更新于：2024-11-04
Omadacycline Tosylate
甲苯磺酸奥马环素
更新于：2024-11-04
概要
基本信息
药物类型 小分子化药 |
别名 Amadacycline、Neopentyl aminomethylminocycline、Omadacycline + [13] |
作用机制 30S subunit抑制剂(30S核糖体亚基抑制剂) |
在研适应症 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (2018-10-02), |
最高研发阶段(中国)批准上市 |
特殊审评快速通道 (美国)、孤儿药 (美国)、孤儿药 (欧盟) |
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结构
分子式C36H48N4O10S |
InChIKeySETFNHZTVGTBHC-XGLFQKEBSA-N |
CAS号1075240-43-5 |
关联
29
项与 甲苯磺酸奥马环素 相关的临床试验一项1期、随机、双盲研究：在健康成人受试者中比较甲苯磺酸奥马环素片口服与盐酸莫西沙星片口服对肠道菌群的影响
A Phase 1, Randomized, Double-Blind Study to Compare the Effect of Omadacycline PO Versus Moxifloxacin PO on the Gut Microbiota in Healthy Adult Volunteers
一项3b期、随机、双盲、多中心临床研究：比较奥马环素IV/PO与莫西沙星IV/PO治疗成人社区获得性细菌性肺炎（CABP）受试者的安全性与有效性
100 项与 甲苯磺酸奥马环素 相关的临床结果
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100 项与 甲苯磺酸奥马环素 相关的转化医学
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100 项与 甲苯磺酸奥马环素 相关的专利（医药）
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285
项与 甲苯磺酸奥马环素 相关的文献（医药）2024-11-01INTERNATIONAL JOURNAL OF TUBERCULOSIS AND LUNG DISEASE
Omadacycline enhances the in vitro activity of clofazimine against Mycobacterium abscessus
Article
作者: de Steenwinkel, J.E.M. ; Mudde, S.E. ; Ammerman, N.C. ; Bax, H.I. ; Meliefste, H.M.
2024-10-08ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
Zidovudine in synergistic combination with nitrofurantoin or omadacycline:
in vitro
and in murine urinary tract or lung infection evaluation against multidrug-resistant
Klebsiella pneumoniae
Article
作者: Li, Qing-Qing ; Yu, Liang ; Liu, Yan-Yan ; Li, Jia-Bin ; Tian, Ping ; Zhu, Yun-Zhu ; Li, Ya-Sheng ; Yang, Yi ; Zhu, Rong-Qing ; Guo, Ya-Qin ; Guo, Ming-Juan
ABSTRACT:
Limited treatment options and multidrug-resistant (MDR)
Klebsiella pneumoniae
present a significant therapeutic challenge, underscoring the need for novel approaches. Drug repurposing is a promising tool for augmenting the activity of many antibiotics. This study aimed to identify novel synergistic drug combinations against
K. pneumoniae
based on drug repurposing. We used the clinically isolated GN 172867 MDR strain of
K. pneumoniae
to determine the reversal resistance activity of zidovudine (AZT). The combined effects of AZT and various antibiotics, including nitrofurantoin (NIT) and omadacycline (OMC), were examined using the checkerboard method, growth curves, and crystal violet assays to assess biofilms. An
in vitro
combination activity testing was carried out in 12 isolates of
K. pneumoniae. In vivo
murine urinary tract and lung infection models were used to evaluate the therapeutic effects of AZT + NIT and AZT + OMC, respectively. The fractional inhibitory concentration index and growth curve demonstrated that AZT synergized with NIT or OMC against
K. pneumoniae
strains. In addition, AZT + NIT inhibited biofilm formation and cleared mature biofilms.
In vivo
, compared with untreated GN 172867-infected mice, AZT + NIT and AZT + OMC treatment decreased colony counts in multiple tissues (
P
< 0.05) and pathological scores in the bladder and kidneys (
P
< 0.05) and increased the survival rate by 60% (
P
< 0.05). This study evaluated the combination of AZT and antibiotics to treat drug-resistant
K. pneumoniae
infections and found novel drug combinations for the treatment of acute urinary tract infections. These findings suggest that AZT may exert significant anti-resistance activity.
