预约演示
更新于：2026-05-12
Telithromycin
泰利霉素
更新于：2026-05-12
概要
基本信息
原研机构 |
权益机构- |
最高研发阶段临床前 |
最高研发阶段(中国)- |
特殊审评- |
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结构/序列
分子式C43H65N5O10 |
InChIKeyLJVAJPDWBABPEJ-PNUFFHFMSA-N |
CAS号191114-48-4 |
关联
29
项与 泰利霉素 相关的临床试验EUCTR2014-002867-13-3RD
Multinational, randomized, double blind, double dummy, pharmacokinetic study of telithromycin oral suspension (25 mg/kg once daily for 7-10 days), with secondary assessments of safety relative to azithromycin oral suspension (10 mg/kg once daily for 1 day followed by 5 mg/kg once daily for 4 days) in children with mild to moderate community-acquired pneumonia
EUCTR2006-003886-15-IT
Steady state telithromycin pharmacokinetics and pharmacodynamic in adult patients with mild-moderate acute exacerbation of chronic obstructive pulmonary disease treated with a standard oral dose 800 mg od for 5 days
NCT00315042
Multinational, Randomized, Double-Blind, Double Dummy, Comparative Study to Evaluate the Efficacy and Safety of 5 Days Telithromycin 25mg/kg od Versus 10 Days Penicillin V 13.3 mg/kg Tid in Children 6 Months to Less Than 13 Years With Streptococcus Pyogenes Tonsillitis/Pharyngitis
100 项与 泰利霉素 相关的临床结果
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100 项与 泰利霉素 相关的转化医学
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100 项与 泰利霉素 相关的专利（医药）
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1,221
项与 泰利霉素 相关的文献（医药）2026-04-01JOURNAL OF FOOD SCIENCE AND TECHNOLOGY-MYSORE
Phytochemical, antioxidant, and antimicrobial properties of Bellardia trixago methanol and ethanol extracts: insights from ADMET and molecular docking approaches
Article
作者: Aydın, Betül ; Torunoğlu, Emine Incilay ; Aytar, Erdi Can ; Durmaz, Alper
Abstract:
This study investigates the antioxidant, antimicrobial, and phytochemical properties of ethanol and methanol extracts derived from
Bellardia trixago
flowers alongside molecular docking and pharmacokinetic assessments of stigmasterol, a key bioactive compound. The antioxidant activities of the ethanol and methanol extracts were determined, with the methanol extract demonstrating higher activity, 0.370 ± 0.002 mg/mL, compared to the ethanol extract, 0.95 ± 0.09 mg/mL. The total phenolic content of the ethanol extract was 79.14 ± 2.30 mg GAE/g extract DW, and its flavonoid content was 244.31 ± 12.51 mg QE/g extract DW. The methanol extract contained a lower phenolic content of 51.50 ± 1.43 mg GAE/g extract DW but a higher flavonoid content of 251.67 ± 6.68 mg QE/g extract DW. The ethanol extract exhibited a superior iron chelation capacity of 8.21 ± 0.09 mg/mL relative to the methanol extract of 6.68 ± 0.28 mg/mL. Antimicrobial assays demonstrated that both extracts exhibited strong bactericidal and bacteriostatic effects, with MIC values ranging from < 0.39 mg/mL to > 125 mg/mL. The highest antimicrobial activity was observed against
Bacillus cereus
NRRL B-3711. Phytochemical analysis identified 25 compounds in the methanol extract and 20 in the ethanol extract. Stigmasterol was the major constituent in both extracts, accounting for 26.51% in ethanol and 12.65% in methanol. Molecular docking studies of stigmasterol revealed strong binding affinities with several protein targets, including
Candida albicans
Complex III2 (-8.7 kcal/mol),
Escherichia coli
HipBST (-7.2 kcal/mol), and the ribosomal subunit of
Staphylococcus aureus
(-7.0 kcal/mol). These interactions highlight stigmasterol’s potential role in modulating bacterial and fungal protein functions, emphasising the potential therapeutic applications of
B. trixago
, particularly in antimicrobial and antioxidant contexts.
