What this study adds
In humans, carotegrast methyl was a moderate CYP3A4 inhibitor, and after 14 days treatment with carotegrast methyl, the combination with CYP3A4 substrates including midazolam and atorvastatin increased their exposure.
The inhibitory effect of carotegrast methyl on CYP3A4 had almost disappeared by 14 days after the end of administration.