The Board of Trustees of the University of Illinois
发明人:
BURKE, Martin, D.,UNO, Brice, E.
申请号：
EP15793421
公开号：
EP3142672A4
申请日:
2015.05.15
申请国别(地区):
EP
年份:
2017
代理人:
摘要：
Disclosed is a derivative of amphotericin B (AmB), denoted C2′epiAmB, with an improved therapeutic index over amphotericin B, pharmaceutical compositions comprising the AmB derivative, methods of making the AmB derivative and the pharmaceutical composition, and their use in methods of inhibiting growth of a yeast or fungus and treating a yeast or fungal infection. C2′epiAmB is an epimer of the parent compound. Specifically, C2′epiAmB differs from the parent compound at the CT stereogenic center on mycosamine. This difference in structure results in (i) retained capacity to bind ergosterol and inhibit growth of yeast, (ii) greatly reduced capacity to bind cholesterol, and (iii) essentially no toxicity to human cells.
