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Table 2 STAT3 inhibitors in currently on-going clinical trials

From: Targeting STAT3 in Cancer Immunotherapy

Therapy

Type

Agent

Indication

Phase

NCT number

Ref

Direct inhibitors

Small molecules

BBI608 (FDA approved)

Advanced malignancies

I/II

NCT01775423

NA

CRC

III

NCT01830621

[117]

Celecoxib* (FDA approved)

CRC

III

NCT00087256

NA

C188-9

BC, CRC, HNSCC, HCC, NSCLC, GAC, Melanoma, Advanced cancer

I

NCT03195699

NA

OPB-111077

Acute myeloid leukemia

I

NCT03197714

NA

Advanced HCC

I

NCT01942083

NA

OPB-31121

Advanced cancer, Solid tumors

I

NCT00955812

NA

HCC

I/II

NCT01406574

NA

OPB-51602

Malignant solid tumors

I

NCT01184807

NA

Hematological malignancies

I

NCT01344876

NA

Nasopharyngeal carcinoma

I

NCT02058017

NA

Pyrimethamine* (FDA approved)

CLL, Small lymphocytic lymphoma

I/II

NCT01066663

NA

Oligonucleotides

AZD9150

Lymphoma

I/II

NCT01563302

[118]

STAT3 decoy

Head and neck cancer

0

NCT00696176

[119]

Indirect inhibitors

JAK1/2

AZD-1480

Solid tumors

I

NCT01112397

NA

CYT 387

Myelofibrosis

I/II

NCT01423058

[120]

PMF, Post-PV, Post-ET MF

III

NCT02101268

NA

Ruxolitinib (FDA approved)

Myelofibrosis

II

NCT03427866

NA

JAK2

LY2784544

Myeloproliferative neoplasms

II

NCT01594723

[121]

SB1518

Myelofibrosis

III

NCT02055781

[122]

EGFR

Cetuximab (FDA approved)

Metastatic CRC

I/II

NCT02117466

NA

Panitumumab (FDA approved)

Advanced CRC

II

NCT03311750

NA

Metastatic CRC

IV

NCT02301962

NA

FGFR

Ponatinib (FDA approved)

CML

II

NCT04043676

NA

CML, ALL

II

NCT04233346

NA

IL-6R

Siltuximab (FDA approved)

Multiple myeloma

II

NCT03315026

NA

Tocilizumab (FDA approved)

HCC

I/II

NCT02997956

NA

VEGF

Bevacizumab (FDA approved)

Metastatic CRC

II

NCT02226289

NA

VEGFR

Apatinib

Lung carcinoma

II

NCT03709953

NA

VEGFR, PDGFR

Sorafenib (FDA approved)

Advanced HCC

IV

NCT02733809

NA

VEGFR, PDGFR, c-KIT

Sunitinib (FDA approved)

Clear cell renal carcinoma

II

NCT03066427

NA

Pancreatic neuroendocrine tumor metastatic

II

NCT02713763

NA

SRC, ABL

Dasatinib (FDA approved)

Chronic-phase CML

IV

NCT01660906

[123]

SRC

Bosutinib (FDA approved)

CML

II

NCT02810990

NA

KX2-391

Bone-metastatic, Castration-resistant PCa

II

NCT01074138

[124]

Combination

Direct inhibitors and ICB

AZD9150, Durvalumab (anti-PD-L1)

NSCLC

II

NCT03334617

NA

PC, CRC, NSCLC

II

NCT02983578

NA

Advanced solid tumors, Metastatic HNSCC

I/II

NCT02499328

NA

Diffuse large B-cell lymphoma

I

NCT02549651

NA

BBI608, Nivolumab (anti-PD-L1)

Metastatic CRC

II

NCT03647839

NA

BBI608, Pembrolizumab (anti-PD-1)

Metastatic CRC

I/II

NCT02851004

NA

Indirect inhibitors and ICB

Apatinib, SHR-1210 (anti-PD-1)

Melanoma

II

NCT03955354

NA

Bevacizumab, Atezolizumab (anti-PD-L1)

Unresectable HCC

III

NCT03434379

[125]

Cetuximab, Pembrolizumab (anti-PD-1)

Recurrent or metastatic HNSCC

II

NCT03082534

NA

Dasatinib, Ipilimumab (anti-CTLA-4)

GIST, Stage III /IV soft tissue sarcoma

I

NCT01643278

[126]

Dasatinib, Nivolumab (anti-PD-L1)

Philadelphia chromosome positive ALL

I

NCT02819804

NA

Ruxolitinib, Pembrolizumab (anti-PD-1)

Hematological malignancies

II

NCT04016116

NA

Metastatic stage IV TNBC

I

NCT03012230

NA

Sorafenib, BGB-A317(anti-PD-1)

HCC

III

NCT03412773

NA

Sorafenib, Nivolumab (anti-PD-L1)

Advanced or metastatic HCC

II

NCT03439891

NA

Indirect inhibitor and CAR-T

Tocilizumab, CAR-T 19

Lymphoblastic leukemia

NA

NCT02906371

NA

  1. ALL Acute lymphoblastic leukemia, BC Breast cancer, Celecoxib* An FDA approved nonsteroidal anti-inflammatory drug, CML Chronic myelogenous leukemia, CLL Chronic lymphocytic leukemia, CRC Colorectal cancer, HNSCC Head and neck squamous cell carcinoma, NA Not available, NSCLC Non-small cell lung cancer, HCC Hepatocellular carcinoma, GAC Gastric adenocarcinoma, Pyrimethamine* An FDA approved anti-parasitic drug, PMF Primary myelofibrosis, Post-PV Post-polycythemia vera, Post-ET MF Post-essential thrombocythemia myelofibrosis, PC Pancreatic cancer, PCa Prostate cancer, GIST Gastrointestinal stromal tumor, TNBC Triple negative breast cancer