Table 1 Select agents targeting amino acid metabolism that are developed, in trials or in the clinic, for the treatment of cancer.

From: Amino acids in 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