更新于：2024-11-04
Orlistat
奥利司他
更新于：2024-11-04
概要
基本信息
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C29H53NO5 |
InChIKeyAHLBNYSZXLDEJQ-FWEHEUNISA-N |
CAS号96829-58-2 |
关联
87
项与 奥利司他 相关的临床试验奥利司他胶囊的人体生物等效性研究
奥利司他胶囊的人体生物等效性试验
圣嘉(滨海)生物医药科技有限公司研制的奥利司他胶囊与持证商为GlaxoSmithKline Consumer Healthcare的奥利司他胶囊（规格：60 mg，商品名：Alli）在中国健康受试者中进行的单中心、随机、开放、两制剂、三序列、三周期、多次给药、交叉设计的生物等效性研究
100 项与 奥利司他 相关的临床结果
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100 项与 奥利司他 相关的转化医学
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100 项与 奥利司他 相关的专利（医药）
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2,163
项与 奥利司他 相关的文献（医药）2025-01-01BRAIN BEHAVIOR AND IMMUNITY
Blockage of ATGL-mediated breakdown of lipid droplets in microglia alleviates neuroinflammatory and behavioural responses to lipopolysaccharides
Article
作者: Manceau, Romane ; Louise Robb, Josephine ; Machuca-Parra, Arturo Israel ; Rodaros, Demetra ; Israel Machuca-Parra, Arturo ; Arbour, Nathalie ; Fioramonti, Xavier ; Layé, Sophie ; Boisjoly, Frédérick ; Bouyakdan, Khalil ; Greffard, Karine ; Fulton, Stephanie ; Laurent, Cyril ; Forest, Anik ; Majeur, Danie ; Bilodeau, Jean-François ; Madore, Charlotte ; Daneault, Caroline ; Ruiz, Matthieu ; Coursan, Adeline ; Robb, Josephine Louise ; Alquier, Thierry
Lipid droplets (LD) are triglyceride storing organelles that have emerged as an important component of cellular inflammatory responses. LD lipolysis via adipose triglyceride lipase (ATGL), the enzyme that catalyses the rate-limiting step of triglyceride lipolysis, regulates inflammation in peripheral immune and non-immune cells. ATGL elicits both pro- and anti-inflammatory responses in the periphery in a cell-type dependent manner. The present study determined the impact of ATGL inhibition and microglia-specific ATGL genetic loss-of-function on acute inflammatory and behavioural responses to pro-inflammatory insult. First, we evaluated the impact of lipolysis inhibition on lipopolysaccharide (LPS)-induced expression and secretion of cytokines and phagocytosis in mouse primary microglia cultures. Lipase inhibitors (ORlistat and ATGListatin) and LPS led to LD accumulation in microglia. Pan-lipase inhibition with ORlistat alleviated LPS-induced expression of IL-1β and IL-6. Specific inhibition of ATGL had a similar action on CCL2, IL-1β and IL-6 expression in both neonatal and adult microglia cultures. CCL2 and IL-6 secretion were also reduced by ATGListatin or knockdown of ATGL. ATGListatin increased phagocytosis in neonatal cultures independently from LPS treatment. Second, targeted and untargeted lipid profiling revealed that ATGListatin reduced LPS-induced generation of pro-inflammatory prostanoids and modulated ceramide species in neonatal microglia. Finally, the role of microglial ATGL in neuroinflammation was assessed using a novel microglia-specific and inducible ATGL knockout mouse model. Loss of microglial ATGL in adult male mice dampened LPS-induced expression of IL-6 and IL-1β and microglial density. LPS-induced sickness- and anxiety-like behaviours were also reduced in male mice with loss of ATGL in microglia. Together, our results demonstrate potent anti-inflammatory effects produced by pharmacological or genetic inhibition of ATGL-mediated triglyceride lipolysis and thereby propose that supressing microglial LD lipolysis has beneficial actions in acute neuroinflammatory conditions.
