生物活性 | |||
---|---|---|---|
描述 | Pleconaril is a capsid inhibitor used previously to treat enterovirus infections[3]. Pleconaril binds to a hydrophobic pocket in the viral capsid inducing conformational changes, which lead to altered receptor binding and viral uncoating. Pleconaril is orally bioavailable and achieves serum concentrations in excess of those required to inhibit 90% of clinical rhino- and enteroviral isolates in vitro. It possesses the additional advantage of achieving several fold higher concentrations within the central nervous system and nasal secretions than in serum, a characteristic that is highly desirable for an antiviral targeted towards viruses known to cause central nervous system and upper respiratory tract infections. And pleconaril has demonstrated efficacy in the treatment of severe life-threatening enteroviral infections of the newborn and in immunosuppressed individuals[4]. Moreover, pleconaril dramatically reduced virus levels in target tissues of coxsackievirus serotype B3 strain M-infected animals[5]. |
临床研究 | |||||
---|---|---|---|---|---|
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00031512 | Enteroviral Sepsis | Phase 2 | Completed | - | - |
NCT00394914 | Asthma Common... 展开 >> Cold Picornavirus Infection Rhinovirus 收起 << | Phase 2 | Completed | - | - |
NCT00394914 | - | Completed | - | - |
实验方案 | |||
---|---|---|---|
1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.62mL 0.52mL 0.26mL |
13.11mL 2.62mL 1.31mL |
26.22mL 5.24mL 2.62mL |
参考文献 |
---|