Initial testing (stage 1) of LCL161, a SMAC mimetic, by the Pediatric Preclinical Testing Program.

Journal Article (Journal Article)

LCL161, a SMAC mimetic, was tested against the PPTP in vitro panel (1.0 nM to 10.0 µM) and the PPTP in vivo panels (30 or 75 mg/kg [solid tumors] or 100 mg/kg [ALL]) administered orally twice in a week. LCL161 showed a median relative IC(50) value of >10 µM, 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.

Full Text

Duke Authors

Cited Authors

  • Houghton, PJ; Kang, MH; Reynolds, CP; Morton, CL; Kolb, EA; Gorlick, R; Keir, ST; Carol, H; Lock, R; Maris, JM; Billups, CA; Smith, MA

Published Date

  • April 2012

Published In

Volume / Issue

  • 58 / 4

Start / End Page

  • 636 - 639

PubMed ID

  • 21681929

Pubmed Central ID

  • PMC3253328

Electronic International Standard Serial Number (EISSN)

  • 1545-5017

Digital Object Identifier (DOI)

  • 10.1002/pbc.23167


  • eng

Conference Location

  • United States