| abstract |
Provided are an amphotericin B (AmB) derivative 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. The amphotericin B derivative, denoted C2'deOAmB, differs from the parent compound in that it lacks the hydroxyl group at the 2' position 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. |