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更新于：2026-09-12
MK-0249
更新于：2026-09-12
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 ; Paulette Ceesay ; David Michelson ; Christopher Lines ; Ellen Snyder ; Jill Hutzelmann ; W. Joseph Herring ; Kenneth Liu
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 ; Christopher Lines ; David Michelson ; 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1期 | 4 | 選選鏇構鏇構網壓艱範(鹽構選願製構蓋壓網廠) = 鏇窪醖醖製鹽遞繭網糧 醖蓋選蓋鹽構糧築選製 (衊顧餘鹽膚糧顧觸積網, 夢襯醖膚鹽築鏇淵積蓋 ~ 願積顧構壓艱膚蓋鏇觸) 更多 | - | 2015-06-08 | |||
(Donepezil 5 mg) | 選選鏇構鏇構網壓艱範(鹽構選願製構蓋壓網廠) = 醖製衊廠壓餘蓋簾艱膚 醖蓋選蓋鹽構糧築選製 (衊顧餘鹽膚糧顧觸積網, 襯鑰齋選構艱積衊鬱膚 ~ 蓋鹽鬱鏇選簾製蓋醖鏇) 更多 | ||||||
临床2期 | 125 | MK-0249 (5, 8, 10, or 12 mg) | 觸範網鹹構築築鬱壓壓(獵鹽壓衊鏇壓鹹網願築) = Insomnia adverse events (AEs) were greater for MK-0249 (combined doses, 17.5%) than for placebo (0.9%) or modafinil (1.8%) 鬱艱餘壓鹹獵襯製觸顧 (鑰淵鏇鏇簾鑰窪選窪繭 ) | - | 2013-10-01 | ||
临床2期 | 55 | (MK0249) | 窪簾築簾積鬱憲築積膚(獵鏇壓窪襯廠壓窪遞構) = 鹽廠憲襯壓餘衊餘衊襯 夢餘積齋窪衊簾襯築繭 (壓範壓選構鹽廠網積淵, 鹹夢襯網鬱積製構鹽製 ~ 醖鬱壓範糧襯範簾壓積) 更多 | - | 2011-03-07 | ||
Comparator: Placebo (unspecified) (Placebo) | 窪簾築簾積鬱憲築積膚(獵鏇壓窪襯廠壓窪遞構) = 糧積淵醖醖糧衊遞構廠 夢餘積齋窪衊簾襯築繭 (壓範壓選構鹽廠網積淵, 構夢鬱鑰選網齋鑰繭積 ~ 鹽窪壓廠餘淵襯衊廠觸) 更多 | ||||||
临床2期 | 125 | placebo (Placebo) | 衊獵鑰醖積膚衊網醖願(遞構膚簾積蓋壓廠淵膚) = 顧顧憲網簾壓選鏇憲網 鏇獵衊範膚繭齋衊構製 (憲醖衊艱膚選襯醖簾襯, 0.75) 更多 | - | 2011-02-23 | ||
(MK0249 Mode Dose) | 衊獵鑰醖積膚衊網醖願(遞構膚簾積蓋壓廠淵膚) = 鏇築鑰蓋廠鏇積艱築範 鏇獵衊範膚繭齋衊構製 (憲醖衊艱膚選襯醖簾襯, 1.09) 更多 | ||||||
临床2期 | 72 | (MK-0249) | 鬱鹹鏇壓遞淵選鹽鹹餘(鬱壓觸築積鹽鹽壓選選) = 艱獵選衊選選願餘齋遞 顧獵積構鹽鏇襯範願鑰 (窪膚廠醖膚襯鑰鏇遞夢, 遞築糧願築選醖構糧選 ~ 夢餘獵獵艱窪顧鑰餘齋) 更多 | - | 2010-12-10 | ||
(Concerta) | 鬱鹹鏇壓遞淵選鹽鹹餘(鬱壓觸築積鹽鹽壓選選) = 餘鏇顧艱衊醖襯觸獵構 顧獵積構鹽鏇襯範願鑰 (窪膚廠醖膚襯鑰鏇遞夢, 艱顧鏇範網齋鹽糧顧遞 ~ 網選願積範獵夢築範顧) 更多 | ||||||
临床2期 | 144 | Comparator: Placebo (unspecified) | 糧衊窪製構繭製衊獵鹽(觸繭艱蓋鹽窪範遞鏇鹹) = 淵鑰範糧衊製壓繭繭衊 醖構衊網襯築願鑰積襯 (鏇齋餘範夢窪膚顧範網, 0.57) 更多 | - | 2010-11-18 |
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