Assessment of the Intestinal CYP3A Contribution to Drug Interactions with Extended‐Release Tacrolimus (LCPT) Using Grapefruit Juice

Дата публикации: 27-08-2026 00:00:00

Grapefruit juice (GFJ) is a known inhibitor of intestinal cytochrome P450 3A (CYP3A) metabolism leading to increased exposure to CYP3A substrates such as tacrolimus. The extended-release tacrolimus formulation Envarsus (LCPT) exhibits prolonged absorption throughout the entire GI tract. Although a clinically significant drug-drug interaction occurs with immediate-release tacrolimus formulations, this has not been evaluated with extended-release formulations. This study assessed the impact of GFJ on LCPT in adult kidney transplant patients. Eleven adult kidney transplant recipients on a stable dose of LCPT were enrolled in a randomized crossover study. Participants were administered either GFJ or water during each pharmacokinetic visit, with midazolam used as a positive control. A washout period of 2-4 weeks was included between visits. Tacrolimus concentrations were determined using validated LC-MS/MS methods. Tacrolimus AUC0-24 was 28% higher with GFJ (GMR = 1.28,...

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