Preferred Label : Davoceticept;
NCIt synonyms : CD80-vlgD-Fc ALPN-202; CD80 vIgD-Fc Fusion Protein ALPN-202; CD80-Fc Fusion Protein ALPN-202;
NCIt definition : A fusion protein composed of the N-terminal Ig variable-like (IgV) domain of CD80
fused to a human immunoglobulin G1 (IgG1) Fc fragment, with potential immunostimulatory,
immune checkpoint inhibitory and antineoplastic activities. Upon administration, davoceticept
targets and binds to programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation
274; CD274) expressed on tumor cells, which blocks its binding to and activation of
its receptor programmed cell death 1 (PD-1; cluster of differentiation 279; CD279),
and leads to PD-L1-dependent CD28 binding and co-stimulation in the local tumor microenvironment
(TME). This reverses T-cell inactivation caused by PD-1/PD-L1 signaling, leads to
the co-stimulation of T-cell responses including the activation of naïve and memory
T-cells in the TME and enhances the cytotoxic T-lymphocyte (CTL)-mediated anti-tumor
immune response against PD-L1-expressing tumor cells. In addition, davoceticept 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, thereby enabling CD80-CD28 engagement, CD28
signaling, and T-cell activation. This further promotes T-cell activity. PD-L1 is
overexpressed by many human cancer cell types. PD-L1 binding to PD-1 on T-cells suppresses
the immune system and results in immune evasion. 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.;
UNII : DE9GN7CD21;
CAS number : 2307144-64-3;
Molecule name : ALPN-202; ALPN 202;
NCI Metathesaurus CUI : CL1412018;
Origin ID : C174515;
UMLS CUI : C5706689;
Semantic type(s)
- concept_is_in_subset
- has_target
