Table 1.
Compound | Molecular Target | Trial Target and Phase | Trial ID (NCT) | Reference and Comment |
---|---|---|---|---|
Indoximod (1-methyl-D-tryptophan; NLG-8919) |
IDO1 activity inhibition; stimulates mTORC to modulate downstream transduction; promotes kynurenate formation | Metastatic breast cancer Phase 2 |
NCT02913430 | NLG-802 is a prodrug for this, which entered Phase 1 in 2020 |
Indoximod (1-methyl-D-tryptophan) |
As above | Glioblastoma Phase 2 |
NCT04049669 | |
Indoximod (1-methyl-D-tryptophan) |
As above | Metastatic prostate cancer; Phase 2 |
NCT01560923 | [224] Combination with sipuleucel-T yielded radiological and clinical improvement |
Indoximod (1-methyl-D-tryptophan) |
As above | Metastatic pancreatic cancer; Phase 2 |
NCT02077881 | [225] |
Indoximod (1-methyl-D-tryptophan) |
As above | Metastatic breast cancer; Phase 2 |
NCT01792050 | [226] No improvement compared with taxane |
Epacadostat INCB024360 |
IDO1 inhibitor. IC50 = 93 nM in direct enzyme assay; IC50 = 12.5 nM in HeLa cell-based assay |
Prostate cancer; Phase 1 and 2 |
NCT 03493945 | [227,228] |
Epacadostat INCB024360 |
As above | Gliomas; Phase 2 |
NCT03532295 | |
Epacadostat INCB024360 |
As above | Endometrial cancer; Phase 2 |
NCT04463771 | |
Epacadostat INCB024360 |
As above | Head and neck cancer; Phase 2 | NCT03463161 |