Initial testing of aplidin by the pediatric pre-clinical testing program.
Aplidin was tested in vitro at concentrations ranging from from 0.1 nM to 1.0 microM and in vivo at a dose of 0.6 mg/kg administered intraperitoneally on an every 4 days x 3-schedule that was repeated at day 21. In vitro, Aplidin was most active against acute lymphoblastic leukemia (ALL) cell lines. In vivo, Aplidin induced significant differences in EFS distribution in 12 of 28 (43%) solid tumor models and 2 of 6 evaluable ALL models. Aplidin showed potent in vitro activity and induced significant in vivo tumor growth inhibition in some xenografts, but did not induce tumor regressions.
Department of Molecular Pharmacology, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, USA.
Christopher L
CL
Morton
Peter J
PJ
Houghton
Richard
R
Gorlick
E Anders
EA
Kolb
Richard
R
Lock
Hernan
H
Carol
Stephen T
ST
Keir
C Patrick
CP
Reynolds
Min H
MH
Kang
John M
JM
Maris
Catherine
C
Billups
Malcolm A
MA
Smith
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D045744:Cell Line, Tumor; D047630:Depsipeptides / Q000494:pharmacology*; D005260:Female; D006801:Humans; D051379:Mice; D008807:Mice, Inbred BALB C; D016513:Mice, SCID; D010456:Peptides, Cyclic; D023041:Xenograft Model Antitumor Assays
D000970:Antineoplastic Agents; D047630:Depsipeptides; D010456:Peptides, Cyclic; C098980:plitidepsin