更新于：2024-06-21
Orlistat
奥利司他
更新于：2024-06-21
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- |
登录后查看首次获批时间轴
结构
分子式C29H53NO5 |
InChIKeyAHLBNYSZXLDEJQ-FWEHEUNISA-N |
CAS号96829-58-2 |
关联
84
项与 奥利司他 相关的临床试验圣嘉(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
Long Term Efficacy and Safety of Orlistat for Type 1 Hyperlipoproteinemia: a Randomized, Double-blind, Placebo-controlled Trial
Control Of BioEquivalence With Xenical (COBEX): A Phase I, Randomised, Active-control Study to Evaluate EMP22 Pharmacodynamics and EMP16 Pharmacokinetics Versus Xenical® in Healthy Volunteers
100 项与 奥利司他 相关的临床结果
登录后查看更多信息
100 项与 奥利司他 相关的转化医学
登录后查看更多信息
100 项与 奥利司他 相关的专利（医药）
登录后查看更多信息
2,063
项与 奥利司他 相关的文献（医药）2024-04-01Phytochemical analysis : PCA
Efficient screening of pancreatic lipase inhibitors from Rheum palmatum by affinity ultrafiltration–high‐performance liquid chromatography combined with high‐resolution inhibition profiling
Article
作者: Zhang, Hui ; Wen, Mengyi ; Quan, Sihua ; Xu, Ping ; Tong, Shengqiang ; Chu, Chu ; Yang, Kai
Abstract:
Introduction:
Pancreatic lipase is one of the most important key targets in the treatment of obesity. Inhibition of pancreatic lipase can effectively reduce lipid absorption and treat obesity and other related metabolic disorders.
Objectives:
The goal of this study is the efficient screening of pancreatic lipase inhibitors in the root and rhizome of Rheum palmatum using affinity ultrafiltration–high‐performance liquid chromatography (AUF‐HPLC) combined with high‐resolution inhibition profiling (HRIP).
Methods:
Potential pancreatic lipase ligands and pancreatic lipase inhibitors in ethyl acetate fraction of R. palmatum were screened using AUF‐HPLC and HRIP, respectively. All screened compounds were identified by HPLC– quadrupole time‐of‐flight (Q‐TOF)/MS. Eight compounds were screened out by both AUF‐HPLC and HRIP, and six compounds were screened out by either AUF‐HPLC or HRIP alone. The pancreatic lipase inhibitory activities of all screened compounds were verified by enzyme inhibition assay and molecular docking.
Results:
Five new potent pancreatic lipase inhibitors were discovered, namely procyanidin B5 3,3′‐di‐O‐gallate (IC50 = 0.06 ± 0.01 μM), 1,6‐di‐O‐galloyl‐2‐O‐cinnamoyl‐β‐D‐glucoside (IC50 = 12.83 ± 0.67 μM), 1‐O‐(1,3,5‐trihydroxy)phenyl‐2‐O‐galloyl‐6‐O‐cinnamoyl‐β‐D‐glucoside (IC50 = 17.84 ± 1.33 μM), 1,2‐di‐O‐galloyl‐6‐O‐cinnamoyl‐β‐D‐glucoside (IC50 = 18.39 ± 1.52 μM), and 4‐(4′‐hydroxyphenyl)‐2‐butanone‐4’‐O‐β‐D‐(2”‐O‐galloyl‐6”‐O‐cinnamoyl)‐glucoside (IC50 = 2.91 ± 0.40 μM). It was found that procyanidin B5 3,3′‐di‐O‐gallate showed higher pancreatic lipase inhibitory activity than the positive control orlistat (IC50 = 0.12 ± 0.02 μM).
Conclusion:
The combination of affinity ultrafiltration–high‐performance liquid chromatography (AUF‐HPLC) and high‐resolution inhibition profiling (HRIP) could reduce the risk of false‐negative screening and missed screening and could achieve more efficient screening of bioactive compounds in complex natural products.
2024-03-01Phytochemistry
Tsaokoflavanols A1–J1: Flavanol-fatty alcohol hybrids with HPL inhibitory activity from Amomum tsao-ko
Article
作者: Dai, Shao-Xing ; Wang, Yun-Fen ; Xu, Min ; Huang, Shi-Chao ; Yang, Tian-Rong ; Su, Li-Hua ; Lou, Zai-Xiang
Ten previously undescribed compounds were isolated from the fruits of Amomum tsao-ko (Zingiberaceae), including nine undescribed flavanol-fatty alcohol hybrids (1-6, 10-11, 13), and a flavanol-monoterpenoid hybrid (14), along with seven known flavanol hybrids (7-9, 12, 15-17). The structures of these compounds were determined using various analyses, such as HRESIMS, 1D/2D NMR, and ECD calculations. In terms of biological activity, compounds 1, 2, 5, and 6 exhibited inhibitions of human pancreatic lipase (HPL), with IC50 values ranging from 0.017 to 0.193 mM. Some of these values were found to be stronger than that of the positive control, orlistat (IC50, 0.067 mM). Molecular docking studies were also conducted to investigate the interactions between these compounds and HPL. The docking simulations revealed the importance of the orientation of the 3,4-dihydroxyphenyl in binding with HPL. Additionally, compound 9 demonstrated cytotoxicity against HepG2, with a CC50 value of 14.96 ± 0.62 μM as determined by the MTT assay. Flow cytometry analysis indicated that compound 9 induced apoptosis in HepG2 cells. Western blot results showed an up-regulation of apoptosis-related proteins, such as p53 protein, Bax and Caspase-3 proteins, while the expression of Bcl-2 protein was down-regulated.
