The clinical significance of cyclosporine (CsA) concentration 2 h postdose (C(2)) monitoring is widely recognized in organ transplantation, because C(2) value is considered to be a predictable surrogate marker of full area under the concentration-time curve (AUC), and/or a peak concentration value exhibits potent inhibition of calcineurin activity. However, the pharmacological advantage of absorption profile (AP) has not been fully elucidated. In a rat skin allotransplantation model, the authors evaluated the efficacy of AP by different dosage regimens (20, 25 or 30 mg/kg/d, once or twice daily) and routes (p.o. or i.v.), and examined whether high C(2) or AUC(0-4) is intrinsically valuable for effective immunosuppression. Graft survival was CsA dose-dependent and correlated with full AUC(0-24), rather than AP. The difference between the once and twice daily administrations did not influence full AUC(0-24) or immunosuppressive effect. Continuous intravenous infusion with flat pharmacokinetics also produced adequate immunosuppression as was observed in enteral administration at the same level of total exposure. The impact of high peak concentration in AP on immunosuppressive effect could not be found. It was suggested that AP would not have intrinsic pharmacodynamic value. However, absorption profiling was considered to be clinically useful in that C(2) value is a good surrogate marker of total exposure (AUC(0-24)).