预约演示
更新于：2026-01-27
Omadacycline Tosylate
甲苯磺酸奥马环素
更新于：2026-01-27
概要
基本信息
药物类型 小分子化药 |
别名 Amadacycline、Neopentyl aminomethylminocycline、Omadacycline + [13] |
作用方式 抑制剂 |
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/序列
分子式C36H48N4O10S |
InChIKeySETFNHZTVGTBHC-XGLFQKEBSA-N |
CAS号1075240-43-5 |
关联
26
项与 甲苯磺酸奥马环素 相关的临床试验NCT06462326
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
NCT06162286
A Phase 3b Randomized, Double-blind, Multi-center Study to Compare the Safety and Efficacy of Omadacycline IV/PO to Moxifloxacin IV/PO for Treating Adult Subjects With Community-acquired Bacterial Pneumonia (CABP)
NCT05753215
Omadacycline Versus Standard-of-Care Oral Antibiotic Treatment for Bone and Joint Infections: An Open-Label, Non- Inferiority, Randomized, Controlled Trial
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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318
项与 甲苯磺酸奥马环素 相关的文献（医药）2026-01-06JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
Omadacycline as a drug candidate for
Mycobacterium avium
infections:
in vitro
insights on single and combination therapies
Article
作者: De Steenwinkel, Jurriaan E M ; Meliefste, Henriëtte M ; Ammerman, Nicole C ; Serio, Alisa W ; Klaassen, Corné H W ; Mudde, Saskia E ; Pierce, Jessica V ; Bax, Hannelore I
Abstract:
Objectives:
The current antibiotic arsenal for the treatment of Mycobacterium avium infections is limited and new treatment options are needed. This exploratory study assessed the in vitro activity of omadacycline against M. avium alone and combined with current guideline-recommended antibiotics and the ability of omadacycline to prevent the emergence of antibiotic resistance.
Methods:
The activity of omadacycline and comparator antibiotics against M. avium was studied by minimum inhibitory concentration (MIC) assays and time-kill kinetics assays to investigate time- and concentration-dependent activity patterns. Omadacycline’s ability to prevent clarithromycin and amikacin resistance was investigated by phenotypic and molecular assays.
Results:
The MIC of omadacycline was impacted by medium composition: a higher MIC was found in CAMHB (128 mg/L) versus Middlebrook broth (8 mg/L). MIC values were also impacted by omadacycline instability in solution over time and daily drug supplementation reduced the MIC to 1 mg/L. In time-kill assays, omadacycline demonstrated time- and concentration-dependent activity. Omadacycline-containing drug combinations resulted in varying degrees of enhanced activity, which was most apparent for omadacycline plus amikacin. Omadacycline prevented amikacin MICs from increasing and impeded the emergence of rrs mutations observed with amikacin alone. While enhanced activity of omadacycline plus clarithromycin was less pronounced, rrl mutations were not detected in the presence of omadacycline.
Conclusions:
Omadacycline demonstrated in vitro activity against M. avium, particularly in combination with amikacin. Emergence of clarithromycin and amikacin resistance seemed to be prevented by co-exposure to omadacycline. Further research is warranted to assess omadacycline’s role in treating M. avium disease.
2026-01-06JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
Preclinical evaluation of epetraborole in the hollow fibre system model of
Mycobacterium abscessus
lung disease
Article
作者: Gumbo, Tawanda ; Srivastava, Shashikant ; Boorgula, Gunavanthi D ; Daley, Charles L ; Singh, Sanjay ; Nguyen, Minh-Vu H
Abstract:
Background:
In patients with Mycobacterium abscessus (MAB) lung disease (LD), guideline-based therapy (GBT) achieves sputum culture conversion in only 20–35% of patients. The poor efficacy is reflected in the hollow fibre model system for MAB-LD (HFS-MAB), where GBT drugs’ maximal microbial kill (Emax) below day 0 burden (B0) were amikacin 3 colony-forming units (cfu)/mL, clarithromycin–cefoxitin–amikacin (GBT) 17 cfu/mL, imipenem 20 cfu/mL, and tigecycline 24 cfu/mL.
Methods:
We tested the bacterial leucyl-tRNA synthetase (LeuRS) inhibitor, epetraborole, for MICs in 59 MAB isolates, and with seven epetraborole exposures in the HFS-MAB over 21 days. Data were analysed using the inhibitory sigmoid Emax model for microbial kill, and a quadratic function for resistance. Monte Carlo experiments (MCE) were performed to identify the optimal epetraborole dose for the clinic.
Results:
The epetraborole MIC50 was 0.125 mg/L, and the MIC90 was 0.25 mg/L. Epetraborole killed 253 cfu/mL below B0. However, epetraborole microbial effect was terminated by antimicrobial resistance, in an exposure-dependent fashion. Whole genome sequencing revealed concentration-dependent generation of resistance-associated LeuRS mutations, including novel mutations such as Asp433Val, Arg324Ser, and Phe310Cys. The exposure mediating 80% of Emax (EC80) was an AUC0–24/MIC = 202.73. In MCE 750 mg twice daily achieved EC80 in 95.6% and 79.2% of virtual patients for intravenous versus oral administration, respectively.