2024-11-01Pediatric Obesity
Effectiveness of pharmacological interventions for managing obesity in children and adolescents: A systematic review and meta‐analysis framed using minimal important difference estimates based on GRADE guidance to inform a clinical practice guideline
Review
作者: Usman, Ali ; Ball, Geoff D. C. ; Sherifali, Diana ; Birken, Catherine S. ; Henderson, Mélanie ; Hamilton, Jill ; Johnston, Bradley C. ; Fitzpatrick‐Lewis, Donna ; St‐Pierre, Julie ; Moore, Sarah A. ; Morrison, Katherine M. ; Esmaeilinezhad, Zahra ; Merdad, Roah ; Wahi, Gita
Summary:
Objective:
To summarize the literature on pharmacotherapy for managing paediatric obesity.
Methods:
A systematic review and meta‐analysis were conducted of randomized controlled trials (RCTs) with <18‐year‐olds of pharmacotherapeutic agents published up to November 2022. Estimates of effect for outcomes were presented relative to minimal important differences and GRADE certainty of evidence. We examined data on patient/proxy‐reported outcome measures (PROMs), cardiometabolic risk factors, anthropometry and adverse events (AEs).
Results:
Overall, 35 RCTs were included. Trials examined metformin (n = 26), glucagon‐like peptide‐1 receptor agonists (GLP1RAs) (n = 7) and a lipase inhibitor (orlistat; n = 2). Intervention duration varied (3−24 months). Metformin had little to no benefit on PROMs (e.g., health‐related quality of life [HRQoL]; 6 RCTs), moderate reductions in triglycerides, a moderate decline in insulin resistance, a small to moderate decline in BMI z‐score (BMIz) and a moderate increase in mild to moderate gastrointestinal AEs. Response to GLP1RAs was heterogeneous and results of subgroup analysis demonstrated variability of impact. Liraglutide (2 RCTs) resulted in a small reduction in HOMA‐IR and BMIz, but little to no benefit on other outcomes. Exenatide (4 RCTs) had a moderate reduction on blood pressure and a small decrease in BMIz with little to no benefit on other outcomes. Semaglutide (1 RCT) had a small benefit on HRQoL, a small reduction on SBP, a moderate reduction on total cholesterol and LDL‐cholesterol, a large reduction on triglyceride, and a very large decline in BMIz accompanied by a small increase in mild to moderate gastrointestinal AEs. Orlistat had a moderate reduction in DBP and little to no benefit in other outcomes measured, but had a very large increased risk of mild to moderate gastrointestinal AEs. Serious AEs were rare and for interventions with sufficent AE reporting, were considered not likely attributable to the interventions.
Conclusion:
Few studies examined the impact of pharmacotherapy on PROMs. There is evidence that metformin and GLP1RAs lead to important improvements in cardiometabolic and anthropometric outcomes while accompanied by mild to moderate AEs. Long‐term effectiveness and safety of GLP1RAs remain to be evaluated.
2024-11-01INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Preferential inhibition of α-amylase by cinnamaldehyde-based hydrazones: A comparative study
Article
作者: Vashisth, Chanchal ; Raghav, Neera
The escalating issue of obesity and related health conditions, including diabetes mellitus and coronary heart disease, necessitates the development of digestive enzyme inhibitors. Targeting pancreatic lipase to inhibit fatty acid generation to attain reduced lipid absorption is a promising approach for identifying effective agents. Orlistat, the only clinically approved pancreatic lipase inhibitor, is associated with gastrointestinal side effects like oily stools, spotting, and flatulence. Concurrently, α-amylase inhibitors can mitigate rapid spikes in blood sugar levels. With the growing significance of natural products in pharmaceutical research, cinnamaldehyde has been recognized as a potential enzyme inhibitor. This study explores the effects of cinnamaldehyde-derived hydrazone Schiff bases on lipase and α-amylase through in vitro experiments. The synthesized compounds exhibited IC50 value for lipase in the same range ((0.41-12.58) × 10-8 M) as exhibited by the commercial drug orlistat (5.76 × 10-8 M). However, for α-amylase inhibition, the compounds (IC50 value = 0.37-9.54 × 10-9 M) were found effective inhibitors of acarbose (IC50 value = 6.76 × 10-6 M) and curcumin (IC50 value = 467 × 10-9 M). In silico DFT studies, molecular docking, drug likeliness, bioactivity score, ADME, and toxicity are also investigated for these compounds.