2024-10-02Journal of chemotherapy (Florence, Italy)
Evaluating omadacycline dosing regimens against drug-resistant pathogens including
Staphylococcus aureus
,
Streptococcus pneumoniae
and
Haemophilus influenzae
in adults: a pharmacokinetic/pharmacodynamic analysis using Monte Carlo simulation
Article
作者: Zhao, Ming-Feng ; Xiao, Xia ; Wei, Xiao-Chen
The objective of this study was to evaluate the efficacy of various dosing regimens of omadacycline against main drug-resistant pathogens in the treatment of acute bacterial skin and skin structure infections (ABSSSI) and community-acquired bacterial pneumonia (CABP). Monte Carlo simulations were conducted using pharmacokinetic parameters and pharmacodynamic data to calculate cumulative fractions of response (CFRs) in terms of drug area under the concentration curve/minimum inhibition concentration targets.CFR ≥ 90% was considered optimal for a dosage regimen. CFR of any approved oral/intravenous regimen with loading-dose was ≥ 90% against methicillin-resistant Staphylococcus aureus (MRSA) for ABSSSI and penicillin-resistant Streptococcus pneumonia, tetracycline-resistant Streptococcus pneumonia, MRSA and β-lactamase positive Haemophilus influenzae for CABP. In conclusion, approved oral/intravenous loading and maintenance doses of omadacycline showed enough efficacy in the treatment of ABSSI and CABP caused by the main drug-resistant pathogens.
100 项与 甲苯磺酸奥马环素 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 |
|---|---|---|---|
| 社区获得性细菌性肺炎 | 美国 | 2018-10-02 | |
| 皮肤和皮肤结构感染 | 美国 | 2018-10-02 |
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 |
|---|---|---|---|---|
| 社区获得性肺炎 | 临床3期 | 俄罗斯 | 2015-10-09 | |
| 细菌感染 | 临床3期 | 保加利亚 | 2015-06-01 | |
| 细菌感染 | 临床3期 | 克罗地亚 | 2015-06-01 | |
| 细菌感染 | 临床3期 | 匈牙利 | 2015-06-01 | |
| 细菌感染 | 临床3期 | 波兰 | 2015-06-01 | |
| 细菌感染 | 临床3期 | 乌克兰 | 2015-06-01 | |
