Table 1.
Select agents targeting amino acid metabolism that are developed, in trials or in the clinic, for the treatment of cancer.
Enzyme/ transporter | Inhibitor | Phase (status) | Cancer type |
---|---|---|---|
IDO1 |
BMS-986205 Navoximod (NLG-919) Pembrolizumab (in combination trial with epacadostat) PF-06840003 |
Phase I/II Phase I Phase II/III Phase II/III |
Advanced cancer, melanoma, NSCLC Solid tumors RCC, melanoma, head and neck, gastro, malignant solid tumor, NSCLC, neoplasma (Phase I) Oligodendroglioma, astrocytoma, malignant glioma |
IDO and TDO | HTI-1090 (dual inhibitor) | Phase I | Advanced solid tumors |
GLS |
CB-839 + cabozantinib CB-839 + talazoparib CB-839 + nivolumab CB-839 hydrochloride + osimertinib CB-839 + panitumumab, irinoteca hydrochloride CB-839 + azacytidine CB-839 + capecitabine CB-839 + palbociclib |
Phase II Phase Ib/II Phase I/II Phase I/II Phase I/II Phase I/II Phase I/II Phase Ib/II |
Renal cell carcinoma Solid tumors Melanoma, ccRCC, NSCLC Mutated stage iv NSCLC Metastatic and refractory RAS wildtype colorectal Advanced myelodysplastic syndrome Advanced solid tumors, colorectal cancer Solid tumors |
ASCT2 | V-9302 | In vivo mouse models and in vitro | |
xCT |
Sorafenib PRLX 93936 (erastin analog) |
In clinic Phase I |
Kidney, liver, and thyroid cancer Solid tumors |
PHGDH |
NCT-502 NCT-503 |
In vitro In vitro and mouse |
|
GOT/AST | Aspulvinone O | Mouse | |
LAT1 | JPH203 | In vitro |