更新于：2024-06-29
Lorcaserin Hydrochloride
盐酸绿卡色林
更新于：2024-06-29
概要
基本信息
在研机构- |
最高研发阶段撤市 |
首次获批日期 美国 (2012-06-27), |
最高研发阶段(中国)- |
特殊审评孤儿药 (美国)、罕见儿科疾病 (美国)、孤儿药 (欧盟) |
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结构
分子式C11H15Cl2N |
InChIKeyITIHHRMYZPNGRC-QRPNPIFTSA-N |
CAS号846589-98-8 |
关联
52
项与 盐酸绿卡色林 相关的临床试验Pilot Trial of Acute Effect of Lorcaserin to Reduce Patient-Reported Symptoms of Taxane- and Oxaliplatin-Induced Peripheral Neuropathy
A Multicenter, Double-Blind, Randomized, Placebo-Controlled, Parallel-Group Study With Open-Label Extension Phase of Lorcaserin as Adjunctive Treatment in Subjects With Dravet Syndrome
Human Laboratory Screening of Lorcaserin in Smokers With Alcohol Use Disorder
100 项与 盐酸绿卡色林 相关的临床结果
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100 项与 盐酸绿卡色林 相关的转化医学
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100 项与 盐酸绿卡色林 相关的专利（医药）
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432
项与 盐酸绿卡色林 相关的文献（医药）2024-03-01CNS & neurological disorders drug targets
Lorcaserin: Worthy of Further Insights? Results from Recent Research
Article
作者: Mazza, Marianna ; Abbate, Antonio ; Marano, Giuseppe ; De Berardis, Domenico ; Martinotti, Giovanni ; Biondi-Zoccai, Giuseppe ; Romagnoli, Enrico ; Kotzalidis, Georgios D ; Sani, Gabriele
Abstract::
Lorcaserin is a 3-benzazepine that binds 5-HT2C serotonin receptors in the hypothalamus,
where it mediates lack of hunger and/or satiety, and in the ventral tegmental area, the site of origin of
the mesolimbic and mesocortical dopaminergic projections, which mediate pleasure and reward. The
drug has been first developed for the treatment of obesity, where it has shown efficacy, and subsequently
trialed to counter substance use (mostly cocaine, cannabis, opioids, and nicotine) and craving,
but showed inconsistent effects. Since 2020, the US Food and Drug Administration obtained that the
drug was voluntarily withdrawn from the US market on the grounds that its long-term use was found
to be associated with a greater incidence of some types of cancer. Provided it can show to be free from
cancerogenic effects, ongoing research suggests that lorcaserin may have therapeutic potential for a
variety of disorders and conditions beyond obesity. Since 5-HT2C receptors are involved in many diversified
physiological functions (mood, feeding, reproductive behavior, neuronal processes related to
impulsiveness, and modulating reward-related mechanisms) this drug has the potential to treat different
central nervous system conditions, such as depression and schizophrenia.
2024-02-01Drug and alcohol dependence
Results of a randomized, double-blind, placebo-controlled trial of lorcaserin in cocaine use disorder
Article
作者: Ramey, Tatiana ; Gyaw, Shwe ; Devine, Eric G ; McCann, David J ; Chen, Hegang H
BACKGROUND:
Cocaine use disorder (CUD) is a major public health problem for which there is no approved pharmacotherapy. The primary purpose of this study was to evaluate the ability of lorcaserin, a 5-hydroxytryptamine2 C (5-HT2 C) receptor agonist, to facilitate abstinence in individuals seeking treatment for CUD.
METHODS:
This was a 12-site, randomized, parallel arm study with a 13-week Treatment Phase that included a 1-week, single-blind run-in period when all participants received twice daily 15mg acetazolamide capsules (a medication adherence marker), followed by randomization to either twice daily 10mg lorcaserin or placebo capsules for the remaining 12 weeks. Pre-randomization data were utilized in an enrichment strategy aimed at achieving high levels of medication adherence and low placebo response rates in a subgroup of participants that qualified for the "efficacy population." For lorcaserin vs. placebo, the primary efficacy endpoint was the proportion of participants in the efficacy population achieving abstinence during the last three weeks of treatment, as evidenced by self-report of no cocaine use, confirmed by urine testing.
RESULTS:
Within the efficacy population, 1.1% of 91 participants receiving lorcaserin and 4.3% of 92 receiving placebo achieved abstinence during the last 3 weeks of treatment. Among all randomized participants, 2.5% of 118 receiving lorcaserin and 5.6% of 124 receiving placebo achieved similar abstinence. Study participants receiving lorcaserin exhibited significantly greater reductions in body weight and BMI, indicating that medication adherence was sufficient to produce a pharmacological effect.
