NCIt definition : An engineered fragment crystallizable (Fc) domain bispecific human immunoglobulin
G1 (IgG1) monoclonal antibody directed against the human negative immunoregulatory
checkpoint receptors programmed cell death protein 1 (PD-1; PDCD1; CD279) and cytotoxic
T-lymphocyte-associated antigen 4 (CTLA4; CTLA-4), with potential immune checkpoint
inhibitory and antineoplastic activities. Upon administration, volrustomig targets
and binds to both PD-1 and CTLA4 expressed on tumor-infiltrating T lymphocytes (TILs),
and inhibits the PD-1- and CTLA4-mediated downregulation of T-cell activation and
proliferation. In addition, volrustomig is internalized and is able to degrade PD-1.
This restores immune function and activates a sustained cytotoxic T-lymphocyte (CTL)-mediated
immune response against tumor cells. Both PD-1 and CTLA4 are selectively expressed
on TILs in the tumor microenvironment (TME) and negatively regulate the activation
and effector functions of T-cells. They play key roles in the downregulation of the
immune system and tumor evasion from host immunity. Dual checkpoint blockade of PD1
and CTLA4 with volrustomig may enhance T-cell activation and proliferation more than
the blockade of either immune checkpoint receptor alone. It may also decrease toxicity
by avoiding the binding to CTLA-4-expressing T-cells that are devoid of PD-1. The
engineered Fc domain may reduce Fc effector function.;
UNII : K96EGJ218N;
CAS number : 2407760-40-9; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 2407760-40-9
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G-SRS /a ;
Semantic type(s)