PD-1-IN-1

PD-1-IN-1 is an inhibitor of programmed cell death 1 ligand 1 (PD-L1), PD-L2, and V-type immunoglobulin domain-containing suppressor of T-cell activation (VISTA).¹ It rescues PD-L1-, PD-L2-, or VISTA-induced inhibition of IFN-γ release in isolated human peripheral blood mononuclear cells (PBMCs) stimulated with anti-CD3 and anti-CD28 antibodies (EC₅₀s = 66.1, 80.9, and 82.9 nM, respectively). PD-1-IN-1 is selective for these immune checkpoint proteins over B7-1 and cytotoxic T lymphocyte protein 4 (CTLA-4) at 1,000 nM and a panel of 80 receptors, transporters, and enzymes at 10,000 nM. It does not induce IL-2, IFN-γ, or TNF-α release in isolated human PBMCs in an in vitro cytokine storm assay when used at concentrations ranging from 10-1,000 nM. PD-1-IN-1 (10 mg/kg, p.o.) increases proliferation and activation of tumor-infiltrating T cells and decreases tumor volume in a CT26 murine colon cancer model.

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1. Sasikumar, P.G., Sudarshan, N.S., Adurthi, S., et al. PD-1 derived CA-170 is an oral immune checkpoint inhibitor that exhibits preclinical anti-tumor efficacy. Commun. Biol. 4(1), 699 (2021).