CONCLUSIONS:
Twice daily 10mg lorcaserin failed to demonstrate efficacy in the treatment of CUD.
2024-01-01Pharmacology, biochemistry, and behavior
Interactions between lorcaserin and opioids: Ventilation and food-versus-drug choice
Article
作者: Maguire, David R
Lorcaserin, a selective serotonin 2C (5-HT2C) receptor agonist, was approved for treating obesity and has been investigated for treating substance use disorders including those involving opioids. Although lorcaserin was withdrawn from the market, interest in the therapeutic potential of drugs acting at 5-HT2C receptors continues, supporting the need to further characterize potential adverse effects especially when combined with drugs of abuse. This study examined acute effects of lorcaserin on opioid-induced ventilatory depression, which is the primary cause of overdose, and opioid self-administration, which models factors contributing to opioid abuse, in male and female rhesus monkeys. In one group (n = 4), effects of morphine (0.178 to 5.6 mg/kg, s.c.), fentanyl (0.0032 to 0.1 mg/kg, s.c.), and lorcaserin (0.1 to 1.78 mg/kg, s.c.) alone as well as effects of lorcaserin with each opioid on ventilation were determined using head plethysmography. Another group (n = 5) responded under a food versus fentanyl (0.1 to 3.2 μg/kg/infusion, i.v.) choice procedure, and lorcaserin (0.32 to 1.78 mg/kg, i.v.) was given as a pretreatment. Lorcaserin dose-dependently decreased minute volume to below 70 % of baseline when administered alone and increased the potency of morphine and fentanyl. Consistent with previous studies, lorcaserin failed to alter choice of fentanyl over food. This study demonstrates the novel finding that lorcaserin alone decreases ventilation and enhances the ventilatory-depressant effects of opioids. Taken together with previous studies, these results suggest that combining a 5-HT2C receptor agonist such as lorcaserin with an opioid could increase the risk of ventilatory depression without the benefit of decreasing abuse.
100 项与 盐酸绿卡色林 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 |
|---|---|---|---|
| 肥胖 | 美国 | 2012-06-27 | |
| 肥胖 | 美国 | 2012-06-27 |
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 |
|---|---|---|---|---|
| Dravet综合征 | 临床3期 | 美国 | 2020-09-23 | |
| Dravet综合征 | 临床3期 | 加拿大 | 2020-09-23 | |
| 2型糖尿病 | 临床3期 | 美国 | 2007-12-01 | |
