Influence of everolimus on steady-state pharmacokinetics of cyclosporine in maintenance renal transplant patients.

To investigate possible interactions of the novel immunosuppressant everolimus with cyclosporine, a multicenter, randomized, double-blind, placebo-controlled, dose-escalating phase I study was performed. Everolimus regimens (0.75-10 mg/d) were administered for 28 days to stable renal allograft recipients receiving the microemulsion form of cyclosporine.

Tolerability and steady-state pharmacokinetics of everolimus in maintenance renal transplant patients.

Background: Current immunosuppressant regimens need to be improved to prevent acute and chronic graft rejection. The novel macrocyclic immunosuppressant everolimus (Certican, RAD) is currently in clinical development to address this issue.

Methods: The primary objective of this multicentre, randomized, double-blind, placebo-controlled, dose-escalating phase 1 study was to evaluate the safety and tolerability of everolimus at four dose levels (0.

Effect of food on everolimus absorption: quantification in healthy subjects and a confirmatory screening in patients with renal transplants.

Study Objective: To quantify the influence of a high-fat meal on the oral bioavailability of the immunosuppressant everolimus in a single-dose study in healthy subjects and to confirm the results in a small food-effect screening assessment in patients with renal transplants who were receiving multiple-dose everolimus.

Design: Randomized, open-label, crossover, single-dose study and confirmatory screening.

Setting: Phase 1 unit for the single-dose study and two German hospitals for the patient screening.