Dose, Kidney Function, and a Drug-Excipient Interaction Impair Mycophenolate Mofetil Prodrug Activation in Kidney Transplant Recipients.

ABSTRACT:

Background and objective

Current immunosuppressive treatment to prevent graft rejection in organ transplant recipients commonly includes mycophenolate mofetil (MMF) and a calcineurin inhibitor. After absorption, MMF is activated to mycophenolate (MPA) by the carboxylesterase (CES) enzymes, which is considered to occur rapidly and completely. Recent research utilizing pharmacometabolomics (PMx), however, identified an unknown/unreported MMF glucuronide metabolite in several kidney transplant recipients (KTR). This finding indicates incomplete MMF prodrug activation by CES, thereby suggesting enzyme saturation and/or inhibition, which warrants further study. In this work, we aimed to identify clinical factors that could (partially) explain incomplete MMF activation as observed in KTR

SUBMITTER: Nijdam FB 

PROVIDER: S-EPMC12227376 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature