Table 3. Completed clinical trials of GSI in cancer.
| Treatment | Trial type and tumor | Enrolment | Primary endpoint | Therapy effect | NCT trial number | Reference |
|---|---|---|---|---|---|---|
| MK0752 | Phase I; advanced solid tumor | 103 | MTD | 1 CR and 12 SD | 106145 | (38) |
| MK0752 | Phase I; normal | 30 | Notch response signature | NA | 803894 | NR |
| Phase I/II; breast cancer | Phase I/II; breast cancer | 30 | DLT 11 PR, 9 SD, and 3 | PD | 645333 | (39) |
| MK0752 + gemcitabine | Phase I/II; pancreatic cancer | 44 | Safety/MTD | NA | 1098344 | NR |
| RO4929097 | Phase II; renal cell carcinoma | 5 | Efficacy | NA | 1141569 | NR |
| RO4929097 | Phase II; pancreatic cancer | 18 | Survival rate | 3 SD | 1232829 | (40) |
| RO4929097 | Phase II, colorectal cancer | 37 | Efficacy | 6 SD | 1116687 | (41) |
| RO4929097 | Phase II; NSCLC | 6 | Efficacy | NR | 1193868 | NR |
| RO4929097 | Phase I; advanced solid tumor | 17 | Pharmaco-kinetics study | NR | 1218620 | NR |
| RO4929097 | Phase I; advanced solid tumor | 28 | Safety | NR | 1096355 | NR |
| RO4929097+ capecitabine | Phase I; refractory solid | 30 | MTD | 3 PR, 1 PR, 3 SD | 1158274 | (42) |
| RO4929097+ gemcitabine | Tumor phase I; advanced solid tumor | 18 | Safety | 11 SD | 1145456 | (43) |
| RO4929097+ temsirolimus | Phase I; advanced solid tumor | 17 | Safety | – | 1198184 | (27) |
NR, not reported; MTD, maximum tolerated dose; DLT, dose limiting toxicity; NSCLC, non-small cell lung cancer; GSI, γ-secretase inhibitor; CR, complete response; SD, stable disease; PR, partial response; PD, pharmacodynamics.