List of several potential anti-cancer metabolism compounds
| Compound | Pathway target | Mechanism of action | Status | Source (if available) | ||
|---|---|---|---|---|---|---|
| 2-Deoxyglucose | Glycolysis | Reversibly inhibiting hexokinase | Ongoing clinical trials with promising initial data | |||
| 3-Bromopyruvate | Glycolysis | Inhibiting hexokinase and other glycolytic enzymes | Preclinical | |||
| Phloretin | Glucose transport | Glucose transporter Glut 1 and Glut 4 | Preclinical | |||
| Lonidamine | Glycolysis | Hexokinase | Clinical trials | |||
| 3PO | Glycolysis | Inhibiting activation of PFK1 by targeting PFKFB3 (phosphofructose kinase 2) | Preclinical | Advanced Cancer Therapeutics | ||
| BPTES | Glutaminolysis | Inhibiting glutaminase 1, a glutaminolytic enzyme frequently upregulated in many tumors | Preclinical | |||
| 968 | Glutaminolysis | Inhibiting glutaminase 1, a glutaminolytic enzyme frequently upregulated in many tumors | Preclinical | Cornell University | ||
| IDH1/2 inhibitors | Blocking IDH1/2 altered function | Suppressing the function of mutant IDH1 and IDH2 | Agios Pharmaceuticals | |||
| PKM2 inhibitors | Glycolysis | Inhibiting PKM2 function and reducing pyruvate synthesis | Agios Pharmaceuticals | |||
| PKM2 activators | Biosynthesis | Activating PKM2 to reduce glycolytic intermediates shunt to biosynthetic pathways | Agios Pharmaceuticals | |||
| Dichloroacetate | Lactate production | Blocking PDK1 activity thereby increasing PDH1 function and facilitating pyruvate-to-acetyl coA reaction to fuel TCA cycle and mitochondrial respiration | Phase I completed with promising results in glioblastoma multiforme patients | |||
| Metformin | Energy production pathways | Inhibiting 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 | |||
| FX11 | Lactate production | Inhibiting function of Lactate Dehydrogenase A thereby blocking lactate production in cancer | Preclinical | John Hopkins University and University of New Mexico | ||
| AZD-3965 | Lactate transport | Blocking MCT1 activity, thereby inhibiting lactate transport | Clinical trials Phase I ongoing in UK | AstraZeneca | ||
| L-asparaginase | Asparagine and glutamine availability | Promote asparagine and glutamine degradation, thereby cutting the supply of these amino acids for cancer cells | Approved for usage in leukemia. Effective therapy | |||