Osunprotafib promotes anti-tumor immunity as a monotherapy and, when combined with anti-PD-1, leads to significant tumor regression, even in models resistant to anti-PD-1 treatment, such as 4T1 and EMT6[3].
In Vitro
Osunprotafib acts on both tumor cells and the host immune system, inducing unique transcriptional changes in the myeloid and lymphocyte populations of the tumor microenvironment, enhancing CD8+ T cell activation and effector functions while reducing the expression of genes classically associated with T cell depletion and dysfunction[2].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Philip R. Kym, et al. Protein tyrosine phosphatase inhibitors and methods of use thereof. WO2022056281A1.
[2]. Arvin Iracheta-Vellve, et al. Targeting the immune checkpoint PTPN2 with ABBV-CLS-484 inflames the tumor microenvironment and unleashes potent CD8+ T cell immunity. Cancer Res (2022) 82 (12_Supplement): 606.
[3]. Christina K, et al. ABBV-CLS-484: An active site PTPN2/N1 inhibitor that augments the immune response and sensitizes tumors to immune-mediated killing. Cancer Res (2022) 82 (12_Supplement): ND06.
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