Initial testing (stage 1) of ganetespib, an Hsp90 inhibitor, by the pediatric preclinical testing program

Richard B. Lock, Hernan Carol, John M. Maris, Min H. Kang, C. Patrick Reynolds, E. Anders Kolb, Richard Gorlick, Stephen T. Keir, Catherine A. Billups, Raushan T. Kurmasheva, Peter J. Houghton, Malcolm A. Smith

Research output: Contribution to journalArticle

7 Scopus citations

Abstract

Ganetespib, an Hsp90 inhibitor, was tested against the PPTP in vitro cell line panel and selected xenografts in vivo, including JAK2- and BRAF-mutated models. Ganetespib demonstrated potent in vitro cytotoxic activity (median rIC50 8.8nM, range 4.4-27.1nM). In vivo, ganetespib induced significant differences in EFS distribution for 4 of 11 xenografts. Intermediate activity (EFS T/C>2) was noted only for the MV4;11 xenograft, and there were no objective responses. Administered as single agents, Hsp90 inhibitors examined by the PPTP have shown limited evidence for a therapeutic window against both solid tumor and leukemia pediatric preclinical models.

Original languageEnglish (US)
Pages (from-to)E42-E45
JournalPediatric Blood and Cancer
Volume60
Issue number7
DOIs
StatePublished - Jul 1 2013

Keywords

  • Developmental therapeutics
  • Hsp90 inhibitors
  • Preclinical testing

ASJC Scopus subject areas

  • Pediatrics, Perinatology, and Child Health
  • Hematology
  • Oncology

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    Lock, R. B., Carol, H., Maris, J. M., Kang, M. H., Reynolds, C. P., Kolb, E. A., Gorlick, R., Keir, S. T., Billups, C. A., Kurmasheva, R. T., Houghton, P. J., & Smith, M. A. (2013). Initial testing (stage 1) of ganetespib, an Hsp90 inhibitor, by the pediatric preclinical testing program. Pediatric Blood and Cancer, 60(7), E42-E45. https://doi.org/10.1002/pbc.24451