Table 4 Representative drugs targeting Wnt signaling in clinical trials

CWP232291

beta-catenin

acute myeloid leukemia,

chronic myelomonocytic leukemia

phase 1

single group assignment

NCT01398462

Sinecatechins

beta-catenin

superficial basal cell carcinoma

phase 2/3

parallel assignment

NCT02029352

Foxy-5

Wnt-5a

metastatic breast cancer,

colorectal cancer,

prostate cancer

phase 1

single group assignment

NCT02020291

Foxy-5

Wnt-5a

metastatic breast cancer,

metastatic colon cancer,

metastatic prostate cancer

phase 1

single group assignment

NCT02655952

Rosmantuzumab (OMP-131R10)

Wnt/beta-catenin

metastatic colorectal cancer

phase 1

single group assignment. OMP-131R10 as a single agent and in combination with FOLFIRI

NCT02482441

PRI-724

Wnt/beta-catenin

acute myeloid leukemia,

chronic myeloid leukemia

phase 1/2

parallel assignment

NCT01606579

PRI-724

Wnt/beta-catenin

pancreatic cancer

phase 1

all enrolled subjects will be treated with both PRI-724 and gemcitabine

NCT01764477

Onc201

Wnt/beta-catenin

advanced solid tumors,

multiple myeloma

phase 1

single group assignment

NCT02609230

Mesalazine

Wnt/beta-catenin

sporadic colorectal adenoma

phase 2

parallel assignment

NCT01894685

Resveratrol

Wnt

colon cancer

phase 1

single group assignment

NCT00256334

Diclofenac

Wnt

basal cell carcinoma

phase 2

topical vitamin D3, diclofenac or a combination of both

NCT01358045

Genistein

Wnt

colon cancer,

rectal cancer,

colorectal cancer

phase 1/2

Genistein combined with FOLFOX or FOLFOX-Avastin

NCT01985763

Ipafricept

(OMP-54F28)

Wnt

sarcomas,

basal cell carcinoma,

ovarian cancer,

desmoid tumors and prostate cancer

phase 1

after OMP-54F28 is discontinued, all subjects will receive vitamin D3 and calcium carbonate twice daily

NCT01608867

WNT974 (LGK974)

RNF43

metastatic colorectal cancer

phase 1/2

phase l: dose escalation phase;

phase ll: single group assessing the triple combination of WNT974, LGX818 and cetuximab

NCT02278133

ETC-1922159

Porcupine

advanced solid tumors

phase 1

ETC-1922159 as a single agent and in combination with pembrolizumab

NCT02521844

BI 905677

LRP5/6

different types of advanced cancer

phase 1

sequential assignment

NCT03604445

LY2090314

GSK-3β

advanced or metastatic cancer

phase 1

LY2090314 in combination with pemetrexed and carboplatin

NCT01287520

LY2090314

GSK-3β

leukemia

phase 2

single group assignment

NCT01214603

Vantictumab (OMP-18R5)

FZD

stage IV pancreatic cancer

phase 1

single group assignment, vantictumab in combination with nab-paclitaxel and gemcitabine

NCT02005315

Vantictumab (OMP-18R5)

FZD

non-small cell lung cancer

phase 1

single group assignment, vantictumab in combination with docetaxel

NCT01957007

Vantictumab (OMP-18R5)

FZD

metastatic breast cancer

phase 1

single group assignment, Vantictumab in combination with paclitaxel

NCT01973309

Niclosamide

Frizzled

prostate carcinoma

phase 1

niclosamide in combination with enzalutamide

NCT02532114

BHQ880

DKK-1

multiple myeloma

phase 2

parallel assignment, BHQ880 in combination with bortezomib and dexamethasone

NCT01337752

DKN-01

DKK-1

carcinoma of intrahepatic

and extra-hepatic biliary system, carcinoma of gallbladder

phase 1

parallel assignment, DKN-01 in combination with gemcitabine and cisplatin

NCT02375880

Bortezomib

DKK-1

multiple myeloma

phase 4

prospective

NCT01026701

PRI-724

CBP/beta-catenin

pancreatic cancer

phase 1

single group assignment

NCT01764477

PRI-724

CBP/beta-catenin

myeloid malignancies

phase 1/2

parallel assignment, PRI-724 as a single agent and in combination with low dose ara-C therapy or dasatinib

NCT01606579