Pharmacokinetic (PK) data from 28 subjects who received 5‐200‐mg single ascending doses of ANAVEX3‐71, formerly AF710B, were analyzed to characterize the PK of ANAVEX3‐71 and its M8 metabolite. PK data from 12 subjects who received 160 mg ANAVEX3‐71 under fed and fasted conditions were analyzed to characterize the effect of food on the PK of the drug and its M8 metabolite. PK was characterized using the standard 2‐stage approach and the nonlinear mixed‐effects modeling approach. Dose proportionality was determined using the power model. Two‐ and 3‐compartment linear PK models were tested for the characterization of the PK of ANAVEX3‐71 and its M8 metabolite. The PK of ANAVEX3‐71 is linear, dose proportional, and time invariant. The drug is rapidly eliminated with a mean (standard deviation) apparent terminal elimination half‐life of 3.56 (4.09) hours, while the M8 metabolite was eliminated with a mean (standard deviation) apparent terminal elimination half‐life of 6.59 (1.64) hours. The population PK model was used to investigate the effects of covariates on the PK of ANAVEX3‐71 and M8. Age, weight, and creatinine clearance were not explanatory of the variability in apparent clearance and apparent volume of the central compartment of ANAVEX3‐71. Food had no effect on the PK of ANAVEX3‐71 and its M8 metabolite. [ABSTRACT FROM AUTHOR]