Table 2 STAT3 inhibitors in clinical research stage
From: STAT3: Key targets of growth-promoting receptor positive breast cancer
Inhibitor name | Target | Type | Cancer type | Clinical trials | Refs. |
|---|---|---|---|---|---|
S3I-M2001 | SH2 | Peptidomimetic | BC | / | [197] |
S3I-201 | SH2 | Small molecule | AdCC, HNSCC, ASCC | / | |
STA-21 | SH2 | Small molecule | BC | / | [200] |
Stattic | SH2 | Small molecule | NPC | / | [201] |
OPB-51602 | SH2 | Small molecule | Hematological, malignancie, refractory solid malignancies | NCT01344876 NCT01184807 NCT02058017 NCT01867073 | |
OPB-111077 | SH2 | Small molecule | HCC, acute myeloid leukemia | NCT04049825 NCT01711034 NCT03158324 NCT03063944 NCT03197714 NCT02250170 NCT01942083 | |
TTI-101 | SH2, CCD | Small molecule | HCC, HNSCC | NCT03195699 NCT06141031 NCT05440708 NCT05384119 NCT05845307 NCT05668949 | |
YY-201 | SH2 | Small molecule | Refractory solid malignancies | NCT06225856 | / |
HJC0152 | SH2 | Small molecule | GBM, PC | / | [210] |
CJ-1383 | SH2 | Small molecule | Refractory solid malignancies | / | [211] |
DSP-0337 | SH2 | Small molecule | Refractory solid malignancies | NCT03416816 | / |
Napabucasin(BBI608) | SH2 | Small molecule | Refractory solid malignancies | NCT02826161 NCT02851004 NCT02993731 NCT03522649 NCT02315534 NCT02753127 NCT01325441 NCT01776307 NCT02358395 NCT01775423 NCT02279719 NCT02432326 NCT04299880 NCT02178956 NCT03647839 NCT03411122 NCT02467361 NCT02347917 NCT02024607 NCT02352558 NCT01830621 NCT02641873 NCT02231723 | |
Pyrimethamine | SH2 | Small molecule | AL | NCT01066663 | [214] |
WP1066 | JAK2/STAT3 pathway | Small molecule | encephaloma | NCT04334863 NCT01904123 NCT05879250 | [215] |
STAT3 decoy | DBD | Oligodeoxynucleotides | HNSCC, NSCLC | NCT00696176 | |
G-quartet ODN | DBD | Oligodeoxynucleotides | HNSCC, NSCLC | / | |
InS3-54A18 | DBD | Small molecule | LC, BC | / | [220] |
InS3-54 | DBD | Small molecule | NSCLC, BC | / | [221] |
MMPP | DBD | Small molecule | NSCLC, OC | / | |
AZD9150 | STAT3 mRNA | Antisense oligonucleotides | HCC, HNSCC, LC, Lymphoma | NCT02417753 NCT02549651 NCT03421353 NCT02499328 NCT02546661 NCT01839604 NCT03394144 NCT03527147 NCT05986240 NCT03334617 NCT05814666 NCT02983578 NCT03794544 NCT03819465 | |
MiR-124-3p | STAT3 mRNA | miRNA | NPC | / | [227] |
SD-36 | STAT3 protein | PROTAC | Lymphocytic leukemia | / | [228] |