Catalog No.S1465 Synonyms: BAY12-8039 HCl
Molecular Weight(MW): 437.89
Moxifloxacin is a fourth-generation synthetic fluoroquinolone antibacterial agent.
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|Description||Moxifloxacin is a fourth-generation synthetic fluoroquinolone antibacterial agent.|
Moxiﬂoxacin exerts its effects by trapping a DNA drug enzyme complex and speciﬁcally inhibiting ATP-dependent enzymes topoisomerase II (DNA gyrase) and topoisomerase IV. Moxiﬂoxacin shows in-vitro potency against M. tuberculosis H37Rv with MIC of 0.177 μg/mL. Moxiﬂoxacin has broad Grampositive and Gram-negative activity. Moxiﬂoxacin shows in vitro and clinical efﬁcacy against Staphylococcus aureus, Streptococcus pneumoniae, Str. pyogenes, Haemophilus inﬂuenzae, H. parainﬂuenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Chlamydia pneumoniae and Mycoplasma pneumoniae. Moxiﬂoxacin has activity against mycobacteria in addition to M. tuberculosis; Moxiﬂoxacin is more active against M. kansasii than M. avium complex: speciﬁcally MIC90 for M. avium > M. intracellulare > M. kansasii at 4, 2 and 2 μg/mL, respectively. MIC90 for M. chelonae > M. fortuitum at 16 and 0.5 μg/mL, respectively. 
|In vivo||Moxiﬂoxacin combined with RIF/pyrazinamide (PZA) reduces treatment time by up to 2 months compared to regimens with isoniazid (INH)/RIF/PZA in a mouse model designed to mimic human disease. Similar results with a stable cure are reached after 4 months in mice treated twice weekly with RIF/Moxiﬂoxacin/PZA compared to cure in 6 months when daily treated with RIF/INH/PZA. 100 mg/kg Moxiﬂoxacin in mice gives activity comparable to INH; increased dose in mice to 400 mg/kg Moxiﬂoxacin daily results in spleen CFU counts lower than for INH 25 mg/kg although the differences are not statistically signiﬁcant. AUC/MIC ratio correlates best with in-vivo efﬁcacy for the ﬂuoroquinolones in a mouse model of tuberculosis. |
|In vitro||DMSO||88 mg/mL (200.96 mM)|
|In vivo||30% PEG400+0.5% Tween80+5% propylene glycol||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00816426||Completed||Tuberculosis||National Institute of Allergy and Infectious Diseases (NIAID)|Korean Center for Disease Control and Prevention|International Tuberculosis Research Center|Novartis Institute for Tropical Medicine|Asian Medical Center|National Institutes of Health Clinical Center (CC)||December 29, 2008||Phase 1|
|NCT03021616||Not yet recruiting||Cardiovascular Diseases||David Grant U.S. Air Force Medical Center||January 2017||--|
|NCT02589782||Recruiting||Tuberculosis, Multidrug-Resistant|Extensively Drug-Resistant Tuberculosis|Tuberculosis, Pulmonary||Medecins Sans Frontieres, Netherlands|London School of Hygiene and Tropical Medicine|Global Alliance for TB Drug Development|University College, London|Drugs for Neglected Diseases|Swiss Tropical & Public Health Institute|eResearch Technology, Inc.|Ministry of Health, Republic of Uzbekistan|World Health Organization|Ministry of Health, Belarus|TB & HIV Investigative Network (THINK)||January 2017||Phase 2|Phase 3|
|NCT02680080||Not yet recruiting||Long QT Syndrome||Tel-Aviv Sourasky Medical Center|Tel Aviv Medical Center||December 2016||--|
|NCT02754765||Recruiting||Tuberculosis, Multidrug-Resistant||Médecins Sans Frontières France|Partners in Health|Harvard Medical School|Epicentre|Institute of Tropical Medicine, Belgium|Ministry of Health, Kyrgyzstan|National Center for Tuberculosis Problems, Kazakhstan|Ministry of Health, Lesotho|National Center for Tuberculosis and Lung Diseases, Georgia|Socios En Salud, Peru||December 2016||Phase 3|
|NCT02903836||Recruiting||Community-Acquired Bacterial Pneumonia (CABP)||Wockhardt|ACM||September 2016||Phase 2|
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