Low Bioavailability of Oral Tacrolimus Suspension in Pediatric Kidney Transplant Patients

Excerpt

The calcineurin inhibitor tacrolimus is considered a cornerstone of immunosuppressive treatment to prevent rejection in both adult and pediatric kidney transplant recipients. In The Netherlands, immediate-release tacrolimus is commercially available in 0.5, 1, and 5 mg capsules, as well as 0.2 mg granules. In pediatric patients, liquid formulations are essential for the administration of drugs. As granules for oral suspension are considered inappropriate due to the large number of sachets required and due to liquid formulations not being commercially available, hospitals often rely on an extemporaneously prepared formulation. A lower, and age-dependent, bioavailability for oral liquid formulations in children, compared with the original formulation in adults, is a well-known issue for various drugs [1]. Labberton et al. have shown the stability of the extemporaneous preparation using tacrolimus monohydrate [2]; however, the relative bioavailability of this tacrolimus oral suspension is unknown for pediatric kidney transplant patients. …