Dostarlimab (TSR-042) is a programmed cell death protein 1 (PD-1) receptor immune checkpoint inhibitor that blocks interactions with PD-L1 and PD-L2, used in the study of endometrial cancer.

PD-1 (human):2.0 nM (EC50)

Dostarlimab has a strong binding affinity with human and cynomolateral monkey PD-1 protein with Kd of 0.3 and 0.5 nM, respectively. Dostarlimab binds to PD-1 on the surface of recombinant human and cynomophobe monkey cells expressed on CHO-K1 cells with EC50 values of 2.0 and 3.4 nM, respectively. Dostarlimab effectively blocked PD-1/PD-L1 and PD-1/PD-L2 binding with IC50 values of 1.8 and 1.5 nM, respectively. Adding Dostarlimab to the SEB-stimulated PBMC resulted in increased IL-2 production with an EC50 of about 0.1 nM, suggesting that Dostarlimab induced T cell activation. [1]

Dostarlimab(200μg/ pill twice weekly) inhibited tumor growth in the MDA-MB-436 breast cancer model. [1]