Pazufloxacin Advanced Drug Monograph

Pazufloxacin Report

Name: Pazufloxacin Name (English): Pazufloxacin DrugBank ID: DB11774 Type: Small Molecule CAS Number: 127045-41-4

Molecular Formula: $\mathrm{C}{16} \mathrm{H}{15} \mathrm{FN}{2} \mathrm{O}{4}$ Molecular Weight: 318.304 g/mol

Synonyms:

• T-3761
• (3S)-10-(1-aminocyclopropyl)-9-fluoro-3-methyl-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid
• (S)-10-(1-Aminocyclopropyl)-9-fluoro-3-methyl-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid
• 7H-Pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid, 10-(1-aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-, (3S)-
• Pazufloxacine
• Pazufloxacino

Pharmacology: Pazufloxacin is a fluoroquinolone antibiotic. It inhibits bacterial DNA gyrase and topoisomerase IV, enzymes essential for DNA replication and transcription. It demonstrates broad-spectrum antibacterial activity against Gram-negative and some Gram-positive bacteria, including strains resistant to cephalosporins, carbapenems, and aminoglycosides.

Indications: Pazufloxacin is marketed in some regions for the treatment of various bacterial infections, including respiratory and urinary tract infections. Clinical trials have also investigated its use in bacterial conjunctivitis.

Pharmacokinetics: Pazufloxacin exhibits good oral bioavailability and tissue penetration. It is mainly excreted in urine and has a short half-life (2-2.5 hours).

Drug Interactions: Pazufloxacin has the potential for numerous drug interactions. Examples include increased risk of QTc prolongation with certain medications, altered efficacy of antidiabetic agents, increased neuroexcitatory activities with NSAIDs, and decreased absorption with antacids containing aluminum or magnesium. It can also affect the metabolism of various drugs.

Adverse Effects: Reported adverse effects are similar to other quinolones and may include gastrointestinal disturbances. Drug-induced convulsions and hypotension have been reported but may be less frequent compared to other injectable fluoroquinolones. Pazufloxacin has been shown to have phototoxicity similar to ciprofloxacin.

Clinical Trials: Pazufloxacin has been investigated in clinical trials for various conditions. A Phase 3 trial for bacterial conjunctivitis treatment was terminated.

Chemical Properties:

• Melting Point: 269-271 °C
• Water Solubility: 2.41 mg/mL (for Pazufloxacin Mesilate)
• LogP: -0.51 (ALOGPS), -1 (Chemaxon)
• pKa: 5.59 (Strongest Acidic), 8.16 (Strongest Basic)

Safety Information: Pazufloxacin is classified as harmful if swallowed, in contact with skin, or if inhaled. Appropriate personal protective equipment should be used when handling this substance.

Note: This report provides a comprehensive overview based on available data. For specific medical advice and treatment guidelines, consult a healthcare professional.