Disclosed are methods and compositions which may be used in human cytochrome P450 (CYP450) enzyme phenotyping. The methods and compositions typically utilize substrate for CYP3A5 comprising eplerenone which may be administered orally to a subject. Subsequently, metabolites of eplereone may be detected in the subject's saliva as well as any non- metabolized eplerenone to calculate a metabolic ratio for CYP3A5 enzyme in order to generate a phenytopic CYP3A5 enzyme profile for the subject.