期刊
CLINICAL PHARMACOLOGY IN DRUG DEVELOPMENT
卷 1, 期 4, 页码 121-130出版社
WILEY
DOI: 10.1177/2160763X12454714
关键词
fluoroquinolone; pharmacokinetics; lung penetration
资金
- Furiex Pharmaceuticals Inc.
This article summarizes key pharmacokinetic properties of JNJ-Q2, a broad-spectrum fluoroquinolone, being developed for acute bacterial skin and skin structure infections and community-acquired bacterial pneumonia. Two randomized placebo-controlled studies and one open-label study are presented: single and multiple ascending-dose studies evaluating intravenous (IV) and oral pharmacokinetics, absolute bioavailability accumulation, and lung penetration. Fifty-seven participants received JNJ-Q2, which was safe and well tolerated. The half-life was 13 to 20 hours, clearance (CL tot) was 4.41 to 6.22 L/h, volume of distribution (V-d) was 86 to 148 L, renal clearance (CLren) was 0.58 L/h, and the fraction excreted in urine (% Fe) was 12%. Accumulation ratio was 1.63, and absolute bioavailability was 0.65. The lung penetration study demonstrated substantial concentration of JNJ-Q2 in epithelial lining fluid and alveolar macrophages with ratios to free plasma of 50.6 and 156.9, respectively, at 6 hours postdose. JNJ-Q2 doses under consideration for future clinical trials are 150 mg for IV and 250-mg tablets for oral administration.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据