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. 2020 Jan 24;52(1):15–30. doi: 10.1038/s12276-020-0375-3

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