product name Moxifloxacin HCl
Description: Moxifloxacin (also known as BAY12-8039 HCl) is a fourth generation fluoroquinolone antibacterial agent with a broad antibacterial spectrum against Gram positive bacteria and Gram negative bacteria in vitro. The antibacterial activity of moxifloxacin is from the inhibition effect of DNA topoisomerase II and topoisomerase IV which are involved in bacterial DNA replication, transcription, recombination and repair. The oral bioavailability of moxifloxacin is absolutely good which can be up to 90%. There are no many potenti[al drug interactions because that moxifloxacin is not a inhibitor or substrate of the hepatic cytochrome P-450 isoenzyme system.
References: Tuberculosis (Edinb). 2008 Mar;88(2):127-31; J Pharm Biomed Anal. 2005 Jun 1;38(1):8-13.
437.89
Formula
C21H24FN3O4.HCl
CAS No.
186826-86-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 88 mg/mL (201 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
30% PEG400+0.5% Tween80+5% Propylene glycol: 30 mg/mL
Synonyms
BAY12-8039 HCl
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
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| Formulation & Dosage | |
| References | Tuberculosis (Edinb). 2008 Mar;88(2):127-31; J Pharm Biomed Anal. 2005 Jun 1;38(1):8-13. |
