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Liposomal Amphotericin B
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- Fukasawa Masatomo
- Sumitomo Pharmaceuticals Co., Ltd., Product Development Division presently, Dainippon Sumitomo Pharma Co., Ltd., Drug Development Division
Bibliographic Information
- Other Title
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- リポソーマル アムホテリシンＢ
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Description
Liposomal amphotericin B (AmBisome™) is a DDS (drug delivery system) formulation of amphotericin B (AMPH-B), and has been developed in an attempt to reduce the toxicity of AMPH-B while retaining its therapeutic efficacy. AMPH-B has been the “gold standard” of antifungal therapy over the past four decades. It has a broad spectrum of fungicidal activity against a number of clinically important pathogens including Aspergillus and Candida. The mechanism of action of AMPH-B involves binding to ergosterol, the principal sterol in fungal cell membranes. Binding to ergosterol causes an increase in fungal membrane permeability, electrolyte leakage, and cell death. AMPH-B has affinity for cholesterol in mammalian membranes, which leads to severe side-effects including kidney damage.<br>AmBisome is a unilamellar vesicle composed of AMPH-B and phospholipid. Upon administration, AmBisome remains intact in the blood and distributes to the tissues where fungal infection may occur, and is disrupted after attachment to the outside of fungal cells, resulting in fungal cell death.<br>AmBisome and AMPH-B show similar in vitro and in vivo antifungal activity and clinical efficacy. However, AmBisome has less infusion-related toxicity and nephrotoxicity than AMPH-B.
Journal
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- Nippon Ishinkin Gakkai Zasshi
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Nippon Ishinkin Gakkai Zasshi 46 (4), 229-231, 2005
The Japanese Society for Medical Mycology