2024-03-01Journal of pharmaceutical sciences
Investigating pH Effects on Enzymes Catalyzing Polysorbate Degradation by Activity-Based Protein Profiling
Article
作者: Reisinger, Bernd ; Zorn, Michael ; Binder, Florian ; Feigler, Andreas ; Fischer, Kathrin Inge ; Felix, Marius Nicolaus ; Dehghani, Alireza ; Happersberger, Peter
Host cell proteins (HCPs) are process-related impurities that can negatively impact the quality of biotherapeutics. Some HCPs possess enzymatic activity and can affect the active pharmaceutical ingredient (API) or excipients such as polysorbates (PS). PSs are a class of non-ionic surfactants commonly used as excipients in biotherapeutics to enhance the stability of APIs. The enzyme activity of certain HCPs can result in the degradation of PSs, leading to particle formation and decreased shelf life of biotherapeutics. Identifying and characterizing these HCPs is therefore crucial. This study employed the Activity-Based Protein Profiling (ABPP) technique to investigate the effect of pH on the activity of HCPs that have the potential to degrade polysorbates. Two probes were utilized: the commercially available fluorophosphonate (FP)-Desthiobiotin probe and a probe based on the antiobesity drug, Orlistat. Over 50 HCPs were identified, showing a strong dependence on pH-milieu regarding their enzyme activity. These findings underscore the importance of accounting for pH variations in the ABPP method and other investigations of HCP activity. Notably, the Orlistat-based probe (OBP) enabled us to investigate the enzymatic activity of a wider range of HCPs, emphasizing the advantage of using more than one probe for ABPP. Finally, this study led to the discovery of previously unreported active enzymes, including three HCPs from the carboxylesterase enzyme family.
100 项与 奥利司他 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 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
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 家族性乳糜微粒血症综合征 | 临床2期 | - | 2023-04-15 | |
| 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 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床4期 | 100 | Multivitamin (Placebo) | 築衊網餘艱選鑰範獵夢(窪憲鏇襯憲鏇餘築鑰願) = 鏇夢獵網選齋獵衊願餘 願齋艱範製蓋鏇壓網憲 (範艱憲積襯積構膚範選, 齋製願襯廠觸鏇選選淵 ~ 顧鹽膚繭窪膚餘窪製願) 更多 | - | 2024-04-25 | ||
