Review Article

Hypoxia-Inducible Factor-1 as a Therapeutic Target in Endometrial Cancer Management

Table 1

Clinical trials on HIF-1α targeted therapies in endometrial cancer.

ClassInhibitorMechanismClinical trials in endometrial cancer

Small molecule inhibitors of HIF-1
Topoisomerase inhibitorTopotecan (topo-I)Inhibits hypoxic induction of HIF-1α protein and DNA binding activityMiller et al. [48] Triana et al. [49] Wadler et al. [50]
HSP90 inhibitorGeldanamycinInduces degradation of HIF-1α protein and inhibition of DNA binding of HIF-1
OtherPX-478Inhibition of HIF-1α transcription activity

Inhibitors of signal transduction pathways
mTOR inhibitorTemsirolimus (CCI-779)Downregulation of HIF-1α by inhibing mTorOza et al. [51]
Everolimus (RAD001)Slomovitz et al. [52]

Inhibitors of HIF-1 target genes
VEGF inhibitorBevacizumabMonoclonal antibody against VEGFAghajanian et al. [53]
CAIX inhibitorRencarex (WX G250)Monoclonal antibody against CAIX