Table 1.
Drugs in clinical development.
| Class | Drug(s) | Target | Phase | Enrollment or estimated | Primary endpoint; subjects | Trial status | Trial IDa |
|---|---|---|---|---|---|---|---|
| γ-Secretase inhibitors | MK0752 | γ-Secretase | I | 50 | Safety/efficacy; relapsed or refractory T-ALL/T-LL | Terminated | NCT00100152 |
| MK0752 | I | 103 | Safety/MTD; advanced breast cancer/advanced solid tumors | Completed | NCT00106145 | ||
| MK0752 | I | 33 | Safety; recurrent or refractory CNS malignancies | Terminated | NCT00572182 | ||
| MK0752 + Docetaxel | I/II | 30 | DLT; locally advanced or metastatic breast cancer | Completed | NCT00645333 | ||
| MK0752 + Gemcitabine | I/IIa | 60 | Safety/MTD; stage IV pancreatic cancer | Recruiting | NCT01098344 | ||
| MK0752 | I | 30 | Notch response signature; healthy young adults | Completed | NCT00803894 | ||
| MK0752 | Pre-surgical | 20 | Safety/tolerability; early stage ER-positive breast cancer | Unknown | NCT00756717 | ||
| RO4929097b | - | - | - | Terminated | - | ||
| PF03084014 | I | 60 | Safety/DLT; advanced solid Tumors/T-ALL/T-LL | Ongoing | NCT00878189 | ||
| BMS-906024 | I | 95 | Safety/tolerability; advanced solid tumors | Recruiting | NCT01292655 | ||
| BMS-906024 | I | 42 | Safety/tolerability; T-ALL/T-LL | Recruiting | NCT01363817 | ||
| BMS906024 + chemotherapy c | Ib | 60 | Safety; advanced or metastatic solid tumors | Recruiting | NCT01653470 | ||
| LY3039478 | I | 80 | DLTs; advanced or metastatic cancer | Recruiting | NCT01695005 | ||
| mAbs to Notch receptors or ligands | OMP-59R5 | Notch2/3 | I | 44 | Safety; advanced solid tumors | Recruiting | NCT01277146 |
| OMP-59R5 + Nab-P & Gemcitabine | Notch2/3 | Ib/II | 154 | DLT/MTD; first line for stage IV pancreatic cancer | Recruiting | NCT01647828 | |
| OMP21M18 | DLL4 | I | 30 | Safety; advanced solid tumors | Recruiting | NCT00744562 | |
| OMP21M18 + FOLFIRI c | DLL4 | Ib | 32 | MTD; first or second line for advanced colorectal cancer | Recruiting | NCT01189942 | |
| OMP21M18 + CP c | DLL4 | Ib | 32 | MTD; first line for advanced non-squamous NSCLC | Recruiting | NCT01189968 | |
| OMP21M18 + Gemcitabine | DLL4 | Ib | 40 | MTD; first line for advanced or metastatic pancreatic cancer | Recruiting | NCT01189929 | |
| REGN421 | DLL4 | I | 80 | Safety/tolerability; advanced solid tumors | Recruiting | NCT00871559 | |
| OMP52M51 | Notch1 | I | 33 | Safety; relapsed or refractory solid tumors | Recruiting | NCT01778439 | |
| OMP52M51 | Notch1 | I | 53 | Safety; relapsed or refractory lymphoid malignancies | Recruiting | NCT01703572 | |
| γ-Secretase modifier | MPC-7869/R-flurbiprofen | γ-Secretase | IIb | Unknown | TTP c; localized prostate cancer at risk of recurrence following radiation therapy and/or prostatectomy | Unknown | NCT00045123 |
a
Clinical trial registration and information at www.clinicaltrials.gov.
b
Clinical trials with RO4929097 are not shown due to the termination of its development.
c
Chemotherapy, weekly paclitaxel, FOLFIRI or carboplatin plus paclitaxel; FOLFIRI, FOLolinic acid (leucovorin), 5-Fluorouracil (5-FU) plus IRInotecan (irinotecan) or carboplatin plus paclitaxel; CP, carboplatin and pemetrexed; Nab-P, Nab-paclitaxel; TTP, time to progression.