Cilofungin – Knowledge and References

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History of antifungals

Published in Mahmoud A. Ghannoum, John R. Perfect, Antifungal Therapy, 2019

Emily L. Larkin, Ali Abdul Lattif Ali, Kim Swindell

Anidulafungin is a derivative of a naturally occurring candin, echinocandin B, produced by Aspergillus nidulans or A. rugulosis [83]. Cilofungin was the first semisynthetic derivative of echinocandin B to be evaluated in clinical trials; however, the trials were discontinued due to associated nephrotoxicity. Further structure modification of cilofungin led to the synthesis of anidulafungin [83].

Echinocandins – structure, mechanism of action and use in antifungal therapy

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Journal Information

Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022

Mateusz Szymański, Sandra Chmielewska, Urszula Czyżewska, Marta Malinowska, Adam Tylicki

In 1974, in Switzerland the first antifungal drug of the echinocandin class – echinocandin B was discovered, which showed good antifungal properties but at the same time strong haemolytic effects. To counteract this, cilofungin, a semi-synthetic analogue of echinocandin B with a 4-octyloxybenzoate side chain, was synthesised. This compound significantly reduced haemolytic activity while retaining antifungal properties11. However, cilofungin was withdrawn from Phase II clinical trials due to the poor water solubility and toxicity of its co-solvent12. An important step in echinocandin research was the discovery of pneumocandin A0 and pneumocandin B0, of which pneumocandin B0 was used to synthesise a new antifungal agent13 (Table 2).