Initial testing (stage 1) of lapatinib by the pediatric preclinical testing program.

ABSTRACT:

Background

Lapatinib is a small molecule reversible tyrosine kinase inhibitor of EGFR and ErbB2 that shows in vitro and in vivo activity against a range of EGFR and ErbB2-dependent adult cancer cell lines and that has clinical efficacy against ErbB2-overexpressing breast cancer.

Methods

Lapatinib was tested against the cell lines of the PPTP in vitro panel at concentrations ranging from 1.0 nM to 10.0 microM. Lapatinib was tested against the xenografts of the PPTP in vivo panels using a twice-daily oral administration schedule for 6 weeks (5 days on, 2 days off) at a dose of 160 mg/kg (320 mg/kg/day). Lapatinib pharmacokinetic parameters were determined in scid(-/-) mice.

Results

The median IC(50) value for lapatinib against the entire PPTP cell line panel was 6.84 mi

SUBMITTER: Gorlick R 

PROVIDER: S-EPMC2731000 | biostudies-literature | 2009 Oct

REPOSITORIES: biostudies-literature