Cempra Pharmaceuticals Inc., Chapel Hill, North Carolina 27517, USA.
Clin Infect Dis. 2011 Jun;52 Suppl 7:S504-12. doi: 10.1093/cid/cir174.
A phase 1 trial of fusidic acid (CEM-102), an oral fusidane class antibiotic under development for treatment of gram-positive acute bacterial skin and skin structure infections, evaluating pharmacokinetics and safety is described. A randomized, double-blinded, placebo-controlled, dose escalation study was conducted in healthy adult subjects in the fasting state. Plasma exposure after multiple doses was higher than for single doses, indicating accumulation. Loading doses designed to optimize pharmacodynamic effects were well tolerated and achieved near-steady state concentrations of CEM-102 at 24 h. CEM-102 was safe and generally well tolerated at all single, multiple, and loading doses administered.
一项正在开发中的口服 Fusidane 类抗生素 fusidic acid（CEM-102）的 1 期临床试验，用于治疗革兰氏阳性急性细菌性皮肤和皮肤结构感染，评估其药代动力学和安全性。在空腹状态下，对健康成年受试者进行了一项随机、双盲、安慰剂对照、剂量递增研究。多次给药后的血浆暴露量高于单次剂量，表明有蓄积。旨在优化药效学效果的负荷剂量耐受良好，并在 24 小时时达到 CEM-102 的近似稳态浓度。CEM-102 在所有单次、多次和负荷剂量的给药下均安全且通常具有良好的耐受性。
