Preferred Label : Pegenzileukin;
NCIt synonyms : IL-2 Variant THOR-707; Pegylated Recombinant IL-2 Variant THOR-707; Pegylated Recombinant Interleukin-2 THOR-707;
NCIt definition : A pegylated recombinant, engineered variant of cytokine interleukin-2 (IL-2; IL2)
where novel amino acid is encoded in the IL-2 gene that is leveraged for use in site-specific
pegylation, with potential immunostimulating activity. Upon administration of pegenzileukin,
the IL-2 variant moiety binds to dimers containing the IL-2 receptor beta and gamma
chains (IL2Rbg; IL2Rbetagamma) on immune cells, such as cytotoxic T-lymphocytes (CTLs)
and natural killer (NK) cells, thereby activating these cells and inducing their expansion.
It also induces the expression of certain cytotoxic cytokines, such as interferon-gamma
(IFNg) and transforming growth factor-beta (TGFb). The specific induction of T-cell-mediated
cytotoxic immune responses against tumor cells causes tumor cell destruction. The
addition of the novel amino acid and the concurrent pegylation prevents the binding
of the IL-2 moiety to the IL-2 receptor alpha chain (IL2Ra), thereby blocking the
IL2Ra-mediated activation of CD4-positive regulatory and immunosuppressive T-cells
(Tregs). Since it cannot bind to IL2Ra expressed on innate lymphoid cells in the vascular
endothelium, pegenzileukin prevents IL-2-mediated recruitment and activation of eosinophils,
and inhibits the induction of eosinophil-mediated vascular leak syndrome (VLS). Pegylation
also extends the half-life of pegenzileukin. Compared to recombinant IL-2, pegenzileukin
allows for increased IL-2Rbg binding and proliferation of CTLs without stimulating
the toxicity caused by binding to IL-2Ra.;
UNII : 10WR240QN7;
CAS number : 2573074-47-0; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 2573074-47-0
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G-SRS /a ;
Molecule name : THOR 707; THOR-707; SAR-444245; SAR 444245;
NCI Metathesaurus CUI : CL971032;
Origin ID : C162645;
UMLS CUI : C5706653;
Semantic type(s)
- chemical_or_drug_affects_gene_product
- chemical_or_drug_has_mechanism_of_action
- chemical_or_drug_has_physiologic_effect
- concept_is_in_subset
