在静脉内和口服 [C]SCY-078 于白化和色素沉着大鼠的体内物质平衡研究中，新型杀真菌剂 SCY-078 显示向与真菌感染相关的组织分布。
SCY-078, a Novel Fungicidal Agent, Demonstrates Distribution to Tissues Associated with Fungal Infections during Mass Balance Studies with Intravenous and Oral [C]SCY-078 in Albino and Pigmented Rats.
机构信息
SCYNEXIS, Inc., Jersey City, New Jersey, USA.
QPS, Newark, Delaware, USA.
出版信息
Antimicrob Agents Chemother. 2019 Jan 29;63(2). doi: 10.1128/AAC.02119-18. Print 2019 Feb.
Abstract
SCY-078, a fungicidal β-1,3-glucan synthesis inhibitor administered as intravenous or oral [C]SCY-078 to rats, was distributed primarily into tissues associated with invasive fungal disease (kidney, lung, liver, spleen, bone marrow, muscle, vaginal tissue, and skin) to levels exceeding those in plasma. Oral fraction absorbed was ∼40%. Elimination was primarily via bile and feces (∼90%) and urine (∼1.5%). Mean half-time was ∼8 h. Quantitative whole-body autoradiography showed a rapid distribution at 8 h and elimination by 168 h postdose.
摘要
SCY-078 是一种杀真菌的β-1,3-葡聚糖合成抑制剂，以静脉注射或口服[C]SCY-078 的形式给予大鼠，主要分布于与侵袭性真菌感染（肾脏、肺部、肝脏、脾脏、骨髓、肌肉、阴道组织和皮肤）相关的组织中，其水平超过血浆。口服吸收部分约为 40%。消除主要通过胆汁和粪便（约 90%）和尿液（约 1.5%）。平均半衰期约为 8 小时。定量全身放射自显影显示，在给药后 8 小时迅速分布，168 小时后消除。
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