In vitro and in silico identification and characterisation of thiabendazole as a mechanism-based inhibitor of CYP1A2 and simulation of possible pharmacokinetic drug-drug interactions.

Thiabendazole (TBZ) and its major metabolite 5-hydroxythiabendazole (5OH-TBZ) were screened for potential time-dependent inhibition (TDI) against CYP1A2. Screen assays were carried out in the absence and presence of NADPH. TDI was observed with both compounds, with Kinact and KI values of 0.08 and 0.02 min-1 and 1.4 and 63.3 µM for TBZ and 5OH-TBZ, respectively. Enzyme inactivation […]

Read More
Learn More