Table 1

Toxicity of carmustine (BCNU) and TMZ: Effect of BG and dBG on potentiating the toxicity of BCNU and TMZ in athymic mice

Alkylating drugaDoseb mg/m2AGT inhibitoraDoseb mg/m2Weight loss % of controlDeathsc
BCNU65none05 ± 2d0 /10e
BCNU70none10 ± 30 /10
BCNU75none15 ± 33 /10
BCNU85none24 ± 46 /10
BCNU35BG20022 ± 65 /10
BCNU35BG18023 ± 34 /10
BCNU30BG20014 ± 41 /10
BCNU30BG18010 ± 20 /10
BCNU35dBG30021 ± 47 /10
BCNU35dBG25012 ± 30 /10
BCNU35dBG20010 ± 20 /10
TMZ600none21 ± 45 /10
TMZ400none16 ± 41 /10
TMZ200none05 ± 20 /10
TMZ400dBG25015 ± 34 /10
TMZ200dBG25012 ± 31 /10
TMZ180dBG25003 ± 10 /10
TMZ180BG18003 ± 20 /10
TMZ200BG18006 ± 32 /10
  • a BCNU stock 10 mg/ml in 100% ethanol was diluted to appropriate concentrations with 5% ethanol. TMZ was dissolved in DMSO.

  • b dBG and BG were dissolved in 40% PEG in PBS. BCNU and TMZ were injected i.p. (injection volume, 0.15–0.2 ml/animal) 2 h after treatment with i.p. dBG, BG, or vehicle (injection volume, 0.2–0.3 ml/animal).

  • c Number of deaths per number of animals treated.

  • d Mean ± SD.

  • e Animals were monitored for 20 days from initiation of treatment.