In vitro and in vivo comparisons of amphotericin B and N-D-ornithyl amphotericin B methyl ester.
N-D-Ornithyl amphotericin B methyl ester (N-D-ornithyl AmE) has a lower toxicity for animals than does amphotericin B (AmB), and peak serum levels can be achieved that are fourfold higher than those obtained with an equivalent dose of AmB. However, N-D-ornithyl AmE has one-fourth the in vitro activity and between one-fifth and one-eighth the in vivo activity of AmB. N-D-ornithyl AmE and the corresponding lysyl derivative also lack the immunoadjuvant effects of AmB.
D000276:Adjuvants, Immunologic; D000666:Amphotericin B / Q000031:analogs & derivatives* / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D000818:Animals; D000935:Antifungal Agents / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D005260:Female; D006658:Histoplasma / Q000187:drug effects; D006660:Histoplasmosis / Q000188:drug therapy; D051379:Mice; D008806:Mice, Inbred AKR; D008826:Microbial Sensitivity Tests
D000276:Adjuvants, Immunologic; D000935:Antifungal Agents; C040293:ornithylamphotericin methyl ester; D000666:Amphotericin B