Preferred Label : Indoximod Prodrug NLG802;
NCIt synonyms : Indoleamine 2,3-Dioxygenase (IDO) Inhibitor; IDO1 Inhibitor NLG802;
NCIt related terms : ETHYL LEUCYL-1-METHYL-D-TRYPTOPHANATE;
NCIt definition : An orally bioavailable prodrug of indoximod, a methylated tryptophan, with immune
checkpoint inhibitory and antineoplastic activities. Upon oral administration, the
indoximod prodrug NLG802 is converted to indoximod. Indoximod targets, binds to and
inhibits the enzyme indoleamine 2,3-dioxygenase (IDO; IDO1), which converts the essential
amino acid tryptophan into the immunosuppressive metabolite kynurenine. By increasing
tryptophan levels and decreasing kynurenine levels, indoximod restores and promotes
the proliferation and activation of various immune cells, including dendritic cells
(DCs), natural killer (NK) cells, and T-lymphocytes, and causes a reduction in tumor-associated
regulatory T-cells (Tregs). Activation of the immune system, which is suppressed in
many cancers, may induce a cytotoxic T-lymphocyte (CTL) response against IDO1-expressing
tumor cells, thereby inhibiting their growth. IDO1, overexpressed by multiple tumor
cell types, plays an important role in immunosuppression. Tryptophan depletion inhibits
T-lymphocyte proliferation and activation, and subsequently suppresses the immune
system. NLG802 elicits increased plasma concentrations of indoximod and improves its
efficacy, compared to the direct administration of indoximod.;
UNII : NVJ85QZ036;
CAS number : 2071683-98-0;
Molecule name : NLG 802; NLG-802; NLG-1564;
NCI Metathesaurus CUI : CL552162;
Origin ID : C150393;
UMLS CUI : C4725696;
Semantic type(s)
concept_is_in_subset
has_target