Figure 1. Pharmacokinetics of oral rigosertib.
A. Three patients were treated with single escalating weekly doses of oral rigosertib to determine pharmacokinetics. Data are shown for one patient as the profiles were similar for all 3 patients. Following a single oral dose (fasting) the rigosertib pharmacokinetics were linear and dose-proportional over the dose range of 70–700 mg. B. Bioavailability of oral rigosertib (560 mg), under fasting and fed conditions, was compared to that of intravenously administered rigosertib (800 mg/m2/24 h) in 12 patients in the expansion cohort.