Sitafloxacin

Citafloxacin is a broad-spectrum quinolone antibacterial drug successfully developed by Daiichi Sankyo Co., LTD., which has good pharmacokinetic properties and can alleviate adverse reactions due to the presence of a cis-fluorocyclopropyl group in its molecular structure, and its antibacterial activity in vitro is significantly enhanced compared with most similar drugs. Oral tablets and fine granules were first marketed in Japan in June 2008 for the treatment of severe refractory infectious diseases. The injectable form is being tested in Phase III clinical trials in Japan by Daiichi Pharmaceutical for the treatment of bacterial infections. The injectable form is in Phase II clinical trials in the United States and Europe. The tablets are in Phase III clinical trials in the United States and Phase II clinical trials in Europe. Although the compound itself does not have antifungal activity, it can enhance the activity of existing antifungal drugs and therefore has potential in the treatment of fungal infections. Animal toxicity studies have shown that the compound has no central nervous system adverse reactions common to other 4-quinolone chemicalbooks. Clinical trials have shown that sitafloxacin can be used for the treatment of urinary tract infections, respiratory infections, and skin and soft tissue infections, but no comparative study data are available. Citafloxacin has a broad spectrum of antibacterial activity, and has significant antibacterial activity against gram-negative bacteria, which is stronger than ciprofloxacin and ofloxacin. At the same time, it has strong antibacterial activity against Gram-positive bacteria (methicillin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis), anaerobic bacteria (including fragile bacilli), mycoplasma and chlamydia. It also has good bactericidal effect on many common clinical fluoroquinolone-resistant strains. This product has good oral absorption, bioavailability greater than 70%, wide tissue distribution, and drug concentration in a variety of tissues outside the central nervous system is higher than the serum drug concentration. Therefore, this product is expected to become an important drug for the treatment of single or mixed bacterial infections such as respiratory tract, urogenital tract, abdominal cavity, skin and soft tissue.