Table 1. Overview of clinical trials with drugs targeting the Wnt pathway.
| Compound | Mode of action | Trial Phase | Tumor entities | Originator | Preliminary clinical results | Starting date | Trial identifier |
|---|---|---|---|---|---|---|---|
| LGK974 (WNT974) | Inhibitor of Porcupine | 1/2 | Metastatic colorectal cancer with Wnt pathway mutations; head and neck squamous cell carcinoma with Notch receptor mutations | Novartis | None | October 2014 January 2016 | NCT02278133 NCT02649530 |
| ETC-159 | Inhibitor of Porcupine | 1 | Solid tumors | D3-Institute, experimental Therapeutics Centre (ETC), Duke-NUS | None | July 2015 | NCT02521844 |
| OMP-54F28 (Ipafricept) | Fzd8-Fc Decoy receptor | 1 | Hepatocellular carcinoma; ovarian cancer; pancreatic ductal adenocarcinoma | Bayer HealthCare Pharmaceutical; OncoMed Pharmaceuticals | None | February 2014 | NCT02092363 NCT02092363 NCT02050178 |
| OMP18R5 (Vantictumab) | Anti-Fzd7 antibody | 1 | Non-small cell lung cancer; pancreatic ductal adenocarcinoma; metastatic breast cancer | Bayer HealthCare Pharmaceuticals; OncoMed Pharmaceuticals | Well tolerated; Increased bone turnover;188 LEF1 is a potential biomarker for treatment response209 | September 2013 December 2013 October 2013 | NCT01957007 NCT02005315 NCT01973309 |
| OTSA101 | Yttrium90 radiolabeled Anti-Fzd10 antibody | 1 | Synovial sarcoma | OncoTherapy Science | Heterogeneous uptake; one case of thrombopenia complicated by hemoptysis with fatal outcome191 | November 2011 | NCT01469975 |
| OMP131R10 | Anti-R-spondin3 antibody | 1 | RSPO3 biomarker-positive metastatic colorectal cancer | OncoMed Pharmaceutical; Celgene | None | June 2015 | NCT02482441 |
| Foxy-5 | Wnt5a mimetic | 1 | Breast cancer; colorectal cancer; prostate cancer | WntResearch | No dose-limiting toxicity identified; Phase 1b trial planned199 | January 2016 | NCT02655952 |
| PRI-724 | Inhibitor of TCF-CBP interaction | 1/2 | Acute and chronic myelogenous leukemia; colorectal adenocarcinoma, pancreatic adenocarcinoma | PRISM BioLab and University of Southern California | No dose-limiting toxicity in pancreatic cancer trial, some evidence of clinical activity194 | April 2015 | NCT01606579 NCT02413853 NCT01764477 |
Abbreviation: TCF, T-cell factor.