nlg802

NLG802 is an orally bioavailable prodrug of indoximod (a methylated tryptophan derivative) designed to enhance the pharmacokinetic exposure and efficacy of indoximod. Upon administration, it is rapidly converted to indoximod in vivo. Indoximod acts as an inhibitor of the enzyme indoleamine 2,3-dioxygenase 1 (IDO1), which catalyzes the conversion of tryptophan into kynurenine—a pathway that contributes to immunosuppression in the tumor microenvironment. By inhibiting IDO1 and increasing systemic tryptophan while reducing kynurenine levels, NLG802 restores immune cell proliferation and activation (including dendritic cells, NK cells, and T lymphocytes), reduces tumor-associated regulatory T-cells (Tregs), and may promote anti-tumor cytotoxic T-cell responses. Clinical studies have shown that NLG802 achieves higher plasma concentrations of active drug compared to direct administration of indoximod[2][6][7]. It has been evaluated primarily for advanced solid tumors including glioblastoma multiforme[5].

Other names

Indoximod Prodrug NLG802Ethyl leucyl-1-methyl-D-tryptophanateL-leucyl-N1-methyl-D-tryptophan ethyl esterL-leucyl-N-1-methyl-D-tryptophan ethyl esterL-leucyl-N 1-methyl-D-tryptophan ethyl ester