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 | – | – |