Preferred Label : Anzurstobart;
NCIt synonyms : Anti-SIRPa Monoclonal Antibody CC-95251;
NCIt definition : An immunoglobulin G1 (IgG1) monoclonal antibody targeting signal-regulatory protein
alpha (SIRPa; CD172a) with potential immunostimulating and antineoplastic activities.
Upon intravenous administration, anzurstobart targets and binds to SIRPa, a cell surface
protein expressed on macrophages, thereby blocking the interaction between SIRPa and
cluster of differentiation 47 (CD47) expressed on tumor cells. This prevents CD47/SIRPa-mediated
signaling and abrogates the CD47/SIRPa-mediated inhibition of phagocytosis. This induces
pro-phagocytic signaling mediated by the binding of calreticulin (CRT), which is specifically
expressed on the surface of tumor cells, to low-density lipoprotein (LDL) receptor-related
protein (LRP), expressed on macrophages. This results in macrophage activation and
the specific phagocytosis of tumor cells. In addition, blocking CD47/SIRPa-mediated
signaling activates both an anti-tumor T-lymphocyte immune response and T cell-mediated
killing of CD47-expressing tumor cells. SIRPa, also known as tyrosine-protein phosphatase
non-receptor type substrate 1, mediates negative regulation of phagocytosis, mast
cell activation and dendritic cell activation. CD47, also called integrin-associated
protein (IAP), is a tumor-associated antigen (TAA) expressed on normal, healthy hematopoietic
stem cells (HSCs) and overexpressed on the surface of a variety of cancer cells. Expression
of CD47, and its interaction with SIRPa, leads to the inhibition of macrophage activation
and protects cancer cells from phagocytosis, which allows cancer cells to proliferate.;
UNII : 61FKP5V847;
CAS number : 2543693-10-1;
Molecule name : CC 95251; CC-95251; BMS-986351;
NCI Metathesaurus CUI : CL937061;
Origin ID : C157501;
UMLS CUI : C5706646;
Semantic type(s)
chemical_or_drug_has_mechanism_of_action
concept_is_in_subset
has_target