PHARMACOKINETIC STUDY OF CONVERSION BETWEEN TWO FORMULATIONS OF ONCE-DAILY EXTENDED-RELEASE TACROLIMUS IN STABLE LUNG TRANSPLANT PATIENTS

BACKGROUND: The aim of this study was to compare the pharmacokinetic profile, tolerability, and safety of a novel once-daily extended-release formulation of tacrolimus (LCPT) with that of once-daily prolonged-release tacrolimus (ODT) in stable adult lung transplant (LT) recipients. METHODS: Phase II, open-label, single-arm, single-center, prospective pilot pharmacokinetic study. Study population comprised 20 stable LTR receiving ODT, mean age 55.9 (r: 38-67) years, 13 (65%) men. Patients were switched to LCPT in a 1:0.7 (mg/mg) conversion dose. Follow-up was 6 months, and cystic fibrosis patients were excluded. Two 24-hour pharmacokinetic profiles were obtained for each patient, the first on day -14 and the second on day +14 after switching to LCPT. Pharmacokinetic parameters and safety were compared. RESULTS: Mean (SD) AUC0-24 was 253.97 (61.90) ng/mL/h for ODT and 282.44 (68.2) ng/mL/h for LCPT. Systemic exposure was similar in both (Schuirmann two 1-sided test). Mean (SD) dose was 5.05 (1.67) mg in ODT and 3.36 (1.03) mg in LCPT (p: 0.0002). Time to maximum concentration was 125 minutes for ODT and 325 minutes for LCPT (p

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