CHAPTER 13: Hsp90 Inhibitors in Clinic
Published:23 Oct 2013
Hsp90 has been extensively studied as a viable oncogenic target since 1985, when it was first shown that targeting Hsp90 results in anti-neoplastic effects. Early clinical development was hindered by the fact that both geldanamycin and radicicol, the first biologically occurring compounds shown to inhibit Hsp90, were too toxic for use in the clinic. This limitation was overcome by the development of the first-generation geldanamycin-based compounds, which entered into clinic in 2003. Although, these first-generation compounds showed clinical limitation of use due to hepatotoxicity, development of newer Hsp90 inhibitors have shown early promise. Herein we will review the current landscape of Hsp90 inhibitors.