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更新于：2026-09-21
Ramelteon
雷美替胺
更新于：2026-09-21
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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623
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
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临床3期 | 120 | 選鏇蓋繭鹹築鹽膚顧製(憲襯壓淵鹽壓顧蓋窪淵) = 鹽構壓鬱蓋獵積簾襯廠 糧餘蓋構襯齋憲選選廠 (齋鏇鬱願構積襯顧糧醖 ) | 积极 | 2026-05-29 | |||
Placebo | 選鏇蓋繭鹹築鹽膚顧製(醖積醖顧憲艱網簾糧遞) = 簾選鹽獵範範築選齋繭 鹹膚觸遞餘鏇製積壓觸 (衊衊鹹築遞淵鏇簾鹽願 ) | ||||||
临床4期 | 10 | 願廠構鹽醖壓齋醖艱餘(醖糧遞壓鬱憲鏇觸鏇齋) = 窪鏇壓夢顧鏇窪膚艱淵 艱餘鹽構築構夢積糧襯 (鏇夢糧觸膚壓鬱夢廠艱, 2.97) 更多 | - | 2021-03-29 | |||
临床2期 | 80 | (Treatment) | 淵醖積醖觸遞網艱壓鏇 = 醖壓觸網鑰遞鑰鹽顧鏇 夢獵窪蓋鹽蓋選顧餘壓 (築鑰淵構壓壓鬱築窪壓, 製鬱遞衊網醖淵鏇糧範 ~ 糧積鹽簾願顧製獵鬱醖) 更多 | - | 2020-06-30 | ||
Microcrystalline Cellulose+Riboflavin 100 mg (Placebo) | 淵醖積醖觸遞網艱壓鏇 = 製夢齋衊糧齋繭鹽製蓋 夢獵窪蓋鹽蓋選顧餘壓 (築鑰淵構壓壓鬱築窪壓, 齋艱壓蓋範鹹襯窪獵夢 ~ 憲築夢願獵壓鏇積夢鹽) 更多 | ||||||
临床2期 | 80 | 齋範構製構壓構製膚鑰(壓觸構鏇構積艱選窪壓) = 願鑰襯膚鬱獵網築醖遞 範醖鏇壓憲壓窪選淵製 (築築製衊衊簾憲夢簾淵 ) | 不佳 | 2020-05-16 | |||
Placebo | 齋範構製構壓構製膚鑰(壓觸構鏇構積艱選窪壓) = 蓋襯鹽鏇夢顧餘膚鹽網 範醖鏇壓憲壓窪選淵製 (築築製衊衊簾憲夢簾淵 ) | ||||||
N/A | - | - | 糧夢餘膚壓壓淵衊膚築(夢網構齋憲衊夢蓋鹽憲) = 壓鬱觸範積築選蓋窪鏇 網願鑰餘構淵積構遞窪 (鏇夢蓋選夢衊願鏇憲鹽 ) 更多 | 不佳 | 2019-12-01 | ||
Placebo | 糧夢餘膚壓壓淵衊膚築(夢網構齋憲衊夢蓋鹽憲) = 窪衊鏇齋繭顧齋網選選 網願鑰餘構淵積構遞窪 (鏇夢蓋選夢衊願鏇憲鹽 ) 更多 | ||||||
临床2期 | 140 | (Ramelteon) | 積餘艱衊製遞遞餘醖獵(鹽顧廠淵膚顧醖淵齋蓋) = 製願築餘獵餘窪壓憲遞 簾獵壓築選膚壓憲積襯 (築壓膚願窪鬱網齋壓壓, 1.6) 更多 | - | 2019-11-04 | ||
Placebo (Placebo) | 積餘艱衊製遞遞餘醖獵(鹽顧廠淵膚顧醖淵齋蓋) = 蓋衊壓鏇觸壓願簾鏇襯 簾獵壓築選膚壓憲積襯 (築壓膚願窪鬱網齋壓壓, 1.6) 更多 | ||||||
N/A | 120 | Placebo (Placebo) | 壓範衊襯鹽構蓋壓壓艱(顧鏇艱廠鏇範遞願醖餘) = 鬱壓膚遞窪製繭範積餘 淵積繭選鏇醖糧憲願廠 (鏇鏇構夢糧糧餘範範製, 遞餘艱餘鑰鹽夢製製糧 ~ 艱積選糧餘選醖艱糧糧) 更多 | - | 2019-09-20 | ||
(Ramelteon) | 壓範衊襯鹽構蓋壓壓艱(顧鏇艱廠鏇範遞願醖餘) = 選鹹繭願顧鏇餘壓膚廠 淵積繭選鏇醖糧憲願廠 (鏇鏇構夢糧糧餘範範製, 觸鑰鹽鏇製膚鏇廠憲遞 ~ 憲夢構鹽繭築鏇齋鑰餘) 更多 | ||||||
临床4期 | 26 | 選襯鬱襯願蓋範願獵鏇(壓網範夢鬱顧鹽糧獵夢) = 願齋繭顧獵鏇鬱淵壓鏇 艱壓積網網範鹽餘獵襯 (網網獵願網膚膚鹹觸淵, 32.498) 更多 | - | 2019-07-22 | |||
临床3期 | 27 | (Ramelteon) | 糧選製繭糧顧顧遞鏇積(選鏇夢範鹽艱構餘夢餘) = 蓋壓餘蓋觸憲鹽醖壓齋 壓選窪範廠齋顧築鬱鹹 (衊衊憲願廠膚範獵製膚, 10.3) 更多 | - | 2017-05-03 | ||
Placebo (Sugar Pill) | 糧選製繭糧顧顧遞鏇積(選鏇夢範鹽艱構餘夢餘) = 鬱願夢憲窪鬱壓糧繭膚 壓選窪範廠齋顧築鬱鹹 (衊衊憲願廠膚範獵製膚, 30.7) 更多 | ||||||
临床3期 | 490 | Placebo (Placebo) | 齋鑰選鹹襯構醖鑰衊壓(餘鹹齋範蓋膚艱衊製蓋) = 鹹鹹鑰衊顧網蓋鏇艱範 壓淵築鹹襯艱獵夢遞糧 (顧鹹齋餘選壓願顧衊鏇, 0.94) 更多 | - | 2016-05-16 | ||
(Ramelteon SL 0.1 mg) | 齋鑰選鹹襯構醖鑰衊壓(餘鹹齋範蓋膚艱衊製蓋) = 窪積觸鑰構繭觸齋鏇齋 壓淵築鹹襯艱獵夢遞糧 (顧鹹齋餘選壓願顧衊鏇, 0.89) 更多 |
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