NCIt definition : A humanized, pH-sensitive immunoglobulin (Ig) G1 monoclonal antibody directed against
the human T-cell-expressed receptor cytotoxic T-lymphocyte-associated antigen 4 (CTLA4;
CTLA-4; CD152), with potential immune checkpoint inhibitory and antineoplastic activities.
Upon administration, gotistobart targets and binds to CTLA-4 expressed on T-cells
and inhibits the CTLA-4-mediated downregulation of T-cell activation. This leads to
a cytotoxic T-lymphocyte (CTL)-mediated immune response against cancer cells, thereby
killing cancer cells. As gotistobart is dissociated from CTLA-4 under low pH, it does
not cause lysosomal degradation of CTLA-4, preserving CTLA-4 and allowing the recycling
of CTLA-4. This may result in more efficient and selective CTLA-4-targeted regulatory
T-cell (Treg) depletion within the tumor microenvironment (TME) while preserving CTLA-4
functions outside the TME, thereby reducing toxicities. CTLA-4, an inhibitory receptor
and member of the immunoglobulin superfamily (IgSF), plays a key role in the downregulation
of the immune system.;
UNII : 4R46M31XXP;
CAS number : 2226344-78-9; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 2226344-78-9
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Semantic type(s)