NCIt definition : An orally bioavailable inhibitor of protein tyrosine phosphatase (PTP) non-receptor
type 2 (PTPN2; T-cell protein tyrosine phosphatase; TCPTP) and type 1 (PTPN1; PTP1B),
with potential immunomodulating and antineoplastic activities. Upon oral administration,
osunprotafib targets, binds to and inhibits the activity of PTPN2 and PTPN1. This
prevents PTPN2/1-mediated signaling and prevents PTPN2/1-mediated negative regulation
of immune response pathways. This may promote antitumor immune responses by increasing
the activation and function of certain immune cells, including T-cells and dendritic
cells (DCs), inducing cytokine production, and enhancing interferon gamma (IFNg)-mediated
tumor growth arrest. In addition, osunprotafib disrupts mitochondrial function and
mitophagy in certain tumor cells. PTPN1 and PTPN2, members of the PTP superfamily,
are intracellular T-cell checkpoints and negative regulators of several cytokine signaling
pathways and T-cell receptor (TCR) signaling. They play key roles in tumor immune
suppression and tumor growth.;