Table 1

List of several potential anti-cancer metabolism compounds

CompoundPathway targetMechanism of actionStatusSource (if available)
2-DeoxyglucoseGlycolysisReversibly inhibiting hexokinaseOngoing clinical trials with promising initial data
3-BromopyruvateGlycolysisInhibiting hexokinase and other glycolytic enzymesPreclinical
PhloretinGlucose transportGlucose transporter Glut 1 and Glut 4Preclinical
LonidamineGlycolysisHexokinaseClinical trials
3POGlycolysisInhibiting activation of PFK1 by targeting PFKFB3
(phosphofructose kinase 2)
PreclinicalAdvanced Cancer
Therapeutics
BPTESGlutaminolysisInhibiting glutaminase 1, a glutaminolytic enzyme frequently upregulated in many tumorsPreclinical
968GlutaminolysisInhibiting glutaminase 1, a glutaminolytic enzyme frequently upregulated in many tumorsPreclinicalCornell University
IDH1/2 inhibitorsBlocking IDH1/2 altered functionSuppressing the function of mutant IDH1 and IDH2Agios
Pharmaceuticals
PKM2 inhibitorsGlycolysisInhibiting PKM2 function and reducing pyruvate synthesisAgios
Pharmaceuticals
PKM2 activatorsBiosynthesisActivating PKM2 to reduce glycolytic intermediates shunt to biosynthetic pathwaysAgios
Pharmaceuticals
DichloroacetateLactate productionBlocking PDK1 activity thereby increasing PDH1 function and facilitating pyruvate-to-acetyl coA reaction to fuel TCA cycle and mitochondrial respirationPhase I completed with promising results in glioblastoma multiforme patients
MetforminEnergy production pathwaysInhibiting mitochondrial complex I and lipid and protein synthesis, modulating glycolysis, decreasing glucose supply, insulin and insulin-like growth factor signaling availability for tumor cells
Ongoing clinical trials for cancer
FX11Lactate productionInhibiting function of Lactate Dehydrogenase A thereby blocking lactate production in cancerPreclinicalJohn Hopkins
University and
University of New
Mexico
AZD-3965Lactate transportBlocking MCT1 activity, thereby inhibiting lactate transportClinical trials Phase I ongoing in UKAstraZeneca
L-asparaginaseAsparagine and glutamine availabilityPromote asparagine and glutamine degradation, thereby cutting the supply of these amino acids for cancer cellsApproved for usage in leukemia. Effective therapy