100 项与 奥利司他 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 | 欧盟 | 1998-07-29 | |
| 肥胖 | 冰岛 | 1998-07-29 | |
| 肥胖 | 列支敦士登 | 1998-07-29 | |
| 肥胖 | 挪威 | 1998-07-29 | |
| 超重 | 欧盟 | 1998-07-29 | |
| 超重 | 冰岛 | 1998-07-29 | |
| 超重 | 列支敦士登 | 1998-07-29 | |
| 超重 | 挪威 | 1998-07-29 |
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 |
|---|---|---|---|---|
| 代谢性疾病 | 临床3期 | 俄罗斯 | 2008-04-01 | |
| 家族性乳糜微粒血症综合征 | 临床2期 | 美国 | 2024-01-26 | |
| 高甘油三酯血症 | 临床2期 | 美国 | 2015-12-01 | |
| I型高脂蛋白血症 | 临床2期 | 美国 | 2015-11-01 | |
| 糖尿病 | 临床2期 | 美国 | 1998-05-01 | |
| 高血压 | 临床2期 | 美国 | 1998-05-01 | |
| 睡眠呼吸暂停综合征 | 临床2期 | 美国 | 1998-05-01 |
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临床结果
临床结果
适应症
分期
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临床4期 | 74 | Weight Management Program (WMP)+Orlistat+liraglutide 3.0 mg+Phentermine / Topiramate Extended Release Oral Capsule+naltrexone/bupropion extended-release (Obesity-centric Approach + AOM) | 範餘醖餘獵壓顧顧築鏇(淵鑰鹹鑰齋選鏇艱鬱夢) = 鬱範鹹鹽膚範遞積遞鬱 簾選夢鑰襯構獵窪選糧 (窪餘鑰築鑰構鹽獵築窪, 鏇襯範艱願鑰窪襯構獵 ~ 鹹構鹹鏇範構艱襯淵繭) 更多 | - | 2024-07-22 | ||
Weight Management Program (WMP) (Obesity-centric Approach Without AOM) | 範餘醖餘獵壓顧顧築鏇(淵鑰鹹鑰齋選鏇艱鬱夢) = 鹹鹹觸選鹽齋築糧糧獵 簾選夢鑰襯構獵窪選糧 (窪餘鑰築鑰構鹽獵築窪, 網艱壓窪顧憲夢蓋醖壓 ~ 壓願鑰願簾簾廠鏇選選) 更多 | ||||||
临床3期 | 72 | 蓋夢鑰憲簾繭範築膚夢(鑰憲襯衊構製獵觸網齋): HR = 0.31 (95% CI, 0.11 ~ 0.85), P-Value = 0.023 | 积极 | 2024-06-24 | |||
Placebo | |||||||
临床4期 | 100 | Multivitamin (Placebo) | 簾願餘夢積網鹽壓餘膚(廠願糧襯簾鑰糧廠窪獵) = 願鏇膚膚壓艱艱艱顧蓋 簾鹹繭鏇憲構積遞壓鏇 (壓顧齋獵選簾願鑰鹹築, 構顧鏇襯構鑰願艱遞膚 ~ 築壓鬱觸醖鏇糧餘淵選) 更多 | - | 2024-04-25 | ||
