| Description | Garenoxacin (BMS284756) is a novel oral des-fluoro(6) quinolone for the treatment of Gram-positive and Gram-negative bacterial infections. |
| In vivo | 平均最大血浆浓度(Cmax)为3.00 ± 1.12 μg/mL，达到最大血浆浓度时间(Tmax)为3.0 ± 2.0小时，24小时内曲线下面积(AUC0-24)为40.7 ± 16.7 μg·h/mL。由于GRNX给药后24小时血浆浓度仍然较高，其半衰期(T1/2)无法计算。Cmax与GRNX每千克体重剂量强烈相关(r = 0.85, P = 0.03)。临床上，GRNX给药后3天内热症状消失，C反应蛋白水平在给药后14天回归正常。一位患者经历了血清转氨酶水平暂时性增加[1]。 |
| Animal experiments | Six male patients with infections who were undergoing MH received 200 mg GRNX once daily. Blood samples were taken before and at 1, 2, 4, 6, 12, and 24 hours after GRNX administration. Plasma GRNX concentrations were measured using high-performance liquid chromatography[1]. |
| Synonyms | BMS284756, 加雷沙星 |
| molecular weight | 426.41 |
| Molecular formula | C23H20F2N2O4 |
| CAS | 194804-75-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 2 mg/mL (4.69 mM) |
| References | 1. Aoyama T , Kamata K , Kishino S . Garenoxacin pharmacokinetics in patients undergoing maintenance hemodialysis[J]. Hemodialysis International, 2016. 2. Yuka Y , Tatsuya S , Satoshi N , et al. Proposed Pharmacokinetic-Pharmacodynamic Breakpoint of Garenoxacin and Other Quinolones[J]. Japanese Journal of Infectious Diseases, 2017, 70(6):616-620. |