2006
DOI: 10.1200/jco.2005.05.3447
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Abstract: On the basis of plasma exposures and safety data, enzastaurin 525 mg once daily is the recommended phase II dose. Enzastaurin is well tolerated up to 700 mg/d. Evidence of early activity was seen with significant stable disease.

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Cited by 172 publications
(176 citation statements)
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“…On the basis of phase 1 and 2 studies, QTc prolongation occurs in 12% of treated patients. No reports about arrhythmia have been published, but careful use is recommended with periodic monitoring of ECGs 110, 111, 112, 113, 114…”
Section: Resultsmentioning
confidence: 99%
“…On the basis of phase 1 and 2 studies, QTc prolongation occurs in 12% of treated patients. No reports about arrhythmia have been published, but careful use is recommended with periodic monitoring of ECGs 110, 111, 112, 113, 114…”
Section: Resultsmentioning
confidence: 99%
“…28 The drug is orally available with minimal toxicity and to date has been tested in several solid and hematological malignancies. 29 Leukemic cells from CLL patients were exposed to increasing PKC-bII in ZAP-70-positive CLL C Meyer zum Büschenfelde et al doses of Enzastaurin for 24 h. As determined by Annexin-V/ phosphatidyl-inositol staining and by measuring the mitochondrial membrane potential delta-c, Enzastaurin killed leukemic cells in a dose-dependent manner with significant induction of apoptosis evident at a dose of 5 mM (Figure 6a). The proapoptotic effect of Enzastaurin was evident in ZAP-70-positive cells, although not exclusive in this subgroup (data not shown).…”
Section: The Pkc-b-specific Inhibitor Enzastaurin Kills B-cll Cells Amentioning
confidence: 99%
“…As the CI method recommends a ratio of concentrations at which drugs are equipotent, the following combination studies were performed using fixed ratios with IC 50 values calculated from the previous cytotoxicity analysis for the different drug treatments in each cell line (i.e., 1 : 50 and 1 : 450 in A549 and SW1573 cells, respectively). However, as enzastaurin is administered orally (Carducci et al, 2006) and reaches a relatively stable plasma concentration for a prolonged time, we also used enzastaurin at a fixed IC 25 concentration in simultaneous combination in both cell lines and in the sequential combination in the less sensitive SW1573 cells. Figure 1A and B.…”
Section: Growth Inhibition Studies Of Pemetrexed and Enzastaurinmentioning
confidence: 99%