Table 1.
Select agents targeting metabolism that are approved, or are in trials, for the treatment of cancer, focusing on targets discussed in this review.
| Drug | Target Enzyme |
|---|---|
| Methotrexate | Dihydrofolate reductase (DHFR) |
| Pemetrexed | DHFR Thymidylate synthase (TS) Glycinamide ribonucleotide formyltransferase (GARFT) |
| 6-Mercaptopurine 6-Thioguanine |
PRPP amidotransferase |
| Capecitabine 5-Fluorouracil |
Thymidylate synthase (TS) |
| Gemcitabine Cytarabine |
DNA polymerase/ribonucleotide reductase (RnR) |
| Leflunomide | Dihydroorotate dehydrogenase (DHODH) |
| CB-839 | Glutaminase (GLS) |
| PEG-BCT-100 (ADI-PEG20) AEB-1102 |
Depletion of circulating arginine |
| L-Asparaginase | Depletion of circulating asparagine |
| TVB-2640 | Fatty-acid synthase (FASN) |
| AG-120 (Ivosidenib) IDH305 BAY1436032 FT-2102 AG-221 (Enasidenib) AG-881 |
mutant IDH1 mutant IDH2 mutant IDH1/2 |
| AZD3965 | Monocarboxylate transporter 1 (MCT1) |
| CPI-613 | Pyruvate dehydrogenase (PDH)/α-ketoglutarate dehydrogenase |
| Metformin | Mitochondrial complex I |