Table 1.
Selected agents that target tumour metabolism that are either approved or in clinical trials
| Drug | Target | Metabolic pathway | Development phase |
|---|---|---|---|
| Methotrexate | Dihydrofolate reductase | Nucleotide metabolism | Approved cytotoxic chemotherapy agent |
| 5-Fluorouracil | Thymidylate synthase | Nucleotide metabolism | Approved cytotoxic chemotherapy agent |
| Gemcitabine | DNA polymerases | Nucleotide metabolism | Approved cytotoxic chemotherapy agent |
| Metformin | Mitochondrial complex I | OXPHOS | Under investigation for repurposing |
| Phenformin | Mitochondrial complex I | OXPHOS | Under investigation for repurposing |
| Atovaquone | Mitochondrial complex III | OXPHOS | Under investigation for repurposing |
| IM156 | Mitochondrial complex I | OXPHOS | Phase 1 trials |
| IACS-10759 | Mitochondrial complex I | OXPHOS | Phase 1 trials |
| Ivosidenib | Mutant IDH1 | TCA cycle metabolism | Approved for acute myeloid leukaemia |
| Enasidenib | Mutant IDH2 | TCA cycle metabolism | Approved for acute myeloid leukaemia |
| AG-881 | Mutant IDH1/2 | TCA cycle metabolism | Phase 3 trials |
| FT-2102 | Mutant IDH1 | TCA cycle metabolism | Phase 2 trials |
| Devimistat | Pyruvate dehydrogenase/α-ketoglutarate dehydrogenase | TCA cycle metabolism | Phase 3 trials |
| CPI-613 | PDK-1 | TCA cycle metabolism | Phase 2 trials |
| CB-839 | Glutaminase | Glutamine metabolism | Phase 2 trials |
| INCB001158 | Arginase inhibitor: maintains arginine levels | Arginine metabolism | Phase 2 trials with checkpoint immunotherapy |
| Pegzilarginase | Arginine catabolism: depletes arginine levels | Arginine metabolism | Phase 1 trials |
| PEG-BCT-100 | Arginine catabolism: depletes arginine levels | Arginine metabolism | Phase 1/2 trials |
| L-asparginase | Asparagine catabolism: depletes asparagine levels | Asparagine metabolism | Approved |
| AZD3965 | Monocarboxylate transporter 1 | Lactate metabolism | Phase 1 trials |
| TVB-2640 | Fatty acid synthase | Lipid metabolism | Phase 2 trials |