Preferred Label : Pertuzumab Zuvotolimod;
NCIt synonyms : TLR8 Agonist-HER2-directed Monoclonal Antibody Conjugate SBT6050; ImmunoTAC SBT6050; HER2-directed TLR8 ImmunoTAC SBT6050; HER2-directed TLR8 Agonist SBT6050;
NCIt definition : An immunotherapeutic composed of a monoclonal antibody directed against the tumor-associated
antigen (TAA) human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2) conjugated
to a Toll-like receptor 8 (TLR8; CD288) agonist, with potential immunostimulating
and antineoplastic activities. Upon intravenous administration pertuzumab zuvotolimod,
the anti-HER2 monoclonal antibody targets and binds to HER2 expressed on tumor cells,
thereby localizing the TLR8 agonist directly to the tumor site. In turn, the TLR8
agonist moiety binds to TLR8 expressed on myeloid cells within the tumor microenvironment
(TME). This activates myeloid cells, including tumor-associated macrophages (TAMs),
myeloid cell-derived suppressive cells (MDSCs), and conventional dendritic cells (cDCs).
This may lead to the activation of nuclear factor NF-kappa-B, the production of pro-inflammatory
cytokines and chemokines, macrophage-induced tumor cell killing, inflammasome activation,
activation of cytolytic natural killer (NK) cells and neutrophils, and the induction
of a Th1-weighted anti-tumor immune response. It also reverses the suppression of
senescent naive and tumor-specific T-cells, and enhances the anti-tumor cytotoxic
T-lymphocyte (CTL) immune response. TLR8, like other TLRs, recognizes pathogen-associated
molecular patterns (PAMPs) and plays a key role in innate and adaptive immunity. HER2,
a tyrosine kinase receptor, is overexpressed by many cancer cell types.;
UNII : H4LR6V1LWG;
CAS number : 2500674-05-3;
Molecule name : SBT 6050; SBT-6050;
NCI Metathesaurus CUI : CL1407923;
Origin ID : C174010;
UMLS CUI : C5706686;
Semantic type(s)
chemical_or_drug_has_mechanism_of_action
concept_is_in_subset
has_target