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Bupropion, widely used as an antidepressant and smoking cessation aid, undergoes complex metabolism to yield numerous metabolites with unique disposition, effect, drug–drug interactions (DDIs) in humans. The stereoselective plasma urinary pharmacokinetics of bupropion its were evaluated understand their potential contributions effects. Healthy human volunteers (n = 15) administered a single oral dose racemic (100 mg), which was followed by collection urine samples determination metabolite concentrations using novel liquid chromatography–tandem mass spectrometry assays. Time-dependent, elimination rate–limited, observed for all metabolites. Area under the concentration-time curve from zero infinity ratios on average approximately 65, 6, 4 Cmax 35, 3, 0.5 (2R,3R)-/(2S,3S)-hydroxybupropion, R-/S-bupropion, (1S,2R)-/(1R,2S)-erythrohydrobupropion, (1R,2R)-/(1S,2S)-threohydrobupropion, respectively. R-/S-bupropion (1R,2R)-/(1S,2S)-threohydrobupropion are likely indicative higher presystemic S- versus R-bupropion carbonyl reductases. Interestingly, apparent renal clearance (2S,3S)-hydroxybupropion almost 10-fold than that (2R,3R)-hydroxybupropion. prediction steady-state demonstrated differential stereospecific accumulation [partial area after final simulated (300–312 hours) 185 37,447 nM⋅h] [terminal half-life 7–46 hours] metabolites, may explain differences effect DDI risk CYP2D6 at steady state. Further elucidation disposition suggests is not reliable vivo marker CYP2B6 activity. In summary, our knowledge, this first comprehensive report provide insight into mechanisms underlying detailing individual will enhance clinical understanding bupropion’s effects DDIs CYP2D6.