Table 2.
Summary of The-0504 and Genz-644282 efficacies in tumor-bearing mice models of several human cell lines using different administration schedules.
| TUMOR MODEL DOSE (mg/kg) |
TGI (%) ORR (%) |
RESPONSE (%) |
||
|---|---|---|---|---|
| Genz-644282 | The-0504 | Genz-644282 | The-0504 | |
|
Pancreatic (PaCa44) 1.9 mg/kg [11] |
64.2 16.7 |
100 100 |
33.3 SD 66.7 PD |
100 CR |
|
Pancreatic (HPAF II) 1.9 mg/kg [5] |
33.3 0 |
93.3 83.3 |
33.3 SD 66.7 PD |
16.7 CR 50.0 PR 16.7 SD |
| Pancreatic (PDX)a [11] | 0 0 |
93.6 83.3 |
100 PD | 50 CR 33.3 PR 16.7 SD |
|
Colorectal (HT29) 1.9 mg/kg [11] |
na 16.6 |
na 100 |
33.3 SD 66.7 PD |
66.7 CR 33.3 PR |
|
Breast (MDA-MB 231) 1.9 mg/kg [11] |
70.1 0 |
100 100 |
16.7 SD 83.3 PD |
100 CR |
|
Liver (HepG2) 1.9 mg/kg [11] |
55.5 25.0 |
100 100 |
25.0 PR 75.0 PD |
100 CR |
|
Fibrosarcoma (HT-1080) 1.9 mg/kg |
20.0 0 |
100 100 |
100 PD | 100 CR |
|
Breast (MDA-MB 157) 2.0 mg/kg |
na | 92.2 66.7 |
na | 33.3 CR 33.3 PR 33.3 SD |
|
Breast (MDA-MB 468) 2.0 mg/kg |
na | 92.2 66.7 |
na | 33.3 CR 33.3 PR 33.3 SD |
|
Lung (H1339) 2.0 mg/kg |
na | 96.5 66.7 |
na | 16.7 CR 50.0 PR 16.7 SD 16.7 PD |
|
Lung (A549) 2.0 mg/kg |
na | 89.0 33.3 |
na | 33.3 PR 50.0 SD 16.7 PD |
|
Pancreatic (MiaPaca2) 2.0 mg/kg |
na | 100 100 |
na | 66.7 CR 33.3 PR |
|
Pancreatic (PaCa44)b 3.0 mg/kg |
na | 100 100 |
na | 100 CR |
|
Pancreatic (PaCa44)b 6.0 mg/kg |
na | 100 100 |
na | 100 CR |
|
Pancreatic (MiaPaca2)b 1.5 mg/kg |
na | 92.2 66.6 |
na | 16.6 CR 50.0 PR 33.3 SD |
Regimen = BIWx3.
a
Nab-paclitaxel at 10 mg/kg instead of Genz-644282 was used in Patient-Derived Xenograft (PDX) model.
b
Regimen = Q7dx3.