TABLE 5.
Targeted therapies of HIF in cancer.
| Mechanism | Target | Agent | Preclinical | Clinical | Tumor Type |
|---|---|---|---|---|---|
| HIFα RNA expression | HIF1α | Antisense | + | − | Various |
| HIF2α | sh-RNA | + | − | Various | |
| HIF1α | ZnSO4 | + | − | Melanoma | |
| HIFα protein synthesis | HIF1α | Digoxin | + | − | Various |
| HIF2α | 2-ME | + | − | Various | |
| Topotecan | + | − | Various | ||
| HIFα stabilization | HIFα | HSP-90 inhibitor | + | + | BRC |
| mTOR | Everolimus | + | + | RCC | |
| Temsirolimus | + | + | BRC | ||
| Direct HIFα inhibitors | HIF1α | Acryflavine | + | − | Various |
| YC-1 | + | − | Various | ||
| HIF2α | PT2385 | + | + | Various | |
| HIF2α | MK6482 | + | + | VHL syndrome related tumors | |
| DNA binding | HRE | Echinomycin | + | − | Various |
BRC, breast cancer; HIF, hypoxia-inducible factor; HRE, HIF-responsive element; RCC, renal cell cancer; sh-RNA, short hairpin RNA; VHL, von-hippel lindau.
Grey shade: FDA approvals.