Table 1

Enhancement of efficacy of BCNU in human pancreatic xenografts in athymic mice with the MGMT inhibitors BG and dBG

Mice no.Treatment (dose)aWeight lossRegressionb %cT to 5× (days)dT-C (days)e
PANC-1 (MGMT = 680 fmol/mg protein)
7None0.011 (8–14)
12BCNU (75)3.71/1214 (11–24)3
9BCNU (35)f BG (160)15.13/923 (20–32)12
10BCNU (35) dBG (235)5.33/1022 (14–38)11
11BCNU (35) dBG (260)13.36/1127 (19–48)16
MIA PaCa-2 (MGMT = 890 fmol/mg protein)
10None0.014 (11–25)
10BCNU (75)3.71/1017 (11–24)3
10BCNU (35) BG (160)15.15/1032 (26–45)18
10BCNU (35) dBG (235)5.34/1028 (22–23)14
10BCNU (35) dBG (260)13.37/1041 (31–49)30
BxPC-3 (MGMT = 330 fmol/mg protein)
10None0.09 (7–12)
10BCNU (75)3.40/1016 (9–22)6
10BCNU (35) BG (160)16.43/1025 (19–31)16
10BCNU (35) dBG (235)6.72/1024 (17–24)15
10BCNU (35) dBG (260)16.34/1031 (19–66)22
CAPAN-2 (MGMT = 620 fmol/mg protein)
10None0.017 (17–21)
10BCNU (75)7.60/1018 (15–19)1
10BCNU (35) BG (160)18.23/1031 (23–41)14
10BCNU (35) dBG (260)16.43/1038 (33–40)21
CFPAC-1 (MGMT = 1680 fmol/mg protein)
10None0.024 (18–26)
10BCNU (75)4.60/1020 (17–25)−4
14BCNU (35) BG (160)16.94/1440 (27–55)16
10BCNU (35) dBG (235)4.72/1030 (22–35)6
10BCNU (35) dBG (260)16.46/1043 (38–60)19
  • a mg/m2.

  • b Reduction of tumor volume by ≥10%.

  • c Average weight loss after treatment.

  • d Time for tumor to quintuple from its treatment size of 180–200 mm3.

  • e Tumor delay.

  • f BCNU was administered 2 h after BG and 4 h after dBG.