Table 1.
Summary of PTP1B inhibitors (undergone/undergoing clinical trials).
Compound | Company | IC50 or Ki (µM) | Clinical Phase | Continued or Not | Indications | Trials’ Registration Number | |
---|---|---|---|---|---|---|---|
PTP1B | TCPTP | ||||||
Ertiprotafib | Pfizer | IC50 > 20 | Unknown | Phase II | × | T2DM | Unknown |
JTT-551 | Tobacco | Ki = 0.22 | Ki = 9.30 | Pre-clinical | × | T2DM, obesity | Unknown |
KQ-791 | Kaneq Bioscience |
Unknown | Unknown | Phase I | Unknown | T2DM | ClinicalTrials.gov: NCT02445911 |
TTP-814 | TransTech Pharma |
Unknown | Unknown | Phase II | × | T2DM | Unknown |
Trodusquemine | DepYmed | IC50 = 1.0 | IC50 = 224 | Phase I | × | T2DM, obesity Metastatic breast cancer |
ClinicalTrials.gov: NCT00606112 ClinicalTrials.gov: NCT02524951 |
DPM-1001 | DepYmed | IC50 = 0.10 | Unknown | Pre-clinical | √ | T2DM, obesity | Unknown |
IONIS 113715 | IONIS Pharmaceuticals | IC50 < 0.01 | Unknown | Phase II | × | T2DM | ClinicalTrials.gov: NCT00330330 |
IONIS PTP1BRx | IONIS Pharmaceuticals | Unknown | Unknown | Phase II | √ | T2DM | ClinicalTrials.gov: NCT01918865 |