Amphotericin B (AmB) remains a drug of first choice for treatment of most severe mycoses despite significant toxicity and solubility problems. Screening of a series of new semisynthetic polyene macrolide derivatives identified AmB N-(2-aminoethyl)amide (amphamide) as having several competitive advantages over the parent polyene. Aprototype parenteral amphamide dosage form in which the active ingredient was highly soluble and stable during storage was developed. Chronic toxicity of the finished amphamide dosage form was studied in rabbits. The amphamide dosage form displayed dose-dependent reversible toxicity.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 53, No. 11, pp. 30 – 33, November, 2019.
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Pereverzeva, E.R., Treshchalin, M.I., Bychkova, E.N. et al. Experimental Evaluation of Chronic Toxicity of Amphamide – a New Semisynthetic Derivative of Amphotericin B. Pharm Chem J 53, 1018–1021 (2020). https://doi.org/10.1007/s11094-020-02116-y
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DOI: https://doi.org/10.1007/s11094-020-02116-y