P1, N=74, Completed, NervGen Pharma Corp. | Recruiting --> Completed

In a protein-chip assay, actinomycete extract 4585DW showed PTP1B inhibitory activity comparable to the positive controls, suramin and vanadate. The extract was non-cytotoxic in mammalian and yeast cells and inhibited PTP1B with Km and Vmax values of 10.91 ± 0.50 mM and 0.02 ± 0.00 μmol/min, respectively. In conclusion, 4585DW is a promising candidate for further investigation as a PTP1B inhibitor.

P2, N=184, Active, not recruiting, BioNTech SE | Trial completion date: Jul 2026 --> Dec 2025

Our findings demonstrate that suramin significantly attenuates inflammatory and oxidative damage in an experimental model of acute colitis. These results suggest that suramin may possess therapeutic potential in intestinal inflammation; however, this effect requires further support through advanced experimental and clinical studies.

This improvement in the somatosensory experience was reflected in alleviating depressive-like behavior in the forced swimming test. These findings highlight the therapeutic potential of blocking thalamic P2X receptors in alleviating fibromyalgia symptoms.

P2, N=45, Recruiting, Children's Hospital of Orange County | Not yet recruiting --> Recruiting

LDLR-OTNs demonstrated receptor-mediated uptake and potent cytotoxicity in LDLR- and FAS- overexpressing breast cancer cells. These findings support LDLR-targeted nanoparticles as a promising approach for delivering FAS inhibitors to LDLR-rich tumours, meriting further investigation in targeted cancer therapy development.

CENPA knockdown inhibited rectal cancer cell growth and attenuated xenograft tumor growth through regulating the MGMT/PTPN4 axis.

P2, N=45, Not yet recruiting, Children's Hospital of Orange County

The negative correlations between HMGA2 and thyroid-specific gene expressions were confirmed in a transgenic mouse model of PTC and in human PTC. Finally, we showed that HMGA2 inhibition by suramin reduced cell invasion and induced differentiation expression in vitro, indicating a new therapeutic strategy for treating thyroid cancer.

Although there are only few studies that investigated PTPN2 expression in the GI system cancers, which is a potential limitation, the association of this protein with tumor behavior and the influence of PTPN2 on many therapy-related signaling pathways emphasize that PTPN2 could serve as a new molecular biomarker to predict tumor behavior and as a target for therapeutic intervention against GI cancers. In conclusion, more studies should be performed to better understand the prognostic and therapeutic potential of PTPN2 in GI tumors, especially in tumors resistant to therapy.

This review outlines the structural modification processes of PTPN2-targeted agents, focusing primarily on inhibitors and degraders. Finally, this review endeavors to provide a comprehensive perspective on the evolving field of PTPN2-targeted drug discovery for tumor immunotherapy, offering valuable insights for future drug development.