2026-03-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Dual-targeting ketolide-quinolone hybrids overcome erm-mediated resistant pathogens via ribosomal and DNA gyrase inhibition
Article
作者: Liu, Rui-Chen ; Ma, Cong-Xuan ; Liu, Si-Meng ; Li, Yi-Lan ; Zhang, Jue-Ru ; Liu, Wen-Tian ; Wang, Si-Xi ; Li, Yun ; Liang, Jian-Hua ; Ding, Jing ; Guo, Li-Fan ; Yu, Ming-Jia
Macrolide antibiotics are classical protein synthesis inhibitors. However, the frequent development of clinical resistance significantly limits their utility. We report a novel series of ketolide-quinolone hybrids (26-31) that uniquely disrupt both protein synthesis and DNA replication. The new lead 26l exhibited balanced dual inhibition with IC50 values of 1.11 μM against ribosomes and 3.31 μM against DNA gyrases. In vivo mechanistic studies, including resistance mutation mapping in E. coli SQ110DTC strains and MIC profiling against ribosome- or/and gyrase-mutated E. coli SQ110DTC, confirmed concurrent target engagement of 26l. This bifunctional activity not only restored in vitro efficacy against macrolide-resistant erm-mediated resistant Gram-positive pathogens (S. pneumoniae and S. pyogenes), but also significantly enhanced activity against Gram-negative H. influenzae and M. catarrhalis. Notably, compound 26l demonstrated reduced CYP3A4 inhibition-a common side effect associated with macrolide antibiotics-compared to telithromycin. Compound 26l exhibited good stability in both mouse plasma and liver microsomes. Molecular docking studies elucidated how the hybrid simultaneously occupies two key bacterial targets-the ribosome and DNA gyrase-through specific interactions mediated by its macrolide core and quinolone moiety. With its dual-targeting mechanism, expanded spectrum coverage, and optimized safety properties, the new lead 26l emerges as a strategic solution to the escalating crisis of macrolide resistance in community-acquired bacterial pneumonia.
2026-02-01International Journal of Surgery
Retrospective cohort study of ocular adverse reactions to systemic drugs: insights from a multi-country spontaneous reporting database
Article
作者: Chen, Lin ; Wang, Shao-Pan ; Liu, Zuguo ; Hu, Jiaoyue ; Wu, Shi-Nan ; Huang, Caihong ; Chen, Xiao-Dong ; Liu, Qian-Ting
Background::
With the rise in long-term medication use, assessing ocular adverse reactions (OARs) from systemic drugs has gained importance. Using large real-world databases like the FDA Adverse Event Reporting System (FAERS) offers valuable clinical and pharmacovigilance insights.
Methods::
Disproportionality analysis, including the ratio of reported odds (ROR), was performed on all OAR reports related to systemic medications in the FAERS database from 2004 Q1 to 2024 Q3. The OARs were categorized into disease-based and symptom-based classifications to identify systemic medications with positive signals.
Results::
In the FAERS database, the most common OARs were cataract, dry eye, and glaucoma, with blurred vision, visual impairment, and eye pain as the leading symptoms. Through disproportionality analysis, 141 systemic medications with positive signal drugs for OAR risks were identified, which were concentrated in the following categories: antineoplastic medication [30 drugs, belantamab mafodotin ROR (95% confidence interval): 59.59 (56.25–63.13)], central nervous system medication [21 drugs, fingolimod, 2.69 (2.63–2.75)], anti-infective medication [15 drugs, moxifloxacin, 6.52 (6.21–6.84)], immunological and inflammation-related medication [15 drugs, dupilumab, 4.74 (4.7–4.79)], cardiovascular system medication [10 drugs, ivabradine, 3.06 (2.61–3.58)], endocrine and metabolic disease medication [10 drugs, insulin lispro, 3.63 (3.4–3.89)], respiratory system medication [6 drugs, telithromycin, 3.51 (3.14–3.93)], and other medication [34 drugs, botulinum toxin type A, 4.24 (4.12–4.36)].
