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. 2022 Jun 24;23(13):7027. doi: 10.3390/ijms23137027

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