Antibodies
Moxifloxacin is a fourth-generation synthetic fluoroquinolone antibacterial agent.
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| Description | Moxifloxacin is a fourth-generation synthetic fluoroquinolone antibacterial agent. | |||||
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| In vitro | Moxifloxacin exerts its effects by trapping a DNA drug enzyme complex and speciï¬cally 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 efï¬cacy 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: speciï¬cally 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. [1] | |||||
| 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 signiï¬cant. AUC/MIC ratio correlates best with in-vivo efï¬cacy for the fluoroquinolones in a mouse model of tuberculosis. [1] | |||||
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| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
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| NCT01936480 | Not yet recruiting | Cardiac Arrhythmias | Massachusetts General Hospital | 2013-10 | Phase 4 |
| NCT01968733 | Recruiting | Community-acquired Bacterial Pneumonia | Cempra Pharmaceuticals | 2013-11 | Phase 3 |
| NCT01803399 | Not yet recruiting | Infections, Bacterial | GlaxoSmithKline | 2014-03 | Phase 1 |
| NCT01984827 | Not yet recruiting | Diabetes | Richmond Pharmacology Limited | 2014-03 | Phase 1 |
| NCT01515826 | Not yet recruiting | Cataracts | Alcon Research | 2014-03 | Phase 3 |
| Molecular Weight (MW) | 437.89 |
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| Formula | C21H24FN3O4.HCl |
| CAS No. | 186826-86-8 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | Avelox, Avalox |
| Solubility (25°C) * | In vitro | DMSO | 88 mg/mL (200 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 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. | |||
| Chemical Name | 1-cyclopropyl-6-fluoro-8-methoxy-7-((4aS,7aS)-octahydropyrrolo[3,4-b]pyridin-6-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid hydrochloride |
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| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.43789 | 4.3789 | 8.7578 | 13.1367 |