Preferred Label : Epacmarstobart;
NCIt synonyms : Anti-SIRPa Antibody FSI-189;
NCIt definition : An antibody targeting human signal-regulatory protein alpha (SIRPa; CD172a), with
potential immune checkpoint inhibitory, phagocytosis-inducing and antineoplastic activities.
Upon administration, epacmarstobart 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, and results in macrophage activation and
the specific phagocytosis of 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 : IET3OXF3TO;
CAS number : 2518200-89-8;
Molecule name : FSI 189; FSI-189; GS-0189; GS 0189;
NCI Metathesaurus CUI : CL1413022;
Origin ID : C175555;
UMLS CUI : C5706691;
Semantic type(s)
- chemical_or_drug_has_mechanism_of_action
- concept_is_in_subset
- has_target
