B.
Summary of in vivo data for SG2285 and appropriate standard agents in human tumor xenograft models LS174T (colon), A549 (non small cell lung), PC3 (prostate) and Bx-PC-3 (pancreatic).
| Model | Drug | Dose (batch) (mg/kg) |
Schedule1 | Duration (days) |
%TGI2 | PR3 |
|---|---|---|---|---|---|---|
| LS174T (colon) |
SG2285 Irinotecan 5-FU |
0.85 (3) 1.0 (3) 100 100 |
q4d × 3 q4d × 3 qwk × 3 (ip) qwk × 3 (ip) |
26 26 26 26 |
83 82 46 65 |
0 0 0 0 |
| A549 (NSCLC) |
SG2285 Docetaxel |
1.0 (5) 30 |
q4d × 4 q4d × 3 |
29 29 |
63 89 |
0 0 |
| PC3 (prostate) |
SG2285 Paclitaxel Cisplatin |
0.75 (5) 1.0 (5) 30 10 |
q4d × 4 q4d × 3 qod × 5 qwk × 3 (ip) |
30 30 30 30 |
96 96 99 72 |
5/10 4/10 8/10 0 |
| Bx-PC-3 (pancreatic) |
SG2285 Paclitaxel |
1.0 (3) 1.0 (3) 1.0 (5) 1.0 (5) 30 |
q4d × 4 q4d × 3 q4d × 4 q4d × 3 qod × 5 |
30 30 30 30 30 |
86 69 81 84 47 |
2/9 1/9 1/8 2/8 0 |
1
Drug given i.v. unless indicated otherwise
2
%TGI = [1-(T/C)] × 100 = % tumor growth inhibition compared to vehicle controls. TGI≥ 60% indicates therapeutic activity.
3
PR = partial regression (tumor volume 50% or less than its day 1 volume for three consecutive measurements)