Abstract
Mobocertinib is an oral tyrosine kinase inhibitor designed to selectively target epidermal growth factor receptor (EGFR) exon 20 insertion (EGFR ex20ins) mutations in non-small cell lung cancer (NSCLC). In vitro studies indicated the potential for time-dependent inhibition and/or induction of cytochrome P450 (CYP) 3A after mobocertinib administration. Thus, a phase 1 drug-drug interaction study (NCT04051827) was conducted to assess the effect of repeat-dose administration of mobocertinib on the pharmacokinetics (PK) of midazolam, a sensitive CYP3A substrate.
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