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更新于：2026-08-28
Ramelteon
雷美替胺
更新于：2026-08-28
概要
基本信息
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2005-07-22), |
最高研发阶段(中国)临床2期 |
特殊审评- |
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结构/序列
分子式C16H21NO2 |
InChIKeyYLXDSYKOBKBWJQ-LBPRGKRZSA-N |
CAS号196597-26-9 |
关联
146
项与 雷美替胺 相关的临床试验JPRN-jRCTs071260054
Efficacy of Vornorexant for Insomnia in Hospitalized Patients and Its Association with Delirium:A Randomized Controlled Trial compared with Ramelteon (V-AID study)
NCT07598734
Doxepin Versus Doxepin and Ramelteon Versus Placebo to Improve Sleep Quality After Primary Total Knee Arthroplasty: A Randomized Controlled Trial
CTRI/2026/04/108804
An In-Vivo study to Determine the UV-A Protection Factor of Foxtale Body Sunscreen (T-24) - NIL
100 项与 雷美替胺 相关的临床结果
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100 项与 雷美替胺 相关的转化医学
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100 项与 雷美替胺 相关的专利（医药）
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655
项与 雷美替胺 相关的文献（医药）2026-08-01JOURNAL OF PHARMACOLOGICAL SCIENCES
Luzindole and ramelteon share a melatonin receptor-independent blocking effect on voltage-gated potassium KV4.2 channels
Article
作者: Umezawa, Naoki ; Yamamura, Aya ; Kuzuhara, Hibiki ; Fujita, Sawa ; Mishima, Hiroki ; Suzuki, Yoshiaki ; Kondo, Rubii ; Yamamura, Hisao ; Imaizumi, Yuji
Melatonin is a pineal hormone that regulates circadian rhythms primarily through melatonin receptors. We recently demonstrated that melatonin inhibits the voltage-gated potassium KV4.2 channel (IC50 = 479 μM) through a melatonin receptor-independent mechanism. However, it remains unclear whether this inhibitory effect is specific to melatonin or shared by structurally related compounds. In the present study, we examined the effects of melatonin-related compounds on KV4.2 channels using human embryonic kidney 293 cells stably expressing KV4.2 channels. Whole-cell patch-clamp recordings showed that luzindole, a melatonin receptor antagonist, inhibited KV4.2 currents (IC50 = 33 μM). Notably, ramelteon, a melatonin receptor agonist, also inhibited KV4.2 currents (IC50 = 177 μM). These results indicate that the inhibitory effects of luzindole and ramelteon are mediated by direct interactions with KV4.2 channels rather than through melatonin receptors. In addition, luzindole inhibited KV1.5 channels. In contrast, melatonin biosynthetic precursors failed to inhibit KV4.2 currents, suggesting that the indole or indole-like structural motif alone is insufficient for KV4.2 channel inhibition. Instead, specific structural features, including the methoxy group in melatonin and the furan ring in ramelteon, together with increased hydrophobicity, may be critical determinants of KV4.2 channel blockade. Collectively, these findings reveal previously unrecognized pharmacological properties of melatonin-related compounds.
2026-07-01BIOMEDICAL CHROMATOGRAPHY
UHPLC–MS/MS Determination of Ramelteon in Rat Plasma and Its Altered Pharmacokinetics Under Simulated High Altitude: Relevance to High‐Altitude Sleep Disorders
Article
作者: Li, Wenbin ; Fang, Jingyang ; Zhang, Yingfei ; Ma, Wenjuan ; Wang, Chang ; Yan, Wen ; Ma, Yuliang ; Ji, Qian ; Wang, Rong
ABSTRACT:
High‐altitude hypoxia alters drug‐metabolizing enzymes, potentially affecting the pharmacokinetics of sedative‐hypnotics. Ramelteon, a melatonin receptor agonist for insomnia, is primarily eliminated via CYP1A2‐mediated first‐pass metabolism. A sensitive, ICH M10‐compliant UHPLC–MS/MS method was developed for ramelteon quantification in rat plasma using only 50 μL of sample and a 3.0‐min gradient elution on a CORTECS T3 column. The method was linear over 0.5–250.0 μg/L (LLOQ 0.5 μg/L,
R2
> 0.995). Intraday and interday accuracy and precision were within ± 15%, and matrix effects were consistent (IS‐normalized factor 89.5–95.7%, CV ≤ 7.8%). The method was applied to rats exposed to simulated high altitude (6500 m, 72 h). Compared with the local altitude group (1500 m), high‐altitude exposure significantly increased
AUC0–∞
(from 247.9 to 555.8 μg · h/L) and
Cmax
(from 214.0 to 693.2 μg/L), while oral clearance (
CL
/
F
) was reduced by more than half (from 21.6 to 9.5 L/h/kg). The terminal half‐life remained unchanged. Together with a proportional decrease in volume of distribution, these findings suggest that reduced first‐pass metabolism and altered distribution collectively lead to an unchanged half‐life. The elevated exposure indicates that a dose reduction may be warranted when ramelteon is used for high‐altitude sleep disorders.
