Table 2.
STAT3 inhibitors in currently on-going clinical trials
| 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 |
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