Table 2.

Drugs targeting amino acid metabolism therapy and their targets

Type	Target	Drug	Clinical phase	Ref
Amino acid degrading enzymes	Asparagine	ASNase	Clinical application	[72]
	Arginine	PEG-Arg I (BCT-100)	III	[132]
	Arginine	ADI-PEG20	III	[133]
	Cysteine	Cysteinase	Experimental	[134]
	Cysteine	Cysteinase-PEG	Experimental	[135]
	Cystine	Cystinase	Experimental	[136]
Amino acid transporter inhibitors	LAT1(SLC7A5)	LAT1-IN-1 (BCH)	Experimental	[137]
		JPH203	II	[138]
		SKN101	Experimental	[139]
	SLC1A5(ASCT2)	γ-L-glutamyl-p-nitroanilide (GPNA)	Experimental	[140]
		V-9302	Experimental	[141]
		Benzylserine (BenSer)	Experimental	[142]
	SLC6A14	α-methyltryptophan (α-MT)	Experimental	[143]
	SLC3A2	IGN523	I	ClinicalTrials.gov
	SLC7A11(xCT)	Sulfasalazine	I/II	ClinicalTrials.gov
Amino acid antagonists	Glutamine	6-diazo-5-oxo-L-norleucine (DON)	II	[144]
		JHU083	Experimental	[145]
Amino acid metabolic enzyme inhibitors	IDO	Indoximod (1-MT)	II	[146]
		NLG-802	I	ClinicalTrials.gov
		Epacadostat (INCB024360)	III	[147]
		NTRC 3883–0	Experimental	[148]
		BMS-986205	III	[149]
		KHK2455	I	ClinicalTrials.gov
		PCC0208009	Experimental	[150]
		PF-06840003	I	ClinicalTrials.gov
		GDC-0919	I	ClinicalTrials.gov
		MK-7162	I	ClinicalTrials.gov
		LY3381916	I	ClinicalTrials.gov
	IDO/TDO	Navoximod (NLG919)	I	[151]
		N-Benzyl/Aryl Substituted Tryptanthrin	Experimental	[152]
		pf06840003	I	ClinicalTrials.gov
		SHR9146	I	ClinicalTrials.gov
		DN1406131	I	ClinicalTrials.gov
		HTI-1090	I	ClinicalTrials.gov
	TDO	680C91	Experimental	[153]
		LM10	Experimental	[153]
	ARG	NOHA	Experimental	[154]
		nor NOHA	I	ClinicalTrials.gov
		CB-1158	I/II	ClinicalTrials.gov
	GLS	Telaglenastat (CB-839)	II	[155]
		BPTES	Experimental	[60]
		Glutaminase inhibitor 968	Experimental	[156]
	GDH	R162	Experimental	[157]
	PHGDH	CBR-5884	Experimental	[158]
		NCT-503	Experimental	[159]
Kyn/AhR pathway	Kyn	PEG-KYNase	Experimental	[160]
	AhR	IDB-AHRi	Experimental	[161]
		CH223191	Experimental	[162]

Abbreviations: IDO indoleamine 2, 3-dioxygenase, TDO tryptophan 2, 3-dioxygenase, ARG arginase, GLS glutaminase, GDH gutamate deaminase, PHGDH phosphate dehydrogenase, Kyn kynurenine, AhR aryl hydrocarbon receptor