Conclusion::
This pharmacovigilance study underscores the importance of identifying under-recognized OARs from systemic drugs to prevent secondary eye diseases and improve drug safety.
100 项与 泰利霉素 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 |
|---|---|---|---|
| 急性细菌性鼻窦炎 | 美国 | 2004-04-01 | |
| 感染 | 美国 | 2004-04-01 | |
| 急性鼻窦炎 | 欧盟 | 2001-07-09 | |
| 急性鼻窦炎 | 冰岛 | 2001-07-09 | |
| 急性鼻窦炎 | 列支敦士登 | 2001-07-09 | |
| 急性鼻窦炎 | 挪威 | 2001-07-09 | |
| 慢性支气管炎 | 欧盟 | 2001-07-09 | |
| 慢性支气管炎 | 冰岛 | 2001-07-09 | |
| 慢性支气管炎 | 列支敦士登 | 2001-07-09 | |
| 慢性支气管炎 | 挪威 | 2001-07-09 | |
| 社区获得性肺炎 | 欧盟 | 2001-07-09 | |
| 社区获得性肺炎 | 冰岛 | 2001-07-09 | |
| 社区获得性肺炎 | 列支敦士登 | 2001-07-09 | |
| 社区获得性肺炎 | 挪威 | 2001-07-09 | |
| 咽炎 | 欧盟 | 2001-07-09 | |
| 咽炎 | 冰岛 | 2001-07-09 | |
| 咽炎 | 列支敦士登 | 2001-07-09 | |
| 咽炎 | 挪威 | 2001-07-09 | |
| 扁桃体炎 | 欧盟 | 2001-07-09 | |
| 扁桃体炎 | 冰岛 | 2001-07-09 |
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 |
|---|---|---|---|---|
| 急性扁桃体炎 | 临床3期 | 美国 | 2006-02-01 | |
| 急性扁桃体炎 | 临床3期 | 阿根廷 | 2006-02-01 | |
| 急性扁桃体炎 | 临床3期 | 智利 | 2006-02-01 | |
| 急性扁桃体炎 | 临床3期 | 哥斯达黎加 | 2006-02-01 | |
| 链球菌感染 | 临床3期 | 美国 | 2006-02-01 | |
| 链球菌感染 | 临床3期 | 阿根廷 | 2006-02-01 | |
| 链球菌感染 | 临床3期 | 智利 | 2006-02-01 | |
| 链球菌感染 | 临床3期 | 哥斯达黎加 | 2006-02-01 | |
| 化脓性中耳炎 | 临床3期 | 美国 | 2006-01-01 | |
| 化脓性中耳炎 | 临床3期 | 阿根廷 | 2006-01-01 |
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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4期 | 298 | 願繭鑰願築餘築繭淵構(鏇獵蓋願遞廠鏇衊鑰簾) = 糧獵網製衊淵齋醖衊夢 鬱糧範蓋製鏇願鬱遞構 (夢窪蓋醖艱積艱艱醖鹽 ) 更多 | 积极 | 2008-06-01 | |||
Amoxicillin-clavulanate 875/125 mg | 願繭鑰願築餘築繭淵構(鏇獵蓋願遞廠鏇衊鑰簾) = 廠淵淵鏇築夢窪壓廠製 鬱糧範蓋製鏇願鬱遞構 (夢窪蓋醖艱積艱艱醖鹽 ) 更多 | ||||||
临床3期 | 278 | 顧衊鬱餘憲築鏇遞築夢(鑰窪願壓蓋鹹獵築觸蓋) = 範艱鬱遞願遞範鑰壓鹹 鹽簾淵鏇網鹽壓顧積壓 (窪鹹衊鏇憲簾築襯壓構 ) | - | 2006-04-13 | |||
Placebo | 顧衊鬱餘憲築鏇遞築夢(鑰窪願壓蓋鹹獵築觸蓋) = 醖鏇簾鏇築艱衊顧窪壓 鹽簾淵鏇網鹽壓顧積壓 (窪鹹衊鏇憲簾築襯壓構 ) |
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