Sitafloxacin

Sitafloxacin is a new‑generation, broad‑spectrum oral fluoroquinolone antibiotic approved for the treatment of respiratory and urinary tract infections. As a fluoroquinolone antibiotic, Sitafloxacin effectively inhibits the activity of bacterial DNA gyrase and topoisomerase IV, enzymes critical for bacterial DNA replication. Sitafloxacin is supplied as a crystalline solid with a purity of ≥98%. The unique spirocyclic substituent at the C7 position of Sitafloxacin contributes to its enhanced activity against fluoroquinolone‑resistant strains. Sitafloxacin is also available as a reference standard for analytical method development, method validation, quality control applications, and ANDA filings.

 

Product Parameters

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Parameter	Specification
Product Name	Sitafloxacin
CAS Number	127254-12-0
Molecular Formula	C₁₉H₁₈ClF₂N₃O₃
Molecular Weight	409.81 g/mol
Appearance	White crystalline solid
Density	1.63 ± 0.1 g/cm³ (predicted)
Boiling Point	629.2 ± 55.0 °C (predicted)
Storage Condition	Store at -20°C

 

Antibacterial activity

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In a study, ceftazidime demonstrated superior activity compared to ciprofloxacin and ofloxacin against the majority of Gram-negative bacteria among over 5,000 clinically isolated strains. It exhibited stronger efficacy than sparfloxacin, fleroxacin, or ofloxacin against Streptococcus pneumoniae, S. pyogenes, methicillin-or quinolone-sensitive or resistant Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis, Pseudomonas species, Xanthomonas aliphatica, Haemophilus influenzae, Neisseria gonorrhoeae, and Bacteroides fragilis (MIC90:0.006–3.13 μg/mL; Chemical Book). Ceftazidime was the most active compound against Enterobacteriaceae. Its activity against Moraxella (MIC90 = 0.025 μg/mL) and Acinetobacter calcoaceticus (MIC90 = 0.39 μg/mL) was comparable to that of sparfloxacin. Ciprofloxacin and tosufloxacin showed activity equivalent to ceftazidime against Klebsiella oxytoca, while ciprofloxacin exhibited comparable activity to ceftazidime against Proteus mirabilis. For all other tested strains, ceftazidime demonstrated superior activity compared to the aforementioned antibiotics (including lomefloxacin).

 

Pharmacokinetics

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Health volunteers administered a single oral dose of ceftazidime ranging from 25 to 200 mg, showing dose-dependent increases in Cmax values (0.29–1.86 μg/mL) and AUC values (1.52–12.03 μg·mL⁻¹·h). Under fasting conditions, the half-life (t₁/₂β) ranged from 4.40 to 5.02 h; volume of distribution (VdSS) was 1.46–1.96 L/kg; peak plasma concentration (tmax) occurred at 1.0–1.3 h; and clearance (CL) was 28–32 mL/min. The urinary recovery rate over 48 hours ranged from 69% to 74% of the administered dose, with fecal excretion accounting for only 3%. At a dose of 100 mg, the serum protein binding rate was approximately 50%. Multiple administrations did not significantly affect pharmacokinetics, indicating low accumulation potential of ceftazidime. The primary metabolite is a glucoside ester derivative, constituting 30–38% of the serum concentration and 5–12% of the urinary concentration in rats.

 

Bioactivity

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Sitafloxacin (DU6859a) is an effective oral fluoroquinolone antibiotic with in vitro activity against a broad spectrum of Gram-positive and Gram-negative bacteria, including anaerobic species and atypical pathogens. It is indicated for the treatment of respiratory tract infections and urinary tract infections.

 

Contact Us

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