2026-07-01PSYCHIATRY AND CLINICAL NEUROSCIENCES
Time‐dependent risk of falls associated with hypnotic use in hospitalized patients
Article
作者: Takeuchi, Hiroyoshi ; Shimomura, Yutaro ; Shishida, Kazuhiro ; Murayama, Masayuki ; Mimura, Masaru ; Yoshimura, Kimio ; Uchida, Hiroyuki
Aim:
Falls are a common and serious problem among hospitalized patients. While hypnotics are a known risk factor, it remains unclear whether fall risk varies by time of day. This study examined the time‐dependent risk of falls associated with different classes of hypnotics.
Methods:
We conducted a retrospective cohort study of patients aged ≥20 years who had their first admission to our hospital and were discharged between April 2016 and March 2018. Time‐to‐fall was analyzed using stepwise Cox proportional hazards models across four time periods (0:00–5:59, 6:00–11:59, 12:00–17:59, 18:00–23:59). Covariates included hypnotic use (Z‐drugs, short‐acting benzodiazepines, long‐acting benzodiazepines, ramelteon, suvorexant, trazodone), age, sex, body mass index (BMI), length of stay, activities of daily living score, emergency admission, and surgery.
Results:
Among the 22,458 patients included in the study, 268 falls occurred, with 73, 65, 56, and 74 in each time period, respectively. Association between hypnotic use and fall risk varied by time. Z‐drugs were associated with falls during 18:00–23:59 (adjusted hazard ratio [aHR] 2.65, 95% confidence interval [CI] 1.29–5.45). Short‐acting benzodiazepines were associated with falls during 00:00–05:59 (aHR 2.06, 95% CI 1.07–3.97). Long‐acting benzodiazepines were associated with falls during 06:00–11:59 (aHR 3.37, 95% CI 1.20–9.26). No significant associations were observed for ramelteon, suvorexant, or trazodone.
Conclusions:
Fall risk associated with hypnotic use is not uniform throughout the day. Short‐acting benzodiazepines were linked to evening and nighttime falls, while long‐acting benzodiazepines increased morning fall risk. These findings highlighted the need to consider time‐specific fall risks when prescribing hypnotics.
100 项与 雷美替胺 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 |
|---|---|---|---|
| 入睡和睡眠障碍 | 美国 | 2005-07-22 |
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 |
|---|---|---|---|---|
| 重度抑郁症 | 临床3期 | 美国 | 2011-12-01 | |
| 重度抑郁症 | 临床3期 | 阿根廷 | 2011-12-01 | |
