预约演示
更新于：2026-04-18
Levalbuterol Tartrate
左沙丁胺醇
更新于：2026-04-18
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
32
项与 左沙丁胺醇 相关的临床试验CTRI/2025/07/091233
Randomized controlled clinical trial to compare the efficacy of oral administration of tekrajras syrup with levosalbutamol syrup in kaphaj kasa in children - NIL
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
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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356
项与 左沙丁胺醇 相关的文献（医药）2026-02-02Pakistan Journal of Pharmaceutical Sciences
Efficacy Of Levosalbutamol For Lung Cancer Patients Receiving Postoperative Sputum Expectoration By High-Frequency Chest Wall Oscillation
Article
作者: Leng, Hongrui ; Wang, Yongmei
Background: Sputum expectoration is an important nursing link for lung cancer patients after thoracoscopic lobectomy. Objectives: To evaluate the efficacy of levosalbutamol as an adjunct to high-frequency chest wall oscillation (HFCWO) for sputum expectoration in lung cancer patients after thoracoscopic lobectomy. Methods: Sixty lung cancer patients who underwent thoracoscopic lobectomy were retrospectively divided into control (n = 30) and study (n = 30) group. After thoracoscopic lobectomy, both groups received the sputum expectoration by HFCWO for one week. In addition, the study group was treated with levosalbutamol for one week. The postoperative sputum volume was recorded. The pulmonary complications were observed. The preoperative and postoperative pulmonary function indices, blood gas indices and inflammatory response indices were also observed. Results: The study group showed a significantly lower sputum volume on postoperative day 2, 3, 4 and 5, compared to control group. On postoperative day 7, the study group demonstrated significantly better function indices, blood gas indices and inflammatory response indices compared to control group. The pulmonary complications showed no significant different between two groups. Conclusion: Levosalbutamol as an adjunct can enhance the efficacy for lung cancer patients receiving postoperative sputum expectoration by HFCWO, which is evidenced by elevated sputum clearance, enhanced pulmonary function, increased oxygenation and declined inflammatory response.
2025-08-03JOURNAL OF ASTHMA
Safety and effectiveness of mepolizumab in adult patients with severe asthma with an eosinophilic phenotype from India: a Phase IV, open-label, single-arm, 24-week study (PRISM)
Article
作者: Swarnakar, Rajesh ; Adsule, Samir ; Meshram, Priti ; Hegde, Rashmi ; Maturu, Venkata Nagarjuna ; Deb, Pooja ; Gupta, Disha
OBJECTIVE:
Existing mepolizumab trials have excluded patients with severe asthma with an eosinophilic phenotype (SAEP) from India. This study (NCT04276233) investigated the safety and effectiveness of mepolizumab in Indian adults with SAEP.
METHODS:
Multi-center, open-label, single-arm, interventional study; patients received 100 mg mepolizumab subcutaneously every four weeks for 24 weeks. Primary endpoint: incidence of adverse events (AEs), serious AEs (SAEs), and AEs of special interest (AESIs). Secondary endpoints: clinically significant exacerbation (CSEs) frequency (including exacerbations requiring hospitalization); change from baseline to Week 24 in forced expiratory volume/second (FEV1), peak expiratory flow (PEF), and Asthma Control Questionnaire (ACQ-5) scores.
RESULTS:
Overall, 100 patients received ≥1 mepolizumab dose. Baseline characteristics: female, 51.0%; mean (standard deviation [SD]) age, 44.8 (12.0) years; mean (SD) body mass index, 24.4 (4.7) kg/m2. On-treatment AEs and SAEs were reported by 18.0% and 3.0% of patients, respectively; regarding AESIs, 5.0% reported infection and 2.0% reported systemic reaction. One fatal event occurred (unrelated to mepolizumab). CSEs were reported by 8.0% of patients; 2.0% had an exacerbation requiring hospitalization. Least squares (LS) mean change (95% confidence interval) in pre- and post-bronchodilator FEV1 and PEF by Week 24 was 0.081 L (-0.05, 0.21; p = 0.231), 0.055 L (-0.06, 0.17; p = 0.325), and 13.67 L/min (3.08, 24.25; p = 0.012), respectively. By Week 24, ACQ-5 scores had significantly improved (LS mean change [standard error]: -0.69 [0.121]; p < 0.001).
CONCLUSIONS:
Mepolizumab was well tolerated in Indian adults with SAEP and improved asthma control and health-related quality of life.
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.
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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N/A | 57 | 鹹糧鏇繭製選壓壓窪艱(淵糧餘獵壓蓋齋遞醖鑰) = 積夢糧簾憲鹽遞憲衊艱 鹽憲餘窪鏇獵醖繭蓋糧 (積蓋積製製遞鬱願鏇廠 ) 更多 | 积极 | 2023-09-09 | |||
临床3期 | 18 | (Levalbuterol Tartrate HFA Inhalation Aerosol Plus Placebo HFA) | 衊膚膚鹽醖窪觸製鑰網 = 鹽鏇繭襯膚壓窪襯鬱顧 蓋遞艱積鑰繭獵鑰膚獵 (鏇膚窪鏇艱獵蓋壓淵鏇, 憲夢鹹憲餘簾鬱鑰醖襯 ~ 窪鑰選膚觸鹽選顧憲繭) 更多 | - | 2016-02-03 | ||
(Levalbuterol Tartrate HFA Inhalation Aerosol Plus Levalbuterol) | 衊膚膚鹽醖窪觸製鑰網 = 範簾製廠獵觸齋鑰鑰艱 蓋遞艱積鑰繭獵鑰膚獵 (鏇膚窪鏇艱獵蓋壓淵鏇, 襯簾積糧壓製鬱蓋鑰齋 ~ 壓淵襯憲膚築願觸蓋淵) 更多 | ||||||
临床3期 | 197 | Placebo (Placebo) | 觸廠襯窪繭蓋衊醖鬱壓(廠繭顧襯艱網選願憲鹹) = 顧餘製鬱鑰鬱鏇觸壓醖 醖鑰範廠憲製窪願網餘 (鏇憲顧鏇蓋窪繭襯網顧, 2.722) 更多 | - | 2014-07-28 | ||
(Levalbuterol MDI) | 觸廠襯窪繭蓋衊醖鬱壓(廠繭顧襯艱網選願憲鹹) = 觸蓋鑰窪構鹽鹹窪築蓋 醖鑰範廠憲製窪願網餘 (鏇憲顧鏇蓋窪繭襯網顧, 2.092) 更多 | ||||||
临床4期 | 81 | (Continuous Levalbuterol (R) Nebulized Solution) | 艱鑰鏇襯鹹蓋窪製遞醖(醖觸鬱淵築壓鬱製襯襯) = 壓構襯醖鬱製鏇壓築鬱 襯製選憲襯艱遞憲廠築 (鹹鹹糧襯網遞憲鹹壓鹽, 獵憲觸夢簾鬱淵蓋顧壓 ~ 願構繭製遞鏇觸鏇窪繭) 更多 | - | 2013-03-14 | ||
(Continuous Racemic (R+S) Albuterol) | 艱鑰鏇襯鹹蓋窪製遞醖(醖觸鬱淵築壓鬱製襯襯) = 齋衊鏇網構構壓窪憲觸 襯製選憲襯艱遞憲廠築 (鹹鹹糧襯網遞憲鹹壓鹽, 醖鬱繭築願淵鏇膚齋壓 ~ 廠艱網鏇積選糧積窪襯) 更多 |
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