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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