A novel approach to cancer therapy using PX-478 as a HIF-1α inhibitor

Arch Pharm Res. 2011 Oct;34(10):1583-5. doi: 10.1007/s12272-011-1021-3.


Hypoxia-inducible factor-1α (HIF-1α) is a transcription factor produced by tumor cells under hypoxic conditions, and a key regulator of a number of genes important in cancer biology. Over-expression of HIF-1α in human tumors is associated with poor prognosis and poor therapeutic outcomes and HIF-1α has been suggested as a novel target for cancer therapy. This article provides a review of PX-478 as the first novel HIF-1α inhibitor in clinical stage for the treatment of solid tumors.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Clinical Trials, Phase I as Topic
  • Humans
  • Hypoxia-Inducible Factor 1, alpha Subunit / antagonists & inhibitors*
  • Mustard Compounds / pharmacology*
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Phenylpropionates / pharmacology*


  • 2-amino-3-(4'-N,N-bis(2-chloroethyl)amino)phenylpropionic acid N-oxide
  • Antineoplastic Agents
  • HIF1A protein, human
  • Hypoxia-Inducible Factor 1, alpha Subunit
  • Mustard Compounds
  • Phenylpropionates