Table 3. Notch Inhibition by GSI (in Monotherapy or Combination Therapy), under Clinical Trials.
| type and category of GSI | drug | in combination with another drug | target | clinical trials | reference |
|---|---|---|---|---|---|
| azepine (transition state analogues) | RO4929097 (RG4733) | a | pancreatic cancer | phase II | NCT01232829 |
| RO4929097 (RG4733) | a | advanced or metastatic breast cancer or recurrent TNBC | phase II | NCT01151449 | |
| RO4929097 (RG4733) | a | renal cell carcinoma | phase II | NCT01141569 | |
| RO4929097 (RG4733) | a | colorectal cancer | phase II | NCT01116687 | |
| RO4929097 (RG4733) | a | NSCLC | phase II | NCT01193868 | |
| RO4929097 (RG4733) | a | recurrent or metastatic ovarian cancer, fallopian tube cancer, or peritoneal cancer | phase II | NCT01175343 | |
| RO4929097 (RG4733) | a | melanoma | Huynh et al.117 | ||
| RO4929097 (RG4733) | a | metastatic colorectal cancer | phase II | Schell et al.118 | |
| RO4929097 (RG4733) | Vismodegib | advanced or metastatic sarcoma | phase I/II | NCT01154452 | |
| RO4929097 (RG4733) | Letrozole | ER+/PR+ stage I or II breast cancer | phase Ib | NCT01208441 | |
| azepine (nontransition state analogues) | Nirogacestat, PF-03084014 | a | fibromatosis | phase II | NCT01981551 |
| Nirogacestat, PF-03084014 | a | desmoid tumor/aggressive fibromatosis | phase III | NCT03785964 | |
| sulfonamide (nontransition state analogues) | MK-0752 | a | early stage ER+ breast cancer | presurgical | NCT00756717 |
| MK-0752 | Gemcitabine | stage III and IV pancreatic cancer | phase I/II | NCT01098344 | |
| MK-0752 | Docetaxel | locally advanced or metastatic breast cancer | phase I/II | NCT00645333 | |
| MK-0752 | Tamoxifen + Letrozole | early stage ER+ breast cancer | phase IV | NCT00756717 |
a
In monotherapy.