Table 1.
Clinical trials of drugs that target various steps of the glycolytic and mitochondrial metabolic pathways.
| Drug | Pathway | Disease | Trial Status | Identifier # |
|---|---|---|---|---|
| Silibinin | glycolysis (glut1) | liver cancer | phase I | NCT01129570 |
| prostate cancer | phase II | NCT02146118 | ||
| hypertension | phase IV | NCT03538327 | ||
| RO7070179 | HIF1α | Hepatocellular carcinoma | Phase I | NCT02564614 |
| lonidamine | glycolysis (HK) | enlarged prostate | phase III | NCT00435448 |
| 2-DG | glycolysis (HK) | advanced solid tumor | phase I | NCT00096707 |
| prostate cancer | phase I/II | NCT00633087 | ||
| PFK-158 | glycolysis (PFKFB3) | advanced solid tumors | phase I | NCT02044861 |
| TLN-232 | glycolysis (PKM2) | melanoma | phase II | NCT00735332 |
| renal cell carcinoma | NCT00422786 | |||
| AZD3965 | lactate uptake (MCT 1) | advanced solid tumor | phase I | NCT01791595 |
| Indisulam | H+ secretion | gastric cancer | phase I/II | NCT00165594 |
| kidney cancer | phase II | NCT00059735 | ||
| Dichloroacetate | PDK1 | head and neck cancer | phase I | NCT01163487 |
| breast, lung cancer | phase II | NCT01029925 | ||
| CPI-613 | aKGDH | small cell lung cancer | phase I | NCT01931787 |
| lymphoma, leukemia | phase II | NCT03793140 | ||
| AG-120 | isocitrate DH | advanced solid tumor | phase I | NCT02073994 |
| leukemia | phase II | NCT03503409 | ||
| cholangiocarcinoma | phase III | NCT02989857 | ||
| AG-221 | isocitrate DH | leukemia | phase I | NCT03728335 |
| leukemia | phase II | NCT03744390 | ||
| advanced solid tumor | phase I/II | NCT02273739 | ||
| AG-881 | isocitrate DH | glioma | phase I | NCT02481154 |
| metformin | Mitochondrial complex I |
RA | phase I/II | NCT03686657 |
| prostate cancer | phase II | NCT03137186 | ||
| SLE | phase IV | NCT02741960 | ||
| arsenic trioxide | Mitochondrial complex III |
leukemia | phase II | NCT03624270 |
glut1, glucose transporter 1; HK, hexokinase; PFKFB3, 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3; MCT1, monocarboxylate transporter 1; MCT4, monocarboxylate transporter 4; PDK1, pyruvate dehydrogenase kinase 1; α-KGDH, alpha-ketoglutarate dehydrogenase; isocitrate DH, isocitrate dehydrogenase.