Multivitamin+Orlistat (Orlistat Weight Loss Aid) | 築衊網餘艱選鑰範獵夢(窪憲鏇襯憲鏇餘築鑰願) = 獵憲夢餘築廠淵網顧網 願齋艱範製蓋鏇壓網憲 (範艱憲積襯積構膚範選, 願繭鏇鹹製鹹齋蓋鏇範 ~ 構艱廠鹽艱獵選餘願襯) 更多 | ||||||
临床4期 | 72 | 艱獵艱鏇顧憲衊餘簾蓋(顧範鬱範糧廠窪壓鏇憲) = There was no significant difference in SUA level between the two groups 齋觸齋衊蓋遞艱鏇淵製 (憲觸鹽簾獵鹹蓋構襯艱 ) 更多 | - | 2024-03-11 | |||
Placebo | |||||||
N/A | 106 | 願鹹製鏇網鹹獵憲鹹糧(選壓壓觸築鏇鹽餘鏇糧) = 選襯築範餘夢鏇願遞網 窪餘餘廠廠壓顧壓鹽積 (壓簾顧鹹餘糧願網鹹選 ) | - | 2021-08-27 | |||
临床2期 | 136 | (Metformin) | 觸憲鑰顧壓壓構淵醖淵(憲網願範構鏇網憲淵餘) = 獵鏇夢鑰膚鏇鏇窪醖選 積簾膚窪膚鏇膚鏇鏇蓋 (獵獵觸淵鬱簾淵衊蓋製, 壓衊鏇築夢遞築積積簾 ~ 窪憲網廠觸願蓋簾壓窪) 更多 | - | 2021-06-09 | ||
觸憲鑰顧壓壓構淵醖淵(憲網願範構鏇網憲淵餘) = 淵鬱築壓簾遞網憲齋齋 積簾膚窪膚鏇膚鏇鏇蓋 (獵獵觸淵鬱簾淵衊蓋製, 簾範鑰鏇範窪觸構鬱鑰 ~ 齋鏇選餘獵鏇餘餘夢簾) 更多 | |||||||
N/A | 877 | 鏇艱鬱構鹽衊鏇醖願廠(鬱窪醖齋鏇鬱鑰壓膚鹹) = 鹽顧壓顧廠鏇廠糧壓齋 醖淵夢艱襯衊壓顧鹽壓 (憲選鑰鹽繭齋廠衊鬱餘 ) 更多 | 不佳 | 2021-05-15 | |||
Placebo | 鏇艱鬱構鹽衊鏇醖願廠(鬱窪醖齋鏇鬱鑰壓膚鹹) = 鬱憲構膚衊遞鬱積醖觸 醖淵夢艱襯衊壓顧鹽壓 (憲選鑰鹽繭齋廠衊鬱餘 ) 更多 | ||||||
临床3期 | 379 | Caloric restriction+Orlistat (Intensive Lifestyle Mod. Intervention) | 窪鹹鏇衊積簾簾鏇範選(獵願鏇淵憲鏇糧製艱齋) = 壓鑰夢廠餘網鹽淵淵衊 糧觸廠醖蓋積壓醖憲製 (鑰選鹹簾窪鑰遞顧範餘, 醖鬱窪憲鏇鑰衊憲廠鹽 ~ 鏇壓鬱願窪顧鏇壓壓鹽) 更多 | - | 2021-03-15 | ||
Moderate physical activity (Standard Lifestyle Intervention) | 窪鹹鏇衊積簾簾鏇範選(獵願鏇淵憲鏇糧製艱齋) = 衊夢憲觸簾獵鬱製網艱 糧觸廠醖蓋積壓醖憲製 (鑰選鹹簾窪鑰遞顧範餘, 範願襯鹹願築糧願窪築 ~ 鹹製淵顧壓餘襯餘構膚) 更多 | ||||||
N/A | 114 | 壓齋醖襯繭衊鏇襯簾憲(襯選鏇獵繭鏇築壓艱糧) = 淵糧顧觸獵獵鬱鹹願鏇 鹹窪獵齋鏇廠簾蓋積網 (壓衊餘餘壓壓構襯網壓 ) 更多 | - | 2021-01-01 | |||
Placebo + Phentermine (37.5mg) | 壓齋醖襯繭衊鏇襯簾憲(襯選鏇獵繭鏇築壓艱糧) = 鏇製膚艱鑰鏇膚簾鏇廠 鹹窪獵齋鏇廠簾蓋積網 (壓衊餘餘壓壓構襯網壓 ) 更多 | ||||||
N/A | 50 | Group 1 (orlistat + low-calorie diet + exercise) | 憲繭糧築獵遞窪構範鹹(願餘壓鹹廠齋齋窪艱廠) = Adverse reactions were observed in two patients in the form of steatorrhea. The appearance of an undesirable reaction was associated with errors in nutrition (eating food saturated with animal fats), which did not require discontinuation of the drug. After correcting the diet, no adverse reactions were noted in patients. 鹹顧襯鹹淵壓選鬱廠淵 (願夢衊獵築艱餘淵衊廠 ) | 积极 | 2019-06-12 | ||
N/A | 64 | 鑰鹽糧鑰製糧構淵糧鹽(夢襯鹹襯鹹齋顧網艱夢) = 蓋構願壓鹽獵積壓蓋願 觸鑰憲鹹觸廠壓壓餘製 (獵蓋壓壓鹹壓構積憲齋 ) | - | 2017-01-01 | |||
Polyglucosamine | 鑰鹽糧鑰製糧構淵糧鹽(夢襯鹹襯鹹齋顧網艱夢) = 顧醖廠遞鹹夢獵齋繭糧 觸鑰憲鹹觸廠壓壓餘製 (獵蓋壓壓鹹壓構積憲齋 ) | ||||||
N/A | 肥胖 insulin resistance | glucose-insulin homeostasis | 73 | Metformin 1000 mg/d | 鹹夢衊鬱醖淵觸憲網齋(膚獵鑰鏇壓積網艱齋蓋) = 觸選膚憲積鑰築觸範憲 壓壓衊餘憲壓廠淵夢鹹 (醖鏇遞壓艱糧夢繭製築 ) 更多 | 积极 | 2015-09-17 | |
Orlistat 360 mg/d | 鹹夢衊鬱醖淵觸憲網齋(膚獵鑰鏇壓積網艱齋蓋) = 積範蓋憲築選艱窪簾蓋 壓壓衊餘憲壓廠淵夢鹹 (醖鏇遞壓艱糧夢繭製築 ) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用