Table 1.
Selected pTyr isosteres and other inhibitors currently in clinical trials or with notable pre-clinical efficacy.
| Target | Inhibitor | Class | Phase/Trial ID | Indications | Refs |
|---|---|---|---|---|---|
| STAT3 | TTI-101 (C188–9) | Sulfonamide, direct inhibitor | Phase I (NCT03195699) | Advanced solid tumors | 121 |
| LY-17 | Sulfonamide, direct inhibitor | Pre-clinical study | 116 | ||
| OPB-111077 | Undisclosed, SH2 inhibitor | Phase I (NCT04049825) | Diffuse large B-cell lymphoma | 158, 159 | |
| Phase I (NCT03197714) | Acute myeloid leukemia | ||||
| Phase I (NCT03063944) | Acute myeloid leukemia | ||||
| Phase II (NCT02250170) | Refractory solid tumors | ||||
| AZD9150 (Danvatirsen, ISIS-STAT3rx) | STAT3 ASO | Phase l/ll (NCT03421353) | Advanced solid tumors | 162, 163 | |
| Phase II (NCT02983578) | Advanced pancreatic/NSCLC/colorectal cancer | ||||
| Phase l/ll (NCT02499328) | Advanced solid tumors/HNSCC | ||||
| Phase I (NCT02546661) | Bladder cancer | ||||
| Phase I (NCT03527147) | Refractory Non-Hodgkins Lymphoma | ||||
| Phase II (NCT03334617) | Non-small cell lung cancer | ||||
| Phase I (NCT03819465) | Non-small cell lung cancer | ||||
| Phase l/ll (NCT03742102) | Triple-negative breast cancer | ||||
| Grb2 | BP1001 | Grb2 ASO | Phase l/ll (NCT02923986) | Chronic myelogenous leukemia | 164 |
| Phase II (NCT02781883) | AML/Myelodysplastic syndrome | ||||
| Phase I (NCT01159028) | CML/AML/ALL/MDS | ||||
| PTP1B | DPM-1001 | Allosteric inhibitor | Pre-clinical study | 166 | |
| SHP2 | TNO155 | Allosteric inhibitor | Phase I (NCT03114319) | Advanced solid tumors | 18 |
| Phase Ib (NCT04000529) | Advanced solid tumors | ||||
| RMC-4630 | Allosteric inhibitor | Phase I (NCT03634982) | Refractory solid tumors | Unavailable | |
| Phase l/II (NCT03989115) | Refractory solid tumors | ||||
| JAB-3O68 | Undisclosed | Phase I (NCT03518554) | Advanced solid tumors | Unavailable | |
| Phase I(NCT03565003) | Advanced solid tumors |