Omadacycline tosylate is a newly developed aminomethylcycline antibiotic with applications in acute bacterial skin and skin structure infections (ABSSSI) as well as community-acquired bacterial pneumonia (CABP). Derived from minocycline, omadacycline shares similar mechanisms of action with other tetracyclines, inhibiting bacterial protein synthesis by binding to the 30S ribosomal subunit. Notably, omadacycline exhibits broad-spectrum antibacterial properties effective against a range of Gram-positive and Gram-negative aerobic, anaerobic, and atypical bacteria[1-4].
Omadacycline tosylate (0.5、2、8、32mg/kg; i.d) has shown strong efficacy in vivo against specific strains of Streptococcus pneumoniae, with bactericidal activity at all experimental doses [5]. Omacycline tosylate (0.25–64 mg/kg) has potent activity against Staphylococcus aureus, including methicillin-susceptible S. aureus (MSSA) and methicillin-resistant S. aureus (MRSA) in the neutropenic murine thigh infection model [6]. Mice treated with 15 mg/kg is efficacious in a murine model of pulmonary infection due to M. abscessus. Reduction in the CFU counts of Mycobacteroides abscessus Clinical Isolates in the lungs of mice occurred after 2 weeks of treatment with omadacycline tosylate [7]
References:
[1]. Zhanel GG, Esquivel J, et,al. Omadacycline: A Novel Oral and Intravenous Aminomethylcycline Antibiotic Agent. Drugs. 2020 Feb;80(3):285-313. doi: 10.1007/s40265-020-01257-4. PMID: 31970713.
[2]. Gallagher JC. Omadacycline: A Modernized Tetracycline. Clin Infect Dis. 2019 Aug 1;69(Suppl 1):S1-S5. doi: 10.1093/cid/ciz394. PMID: 31367739; PMCID: PMC6669280.
[3]. Watkins RR, Deresinski S. Omadacycline: A Novel Tetracycline Derivative With Oral and Intravenous Formulations. Clin Infect Dis. 2019 Aug 16;69(5):890-896. doi: 10.1093/cid/ciz242. PMID: 30893428.
[4]. Karlowsky JA, Steenbergen J, et,al. Microbiology and Preclinical Review of Omadacycline. Clin Infect Dis. 2019 Aug 1;69(Suppl 1):S6-S15. doi: 10.1093/cid/ciz395. PMID: 31367743; PMCID: PMC6669291.
[5]. Lepak AJ, Zhao M, et,al. In Vivo Pharmacodynamic Evaluation of Omadacycline (PTK 0796) against Streptococcus pneumoniae in the Murine Pneumonia Model. Antimicrob Agents Chemother. 2017 Apr 24;61(5):e02368-16. doi: 10.1128/AAC.02368-16. PMID: 28193651; PMCID: PMC5404567.
[6]. Lepak AJ, Zhao M, et,al. In Vivo Pharmacodynamics of Omadacycline against Staphylococcus aureus in the Neutropenic Murine Thigh Infection Model. Antimicrob Agents Chemother. 2019 Jun 24;63(7):e00624-19. doi: 10.1128/AAC.00624-19. PMID: 31036691; PMCID: PMC6591633.
[7]. Nicklas DA, Maggioncalda EC, et,al. Potency of Omadacycline against Mycobacteroides abscessus Clinical Isolates In Vitro and in a Mouse Model of Pulmonary Infection. Antimicrob Agents Chemother. 2022 Jan 18;66(1):e0170421. doi: 10.1128/AAC.01704-21. Epub 2021 Oct 18. PMID: 34662184; PMCID: PMC8765394.
Omadacycline tosylate是一种新型氨基甲基环素类抗生素。可用于急性细菌性皮肤及皮肤结构感染(ABSSSI)和社区获得性细菌性肺炎(CABP)。Omadacycline是米诺环素的衍生物。与其他四环素类似，Omadacycline tosylate通过结合30S核糖体亚基抑制细菌蛋白质合成。Omadacycline tosylate对革兰氏阳性和革兰氏阴性好氧、厌氧和非典型细菌具有广谱抗菌活性[1-4]。
Omadacycline tosylate (0.5、2、8、32mg/kg; i.d)在体内对特定的肺炎链球菌菌株显示出很强的疗效，在所有实验剂量下都具有杀菌活性[5]。在中性粒细胞减少小鼠大腿感染模型中，Omadacycline tosylate (0.25–64 mg/kg)对包括甲氧西林敏感金黄色葡萄球菌(MSSA)和耐甲氧西林金黄色葡萄球菌(MRSA)在内的金黄色葡萄球菌具有强效活性[6]。Omadacycline tosylate在15 mg/kg剂量对小鼠脓肿支原体肺部感染模型有效，用Omadacycline tosylate治疗2周后，小鼠肺部脓肿分枝杆菌临床分离株CFU计数减少[7]。