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Pediatr Blood Cancer. 2014 May;61(5):922-4. doi: 10.1002/pbc.24800. Epub 2013 Oct 26.

Initial testing (stage 1) of the topoisomerase II inhibitor pixantrone, by the pediatric preclinical testing program.

Author information

1
Nationwide Children's Hospital, Columbus, Ohio.

Abstract

Pixantrone, a novel aza-anthracenedione with cytotoxic activity, was tested against the PPTP in vitro panel (3.0 nM to 30.0 μM) and against a limited panel of PPTP Wilms tumors and sarcomas (7.5 mg/kg) administered intravenously using an every 4 day × 3 schedule. In vitro pixantrone showed a median relative IC50 value of 54 nM (range <3 nM to 1.03 μM). In vivo pixantrone induced significant differences in EFS distribution compared to controls in two of eight solid tumor xenografts at dose levels relevant to human drug exposure. A complete response was observed for one Wilms tumor xenograft.

KEYWORDS:

developmental therapeutics; preclinical testing; topoisomerase 2 inhibitor

PMID:
24166988
PMCID:
PMC3951603
DOI:
10.1002/pbc.24800
[Indexed for MEDLINE]
Free PMC Article
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