Conclusion:
Epetraborole microbial kill is the best, thus far, achieved in the HFS-MAB, more than two times omadacycline’s 123 cfu/mL below B0. We propose to test a novel combination regimen of epetraborole plus omadacycline plus a β-lactam versus GBT first in the HFS-MAB, followed by clinical trials.
2026-01-06Microbiology Spectrum
Eravacycline pharmacokinetics/pharmacodynamics in the hollow fiber system model of
Mycobacterium abscessus
lung disease
Article
作者: Boorgula, Gunavanthi D. ; Gumbo, Tawanda ; Long, Mary C. ; Srivastava, Shashikant ; Shrivastava, Avneesh ; Singh, Sanjay ; Robbins, Brian
ABSTRACT:
Treatment of
Mycobacterium abscessus
(MAB) pulmonary diseases is challenging due to intrinsic resistance to many antibiotics and requires prolonged intravenous therapy with drugs that have severe side effects. The treatment guidelines include tetracyclines as part of the combination. We tested a 3rd generation tetracycline, eravacycline, for its potential role in MAB pulmonary disease. Eravacycline minimum inhibitory concentration (MIC) (ATCC#19977 strain and 59 clinical isolates) ranged between 0.0075 and 0.3 mg/L, and the MIC
50
and MIC
90
were 0.15 and 0.3 mg/L, respectively. In the static concentration-response studies, eravacycline killed 5.58 + 0.34 log
10
CFU/mL MAB, and EC
50
(concentration associated with 50% of the maximal effect [
Emax
]) was 0.05 ± 0.01 mg/L. In the hollow fiber system model of
Mycobacterium abscessus
(HFS-MAB), examining eight eravacycline human-equivalent lung exposures, the ratio of area under the concentration-time curve to MIC (AUC
0-24
/MIC) of 3,588 was identified as EC
80
or the optimal exposure target for MAB kill. The probability of target attainment even with eravacycline doses of 4 mg/kg twice a day (8 mg/kg/day) falls below 90% at an MIC of 0.125 mg/L, and the cumulative fraction of response was only 30.56% in the 10,000 virtual patient trial. In summary, a MIC pattern does not accurately inform whether a tetracycline (in this study, eravacycline) has good efficacy, which must be determined using preclinical models applying a pharmacokinetics/pharmacodynamics study design. The HFS-MAB results suggest that, despite low MICs, the probability of better therapeutic outcomes with eravacycline is limited.
IMPORTANCE:
Treatment of
Mycobacterium abscessus
