Table 1 Overview of clinical trials with drugs targeting the Wnt pathway

From: Wnt signaling in cancer

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

  1. Abbreviation: TCF, T-cell factor.