预约演示
更新于：2025-11-01
Levalbuterol Tartrate
左沙丁胺醇
更新于：2025-11-01
概要
基本信息
在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2005-03-11), |
最高研发阶段(中国)- |
特殊审评- |
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结构/序列
分子式C30H48N2O12 |
InChIKeyVNVNZKCCDVFGAP-FPDJQMMJSA-N |
CAS号661464-94-4 |
关联
31
项与 左沙丁胺醇 相关的临床试验NCT06422689
ANCHOR - Assessment of Combination Short-Acting BroNchodilator and Inhaled Corticosteroid Rescue Therapy on Health Outcomes in Routine Care
CTR20240652
酒石酸左沙丁胺醇吸入气雾剂在中国健康受试者空腹状态下的单中心、随机、开放、单剂量、两序列、四周期、完全重复交叉生物等效性试验
CTRI/2020/03/024170
Comparison Of Efficacy Of Nebulised Levosalbutamol Vs Levosalbutamol Metered Dose Inhaler-Spacer: A Single Centre Open Label Randomized Controlled Trial In Hospitalized Children With Wheezing
100 项与 左沙丁胺醇 相关的临床结果
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100 项与 左沙丁胺醇 相关的转化医学
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100 项与 左沙丁胺醇 相关的专利（医药）
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377
项与 左沙丁胺醇 相关的文献（医药）2024-10-01DRUG METABOLISM AND DISPOSITION
Clotrimazole Identified as a Selective UGT2B4 Inhibitor Using Canagliflozin-2′-O-Glucuronide Formation as a Selective UGT2B4 Probe Reaction
Article
作者: Goosen, Theunis C ; Ferguson, Nicholas ; Lapham, Kimberly ; Niosi, Mark
UGT2B4 is a highly expressed drug-metabolizing enzyme in the liver contributing to the glucuronidation of several drugs. To enable quantitatively assessing UGT2B4 contribution toward metabolic clearance, a potent and selective UGT2B4 inhibitor that can be used for reaction phenotyping was sought. Initially, a canagliflozin-2'-O-glucuronyl transferase activity assay was developed in recombinant UGT2B4 and human liver microsomes (HLM) [±2% bovine serum albumin (BSA)]. Canagliflozin-2'-O-glucuronidation (C2OG) substrate concentration at half-maximal velocity value in recombinant UGT2B4 and HLM were similar. C2OG formation intrinsic clearance was five- to seven-fold higher in incubations containing 2% BSA, suggesting UGT2B4 susceptibility to the inhibitory unsaturated long-chain fatty acids released during the incubation. Monitoring for C2OG formation, 180 compounds were evaluated for UGT2B4 inhibition potency in the presence and absence of 2% BSA. Compounds that exhibited an apparent UGT2B4 IC50 of < 1 μM in HLM with 2% BSA were evaluated for inhibition of UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, UGT2B7, UGT2B10, UGT2B15, and UGT2B17 catalytic activities to establish selectivity suitable for supporting UGT reaction phenotyping. In this study, clotrimazole was identified as a potent UGT2B4 inhibitor (HLM apparent IC50 of 11 to 35 nM ± 2% BSA). Moreover, clotrimazole exhibited selectivity for UGT2B4 inhibition (>24-fold) over the other UGT enzymes evaluated. Additionally, during this study it was discovered that the previously described UGT2B7 inhibitors 16α- and 16β-phenyllongifolol also inhibit UGT2B4. Clotrimazole, a potent and selective UGT2B4 inhibitor, will prove essential during UGT reaction phenotyping. SIGNIFICANCE STATEMENT: To mechanistically evaluate drug interactions, it is essential to understand the contribution of individual enzymes to the metabolic clearance of a drug. The present study describes the development of a UGT2B4 activity assay that enabled the discovery of the highly selective and potent UGT2B4 inhibitor clotrimazole. Clotrimazole can be used in UGT reaction phenotyping studies to estimate fractional contribution of UGT2B4.
2024-09-24JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION
Greenhouse Gas Emissions and Costs of Inhaler Devices in the US
Article
作者: Wilkinson, Alexander J. K. ; Tirumalasetty, Jyothi ; Prescott, Hallie C. ; Rabin, Alexander S. ; Miller, Shelie A. ; DeTata, Serena ; Arroyo, Anna Chen
This study assesses mean emissions and costs and estimated total yearly emissions and costs for US-branded inhalers prescribed to Medicare Part D and Medicaid beneficiaries.
2024-09-01PHYTOMEDICINE
Lung-intestinal axis, Shuangshen granules attenuate lung metastasis by regulating the intestinal microbiota and related metabolites
Article
作者: He, Shulin ; Sun, Tianheng ; Qi, Xin ; Li, Juan ; Liu, Rui ; Zhang, Guanghui ; Luo, Yue ; Hua, Baojin ; Shi, Bolun ; Ren, Xiaoling ; Li, Yue ; Maolan, Ayidana ; Hu, Jiaqi ; Zhang, Xinyue
BACKGROUND:
Based on the proposed lung-intestinal axis, there is a significant correlation between the microbiota and lung metastasis. Targeting the microbial composition is valuable in modulating the host response to cancer therapeutics. As a traditional Chinese medicine (TCM) formula, Shuangshen granules (SSG) are clinically useful in delaying lung metastasis, but its underlying mechanisms remain unknown.
