Preferred Label : Pacmilimab;
NCIt synonyms : PD-L1 Probody Therapeutic CX-072; Probody CX-072;
NCIt definition : A recombinant antibody prodrug composed of a monoclonal antibody directed against
the tumor-associated antigen (TAA) programmed cell death 1 ligand 1 (PD-L1; B7-H1;
CD274) that is linked to a proprietary masking peptide through a protease-cleavable
linker on the amino terminus of the light chain domain of the antibody, with potential
immune checkpoint inhibitory and antineoplastic activities. Upon administration of
pacmilimab, the linkage system is stable in the circulation and, upon extravasation
into the tumor microenvironment, the peptide mask is cleaved by tumor-associated proteases.
These proteases are present in high concentrations and aberrantly activated in the
tumor microenvironment, while expressed as inactive forms, at much lower concentrations,
in normal, healthy tissue. Protease cleavage of the linker enables binding of the
unmasked, fully active monoclonal antibody moiety of CX-072 to PD-L1, which is over
expressed on certain cancer cells. This blocks the binding to and activation of its
receptor programmed cell death 1 (PD-1) on T-lymphocytes, thereby enhancing the T-cell-mediated
anti-tumor immune response and reversing PD-L1/PD-1-mediated T-cell suppression. PD-L1
binding to PD-1 on T-cells suppresses the immune system and results in immune evasion.
Compared to the unmodified PD-L1 antibody, peptide masking of CX-072 minimizes binding
to PD-L1 in normal tissues, thereby decreasing autoimmune-based side effects while
retaining anti-tumor activity.;
UNII : ZXP96ZI2RA;
CAS number : 2101273-62-3; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 2101273-62-3
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G-SRS /a ;
Molecule name : CX-072; CX 072;
NCI Metathesaurus CUI : CL520194;
Origin ID : C132192;
UMLS CUI : C5418181;
- Semantic type(s)
- chemical_or_drug_has_mechanism_of_action
- concept_is_in_subset
- has_target