What is it about?
Hyperbilirubinemia has been observed in patients treated with tyrosine kinase inhibitor (TKI) drugs. Therefore, it would be beneficial to understand whether there is a relationship between inhibition of uridine-5′-diphosphate glucuronosyltransferase (UGT) 1A1 activity and observed bilirubin elevations in TKI drug-treated patients. UGT1A1 is responsible for the glucuronidation of bilirubin which leads to its elimination in the bile.
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Why is it important?
The results suggest that in vitro UGT1A1 inhibition assays have the potential to predict clinical hyperbilirubinemia.
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This page is a summary of: In vitro UGT1A1 inhibition by tyrosine kinase inhibitors and association with drug-induced hyperbilirubinemia, Cancer Chemotherapy and Pharmacology, August 2018, Springer Science + Business Media,
DOI: 10.1007/s00280-018-3665-x.
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