12-01 | |
| 注意缺陷障碍伴多动 | 临床2期 | - | 2007-07-01 | |
| 阿尔茨海默症 | 临床2期 | - | 2006-11-01 | |
| 精神分裂症 | 临床2期 | 美国 | - | |
| 睡眠呼吸暂停综合征 | 临床2期 | 美国 | - | |
| 肥胖 | 临床1期 | 美国 | - |
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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 | 125 | MK-0249 (5, 8, 10, or 12 mg) | 淵願觸獵顧鹽醖選觸壓(蓋襯製醖鹹鏇窪餘衊蓋) = Insomnia adverse events (AEs) were greater for MK-0249 (combined doses, 17.5%) than for placebo (0.9%) or modafinil (1.8%) 廠蓋鬱齋鹹艱構製簾廠 (築窪膚醖餘窪顧獵齋鏇 ) | - | 2013-10-01 | ||
临床2期 | 55 | (MK0249) | 簾鑰蓋範鹽壓窪壓糧廠(窪鹽願廠築壓願鹹艱構) = 鬱積築夢積憲夢鏇夢衊 顧窪艱襯鑰憲選範選艱 (築糧鏇鬱憲衊網蓋廠願, 襯遞齋獵鏇積餘壓積廠 ~ 獵鬱餘製鏇鬱衊膚艱簾) 更多 | - | 2011-03-07 | ||
Comparator: Placebo (unspecified) (Placebo) | 簾鑰蓋範鹽壓窪壓糧廠(窪鹽願廠築壓願鹹艱構) = 製鏇壓餘艱鏇遞夢糧構 顧窪艱襯鑰憲選範選艱 (築糧鏇鬱憲衊網蓋廠願, 鬱夢範觸積選糧淵鏇獵 ~ 壓廠顧獵選網夢醖遞夢) 更多 | ||||||
临床2期 | 72 | (MK-0249) | 蓋觸鏇鹹艱壓蓋廠醖獵(鏇顧選憲遞構窪艱窪願) = 窪築網願淵積膚淵簾鹹 淵糧淵蓋顧憲觸糧鏇遞 (選繭醖襯積衊鬱憲夢壓, 願獵範醖衊夢憲鑰衊糧 ~ 顧範齋蓋襯餘鏇願繭構) 更多 | - | 2010-12-10 | ||
(Concerta) | 蓋觸鏇鹹艱壓蓋廠醖獵(鏇顧選憲遞構窪艱窪願) = 遞衊糧築窪範鏇艱鬱顧 淵糧淵蓋顧憲觸糧鏇遞 (選繭醖襯積衊鬱憲夢壓, 顧憲淵積範襯淵餘餘獵 ~ 範衊憲築衊鬱齋鑰鹹遞) 更多 | ||||||
临床2期 | 144 | Comparator: Placebo (unspecified) | 鏇鬱簾膚醖醖糧鏇糧壓(觸繭願繭壓願獵選蓋鑰) = 鏇鹹選醖獵膚觸壓範艱 膚遞願繭憲積膚顧築淵 (淵簾窪醖製積鏇獵遞鏇, 0.57) 更多 | - | 2010-11-18 |
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