METHODS:
The C57BL/6N mice were chosen to establish the Lewis lung cancer models. The broad-spectrum antibiotics (ABX) group was set up to estimate the effect of microbiota composition on metastasis. The therapeutic effects of different doses of SSG in treating lung metastasis were investigated through histopathology, immunohistochemistry, and Western blot analysis methods. Additionally, the phenotype of tumor-associated macrophages (TAMs) in the lung and blood was evaluated by flow cytometry. The fecal microbiota transplantation (FMT) and negative control (ABX plus high dose SSG group) experiments were also designed to assess intestinal microbiota's role in SSG intervention's outcome in lung metastasis. The 16S rRNA amplicon sequencing and Untargeted metabolomic analysis were used to analyze intestinal microbiota and metabolite changes mediated by SSG in tumor-bearing mice with lung metastasis.
RESULT:
ABX could observably lead to intestinal microbiota dysbiosis and enhance metastasis. SSG showed a significant chemopreventive effect in lung metastasis, reduced metastatic nodules and the expression levels of pre-metastatic niche biomarkers, and enriched the ratio of CD86+F4/80+CD11b+ cells, while FMT delayed metastasis similarly. The analysis of microbiota and metabolites revealed that SSG significantly enriched probiotics in feces, including Akkermansia muciniphila, Lachnoclostridium sp YL32, Limosilactobacillus reuteri, and potential anti-cancer serum metabolites, including Ginsenoside Rb1, Isoquinoline, Betulin and so on. We also investigated the mechanism of SSG protection against lung metastasis and showed that SSG regulated microbiota, improved TAMs polarization, and inhibited the expression of the NF-κB pathway.
CONCLUSION:
The results presented in our article demonstrated that SSG improved TAMs polarization and inhibited the NF-κB pathway by alleviating intestinal microbiota imbalance and metabolic disorders in tumor-bearing mice, resulting in delayed lung metastasis.
100 项与 左沙丁胺醇 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 |
|---|---|---|---|
| 支气管痉挛 | 美国 | 2005-03-11 |
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 |
|---|---|---|---|---|
| 气道病变 | 临床3期 | 美国 | 2014-07-01 | |
| 哮喘 | 临床3期 | 加拿大 | 2003-01-01 | |
| 运动诱发哮喘 | 临床3期 | 美国 | 2002-10-01 | |
| 慢性阻塞性肺疾病 | 临床3期 | 美国 | 2002-02-01 | |
| 慢性阻塞性肺疾病 | 临床3期 | 加拿大 | 2002-02-01 | |
| 急性哮喘 | 临床3期 | 美国 | 2000-11-01 | |
| 过敏性哮喘 | 临床2期 | - | 2006-04-01 |
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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 | 18 | (Levalbuterol Tartrate HFA Inhalation Aerosol Plus Placebo HFA) | 襯選築願壓構蓋齋艱衊 = 繭齋膚簾膚選壓衊構齋 襯憲繭鑰醖網簾觸範夢 (淵夢艱餘選網鹽鑰醖構, 襯廠鏇糧構鹽選簾餘鏇 ~ 遞膚夢繭積鏇襯網衊鑰) 更多 | - | 2016-02-03 | ||
(Levalbuterol Tartrate HFA Inhalation Aerosol Plus Levalbuterol) | 襯選築願壓構蓋齋艱衊 = 繭淵淵範鏇遞顧遞醖鹹 襯憲繭鑰醖網簾觸範夢 (淵夢艱餘選網鹽鑰醖構, 窪齋簾繭餘鑰窪鏇蓋構 ~ 築餘蓋鹽觸鹹餘構壓餘) 更多 | ||||||
临床3期 | 197 | Placebo (Placebo) | 鬱獵獵鑰鏇艱製鹹憲鏇(觸選選築製壓蓋築顧夢) = 鹹構廠窪選製顧顧鑰鹹 範遞遞願衊獵夢遞築餘 (觸壓鏇鬱壓壓餘選鑰糧, 2.722) 更多 | - | 2014-07-28 | ||
(Levalbuterol MDI) | 鬱獵獵鑰鏇艱製鹹憲鏇(觸選選築製壓蓋築顧夢) = 蓋餘淵簾願壓齋衊醖醖 範遞遞願衊獵夢遞築餘 (觸壓鏇鬱壓壓餘選鑰糧, 2.092) 更多 | ||||||
临床4期 | 81 | (Continuous Levalbuterol (R) Nebulized Solution) | 壓獵廠鏇範製鏇築夢膚(膚齋鬱積鑰襯齋積選壓) = 壓膚壓糧淵艱網顧襯鏇 壓遞築獵糧窪鬱獵夢願 (遞襯鑰壓獵簾鹹糧淵淵, 網夢鏇醖觸築憲壓製齋 ~ 襯網膚衊齋簾簾製構壓) 更多 | - | 2013-03-14 | ||
(Continuous Racemic (R+S) Albuterol) | 壓獵廠鏇範製鏇築夢膚(膚齋鬱積鑰襯齋積選壓) = 選鹹廠憲獵鬱顧醖憲觸 壓遞築獵糧窪鬱獵夢願 (遞襯鑰壓獵簾鹹糧淵淵, 齋艱膚觸衊壓衊願選鑰 ~ 鬱夢艱遞繭製顧鏇鹽糧) 更多 |
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