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Table 1 Clinical trials and preclinical evaluations on Wnt/β-catenin targeted agents in solid tumors

From: Targeting the Wnt/β-catenin signaling pathway in cancer

Agents Mechanism Phase Cancer type Side effects Identifier
WNT974 PORCN inhibitor Phase 2 Head and neck squamous cell cancer NR NCT02649530
WNT974 PORCN inhibitor Phase 1 Pancreatic cancer; colorectal cancer; melanoma; breast cancer; head and neck squamous cell cancer; cervical squamous cell cancer; esophageal squamous cell cancer; lung squamous cell cancer NR NCT01351103
*WNT974 (with LGX818 and Cetuximab) PORCN inhibitor Phase 1 Colorectal cancer NR NCT02278133
ETC-159 PORCN inhibitor Phase 1 Solid tumor Reversible hematological disorders NCT02521844
CGX1321 PORCN inhibitor Phase 1 Colorectal adenocarcinoma; gastric adenocarcinoma; pancreatic adenocarcinoma; bile duct carcinoma; hepatocellular carcinoma, esophageal carcinoma, Gastrointestinal cancer NR NCT03507998
*CGX1321 (with pembrolizumab) PORCN inhibitor Phase 1 Solid tumors; Gastrointestinal cancer NR NCT02675946
GNF-6231 PORCN inhibitor Preclinical Breast cancer NR
90γ-OTSA-101 FZD10 antagonist Phase 1 Synovial sarcoma NR NCT01469975
OMP-18R5 Monoclonal antibody against FZD receptors Phase 1 Breast cancer Nausea, alopecia, fatigue, peripheral neuropathy NCT01973309
OMP-18R5 Monoclonal antibody against FZD receptors Phase 1 Solid tumors NR NCT01345201
*OMP-18R5 (with docetaxel) Monoclonal antibody against FZD receptors Phase 1 Solid tumors NR NCT01957007
*OMP-18R5 (with nab-paclitaxel and gemcitabine) Monoclonal antibody against FZD receptors Phase 1 Pancreatic cancer NR NCT02005315
OMP-54F28 FZD8 decoy receptor Phase 1 Solid tumors Dysgeusia, muscle spasms, hypophosphatemia NCT01608867
*OMP-54F28 (with sorafenib) FZD8 decoy receptor Phase 1 Hepatocellular cancer Diarrhea, neutropenia and decreased appetite NCT02069145
*OMP-54F28 (with paclitaxel and carboplatin) FZD8 decoy receptor Phase 1 Ovarian cancer NR NCT02092363
*OMP-54F28 (with nab-paclitaxel and gemcitabine) FZD8 decoy receptor Phase 1 Pancreatic cancer NR NCT02050178
Fz7-21 FZD7 antagonist Preclinical Gastroenteric tumor
Salinomycin LRP5/6 inhibitor Preclinical Hepatocellular carcinoma; gastric cancer; colorectal cancer; bladder cancer; breast cancer
FJ9 DVL inhibitor Preclinical Lung cancer; melanoma
3289–8625 DVL inhibitor Preclinical Ovarian cancer; lung cancer
XAV939 Tankyrase inhibitor Preclinical Ovarian cancer; breast cancer
JW74/ JW55 Tankyrase inhibitor Preclinical Osteosarcoma, colon carcinoma
NVP-TNKS656 Tankyrase inhibitor Preclinical Hepatocellular carcinoma; colorectal cancer
LZZ-02 Tankyrase inhibitor Preclinical Colonic carcinoma
SSTC3 CK1α activator Preclinical Colorectal cancer
LF3 β-catenin/TCF Preclinical Colon cancer
KYA1797K/ KY1220 β-catenin Preclinical Colorectal cancer, breast cancer
iCRT3/5 β-catenin/TCF Preclinical Breast cancer; gastric cancer
ZINC02092166 β-catenin/TCF Preclinical Colorectal cancer
NLS-StAx-h β-catenin/TCF Preclinical Colorectal cancer
*PRI-724 (with leucovorin calcium, oxaliplatin, or fluorouracil) CBP/β-catenin antagonist Phase 2 Colorectal cancer Nausea, fatigue NCT02413853
PRI-724 CBP/β-catenin antagonist Phase 1 Pancreatic cancer NR NCT01764477
PRI-724 CBP/β-catenin antagonist Phase 1 Advanced solid tumors Nausea, vomiting, diarrhea, alopecia, fatigue, neutropenia, thrombocytopenia, neutropenic fever NCT01302405
ICG001 CBP antagonist Preclinical Pancreatic cancer, lung cancer, breast cancer; ovarian cancer
Isoquercitrin CBP antagonist Preclinical Colorectal cancer