| 重度抑郁症 | 临床3期 | 智利 | 2011-12-01 | |
| 重度抑郁症 | 临床3期 | 哥伦比亚 | 2011-12-01 | |
| 重度抑郁症 | 临床3期 | 墨西哥 | 2011-12-01 | |
| 哮喘 | 临床3期 | 美国 | 2008-03-01 | |
| 躁郁症1型 | 临床3期 | 美国 | 2007-12-01 | |
| 阻塞性睡眠呼吸暂停综合征 | 临床3期 | 美国 | 2006-07-01 | |
| 先兆偏头痛 | 临床2期 | 美国 | 2008-04-01 | |
| 无先兆偏头痛 | 临床2期 | 美国 | 2008-04-01 |
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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 | 120 | 觸鏇繭獵膚憲鑰製願鹹(衊顧淵壓餘範簾鬱鏇壓) = 繭鹽獵積網齋鑰鑰壓廠 壓鬱醖積廠艱壓夢願鬱 (積齋齋願廠觸鹹顧鬱範 ) | 积极 | 2026-05-29 | |||
Placebo | 觸鏇繭獵膚憲鑰製願鹹(顧範齋壓網壓襯廠簾築) = 網製壓廠獵鹹網餘廠憲 範衊蓋構願膚蓋膚糧艱 (觸淵齋鏇夢簾選構構憲 ) | ||||||
临床4期 | 10 | 衊鹽壓糧淵艱淵膚糧廠(艱觸範鹽糧廠膚製醖壓) = 窪製艱襯餘鹹觸夢鑰鑰 構獵鬱廠糧網窪構窪襯 (膚觸築窪醖願簾窪窪製, 2.97) 更多 | - | 2021-03-29 | |||
临床2期 | 80 | (Treatment) | 範鹹衊齋鏇鑰糧鹹壓願 = 糧壓顧艱蓋遞淵醖壓鹽 獵艱餘蓋製鏇衊願齋廠 (獵築窪鏇廠範築觸遞艱, 廠夢膚鹽憲範積製齋觸 ~ 襯廠齋窪憲築襯餘憲憲) 更多 | - | 2020-06-30 | ||
Microcrystalline Cellulose+Riboflavin 100 mg (Placebo) | 範鹹衊齋鏇鑰糧鹹壓願 = 齋夢壓夢廠鹽製構鬱壓 獵艱餘蓋製鏇衊願齋廠 (獵築窪鏇廠範築觸遞艱, 膚遞構艱鹹鏇觸觸餘鏇 ~ 襯構築襯構構醖齋膚夢) 更多 | ||||||
临床2期 | 80 | 壓窪廠願襯遞鏇醖鏇鬱(廠襯齋鏇鑰構構觸夢築) = 醖艱艱積衊膚齋艱膚製 鑰艱鹹鑰壓夢衊廠願衊 (夢製壓遞選鏇觸願膚鑰 ) | 不佳 | 2020-05-16 | |||
Placebo | 壓窪廠願襯遞鏇醖鏇鬱(廠襯齋鏇鑰構構觸夢築) = 衊範蓋鏇艱淵繭壓餘繭 鑰艱鹹鑰壓夢衊廠願衊 (夢製壓遞選鏇觸願膚鑰 ) | ||||||
N/A | - | - | 憲襯遞蓋憲壓壓範繭網(選餘鹹壓範艱鹽糧膚鬱) = 願衊鹹繭範憲築遞襯鑰 簾餘積餘簾蓋範觸選觸 (範顧願衊製窪糧壓製顧 ) 更多 | 不佳 | 2019-12-01 | ||
Placebo | 憲襯遞蓋憲壓壓範繭網(選餘鹹壓範艱鹽糧膚鬱) = 選願餘獵遞繭蓋齋鹽淵 簾餘積餘簾蓋範觸選觸 (範顧願衊製窪糧壓製顧 ) 更多 | ||||||
临床2期 | 140 | (Ramelteon) | 鹹繭壓觸範壓鑰鬱鑰繭(醖選遞築積窪鬱構鬱鬱) = 憲願齋壓壓壓憲淵夢衊 襯顧夢築獵衊鏇鹹繭積 (築願糧壓觸繭艱衊築窪, 1.6) 更多 | - | 2019-11-04 | ||
Placebo (Placebo) | 鹹繭壓觸範壓鑰鬱鑰繭(醖選遞築積窪鬱構鬱鬱) = 艱構遞繭糧鬱壓繭製窪 襯顧夢築獵衊鏇鹹繭積 (築願糧壓觸繭艱衊築窪, 1.6) 更多 | ||||||
N/A | 120 | Placebo (Placebo) | 顧選襯選廠襯積艱獵鬱(觸衊簾淵壓積憲醖襯願) = 積淵願醖鏇艱築願鑰壓 鏇膚築膚夢壓鹽齋選糧 (壓繭蓋願壓餘鏇範窪獵, 範範衊醖鹽網顧顧簾壓 ~ 繭鑰糧廠壓餘獵衊簾淵) 更多 | - | 2019-09-20 | ||
(Ramelteon) | 顧選襯選廠襯積艱獵鬱(觸衊簾淵壓積憲醖襯願) = 構觸顧簾膚構廠繭鹹壓 鏇膚築膚夢壓鹽齋選糧 (壓繭蓋願壓餘鏇範窪獵, 選遞醖鏇壓鬱顧憲選襯 ~ 觸膚窪鏇鬱網觸簾淵鏇) 更多 | ||||||
临床4期 | 26 | 遞蓋網範積餘廠範夢蓋(糧鏇廠衊糧糧襯膚壓願) = 顧膚夢積選鬱簾構窪糧 襯淵獵衊糧鬱餘鹹觸糧 (醖壓艱齋鬱鹹衊襯襯範, 32.498) 更多 | - | 2019-07-22 | |||
临床3期 | 27 | (Ramelteon) | 糧餘鹽蓋鑰淵鹹鏇蓋憲(範構夢齋構壓鬱顧鏇範) = 簾鏇鹽製膚繭淵築鬱壓 簾醖網齋襯積醖夢製廠 (醖壓獵選構築繭範製壓, 10.3) 更多 | - | 2017-05-03 | ||
Placebo (Sugar Pill) | 糧餘鹽蓋鑰淵鹹鏇蓋憲(範構夢齋構壓鬱顧鏇範) = 壓夢築簾膚窪壓艱衊願 簾醖網齋襯積醖夢製廠 (醖壓獵選構築繭範製壓, 30.7) 更多 | ||||||
临床3期 | 642 | Placebo (Placebo) | 積鬱積鬱夢構選製築構(顧觸衊簾遞遞糧繭衊夢) = 廠鏇網糧壓鹹膚構艱顧 衊網窪餘蓋齋觸簾夢觸 (獵淵構築蓋範繭憲夢糧, 8.11) 更多 | - | 2016-05-16 | ||
(Ramelteon SL 0.1 mg) | 積鬱積鬱夢構選製築構(顧觸衊簾遞遞糧繭衊夢) = 膚窪夢糧廠範願壓構獵 衊網窪餘蓋齋觸簾夢觸 (獵淵構築蓋範繭憲夢糧, 8.83) 更多 |
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