Preferred Label : Recombinant Human Hyaluronidase and Pembrolizumab;
NCIt synonyms : Pembrolizumab/Hyaluronidase; Hyaluronidase/Pembrolizumab; MK-5180/Pembrolizumab; Pembrolizumab and Hyaluronidase; Hyaluronidase and Pembrolizumab; MK-5180 and Pembrolizumab;
NCIt definition : A fixed-dose co-formulation composed of pembrolizumab, a humanized immunoglobulin
G4 (IgG4) monoclonal antibody directed against human cell surface receptor PD-1 (programmed
death-1; programmed cell death-1; cluster of differentiation 279; CD279), and MK-5180,
a recombinant form of human hyaluronidase, with potential immune checkpoint inhibitory
and antineoplastic activities. Upon subcutaneous administration of recombinant human
hyaluronidase and pembrolizumab, the hyaluronidase reversibly depolymerizes the polysaccharide
hyaluronan in the subcutaneous tissue. This increases the permeability of the subcutaneous
tissue and enhances the absorption of pembrolizumab into the systemic circulation.
In turn, pembrolizumab binds to PD-1, an inhibitory signaling receptor expressed on
the surface of activated T-cells, and blocks the binding to and activation of PD-1
by its ligands, which results in the activation of T-cell-mediated immune responses
against tumor cells. The ligands for PD-1 include programmed cell death ligand 1 (PD-L1;
cluster of differentiation 274; CD274), overexpressed on certain cancer cells, and
programmed cell death ligand 2 (PD-L2), which is primarily expressed on APCs. Activated
PD-1 negatively regulates T-cell activation and plays a key role in in tumor evasion
from host immunity. When administered subcutaneously, hyaluronidase, an endoglycosidase,
increases the dispersion and absorption of co-administered drugs.;
Molecule name : MK 3475A; MK-3475A;
NCI Metathesaurus CUI : CL1907015;
Origin ID : C200181;
UMLS CUI : C5856149;
Semantic type(s)
- chemical_or_drug_has_mechanism_of_action
- concept_is_in_subset
- has_target
