Aim: To study phase Ⅱ metabolites of etofesalamide in filamentous fungi.Methods:Seven fungi were screened to transform etofesalamide.The metabolites of etofesalamide were assayed using liquid chromatography coupled to mass spectrometry.The major metabolite was subject to enzymatic hydrolysis to confirm its structure.Results: Etofesalamide was converted into two phase Ⅱ metabolites: glucoside and riboside conjugates.Glucoside conjugate was the major product with a yield greater than 90%; no phase Ⅰ metabolites were detected.Conclusion: Glucoside and riboside conjugations of etofesalamide in filamentous fungi differ from the phase Ⅱ metabolism of glucuronidation in mammals.