Preferred Label : Efdelikofusp Alfa;
NCIt synonyms : Bispecific Fusion Protein GI-101; Bispecific CD80-lgG4Fc-IL-2v Fusion Protein GI-101;
NCIt definition : A bi-specific Fc fusion protein composed of the N-terminal extracellular domain (ECD)
of human CD80 (B7.1) fused to a human immunoglobulin G4 (IgG4) Fc fragment and linked
to an interleukin (IL)-2 variant (IL-2v) as a C-terminal moiety, with potential immunostimulatory,
immune checkpoint inhibitory and antineoplastic activities. Upon administration of
efdelikofusp alfa, the CD80 moiety targets and binds to CTL-associated antigen 4 (CTLA4;
CTLA-4) expressed on T-cells. This prevents the binding of CTLA-4 to endogenous CD80,
enables the binding of CD80 to CD28, which leads to CD28-mediated signaling, and results
in the activation of T-cells in the tumor microenvironment (TME). This promotes T-cell
activity. The IL-2 moiety may stimulate a local immune response and activate natural
killer (NK) cells and cytotoxic T-cells. This may enhance the activity of neoantigen
specific T-cells and potentiates the T-cell-mediated immune response against tumor
cells. CD80 is a co-stimulatory molecule expressed on activated antigen presenting
cells (APCs) that plays a key role in T-cell activation upon binding to CD28 on T-cells.
On the other hand, binding of CD80 to CTLA-4 prevents CD80-CD28 engagement, thereby
inhibiting T-cell activity and immune activation. CTLA-4 is a member of the immunoglobulin
superfamily (IgSF) and an inhibitory molecule upregulated by T-cells following T-cell
activation. It plays a key role in the downregulation of the immune system. IL-2v
cannot bind to IL-2 receptor-alpha (CD25, IL2Ra) and does not activate regulatory
T-cells (Tregs).;
UNII : 3Y7ANB3DKG;
Molecule name : GI 101; GI-101;
NCI Metathesaurus CUI : CL1664640;
Origin ID : C181773;
UMLS CUI : C5557257;
Semantic type(s)
- concept_is_in_subset
- has_target
