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The aim of this research was to survey the effects of dabrafenib on human UDP\u2010glucuronosyltransferases (UGTs) and to evaluate the risk of drug\u2013drug interactions (DDIs). The formation rates for 4\u2010methylumbelliferone (4\u2010MU) glucuronide and trifluoperazine\u2010glucuronide in 12 recombinant human UGT isoforms with or without dabrafenib were measured and HPLC was used to investigate the inhibitory effects of dabrafenib on UGTs. Inhibition kinetic studies were also conducted. <jats:italic>In vitro\u2013in vivo<\/jats:italic> extrapolation approaches were further used to predict the risk of DDI potentials of dabrafenib via inhibition of UGTs. Our data indicated that dabrafenib had a broad inhibitory effect on 4\u2010MU glucuronidation by inhibiting the activities of UGTs, especially on UGT1A1, UGT1A7, UGT1A8, and UGT1A9, and dabrafenib could increase the area under the curve of co\u2010administered drugs. 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