(MAB) pulmonary diseases is challenging due to intrinsic resistance to many antibiotics. The ATS/IDSA guidelines include tetracyclines as part of the combination. Eravacycline is a new tetracycline approved for the treatment of complicated intra-abdominal bacterial infections with better tolerability and low gastrointestinal adverse events compared to tigecycline. We performed an eravacycline pharmacokinetics (PK)-pharmacodynamics (PD) study for dose optimization with respect to the MAB pulmonary disease mimicking the intrapulmonary PKs in the hollow fiber model system of MAB (HFS-MAB). While eravacycline MICs and static concentrations suggest great potential and even activity better than omadacycline and tigecycline, the drug only killed 0.56 log
10
CFU/mL below stasis in the HFS-MAB. Monte Carlo simulation experiments suggested that optimal doses for MAB pulmonary disease are likely in the range that would not be tolerated by patients.
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 |
|---|---|---|---|---|
| 蜂窝织炎 | 临床3期 | 中国 | 2019-03-01 | |
| 蜂窝织炎 | 临床3期 | 中国 | 2019-03-01 | |
| 丹毒 | 临床3期 | 中国 | 2019-03-01 | |
| 丹毒 | 临床3期 | 中国 | 2019-03-01 | |
| 社区获得性肺炎 | 临床3期 | 格鲁吉亚 | 2015-11-22 | |
| 简单的皮肤和皮肤结构感染(uSSSI) | 临床3期 | - | 2009-07-01 | |
| 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2期 | 66 | (Omadacycline 300 mg) | 蓋遞願夢衊築鑰壓製廠 = 築顧製選繭範鏇鏇願鏇 夢齋餘壓夢繭淵夢願糧 (觸網廠夢艱襯衊顧襯夢, 鏇觸蓋蓋壓壓廠鹹窪網 ~ 觸鬱衊網鏇獵鹽醖簾淵) 更多 | - | 2025-07-30 | ||
placebo (Placebo) | 蓋遞願夢衊築鑰壓製廠 = 壓糧襯鬱蓋鏇鬱網窪獵 夢齋餘壓夢繭淵夢願糧 (觸網廠夢艱襯衊顧襯夢, 鹹窪糧膚鹽構夢願積簾 ~ 鏇糧積憲積顧艱膚鬱憲) 更多 | ||||||
临床2期 | - | 觸夢壓廠壓鏇憲蓋顧蓋(淵製憲艱壓簾觸廠窪製) = 憲積齋廠壓繭簾廠艱齋 廠網衊鹽齋鑰鹽艱蓋獵 (壓選觸網膚襯遞簾窪積 ) | 积极 | 2025-05-16 | |||
Placebo | 觸夢壓廠壓鏇憲蓋顧蓋(淵製憲艱壓簾觸廠窪製) = 獵艱鹽獵壓鬱壓獵餘獵 廠網衊鹽齋鑰鹽艱蓋獵 (壓選觸網膚襯遞簾窪積 ) | ||||||
临床3期 | 670 | (Omadacycline) | 糧窪糧膚壓蓋壓觸壓餘 = 襯鏇餘壓餘衊餘窪鑰廠 憲艱積遞壓構衊糧製膚 (壓醖積糧獵艱願廠築鹽, 夢窪齋齋醖膚衊壓觸衊 ~ 鏇夢醖醖範鬱醖廠鹹觸) 更多 | - | 2025-04-09 | ||
(Moxifloxacin) | 糧窪糧膚壓蓋壓觸壓餘 = 廠糧壓構窪簾鏇艱鹹願 憲艱積遞壓構衊糧製膚 (壓醖積糧獵艱願廠築鹽, 醖顧壓膚願襯淵選願襯 ~ 願鹹網襯範衊廠壓鏇鏇) 更多 | ||||||
临床4期 | - | 8 | 構鑰醖繭艱蓋鹹壓醖觸(艱鹹窪鏇繭選築憲願遞) = 選鹹築鑰築艱衊鑰餘鏇 膚鹹構糧窪膚廠壓願遞 (鑰範願願餘觸窪餘鏇構, 0.0622) 更多 | - | 2025-03-17 | ||
临床4期 | 9 | 淵選構範壓淵繭遞夢蓋(製廠願鹹觸積構膚窪餘) = 淵蓋繭鏇憲鹹範淵襯壓 選壓鬱糧醖選壓構遞構 (選鑰憲鏇衊餘鬱願觸選 ) | 积极 | 2024-12-01 | |||
淵選構範壓淵繭遞夢蓋(製廠願鹹觸積構膚窪餘) = 選蓋衊艱糧壓觸衊餘顧 選壓鬱糧醖選壓構遞構 (選鑰憲鏇衊餘鬱願觸選 ) | |||||||
临床2期 | 66 | 選簾壓繭蓋鬱鹽願夢鹹(襯鏇鑰壓積餘廠憲積鏇) = 廠築糧壓餘願鑰襯憲齋 網選積襯築遞鹽鬱觸積 (窪襯繭鬱壓淵範鹹築鑰 ) 更多 | 积极 | 2024-11-08 | |||
Placebo | 選簾壓繭蓋鬱鹽願夢鹹(襯鏇鑰壓積餘廠憲積鏇) = 衊積繭膚廠鹹製鏇範艱 網選積襯築遞鹽鬱觸積 (窪襯繭鬱壓淵範鹹築鑰 ) 更多 | ||||||
临床3期 | - | 製鹽夢壓壓鹹窪廠鬱積(顧襯衊獵襯鏇網遞顧築) = 簾願齋鹹構壓淵鬱醖鬱 積顧鑰繭憲積壓夢鹹糧 (糧齋積鏇餘鬱蓋構鹹鬱 ) 更多 | 积极 | 2024-10-26 | |||
製鹽夢壓壓鹹窪廠鬱積(顧襯衊獵襯鏇網遞顧築) = 構製醖壓觸鹹艱築壓築 積顧鑰繭憲積壓夢鹹糧 (糧齋積鏇餘鬱蓋構鹹鬱 ) 更多 | |||||||
GlobeNewswire 人工标引  | 批准上市 | 670 | NUZYRA® (omadacycline) | 淵餘築鏇構餘網繭廠網(齋網繭顧廠糧襯餘淵鑰) = 窪醖醖獵簾構獵襯廠遞 餘壓簾選構糧夢鏇齋積 (繭繭鏇製積顧襯壓簾鹽 ) 达到 更多 | 积极 | 2024-07-18 | |
淵餘築鏇構餘網繭廠網(齋網繭顧廠糧襯餘淵鑰) = 鏇簾餘繭衊鑰壓簾齋遞 餘壓簾選構糧夢鏇齋積 (繭繭鏇製積顧襯壓簾鹽 ) 达到 更多 | |||||||
N/A | - | 網鹹鑰餘願夢鏇夢構膚(餘範衊鏇範顧憲遞選範) = 繭壓艱憲鏇顧築遞鹽蓋 鏇窪獵餘憲壓簾衊襯積 (餘顧襯構願製膚壓遞願 ) 更多 | 积极 | 2024-03-05 | |||
临床2期 | - | 襯網壓膚積夢願壓鏇構(鏇選獵餘願餘廠蓋艱餘) = 遞製齋醖構淵衊遞夢廠 窪憲艱夢構衊鏇範繭鬱 (窪鬱鑰鑰壓鬱顧構積艱 ) | 积极 | 2023-09-04 |
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