Otsu Yoshiko, Yanagihara Katsunori, Fukuda Yuichi, Miyazaki Yoshitsugu, Tsukamoto Kazuhiro, Hirakata Yoichi, Tomono Kazunori, Kadota Jun-ichi, Tashiro Takayoshi, Murata Ikuo, Kohno Shigeru
Second Department of Internal Medicine, Nagasaki University School of Medicine, Nagasaki, Japan.
Antimicrob Agents Chemother. 2003 Dec;47(12):3699-703. doi: 10.1128/AAC.47.12.3699-3703.2003.
DQ-113 is a new quinolone with potent activity against gram-positive pathogens. The in vivo activity of DQ-113 against Streptococcus pneumoniae was compared with those of gatifloxacin and ciprofloxacin in a mouse model. For this purpose, two strains of S. pneumoniae were used: penicillin-susceptible S. pneumoniae (PSSP) and penicillin-resistant S. pneumoniae (PRSP). The survival rates of mice infected with PSSP and PRSP at 14 days after infection were 80% in the DQ-113-treated group and 0 to 10% in the other three groups. In murine infections caused by PSSP, the 50% effective doses (ED50s) of DQ-113, gatifloxacin, and ciprofloxacin were 6.0, 41.3, and 131.6 mg/kg, respectively. Against PRSP-caused pneumonia in mice, the ED50s of DQ-113, gatifloxacin, and ciprofloxacin were 7.6, 64.7, and 125.9 mg/kg, respectively. Compared with the other drugs, DQ-113 showed excellent therapeutic efficacy and eradicated viable bacteria in both PSSP- and PRSP-infected mice. The means +/- standard errors of the means of viable bacterium counts in the lungs of gatifloxacin-treated, ciprofloxacin-treated, and untreated control mice infected with PSSP were 2.91 +/- 0.34, 3.13 +/- 0.48, and 3.86 +/- 0.80 log10 CFU/ml, respectively. The same counts in mice infected with PRSP treated with the same three agents were 6.57 +/- 0.99, 6.54 +/- 0.40, and 7.17 +/- 0.43 log10 CFU/ml, respectively. DQ-113 significantly decreased the number of viable bacteria in the lungs compared with gatifloxacin and ciprofloxacin. Of the drugs analyzed, the pharmacokinetic-pharmacodynamic parameter of area under the concentration-time curve (AUC)/MIC ratio for DQ-113 was significantly higher than those for gatifloxacin and ciprofloxacin. Our results suggest that DQ-113 has potent in vivo efficacy against both PSSP and PRSP.
DQ - 113是一种对革兰氏阳性病原体具有强效活性的新型喹诺酮类药物。在小鼠模型中,将DQ - 113对肺炎链球菌的体内活性与加替沙星和环丙沙星进行了比较。为此,使用了两株肺炎链球菌:青霉素敏感肺炎链球菌(PSSP)和青霉素耐药肺炎链球菌(PRSP)。感染后14天,感染PSSP和PRSP的小鼠在DQ - 113治疗组的存活率为80%,在其他三组中为0%至10%。在由PSSP引起的小鼠感染中,DQ - 113、加替沙星和环丙沙星的50%有效剂量(ED50)分别为6.0、41.3和131.6mg/kg。针对小鼠中由PRSP引起的肺炎,DQ - 113、加替沙星和环丙沙星的ED50分别为7.6、64.7和125.9mg/kg。与其他药物相比,DQ - 113在PSSP和PRSP感染的小鼠中均显示出优异的治疗效果并根除了活菌。感染PSSP的加替沙星治疗组、环丙沙星治疗组和未治疗对照组小鼠肺中活菌计数的平均值±平均值标准误分别为2.91±0.34、3.13±0.48和3.86±0.80 log10 CFU/ml。用相同三种药物治疗的感染PRSP的小鼠中的相同计数分别为6.57±0.99、6.54±0.40和7.17±0.43 log10 CFU/ml。与加替沙星和环丙沙星相比,DQ - 113显著降低了肺中的活菌数量。在所分析的药物中,DQ - 113的浓度 - 时间曲线下面积(AUC)/ MIC比值的药代动力学 - 药效学参数显著高于加替沙星和环丙沙星。我们的结果表明,DQ - 113对PSSP和PRSP均具有强大的体内疗效。