Cilofungin is a semi-synthetic anti-Candida agent that is derived from a three-step process: a) fermentation, isolation and purification of echinocandin B (ECB) (I) using an Aspergillus nidulans strain as the producing culture; b) deacylation of ECB by fermentation using an Actinoplanes utahensis culture to give the ECB nucleus (II); and c) N-acylation of the amino terminus of (II) using an activated ester of 4-octyloxybenzoic acid to give cilofungin.