Table 1.
Therapeutics targeting the Warburg effect in cancers
| Process | Target | Compound | Effect | Status | References |
|---|---|---|---|---|---|
| Glucose transport | GLUT1 | WZB117, STF-31 | Inhibits GLUT1 | Preclinical | [102, 154] |
| Glycolysis | HK | 2DG | Inhibits HK | Clinical trials discontinued | [156] NCT00633087 NCT00096707 NCT00247403 |
| PKM2 | TEPP-46 | Activates PKM2 and inhibits PPP | Preclinical | [157, 158] | |
| LDHA | FX11 | Inhibits LDHA | Preclinical | [159] | |
| PPP | G6PD | 6-AN | Induces oxidative stress | Preclinical | [160] |
| Lactate transport | MCT1 | AZD3965 | Inhibits uptake of extracellular lactate | Phase I | [161] NCT01791595 |
| Mitochondrial function | PDK1 | DCA | Inhibits PDK1 | Phase I-II | [162, 163] NCT00566410 NCT01111097 NCT00540176 |
| AKT signaling pathway | AKT | AZD5363 | Inhibits AKT activity | Phase I-II | [164] NCT01895946 NCT01353781 NCT01692262 NCT02077569 NCT01226316 |
| GDC0068 | Phase I | [165] NCT01090960 |
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| GSK2141795 | Phase I completed | [166] NCT00920257 NCT01266954 |
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| GSK2110183 | Phase I–II completed Phase II | [166] NCT00881946 NCT01531894 |
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| MK-2206 | Phase I-II | [167] NCT01283035 NCT01277757 NCT01253447 NCT01231919 NCT01604772 NCT01258998 NCT01307631 NCT01349933 NCT01481129 NCT01802320 NCT01260701 NCT01425879 NCT01319539 NCT01226316 |