Table 5 Inhibitors of Fzds and related factors

OMP-54F28

(Fzd8-Fc fusion)

Wnts

ND

Phase I (NCT02069145): Hepatocellular cancer;

Phase I (NCT02092363): Ovarian cancer;

Phase I (NCT02050178): Pancreatic cancer;

Phase I (NCT01608867): Solid tumors

[408]

OMP-131R10 (mAb)

R-spondin3

ND

Phase I (NCT02482441): Solid tumors

[410]

Niclosamide

Fzd1

0.5 ± 0.05 μM

FDA-approved antihelminth;

Phase I (NCT03123978): Prostate cancer;

Phase II (NCT02519582): Colorectal cancer;

Phase II (NCT02807805): Prostate cancer

[411]

DK-520

Fzd1

0.23 ± 0.06 μM

Preclinical

[412]

DK-419

Fzd1

0.19 ± 0.08 μM

Preclinical

[413]

OMP-18R5 (mAb)

Fzd1/2/5/7/8

ND

Phase I (NCT01345201): Solid tumors;

Phase I (NCT02005315): Pancreatic cancer;

Phase I (NCT01957007): NSCLC;

Phase I (NCT01973309): Breast cancer

[414]

IgG-2919 (mAb)

Fzd5/8

ND

Preclinical

[415]

Fz7–21

Fzd7

50–100 nM

Preclinical

[416]

RHPD-P1

7–40 μM

Preclinical

[417]

SRI37892

0.66 μM

Preclinical

[418]

1094–0205

Fzd8

5.0 ± 1.1 μM

Preclinical

[419]

2124–0331

10.4 ± 2.0 μM

Preclinical

[419]

3235–0367

7.1 ± 1.4 μM

Preclinical

[419]

NSC36784

6.5 ± 0.9 μM

Preclinical

[419]

NSC654259

5.7 ± 1.2 μM

Preclinical

[419]

OTSA101-DTPA-¹¹¹In; OTSA101-DTPA-⁹⁰Y

Fzd10

ND

Phase I (NCT04176016): Synovial sarcoma

[420, 421]

Salinomycin

Wnt/Fzd/LRP

163 nM

Preclinical

[422]

LGR5 (mAb)-mc-vc-PAB-MMAE

LGR5

ND

Preclinical

[423]