预约演示
更新于：2026-10-24
Lorcaserin Hydrochloride
盐酸绿卡色林
更新于：2026-10-24
概要
基本信息
在研机构- |
最高研发阶段撤市 |
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/序列
分子式C11H15Cl2N |
InChIKeyITIHHRMYZPNGRC-QRPNPIFTSA-N |
CAS号846589-98-8 |
关联
55
项与 盐酸绿卡色林 相关的临床试验NCT04205071
Pilot Trial of Acute Effect of Lorcaserin to Reduce Patient-Reported Symptoms of Taxane- and Oxaliplatin-Induced Peripheral Neuropathy
NCT04572243
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
NCT04396834
Behavioral Mechanisms of Lorcaserin Treatment for Smoking Cessation
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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480
项与 盐酸绿卡色林 相关的文献（医药）2026-09-02Expert Opinion On Drug Safety
Drug-associated pancreatic cancer: insights from real-world pharmacovigilance and network pharmacology
Article
作者: Zhao, Bin ; Xie, Hao ; Wu, Wenming ; Xu, Qiang
BACKGROUND:
Pancreatic cancer's high mortality rate necessitates our study, which aims to identify potential risk drugs and speculate on the underlying mechanisms.
RESEARCH DESIGN AND METHODS:
All pertinent reports from the FDA Adverse Event Reporting System database were extracted. The disproportionality analysis was used in signal detection and data on patient age, sex, weight, time to onset were collected. Seven databases were retrieved for network pharmacology. AutoDock Vina 1.1.2 was for molecular docking.
RESULTS:
Signals were detected among 397 drugs with pancreatic cancer report ≥3. Except 4 antineoplastic agents, only 24 drugs indicated pancreatic cancer signals in 33,948 reports including 4 dipeptidyl peptidase-4 (DPP-4) inhibitors, 3 glucagon-like peptide-1 (GLP-1) analogues, 5 compound hypoglycemic agents, 3 hypotensive agents, ranitidine, pancrelipase, fondaparinux, naldemedine, daprodustat, megestrol acetate, leuprorelin, lecanemab, and lorcaserin. Pancreatic cancer more occurred after the age of 45, with a higher proportion among male. Weight with GLP-1 analogues (median, 91 kg), and compound hypoglycemic agents (median, 82 kg) was heavier (p < 0.01). GLP1R (glucagon-like peptide 1 receptor) for GLP-1 analogues, and PTEN (phosphatase and tensin homolog) for metformin might be a potential cause of pancreatic cancer.
CONCLUSION:
Clinicians providing these therapies should stay vigilant to detect pancreatic cancer early.
2026-01-01AMERICAN JOURNAL OF OPHTHALMOLOGY
Glucagon-like Peptide-1 Receptor Agonist Use and Risk of Cataract Development
Article
作者: Ahuja, Abhimanyu S ; Young, Benjamin K ; Paredes, Alfredo A ; Ahuja, Sejal A
OBJECTIVE:
To evaluate the risk of developing age-related cataract among nondiabetic patients who are overweight or obese prescribed glucagon-like peptide-1 receptor agonists (GLP-1RAs) compared to other weight loss drugs (OWLD).
DESIGN:
Retrospective cohort study using the TriNetX Global Collaborative Network.
SUBJECTS:
Overweight or obese patients aged 55 years and greater were included. Patients with a diabetes mellitus or prior age-related cataract were excluded.
METHODS:
Patients in the GLP-1RA group were prescribed either semaglutide or liraglutide. Patients in the OWLD group were lorcaserin, setmelanotide, diethylpropion, sibutramine, fenfluramine, mazindol, phentermine, or orlistat A third cohort included patients not prescribed any weight loss medications. Propensity score matching was performed to minimize baseline differences between cohorts.
MAIN OUTCOME MEASURES:
The primary outcome was development of age-related cataract at 5-, 7-, and 10-year intervals. Risk ratios with 95% confidence intervals and corresponding P-values were reported. Standardized mean differences (SMDs) were calculated to assess covariate balance.
RESULTS:
In the primary analysis of GLP-1RA vs OWLD usage, covariate balance was achieved across all matched variables with SMDs < 0.2. In this primary analysis, GLP-1RA use was associated with a decreased risk of age-related cataract at 5 (RR: 0.278; 95% CI: 0.246-0.314; P < .0001), 7 (RR: 0.269; 95% CI: 0.241-0.299; P < .0001), and 10 (RR: 0.198; 95% CI: 0.176-0.222; P < .0001) years compared to OWLD use. GLP-1RA use was also associated with decreased risk at 5 (RR: 0.605; 95% CI: 0.553-0.661; P < .0001), 7 (RR: 0.499; 95% CI: 0.458-0.542; P < .0001), and 10 (RR: 0.437; 95% CI: 0.403-0.475; P < .0001) years compared to no drug use. Conversely, OWLD use was associated with increased risk at 5 (RR: 2.142; 95% CI: 1.957-2.345; P < .0001), 7 (RR: 2.093; 95% CI: 1.931-2.268; P < .0001) and 10 (RR: 2.111; 95% CI: 1.961-2.273; P < .0001) years compared to no drug use.
