Meltdose Tacrolimus Pharmacokinetics.
BACKGROUND
Nonadherence to immunosuppressive therapy contributes to the loss of grafts. One of the problem is the fractioning of immunosuppressive dose. In fact, it was demonstrated that a single daily dose (QD) is associated with an increased adherence to therapy compared with twice daily dosing (BID). Tacrolimus (TAC), calcineurin inhibitor, is one of immunosuppression pillar in organ transplantation and its action is strongly correlated with blood concentration and therefore the therapeutic drug monitoring is recommended in the guidelines. However, one of the critical points of TAC is the poor and variable bioavailability that influences immunosuppression, and is also responsible for adverse effects.


METHODS
MeltDose® Technology is a new technology to improve efficacy and/or reduce side effects. This new technology applied to TAC (Envarsus® or LCP-TAC) has achieved 4 main objectives: (1) improved bioavailability, (2) reduced dose fractioning to one tablet per day, (3) limited variability concentrations of TAC, and (4) lower doses of TAC will be administered.


RESULTS
We analyzed the pharmacokinetic profile, efficacy, and security of Envarsus®.
Department of Experimental and Clinical Medicine, Medical School, University of Udine; SOC Institute of Clinical Pharmacology, University-Hospital S. Maria della Misercordia, Udine, Italy. Electronic address: massimo.baraldo@uniud.it.
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Baraldo
D001682:Biological Availability; D003692:Delayed-Action Preparations; D004334:Drug Administration Schedule; D016903:Drug Monitoring; D006084:Graft Rejection / Q000517:prevention & control*; D006801:Humans; D007166:Immunosuppressive Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D016030:Kidney Transplantation; D016031:Liver Transplantation; D016559:Tacrolimus / Q000008:administration & dosage / Q000493:pharmacokinetics*; D013997:Time Factors
D003692:Delayed-Action Preparations; D007166:Immunosuppressive Agents; D016559:Tacrolimus