Advances in Thiopurine Drug Delivery: The Current State-of-the-Art

Ahmed B. Bayoumy*, Femke Crouwel, Nripen Chanda, Timothy H. J. Florin, Hans J. C. Buiter, Chris J. J. Mulder, Nanne K. H. de Boer

*Corresponding author for this work

Research output: Contribution to journalReview articleAcademicpeer-review


Thiopurines (mercaptopurine, azathioprine and thioguanine) are well-established maintenance treatments for a wide range of diseases such as leukemia, inflammatory bowel disease (IBD), systemic lupus erythematosus (SLE) and other inflammatory and autoimmune diseases in general. Worldwide, millions of patients are treated with thiopurines. The use of thiopurines has been limited because of off-target effects such as myelotoxicity and hepatotoxicity. Therefore, seeking methods to enhance target-based thiopurine-based treatment is relevant, combined with pharmacogenetic testing. Controlled-release formulations for thiopurines have been clinically tested and have shown promising outcomes in inflammatory bowel disease. Latest developments in nano-formulations for thiopurines have shown encouraging pre-clinical results, but further research and development are needed. This review provides an overview of novel drug delivery strategies for thiopurines, reviewing modified release formulations and with a focus on nano-based formulations.
Original languageEnglish
Pages (from-to)743-758
Number of pages16
JournalEuropean Journal of Drug Metabolism and Pharmacokinetics
Issue number6
Early online date2021
Publication statusPublished - Nov 2021

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