TABLE 1.
Inhibitors targeting signal transducer and activator of transcription 3 (STAT3) in cancers
| Inhibitor | Target | Type | Cancer type | Clinical trials |
|---|---|---|---|---|
| Inhibitors targeting upstream receptors | ||||
| Dasatinib 203 , 204 , 205 , 206 , 207 , 208 | Src | Small molecule | Breast cancer, head and neck squamous cell carcinoma (HNSCC), leukemia, non‐small‐cell lung carcinoma (NSCLC), prostate cancer | |
| Cetuximab 209 , 210 , 211 , 212 , 213 | Epidermal growth factor receptor | Antibody | Colorectal cancer, HNSCC | |
| AZD1480 214 , 215 | Janus kinase (JAK) | Small molecule | HNSCC, colorectal cancer | ‐ |
| Ruxolitinib 216 , 217 , 218 | JAK | Small molecule | Breast cancer, pancreatic cancer, NSCLC | |
| Tofacitinib 219 | JAK | Small molecule | Lymphocytic leukemia | ‐ |
| 8αTGH | JAK | Natural compound | HNSCC | ‐ |
| Curcumin 221 , 222 | JAK | Natural compound | Lung cancer, HNSCC, breast cancer | |
| WP1066 223 , 224 , 225 | JAK | Small molecule | HNSCC, gastric cancer, melanoma | ‐ |
| Tocilizumab 226 , 227 , 228 | IL‐6R | Antibody | HNSCC, breast cancer, lymphocytic leukemia | |
| Siltuximab 229 , 230 | IL‐6R | Antibody | Prostate cancer, NSCLC | |
| Bazedoxifene 231 | IL‐6R | Small molecule | Pancreatic cancer | ‐ |
| Metformin 232 , 233 | IL‐6R | Small molecule | HNSCC, ovarian cancer, breast cancer | |
| Inhibitors blocking STAT3 dimerization | ||||
| S3I‐M2001 234 | SH2 | Peptidomimetic | Breast cancer | ‐ |
| S3I‐201 235 , 236 , 237 | SH2 | Small molecule | AdCC, HNSCC, ASCC | ‐ |
| STA‐21 238 | SH2 | Small molecule | Breast cancer | ‐ |
| Stattic 239 | SH2 | Small molecule | Nasopharyngeal carcinoma | ‐ |
| OPB‐51602 240 , 241 , 242 | SH2 | Small molecule | Hematological malignancie, refractory solid malignancies | |
| OPB‐111077 243 | SH2 | Small molecule | Hepatocellular carcinoma (HCC), acute myeloid leukemia | |
| TTI‐101 244 , 245 | SH2 | Small molecule | HCC, HNSCC | ‐ |
| CJ‐1383 246 | SH2 | Small molecule | Breast cancer | ‐ |
| Inhibitors targeting STAT3 DNA‐binding domain (DBD) | ||||
| STAT3 decoy 247 , 248 | DBD | Oligodeoxynucleotides (ODNs) | HNSCC, NSCLC | NCT00696176 |
| G‐quartet ODN 249 , 250 | DBD | ODNs | HNSCC, NSCLC | ‐ |
| InS3‐54A18 251 | DBD | Small molecule | Lung cancer, breast cancer | ‐ |
| InS3‐54 252 | DBD | Small molecule | NSCLC, breast cancer | ‐ |
| BBI608 253 , 254 , 255 | DBD | Small molecule | Colorectal cancer, gastric cancer, glioblastoma | |
| MMPP 256 , 257 | DBD | Small molecule | NSCLC, ovarian cancer | ‐ |
| Inhibitors decreasing STAT3 expression | ||||
| AZD9150 258 , 259 | STAT3 mRNA | Antisense oligonucleotides | Lymphoma, lung cancer, HCC HNSCC | |
| MiR‐124‐3p 260 | STAT3 mRNA | MicroRNA | Nasopharyngeal carcinoma | ‐ |
| SD‐36 261 | STAT3 protein | Small molecule | Lymphocytic leukemia | ‐ |