Amphotericin B derivative with reduced toxicity
US9738677B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | May 15, 2015 |
| Grant date | Aug 22, 2017 |
| Priority date | — |
| Expiry date | May 15, 2035 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P31/10
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
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 C2′ 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.