Phase I study assessing the mass balance, pharmacokinetics, and excretion of [¹⁴C]-pevonedistat, a NEDD8-activating enzyme inhibitor in patients with advanced solid tumors.

ABSTRACT: Pevonedistat (TAK-924/MLN4924) is an investigational small-molecule inhibitor of the NEDD8-activating enzyme that has demonstrated preclinical and clinical activity across solid tumors and hematological malignancies. Here we report the results of a phase I trial characterizing the mass balance, pharmacokinetics, and clearance pathways of [¹⁴C]-pevonedistat in patients with advanced solid tumors (NCT03057366). In part A (n = 8), patients received a single 1-h intravenous infusion of [¹⁴C]-pevonedistat 25 mg/m². In part B (n = 7), patients received pevonedistat 25 or 20 mg/m² on days 1, 3, and 5 in combination with, respectively, docetaxel 75 mg/m² or carboplatin AUC5 plus paclitaxel 175 mg/m² on day 1 every 3 weeks. Following

SUBMITTER: Zhou X 

PROVIDER: S-EPMC7960626 | biostudies-literature | 2021 Apr

REPOSITORIES: biostudies-literature