| 皮肤结构和软组织感染 | 临床3期 | - | 2009-07-01 | |
| 复杂皮肤和皮肤结构感染 | 临床3期 | 美国 | 2009-04-04 | |
| 复杂皮肤和皮肤结构感染 | 临床3期 | 美国 | 2009-04-04 | |
| 传染性皮肤病 | 临床3期 | 美国 | 2009-04-04 |
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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3期 | - | Intravenous Omadacycline | 齋鏇遞廠蓋鏇製鑰築顧(憲壓鑰範選簾積鹹構糧) = 鏇鏇醖築觸蓋襯窪艱構 鏇鏇艱衊淵糧蓋簾簾顧 (鑰艱膚觸衊選顧範願齋 ) 更多 | 积极 | 2024-10-26 | ||
Oral Omadacycline | 齋鏇遞廠蓋鏇製鑰築顧(憲壓鑰範選簾積鹹構糧) = 醖獵襯獵網鑰鬱衊鹽願 鏇鏇艱衊淵糧蓋簾簾顧 (鑰艱膚觸衊選顧範願齋 ) 更多 | ||||||
GlobeNewswire 人工标引  | 批准上市 | 670 | NUZYRA® (omadacycline) | 醖醖顧積觸繭窪願衊壓(鹽選鏇範簾壓餘鹽鏇鏇) = 襯艱簾鏇蓋構簾壓艱鑰 鏇製壓夢構顧鑰獵鏇醖 (範鑰膚艱網製築鹹艱壓 ) 达到 更多 | 积极 | 2024-07-18 | |
醖醖顧積觸繭窪願衊壓(鹽選鏇範簾壓餘鹽鏇鏇) = 願艱顧積鹹壓構簾鬱積 鏇製壓夢構顧鑰獵鏇醖 (範鑰膚艱網製築鹹艱壓 ) 达到 更多 | |||||||
N/A | - | 鏇簾遞膚遞廠衊醖淵繭(築鬱憲鹹廠遞鑰襯壓糧) = 艱鏇遞壓簾鑰廠願製齋 鏇衊糧壓構襯繭繭觸齋 (製獵簾襯獵獵遞艱鬱廠 ) 更多 | 积极 | 2024-03-05 | |||
临床2期 | - | - | 鑰觸廠蓋觸餘糧網選鹽(獵窪構廠觸蓋醖觸鹽艱) = 鏇製醖獵醖鏇網顧膚築 獵憲艱觸醖製鬱顧觸網 (願鏇醖鏇遞鏇構衊製網 ) | 积极 | 2023-10-01 | ||
临床3期 | 774 | 鬱觸積鹽衊願艱鹹鬱膚(糧鑰蓋鹽憲鹹顧鑰夢選) = 築齋網艱積築簾齋願鏇 蓋製鑰衊願餘範壓範壓 (襯齋餘範襯壓鹽積鬱衊 ) | 积极 | 2023-01-01 | |||
鬱觸積鹽衊願艱鹹鬱膚(糧鑰蓋鹽憲鹹顧鑰夢選) = 壓獵遞繭範衊觸餘築窪 蓋製鑰衊願餘範壓範壓 (襯齋餘範襯壓鹽積鬱衊 ) | |||||||
临床3期 | - | 構鑰憲觸鹽糧鏇鏇鏇遞(構顧簾夢鑰鬱鹽積觸醖) = 餘淵窪蓋網簾壓膚廠鏇 艱襯選築齋鑰簾簾夢窪 (夢簾築餘窪願鬱鹹獵選 ) 更多 | 积极 | 2022-06-01 | |||
構鑰憲觸鹽糧鏇鏇鏇遞(構顧簾夢鑰鬱鹽積觸醖) = 衊窪簾齋網鑰衊簾簾夢 艱襯選築齋鑰簾簾夢窪 (夢簾築餘窪願鬱鹹獵選 ) 更多 | |||||||
临床1期 | 18 | 範衊獵網鑰窪簾簾構範(鹽遞簾願積襯觸築窪壓) = 憲顧壓齋餘艱窪夢壓鏇 觸觸壓築願鏇鑰觸顧願 (鹽積蓋鏇糧鏇鹽範窪壓, 窪範願鑰選糧鬱網蓋淵 ~ 蓋鏇簾蓋窪齋鬱糧醖製) 更多 | - | 2021-11-03 | |||
临床3期 | 774 | omadacyc | 醖積鹹範夢襯觸膚構鬱(願窪積鹹範顧夢選廠選) = Clinical success rates (ECR/PTE) were similar between treatment groups (across all subgroups). 淵遞獵鹹願選窪鏇鹽簾 (糧衊觸蓋夢築夢願鑰廠 ) 更多 | 相似 | 2021-06-18 | ||
临床3期 | 143 | 構廠築構製齋憲觸網淵(廠繭製蓋蓋獵衊廠鹽鹹) = 鏇襯願構淵繭艱淵鬱鹽 選繭艱鑰淵築襯顧鑰簾 (壓憲觸齋製遞窪糧積窪, 獵網齋製壓遞網醖築艱 ~ 繭鬱壓鏇範淵遞憲製築) 更多 | - | 2021-03-12 | |||
临床2期 | 234 | 齋蓋壓觸獵顧壓觸窪淵(製糧範繭範顧觸顧餘蓋) = 築築艱糧積範壓獵淵觸 築顧餘窪蓋積襯蓋蓋積 (齋廠鏇艱顧糧淵廠鏇鹹, 積遞壓願餘遞齋蓋窪網 ~ 齋膚襯衊獵襯齋願淵鏇) 更多 | - | 2020-10-12 |
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