Pharmacokinetics and boron uptake of BSH (Na2B12H11SH) in patients with intracranial tumors.

We evaluated retrospectively the pharmacokinetics and boron uptake of BSH (mercaptoundecahydrododecarborate) for Boron Neutron Capture Therapy (BNCT) in 123 patients undergoing craniotomy for intracranial tumors. The pharmacokinetics revealed that BSH could move easily from blood to the peripheral organs; it was retained there and elimination was very slow. BSH after intra-arterial infusion (i.a.) was found to move into the peripheral organs more easily than after intra-venous (i.v.) infusion. In patients with malignant glioma, the average values of boron concentration in tumor and the tumor to blood ratio (T/B ratio) after i.a. infusion were 26.8 +/- 19.5 micrograms/g (range, 6.1-104.7 micrograms/g) and 1.77 +/- 1.30 (range, 0.47-6.65) respectively. On the other hand, after i.v. infusion the values were 20.9 +/- 12.2 micrograms/g (range, 7.0-39.7 micrograms/g) and 1.30 +/- 0.65 (range, 0.61-2.94) respectively. The differences are not statistically significant. Boron uptake in malignant glioma was about three times higher than low grade glioma. We found a good correlation between boron uptake and time interval from BSH infusion, and 15-20 hours after BSH infusion the boron concentration in tumor was above 20 micrograms/g 10B in 69% of the malignant glioma patients; T/B ratio was above one in 75%, and above two in 44% of them. We recommend intra-venous infusion of BSH clinically since it is safer, and results in sufficient boron concentration in tumor, and the planned irradiation might be optimal around 15-20 hours after the BSH infusion for treating malignant glioma.