Igorevich
Member
- Joined
- Mar 23, 2021
- Messages
- 24
Drug–nutrient interactions: discovering prescription drug inhibitors of the thiamine transporter ThTR-2 (SLC19A3)
Transporter-mediated drug–nutrient interactions have the potential to cause serious adverse events. However, unlike drug–drug interactions, these drug–nutrient interactions receive little attention during drug development. The ...
www.ncbi.nlm.nih.gov
Our high-throughput screen of 1360 compounds, including many clinically used drugs, identified 146 potential inhibitors at 200 μM. Inhibition kinetics were determined for 28 drugs with half-maximal inhibitory concentration (IC50) values ranging from 1.03 μM to >1 mM. Several oral drugs, including metformin, were predicted to have intestinal concentrations that may result in ThTR-2–mediated drug–nutrient interactions. Complementary analysis using electronic health records suggested that thiamine laboratory values are reduced in individuals receiving prescription drugs found to significantly inhibit ThTR-2, particularly in vulnerable populations (e.g., individuals with alcoholism).