Creelan BC, et al. - A first-in-human Phase I clinical trial aspired to ascertain the appropriate dose for Phase II studies, characterize pharmacokinetic and pharmacodynamic parameters, and assess antitumor activity. Results revealed the favorable tolerability of omaveloxolone at biologically active doses. However, this trial had a small sample size which limits definitive conclusions. In light of these outcomes, further investigation of omaveloxolone in cancer was proposed.