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Wiley, Pediatric Blood & Cancer, 1(59), p. 185-188, 2011

DOI: 10.1002/pbc.23154

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Initial Testing (Stage 1) of AT13387, an HSP90 Inhibitor, by the Pediatric Preclinical Testing Program

Journal article published in 2011 by Min H. Kang, C. Patrick Reynolds ORCID, Peter J. Houghton, Denise Alexander, Christopher L. Morton, E. Anders Kolb, Richard Gorlick, Stephen T. Keir, Hernan Carol, Richard Lock, John M. Maris, Amy Wozniak, Malcolm A. Smith
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Abstract

AT13387, a non-geldanamycin inhibitor of heat-shock protein 90 (HSP90), was tested against the PPTP in vitro panel (1.0 nM to 10 μM) and against the PPTP in vivo panels (40 mg/kg or 60 mg/kg) administered orally twice weekly. In vitro AT13387 showed a median EC50 value of 41 nM and exhibited activity consistent with a cytotoxic effect. In vivo AT13387 induced significant differences in EFS distribution compared to controls in 17% evaluable solid tumor xenografts, but in none of the ALL xenografts. No objective tumor responses were observed. In vivo AT13387 demonstrated only modest single agent activity.