Abstract
Tacrolimus, a relatively new therapeutic option for patients with corticosteroid-refractory Crohn's disease or ulcerative colitis, is a substrate for the apically directed efflux transporter P-glycoprotein (P-gp). Duodenal biopsy specimens obtained from a patient with corticosteroid-refractory Crohn's disease and with significantly higher-than-average tacrolimus dose requirements were analyzed for P-gp by Western blot. The P-gp content in this patient was more than double that in specimens obtained from 9 of 10 healthy subjects. Elevated intestinal P-gp could have resulted in decreased tacrolimus absorption, thereby leading to decreased blood concentration and decreased efficacy in this patient. The cause and prevalence of this phenomenon are unknown.
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Buchman, A.L., Paine, M.F., Wallin, A. et al. A Higher Dose Requirement of Tacrolimus in Active Crohn's Disease May Be Related to a High Intestinal P-Glycoprotein Content. Dig Dis Sci 50, 2312–2315 (2005). https://doi.org/10.1007/s10620-005-3053-3
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DOI: https://doi.org/10.1007/s10620-005-3053-3