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Initial testing (stage 1) of the topoisomerase II inhibitor pixantrone, by the pediatric preclinical testing program
Author(s) -
Kurmasheva Raushan T.,
Reynolds C. Patrick,
Kang Min H.,
Allievi Cecilia,
Houghton Peter J.,
Smith Malcolm A.
Publication year - 2014
Publication title -
pediatric blood and cancer
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.116
H-Index - 105
eISSN - 1545-5017
pISSN - 1545-5009
DOI - 10.1002/pbc.24800
Subject(s) - medicine , wilms' tumor , in vivo , pharmacology , topoisomerase , ic50 , sarcoma , in vitro , pathology , biology , biochemistry , microbiology and biotechnology
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 IC 50 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. Pediatr Blood Cancer 2014;61:922–924. © 2013 Wiley Periodicals, Inc.