Initial testing (stage 1) of eribulin, a novel tubulin binding agent, by the pediatric preclinical testing program.

ABSTRACT:

Background

Antimitotic agents are essential components for curative therapy of pediatric acute leukemias and many solid tumors. Eribulin is a novel agent that differs from both Vinca alkaloids and taxanes in its mode of binding to tubulin polymers.

Procedures

Eribulin was tested against the PPTP in vitro cell line panel at concentrations from 0.1 nM to 1.0 μM and against the PPTP in vivo xenograft panels at a dose of 1 mg/kg (solid tumors) or 1.5 mg/kg (ALL models) using a q4dx3 schedule repeated at Day 21.

Results

In vitro eribulin demonstrated cytotoxic activity, with a median relative IC50 value of 0.27 nM, (range <0.1-14.8 nM). Eribulin was well tolerated in vivo, and all 43 xenograft models were considered evaluable for efficacy. Eribulin induced significant diff

SUBMITTER: Kolb EA 

PROVIDER: S-EPMC4263960 | biostudies-literature | 2013 Aug

REPOSITORIES: biostudies-literature