Table 1.
Effect of lomeguatrib on tumour MGMT*
| Primary CNS Tumour |
Colorectal Cancer |
Prostate Cancer |
|||||
|---|---|---|---|---|---|---|---|
| Number | 9 | 14 | 8 | ||||
|
Median time (h) between dosing
and tumour removal (range) |
12 (8.0 – 14.5) | 14.5 (11.75 – 17.67) | 13.83 (12.67 – 16.25) | ||||
|
Mean total MGMT (fmol/mg
protein) ± SD |
89.9 ± 44.5 | 244 ± 181 | 554 ± 404 | ||||
|
Range of total MGMT (fmol/mg
protein) |
38 - 165 | 47 - 547 | 47 - 1136 | ||||
|
Patients with total MGMT inactivation |
Mean % MGMT inactivation (range) |
Patients with total MGMT inactivation |
Mean % MGMT inactivation (range) |
Patients with total MGMT inactivation |
Mean % MGMT inactivation (range) |
||
|
Lomeguatrib
dose (mg) |
20 | 0/3 | 43 (25-70) | 0/3 | 82 (77-89) | 0/1 | 94 |
| 40 | 0/1 | 46 | 1/2 | 61 (22-100) | 1/1 | 100 | |
| 80 | 0/1 | 57 | 2/3 | 98 (93-100) | 2/3 | 98 (95-100) | |
| 120 | 0/2 | 73 (62-85) | 5/6 | 100 | 2/3 | 100 (99-100) | |
| 160 | 2/2 | 100 | |||||
MGMT – O6-methylguanine-DNA methyltransferase; SD – standard deviation; CNS – central nervous system
*
two patients with breast cancer were administered 20mg lomeguatrib, one provided an informative tumour biopsy specimen in which all the MGMT was inactivated.