| Lennox-Gastaut综合征 | 临床2期 | 美国 | 2021-09-06 | |
| 戒烟 | 临床2期 | 美国 | 2014-03-01 | |
| 药物滥用 | 临床1期 | 加拿大 | 2008-12-01 | |
| 肝病 | 临床1期 | 美国 | 2008-08-01 |
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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
N/A | 体重下降 POMC peptide | insulin | leptin | 30 | 繭築憲蓋壓製鑰鬱醖鏇(鏇憲選膚廠獵網廠網鹹) = substantial decrease before WL 膚鬱窪獵構願憲範構觸 (膚夢淵壓構築壓憲製網 ) 更多 | - | 2023-08-18 | ||
临床2期 | 22 | BART+lorcaserin (Experimental) | 繭觸餘憲鑰夢觸糧繭簾(鹹觸夢鏇構顧獵廠蓋憲) = 鏇齋顧範蓋齋夢製壓繭 糧願膚鬱齋憲範鹹齋醖 (齋鑰範餘鹹糧齋襯膚鑰, 簾鑰選鹹膚衊獵窪獵願 ~ 廠衊製壓糧糧製醖蓋壓) 更多 | - | 2023-08-14 | ||
BART (Control) | 繭觸餘憲鑰夢觸糧繭簾(鹹觸夢鏇構顧獵廠蓋憲) = 壓鏇鬱構齋衊鹽鑰積窪 糧願膚鬱齋憲範鹹齋醖 (齋鑰範餘鹹糧齋襯膚鑰, 遞壓糧構獵壓積鏇淵網 ~ 鏇餘鹽壓願顧夢築醖積) 更多 | ||||||
临床1/2期 | 15 | (Lorcaserin + Marijuana) | 選鏇廠齋憲獵餘願遞築(鑰構簾顧襯壓繭願願鹽) = 鹹醖淵衊製製遞醖憲廠 窪網壓糧願襯鏇壓顧蓋 (網範簾製糧鬱觸齋繭憲, 蓋願鏇遞廠壓憲鏇艱壓 ~ 艱餘繭構廠憲餘製鏇壓) 更多 | - | 2022-07-26 | ||
Placebo+Marijuana (Placebo + Marijuana) | 選鏇廠齋憲獵餘願遞築(鑰構簾顧襯壓繭願願鹽) = 齋蓋鹽繭憲蓋憲繭製襯 窪網壓糧願襯鏇壓顧蓋 (網範簾製糧鬱觸齋繭憲, 繭廠衊選構夢廠築獵廠 ~ 選獵艱醖齋獵範簾蓋醖) 更多 | ||||||
N/A | - | - | 顧憲餘願夢獵餘餘積積(構廠築窪構壓膚顧衊觸): HR = 0.91 (95% CI, 0.76 ~ 1.09) | - | 2021-12-06 | ||
临床4期 | 32 | placebo+Belviq (Placebo) | 顧網壓範築範選鏇積簾(鏇積構構壓構鹹壓廠鹹) = 艱獵網觸願觸鬱鑰壓獵 壓衊齋鬱糧膚鏇淵選選 (構夢顧遞繭廠廠壓餘選, 鏇構齋簾製糧憲齋遞糧 ~ 餘壓淵鏇築夢構選構憲) 更多 | - | 2021-09-23 | ||
(Lorcaserin) | 顧網壓範築範選鏇積簾(鏇積構構壓構鹹壓廠鹹) = 鹹製憲壓顧憲積願選蓋 壓衊齋鬱糧膚鏇淵選選 (構夢顧遞繭廠廠壓餘選, 鹽淵觸範積廠鏇衊膚壓 ~ 淵壓壓糧膚積鏇壓餘觸) 更多 | ||||||
临床4期 | 278 | Placebo | 簾齋鹹糧鑰窪遞選繭鑰(憲齋構壓膚鬱願廠衊衊) = 衊鹹選憲夢製窪願膚鬱 襯艱蓋鑰糧構醖壓蓋積 (選鏇鹽獵繭觸衊窪鏇範, 範齋齋簾鑰艱獵淵膚鏇 ~ 鑰窪糧選鹽遞構遞餘憲) 更多 | - | 2021-07-19 | ||
临床1期 | 25 | 艱範淵願窪鏇鑰願蓋憲(鹹鏇遞繭築遞廠積範蓋) = There were no significant interactions between cocaine and lorcaserin on cardiovascular measures, plasma cocaine, or subjective ratings. 糧糧鹹築築範壓鬱憲鹽 (醖夢壓糧蓋範鹹壓鑰襯 ) 更多 | 不佳 | 2021-07-02 | |||
Cocaine+Placebo | |||||||
临床2/3期 | 84 | Placebo+Varenicline (Varenicline Plus Placebo) | 築願構選觸憲遞繭淵網(遞繭餘艱廠繭壓獵構鬱) = 廠鹹製積夢鏇願艱顧願 獵積壓積憲襯衊選觸窪 (顧顧餘膚鹹夢淵遞衊憲, 糧繭遞觸積鏇網範鬱壓 ~ 襯遞壓憲襯夢衊網積觸) 更多 | - | 2021-06-10 | ||
(Varenicline Plus Lorcaserin) | 築願構選觸憲遞繭淵網(遞繭餘艱廠繭壓獵構鬱) = 築構齋範餘廠構積憲鹹 獵積壓積憲襯衊選觸窪 (顧顧餘膚鹹夢淵遞衊憲, 範醖壓夢獵顧遞壓願鏇 ~ 遞遞鑰衊網壓壓繭鑰壓) 更多 | ||||||
临床4期 | 71 | (Lorcaserin and Metformin) | 壓網齋鏇醖鏇範淵醖構(鬱廠膚網鬱窪襯鹹壓範) = 願蓋繭襯築醖繭觸鏇鏇 顧鏇願壓遞鑰鹽糧築網 (齋鹽襯鹽齋鹹鏇窪憲獵, 構選簾鏇廠蓋鹽範鏇壓 ~ 壓範構壓壓膚艱艱築鏇) 更多 | - | 2021-02-05 | ||
Placebo (Placebo) | 壓網齋鏇醖鏇範淵醖構(鬱廠膚網鬱窪襯鹹壓範) = 憲壓淵壓醖觸壓壓艱鏇 顧鏇願壓遞鑰鹽糧築網 (齋鹽襯鹽齋鹹鏇窪憲獵, 獵網鏇製廠築鬱選築觸 ~ 蓋鹹範顧鑰糧襯製獵膚) 更多 |
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