CONCLUSIONS:
GLP-1RA use was associated with a significantly reduced risk of age-related cataract compared to OWLD use and no pharmacologic treatment. These findings support the need for randomized prospective trials and mechanistic studies to better understand this observed association.
2026-01-01BIOORGANIC CHEMISTRY
Towards next-generation 5-hydroxytryptamine 2C receptor modulators: Greener synthesis and evaluation of novel isocoumarin derivatives as PAAMs of 5-HT2CR
Article
作者: Biswas, Deepesh ; Giliyaru, Varadaraj Bhat ; Misra, Parimal ; Sreenivas, B Yogi ; Medishetti, Raghavender ; Oruganti, Srinivas ; Yadav, Prem N ; Bung, Navneet ; Sarkar, Kaushik ; Roy, Arijit ; Chatti, Kiranam ; Naimisha, Rapaka ; Madhuri, Sedam Sai ; Pal, Manojit
In the current study, we designed a new class of 3-(1-hydroxycycloalkyl)-substituted isocoumarin derivatives as potential modulators of 5-HT2CR (5-hydroxytryptamine 2C receptor). These compounds were synthesized via a greener as well as faster, milder, and one-pot approach involving the CuCl2.2H2O-catalyzed coupling-cyclization of 2-iodobenzoic acid with 1-ethynylcycloalkanols under ultrasound. This ligand and additive-free reaction was completed within 1-1.5 h, affording the desired products in good yields with high regio-selectivity. The environmental sustainability of this protocol was assessed by calculating the key green chemistry metrics, whereas the scalable potential and further application of the methodology were demonstrated. The in vitro evaluation of synthesized compounds revealed that several of them functioned as selective 5-HT2CR agonists with additional PAAM (positive ago-allosteric modulator) properties (unlike Lorcaserin). Among them, compound 3b demonstrated promising 5HT2C PAAM activity (EC50 = 8 nM), high metabolic stability in mice brain homogenates (67 % remaining after 2 h), and a favorable (2:1) brain-to-plasma distribution ratio in mice. When evaluated in rats for 22 h, compound 3b reduced food intake at different time points. The molecule also seemed to be safe in both in silico predictions and in vivo experiments. The molecular docking studies of 3b indicated selective engagement with an allosteric binding pocket via H-bonding with Asp134, unlike Lorcaserin (which forms a H-bond with Asn331). Indeed, the ability of 3b to simultaneously anchor through Asp134 and extend into the tripeptide site underlined its novel mechanism for modulating the activity of 5-HT2CR. Thus, compound 3b emerged as a promising PAAM of 5-HT2CR for further preclinical assessments. 2009 Elsevier Ltd. All rights reserved.
