Synthetic cannabinoid designer drugs have emerged as drugs of abuse during the last decade, and acute intoxication cases are documented in the scientific literature. Synthetic cannabinoids are extensively metabolized, but our knowledge of the involved enzymes is limited. Here, we investigated the metaboli...
XREM is a regulatory region of the CYP3A4 gene, and binding causes a cooperative interaction with proximal promoter regions of the gene, resulting in increased transcription and expression of CYP3A4. CYP3A4 ligandsSelected inducers, inhibitors and substrates of CYP3A4[3] Substrates Inhibitors ...
in the amount of CYP3A4 will likely lead to an increase in CYP3A4 activity and Drug 1 metabolism. This will cause a reduction in drug exposure and thus a reduction in efficacy, as shown inFigure 3below.Table 1, below, also shows a partial list of CYP3A4 inhibitors and inducers. ...
DDI partners were selected if listed by the FDA as clinical (index) substrates/inhibitors/inducers of CYP enzymes relevant for clopidogrel and recommended for use in clinical DDI studies [28]. The different types of interaction implemented, i.e., induction, competitive inhibition, and mechanism-...