Initial testing (stage 1) of LCL161, a SMAC mimetic, by the pediatric preclinical testing program

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

Producción científica: Articlerevisión exhaustiva

74 Citas (Scopus)

Resumen

LCL161, a SMAC mimetic, was tested against the PPTP in vitro panel (1.0nM to 10.0μM) and the PPTP in vivo panels (30 or 75mg/kg [solid tumors] or 100mg/kg [ALL]) administered orally twice in a week. LCL161 showed a median relative IC 50 value of >10μM, being more potent against several leukemia and lymphoma lines. In vivo LCL161 induced significant differences in EFS distribution in approximately one-third of solid tumor xenografts (osteosarcoma and glioblastoma), but not in ALL xenografts. No objective tumor responses were observed. In vivo LCL161 demonstrated limited single agent activity against the pediatric preclinical models studied.

Idioma originalEnglish (US)
Páginas (desde-hasta)636-639
Número de páginas4
PublicaciónPediatric Blood and Cancer
Volumen58
N.º4
DOI
EstadoPublished - abr 2012
Publicado de forma externa

ASJC Scopus subject areas

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

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