The dissolution profiles of clopidogrel 75 mg tablets in compendial gastric and intestinal media as well as in biorelevant simulated gastric and intestinal media mimicking fasting and fed conditions were determined. In vivo plasma concentration curves, that resulted following the administration of the same formulation of clopidogrel to healthy male and female volunteers in fasting and respectively fed state, were used for compartmental modeling of pharmacokinetic data. Data showed that in vivo exposure to clopidogrel increases significantly, when administration of the tablets is performed in fed state. In vitro – in vivo level A linear correlations were established for the intestinal fasting and fed data, using the Loo-Riegleman based deconvolution approach. The developed models confirm that the low solubility of clopidogrel in the biologically relevant absorption site medium is one of the sources of its increased PK variability. The robustness of the IVIVC recommends it as surrogate for in vivo bioavailability testing, being a cheaper and less time consuming initial screening tool for generic formulations.