Multivitamin+Orlistat (Orlistat Weight Loss Aid) | 簾願餘夢積網鹽壓餘膚(廠願糧襯簾鑰糧廠窪獵) = 築糧憲壓網觸鏇範窪鹽 簾鹹繭鏇憲構積遞壓鏇 (壓顧齋獵選簾願鑰鹹築, 蓋淵網鹽範顧艱選艱餘 ~ 餘夢願積鬱築衊鹽繭簾) 更多 | ||||||
临床4期 | 72 | 齋艱繭艱遞觸夢積範壓(憲築鏇衊鏇網齋窪構選) = There was no significant difference in SUA level between the two groups 淵製鏇構鹹壓醖醖蓋製 (餘網獵糧壓願糧顧廠蓋 ) 更多 | 积极 | 2024-03-11 | |||
Placebo | |||||||
N/A | 106 | 衊艱憲衊衊憲繭構遞製(鹽膚鏇繭憲廠艱夢醖艱) = 窪齋艱膚蓋壓鹹觸醖範 範蓋衊構鑰築淵糧壓蓋 (觸選願築艱願築構蓋築 ) | - | 2021-08-27 | |||
临床2期 | 136 | (Metformin) | 壓醖選網顧觸淵淵廠顧(糧醖襯醖鏇網繭壓餘淵) = 積蓋齋窪壓壓齋觸衊鹽 網衊顧鬱範餘觸糧齋簾 (衊窪範築襯夢選網襯願, 齋膚積憲淵鏇鹽顧製窪 ~ 顧糧憲構衊窪製願廠餘) 更多 | - | 2021-06-09 | ||
壓醖選網顧觸淵淵廠顧(糧醖襯醖鏇網繭壓餘淵) = 選簾鏇築襯鹽鹽簾製齋 網衊顧鬱範餘觸糧齋簾 (衊窪範築襯夢選網襯願, 蓋壓獵範憲構衊構願憲 ~ 艱壓艱衊願夢鹽願範膚) 更多 | |||||||
N/A | 877 | 範積顧憲築壓顧壓鑰襯(鬱餘壓糧蓋築艱築壓願) = 夢願壓觸壓壓壓積築膚 範膚範鑰醖願簾簾夢鹽 (夢淵獵糧窪選範鏇廠選 ) 更多 | 不佳 | 2021-05-15 | |||
Placebo | 範積顧憲築壓顧壓鑰襯(鬱餘壓糧蓋築艱築壓願) = 鹹積窪簾憲廠壓製鑰繭 範膚範鑰醖願簾簾夢鹽 (夢淵獵糧窪選範鏇廠選 ) 更多 | ||||||
临床3期 | 379 | Caloric restriction+Orlistat (Intensive Lifestyle Mod. Intervention) | 繭夢醖鹹夢齋糧鬱廠製(觸壓憲願鹽築鏇構簾廠) = 鑰積醖鹹築鏇醖鑰餘夢 淵觸壓廠艱獵選鹹顧鏇 (願醖鹽構憲壓餘積醖淵, 壓製蓋齋願蓋觸蓋願蓋 ~ 廠夢鏇夢襯繭壓網觸製) 更多 | - | 2021-03-15 | ||
Moderate physical activity (Standard Lifestyle Intervention) | 繭夢醖鹹夢齋糧鬱廠製(觸壓憲願鹽築鏇構簾廠) = 選簾餘窪襯網構衊鑰選 淵觸壓廠艱獵選鹹顧鏇 (願醖鹽構憲壓餘積醖淵, 觸願憲膚構淵窪範淵壓 ~ 築繭醖網繭築蓋願壓艱) 更多 | ||||||
N/A | 64 | 鹽憲選廠築築艱壓憲築(遞網鬱鹽築憲簾繭蓋獵) = 廠顧製壓鹹餘簾鑰醖膚 衊淵網鑰鹽獵鏇積膚艱 (網遞廠膚醖齋構遞願窪 ) | - | 2017-01-01 | |||
Polyglucosamine | 鹽憲選廠築築艱壓憲築(遞網鬱鹽築憲簾繭蓋獵) = 遞顧襯齋餘艱鏇憲簾糧 衊淵網鑰鹽獵鏇積膚艱 (網遞廠膚醖齋構遞願窪 ) |
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