Article Figures & Data
Figures
- Fig. 1.
The structure of CEP-701 and CEP-751.
- Fig. 2.
Long-term survival of rats bearing the R3327H rat prostatic cancer given p.o. BID dosing with 10 mg of CEP-701/kg/dose (n = 24) versus vehicle only (n = 18; P < 0.01 for all of the time points after 366 days for CEP-701 versus corresponding time point for vehicle group).
- Fig. 3.
A, RT-PCR analysis of trk A expression in the CWR-22Rv1 and TSU-Pr1 human prostate cancer cell lines and in the WI38 human fibroblast line. The WI38 cells were analyzed as a known negative control. B, Western blot analysis of the phosphorylation status of trk A receptor in vehicle-treated TSU-Pr1 human prostatic cancer cells versus cells treated in vitro for 24 h with 100 nm CEP-701.
- Fig. 4.
Response of the TSU-Pr1 human prostate cancers growing in nude mice treated 5 days a week BID with s.c. injections of either 10 mg of CEP-701/kg/dose or vehicle alone. (P < 0.01 for all time points of CEP-701 versus corresponding time points for vehicle group.)
- Fig. 5.
Response of the CWR-22Rv1 human prostate cancers growing in the nude mice treated continuously BID with s.c. injections of either 10 mg of CEP-701/kg/dose or vehicle. (P < 0.01 for all time points of CEP-701 versus corresponding time points for vehicle group.)
Tables
- Table 1
Effect of CEP-751 treatment on prostate cancer volume, proliferation, and death rate
Tumor type host Treatment (time) Cancer volumea Percentage of Cancer Cells Proliferation day Dying day AT-2 Rats Vehicle (10 days) 15.2 ± 1.1 49.3 ± 3.2 24.5 ± 1.8 CEP-751b (10 days) 6.1 ± 0.5c 57.6 ± 1.4 37.2 ± 4.1c LNCaP Nude mice Vehicle (21 days) 4.2 ± 0.3 23.4 ± 5.1 14.0 ± 2.1 CEP-751b (21 days) 1.7 ± 0.2c 25.2 ± 6.3 21.8 ± 2.5c -
a Cancer volume expressed as fold increase from initiation of treatment.
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b CEP-751 given s.c. at 10 mg/kg/dose. For AT-2, rats were given one dose/day; for LNCaP and TSU-pr1, nude mice were given two doses/day.
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c P < 0.01 versus vehicle control.
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- Table 2
Concentration of CEP-701 in blood plasma and H rat prostate cancer tissue in animals given two cycles of 10 mg p.o. of CEP-701/kg body weight BID for 5 days/week/cycle
Time after last oral dose, h CEP-701 concentration in Plasma (nm) H tumor (nm) 1 (n = 3) 4.5 ± 2.3 35.6 ± 6.6 2 (n = 3) 49.2 ± 30.0 26.6 ± 18.6 4 (n = 3) 6.8 ± 2.3 30.2 ± 15.0 8–12 (n = 5) <2 50.4 ± 39.7
Volume 7, Issue 8
