Table 4.
Clinical perspectives (phases and trials) of some Mitochondria-targeted therapeutic strategies for cancer management
| Targeted functions | Molecular targets and the drugs used | Phase | ClinicalTrials.gov identifier/reference |
|---|---|---|---|
| TCA cycle | Glutaminase by CB839 | I | NCT02071927, NCT02071888 |
| Pyruvate dehydrogenase and α-ketoglutarate dehydrogenase by CPI613 | I | NCT02168140, NCT02232152 | |
| I/II | NCT01766219 | ||
| Mutant IDH2-R140 and IDH2-R172 by AG221 | I/II | NCT01915498, NCT02273739 | |
| Mutant IDH1/2 by AG881 | I/II | NCT02492737, NCT02481154 | |
| ETC | Complex I by carboxyamidotriazole | Preclinical | 257 |
| Complex I by fenofibrate | Preclinical | 258 | |
| Complex I by metformin | III | NCT01101438 | |
| Complex I by papaverin | I | NCT03824327 | |
| Complex II by lonidamine | II | NCT00237536 | |
| III | NCT00435448 | ||
| Complex III by atovaquone | Phase I | NCT02628080 | |
| Complex IV by arsenic trioxide | Preclinical | 259 | |
| Glycolysis | Mitochondria in cancer cells that would not use ketone bodies as a fuel by ketogenic diet | Pilot | NCT01535911 |
| Not applicable | NCT0307551, NCT0228616, NCT0175435, NCT03278249 | ||
| I | NCT00575146, NCT03451799, NCT01865162 | ||
| I/II | NCT02046187, NCT02939378 | ||
| II | NCT02302235 | ||
| Mitochondria-driven apoptosis | cytochrome c (cyt c) release by photodynamic therapy | I | NCT03053635 |
| II | NCT03945162 | ||
| cytochrome c (cyt c) release by curcumin | III | NCT02064673, | |
| II | NCT02944578, NCT02782949 | ||
| cytochrome c (cyt c) release by aloe-emodin | Preclinical | 260 | |
| cytochrome c (cyt c) release by betulin | Preclinical | 261 | |
| ROS signaling | Superoxide by mito-Tempo | Preclinical | 262 |
| Superoxide by MitoQ | Preclinical | 263 | |
| Fatty acid oxidation | Carnitine palmitoyl transferase I by etomoxir | Preclinical | 264 |
| Mitochondrial anaplerosis | GLUTs, HKs by 2-deoxy-D-glucose | I | NCT00096707 |
| III | 265 | ||
| HK2 and GAPDH by 3-bromopyruvate | Case study | 266 | |
| Mitochondrial turnover | DRP1 by Mdivi1/dynasore | Preclinical | 267 |
| Antioxidant modulators | cytochrome c (cyt c) release by resveratrol | I | NCT00256334, NCT00433576 |
| Mitochondrial destabilization | GSTP1-1 and GSTO1-1 by α-tocopheryl (α-TOS) succinate | Preclinical | 268 |
| DNA replication | Prodrug bioactivated by GSTP1-1 in an alkylating agent by canfosfamide (TLK286) | III | NCT00102973 |
| Pro-drug activated by GSTP and GSTM by brostallicin | II | NCT00060203, NCT01091454 |