NCIt definition : A modified form of the recombinant form of human endogenous cytokine interleukin-2
(IL-2), that is masked with a protein domain, with potential immunoregulatory and
antineoplastic activities. Upon administration of protein-engineered IL-2 XTX202,
IL-2 is bound to the protein and pharmacologically inactive. IL-2 does not become
active until cleaved by specific proteases in the tumor microenvironment (TME). Upon
proteolytic cleavage, unbound and active IL-2 locally binds to the IL-2 receptor beta
(CD122) and gamma (CD132) subunits (IL2Rb/g) that are expressed on CD8 T effector
cells and natural killer (NK) cells, thereby activating IL2R-mediated signaling within
these immune cells. The activation of T- and NK cells mediate cytolytic immune responses
against tumor cells causing tumor cell destruction and inhibition of tumor cell proliferation.
XTX202 does not bind to IL-2 receptor alpha (IL-2Ra) and does not cause IL-2Ra-mediated
toxicities. The selective activation in the TME enhances the IL-2-mediated cytolytic
responses against tumor cells while sparing the unwanted effects of systemic, peripheral
immune activation.;