Fosmanogepix

国际站：Fosmanogepix

CAS：2091769-17-2

品牌：MedChemExpress (MCE)

存储条件：Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

生物活性： Fosmanogepix (APX001) 是一流的口服广谱抗真菌剂，靶向高度保守的Gwt1真菌酶。 Fosmanogepix (APX001) 是一种 N-膦酰氧甲基前药，可被全身性碱性磷酸酶快速完全代谢为活性部分 APX001A。 Fosmanogepix (APX001) 可用于开发治疗侵袭性真菌感染^[1][2]。 IC50 和目标：Gwt1^[1]

体外：Fosmanogepix (APX001) (2-0.002 μg/ml, 40-72小时) 抑制新生梭菌、加蒂梭菌、白色念珠菌和烟曲霉生长的最低有效浓度为 0.008-0.25 μg/ml[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：Fosmanogepix (APX001) (390 mg/kg, 口服给药，每天三次) 降低小鼠隐球菌性脑膜炎 (CM) 模型的真菌负荷[1]。 Fosmanogepix (APX001) (100 mg/kg, 口服给药) 在 CD-1 小鼠中是疗效的驱动因素[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: murine model of cryptococcal meningitis[1] Dosage: 390 mg/kg Administration: Oral gavage (p.o.) Result: Observed significant differences (P Reduced the fungal burden of 0.78 log10 CFU/g compared with control group in brain tissue. Animal Model: CD-1 mice[1] Dosage: 100 mg/kg Administration: Intraperitoneal injection (i.p.) Result: Extended the half-life of the active moiety, APX001A, from 1.3 to 8.8 h, resulting in a 9-fold increase in the area under the curve (AUC). Clinical Trial

参考文献：[1]. Gebremariam T, et al. APX001 Is Effective in the Treatment of Murine Invasive Pulmonary Aspergillosis. Antimicrob Agents Chemother. 2019 Jan 29;63(2). pii: e01713-18.[2]. Shaw KJ, et al. In Vitro and In Vivo Evaluation of APX001A/APX001 and Other Gwt1 Inhibitors against Cryptococcus. Antimicrob Agents Chemother. 2018 Jul 27;62(8). pii: e00523-18.[3]. Shaw KJ, et al. In Vitro and In Vivo Evaluation of APX001A/APX001 and Other Gwt1 Inhibitors against Cryptococcus. Antimicrob Agents Chemother. 2018 Jul 27;62(8):e00523-18.