. Author manuscript; available in PMC: 2013 Dec 31.

Published in final edited form as: Nat Biotechnol. 2012 Jul 10;30(7):10.1038/nbt.2285. doi: 10.1038/nbt.2285

Table 1. Potential therapeutic compounds targeting metabolic enzymes of tumors.

Compound	Target	Tumor type/Cancer cell types	Clinical stages

Glucose metabolism

2-DG	Glucose transporter	Prostate cancer	Phase I (terminated)
Silybin/silibinin		Prostate cancer	Phase I/II

2-DG	HK2	Prostate cancer	Phase I (terminated)
Lonidamine			Phase I (Europe)

TLN-232/CAP-23	PKM2	Metastatic RCC, melanoma	Phase II

Gossypol/AT-101	LDHA	Multiple cancers	Phase I/II

Dichloroacetate (DCA)	PDK	Brain cancer	Phase I
		Non-small cell lung cancer (NSCLC)	Phase II
		Head and neck cancer

AZD3965	MCT1	Advanced solid tumors	Phase I/II

Nucleic acid metabolism

Methotrexate	Folate cycle (DHFR)	Multiple cancers	Registered
Pemetrexel

5-Fluorouracil	Thymidine synthesis (TYMS)	Multiple cancers	Registered

Hydroxyurea	Deoxynucleotide synthesis (Ribonucleotide reductase: RNR)	Multiple cancers	Registered

Gemcitabine, Fludarabine	Nucleotide incorporation (DNA polymerase/RNR)	Multiple cancers	Registered

Amino acid metabolism

L-Asparginase	Asparagine	Leukemia	Registered

Arginine deaminase (ADI-PEG conjugated)	Arginine	Multiple cancers	Phase II

NAD metabolism

FK866/APO866	Nicotinamide phosphoribosyl-transferase (NAMPT)	Cutaneous T cell lymphoma (CTCL), B-Cell Chronic Lymphocytic Leukemia(CLL), melanoma	Phase II
CHS828/GMX1777		Metastatic Melanoma, Solid Tumors, Lymphomas	Phase II