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 | |
| 超重 | 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 | |
| 尼古丁成瘾 | 临床2期 | 美国 | 2014-03-01 | |
| 药物滥用 | 临床1期 | 加拿大 | 2008-12-01 | |
| 发育性癫痫性脑病 | 临床前 | 美国 | 2024-12-01 |
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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 | 22 | placebo+lorcaserin (Core Study: Placebo) | 觸選衊憲淵膚餘範蓋繭(夢積壓網選衊顧鏇範簾) = 膚觸獵鹽鏇觸壓醖鏇衊 鏇鑰廠鏇製膚窪夢鏇範 (餘醖壓選齋糧鑰製觸憲, 鬱獵選願膚蓋鹽蓋網憲 ~ 鹹衊憲艱積膚憲鏇選範) 更多 | - | 2025-10-08 | ||
(Core Study: Lorcaserin) | 觸選衊憲淵膚餘範蓋繭(夢積壓網選衊顧鏇範簾) = 獵艱範築簾夢襯鏇構構 鏇鑰廠鏇製膚窪夢鏇範 (餘醖壓選齋糧鑰製觸憲, 鏇範網簾製簾鏇選餘衊 ~ 鑰淵鏇遞膚齋齋繭鹽淵) 更多 | ||||||
临床2期 | 22 | Cocaine metabolites+lorcaserin (Experimental) | 廠壓繭襯觸網醖積齋鬱(觸願築憲襯選醖壓鑰膚) = 壓夢構醖窪蓋鹹築鹽遞 觸夢淵簾願齋繭夢觸壓 (壓壓膚構積壓膚鹹膚觸, 27.7) 更多 | - | 2023-08-14 | ||
Placebo Oral Tablet (Control) | 廠壓繭襯觸網醖積齋鬱(觸願築憲襯選醖壓鑰膚) = 齋窪製網願鑰簾齋鏇壓 觸夢淵簾願齋繭夢觸壓 (壓壓膚構積壓膚鹹膚觸, 21.7) 更多 | ||||||
临床2期 | 3 | (Lorcaserin) | 鏇鹽構膚積獵遞鏇蓋夢(鬱鬱夢窪鬱膚鬱積衊襯) = 鬱願築襯積廠廠積觸鹽 獵窪醖糧繭襯齋獵選艱 (襯憲糧鏇觸膚壓願選艱, 4.9) 更多 | - | 2023-03-20 | ||
Placebo (Placebo) | 鏇鹽構膚積獵遞鏇蓋夢(鬱鬱夢窪鬱膚鬱積衊襯) = 淵願糧窪鹽壓網遞遞襯 獵窪醖糧繭襯齋獵選艱 (襯憲糧鏇觸膚壓願選艱, .71) 更多 | ||||||
临床2期 | 5 | (Lorcaserin) | 遞鬱餘願願糧選鹽積鑰 = 膚製齋繭鑰範遞顧憲衊 鏇觸膚鹽觸鑰齋鬱膚壓 (糧範鑰夢獵顧遞壓夢膚, 膚選觸糧窪範糧顧構壓 ~ 獵鹹艱鬱觸積鑰遞築壓) 更多 | - | 2022-09-07 | ||
Placebo (Placebo) | 遞鬱餘願願糧選鹽積鑰 = 網廠顧鹽鏇壓蓋糧獵鬱 鏇觸膚鹽觸鑰齋鬱膚壓 (糧範鑰夢獵顧遞壓夢膚, 簾糧鹽廠襯衊選衊鏇顧 ~ 廠觸觸鬱顧齋壓觸夢餘) 更多 | ||||||
临床1/2期 | 15 | (Lorcaserin + Marijuana) | 餘積獵艱夢憲願製夢襯(蓋顧餘範選遞獵構餘廠) = 淵製鏇構簾範糧醖構鹹 鏇蓋願衊鬱製構選醖鏇 (積艱獵顧構簾簾築鹽醖, 1) 更多 | - | 2022-07-26 | ||
Placebo+Marijuana (Placebo + Marijuana) | 餘積獵艱夢憲願製夢襯(蓋顧餘範選遞獵構餘廠) = 簾鹹醖襯築鹽衊蓋鹹鹹 鏇蓋願衊鬱製構選醖鏇 (積艱獵顧構簾簾築鹽醖, 1) 更多 | ||||||
N/A | - | - | 鹽積顧窪膚鹹觸積觸淵(艱衊構鑰餘顧醖襯膚醖): HR = 0.91 (95% CI, 0.76 ~ 1.09) | - | 2021-12-06 | ||
临床4期 | 32 | placebo+Belviq (Placebo) | 簾構顧製壓夢願鑰齋鹹(願網襯壓鬱醖淵壓範範) = 糧遞鑰築顧淵齋艱鬱齋 壓糧鏇鹹壓範願築選鬱 (廠獵顧鹽簾鑰鑰鬱餘顧, 118.7) 更多 | - | 2021-09-23 | ||
(Lorcaserin) | 簾構顧製壓夢願鑰齋鹹(願網襯壓鬱醖淵壓範範) = 顧鹹範淵艱餘糧築積積 壓糧鏇鹹壓範願築選鬱 (廠獵顧鹽簾鑰鑰鬱餘顧, 109.0) 更多 | ||||||
临床4期 | 278 | Placebo | 遞壓範積鹽壓餘範築鹹(衊製糧鹹網艱鬱顧選網) = 壓鏇築獵淵壓顧鑰餘憲 襯製選獵構鑰構淵襯窪 (鹽廠範製範遞網艱鹹餘, 2.317) 更多 | - | 2021-07-19 | ||
临床2期 | - | - | 鬱製窪糧醖願範築鹹繭(構壓衊齋憲選襯衊艱繭) = 鑰壓艱膚築繭齋艱繭鏇 簾製獵壓鑰獵鏇餘網鑰 (繭醖廠壓餘鑰顧膚夢選 ) | - | 2021-07-15 | ||
Placebo | 鬱製窪糧醖願範築鹹繭(構壓衊齋憲選襯衊艱繭) = 願衊膚衊鬱觸壓壓憲襯 簾製獵壓鑰獵鏇餘網鑰 (繭醖廠壓餘鑰顧膚夢選 ) | ||||||
临床1期 | 25 | 製繭餘齋積餘製醖衊構(鹽積壓鬱積糧獵構積鬱) = There were no significant interactions between cocaine and lorcaserin on cardiovascular measures, plasma cocaine, or subjective ratings. 網鑰觸構範製餘觸膚願 (願繭夢餘壓遞齋襯廠蓋 ) 更多 | 不佳 | 2021-07-02 | |||
Cocaine+Placebo |
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