Table 1.

Compounds targeting cancer metabolomics: The table lists the most common and recent small molecules, compounds, anti-metabolites, and cytotoxins.

Compound	Target	Effect	Tumour Types Targeted
2-deoxyglucose	Hexokinase	Inhibits glycolysis	Advanced solid tumors (e.g., lung, breast, prostate, and gastric)
Lonidamine	Hexokinase	Inhibits glycolysis	Benign prostatic hyperplasia
3-bromopyruvate	Hexokinase	Inhibits glycolysis	N/A
TLN-232	Pyruvate kinase	Inhibits glycolysis	Metastatic melanoma and renal cell carcinoma
Dichloroacetate	PDK1	Reactivates PDH	Metastatic solid tumors, glioma, and GBM
Phenylacetate	Glutamine	Reduces plasma glutamine levels	Brain tumors (e.g., glioma, astrocytoma and medulloblastoma)
Asparaginase and Pegasparaginase	Asparagine	Reduces plasmaasparagine levels	ALL, TCL, and BCL
Arginine deiminase	Arginine	Reduces plasma asparagine levels	Metastatic melanoma and hepatocellular carcinoma
Acetazolamide, Indisulam and other sulfonamides	Carbonic anhydrases	pH regulation	Solid tumors (e.g., pancreatic, lung, melanoma and metastatic breast)
Cariporide	NHE1	pH regulation	N/A
SB-204990	ATP-citrate lyase	Inhibits fatty acid synthesis	N/A
Orlistat, GSK837149A, and C75	FASN	Inhibits fatty acid synthesis	N/A
Temsirolimus and Everolimus	mTORC1	Inhibits mTORC1	Solid tumors (both metastatic and non-metastatic)
Other rapalogues	mTORC1	Inhibits mTORC1	Solid tumors (e.g., pancreatic, endometrial and glioblastoma) and lymphoma
Torin1 and PP242	mTORC1 and mTORC2	Inhibits mTORC1 andmTORC2	N/A
PX-478	HIF1α	Inhibits HIF signaling	Advanced solid tumors and lymphoma
Acriflavine	HIF1α	Inhibits HIF signaling	N/A
Tirapazamine and other bioreductivecompounds	Hypoxia	Resensitizes cells to other treatments	Solid tumors (e.g., cervical, SCLC and NSCLC)
Bevacizumab and related compounds	Hypoxia, VEGF and VEGFR	Blocks angiogenesis	Solid tumors (e.g., malignant glioma, NSCLC, ovarian, and colorectal)
MK-0646, BIIB022, AVE1642, and others	IGF1R	Blocks IGF signaling	Solid tumors (e.g., NSCLC, pancreatic, hepatocellular carcinoma and metastatic breast)
BEZ235, XL765, SF1126, and BGT226	PI3K and mTOR	Inhibits signaling from PI3K andmTORC1 andmTORC2	Advanced solid tumors (e.g., malignant glioma and NSCLC)
GDC-0941 and PX866	PI3K	Inhibits PI3Ksignaling	Advanced solid tumors (metastatic breast and non-Hodgkin’s lymphoma)
Perifosine andGSK690693	AKT	Inhibits AKT	Solid tumors (e.g., renal cancer and NSCLC) and lymphoma
Metformin	AMPK andComplex I(mitochondrial)	Activates AMPK	Solid tumors and lymphoma
Antimetabolites (e.g., 5-FU, cytarabine andmethotrexate	Nucleotidebiosyntheticpathway	Inhibits cell proliferation	Many tumor types