A Pharmacokinetic Model for the Concentration of 10B in Blood after Boronophenylalanine-Fructose Administration in Humans

Abstract Kiger, W. S., III, Palmer, M. R., Riley, K. J., Zamenhof, R. G. and Busse, P. M. A Pharmacokinetic Model for the Concentration of 10B in Blood after Boronophenylalanine- Fructose Administration in Humans. An open two-compartment model has been developed for predicting 10B concentrations in blood after intravenous infusion of the l-p-boronophenylalanine-fructose complex (BPA-F) in humans and derived from studies of pharmacokinetics in 24 patients in the Harvard-MIT Phase I clinical trials of BNCT. The 10B concentration profile in blood exhibits a characteristic rise during the infusion to a peak of ∼32 μg/g (for infusion of 350 mg/kg over 90 min) followed by a biphasic exponential clearance profile with half-lives of 0.34 ± 0.12 and 9.0 ± 2.7 h, due to redistribution and primarily renal elimination, respectively. The model rate constants k1, k2 and k3 are 0.0227 ± 0.0064, 0.0099 ± 0.0027 and 0.0052 ± 0.0016 min–1, respectively, and the central compartment volume of distribution, V1, is 0.235 ± 0.0...