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Annals of Oncology Advance Access published online on November 9, 2009

Annals of Oncology, doi:10.1093/annonc/mdp521
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© The Author 2009. Published by Oxford University Press on behalf of the European Society for Medical Oncology. All rights reserved. For permissions, please email: journals.permissions@oxfordjournals.org

A window of opportunity phase II study of enzastaurin in chemonaive patients with asymptomatic metastatic colorectal cancer

B. Glimelius1,2,*, M. Lahn3, S. Gawande3, A. Cleverly3, C. Darstein3, L. Musib3, Y. Liu4, K. L. Spindler5, J.-E. Frödin2, Å. Berglund1, P. Byström2, C. Qvortrup6, A. Jakobsen5 and P. Pfeiffer6

1 Department of Oncology, Radiology and Clinical Immunology, Uppsala University, Uppsala
2 Department of Oncology and Pathology, Karolinska Institutet, Stockholm, Sweden
3 Early Phase Oncology Clinical Investigation, Eli Lilly and Company, Indianapolis, IN
4 Department of Statistics, i3 Statprobe Inc., Austin, TX, USA
5 Department of Medical Oncology, Vejle Hospital, Vejle
6 Department of Medical Oncology, Odense University Hospital, Odense, Denmark

* Correspondence to: Dr B. Glimelius, Department of Oncology, Radiology and Clinical Immunology, University Hospital, Uppsala, SE-751 85 Uppsala, Sweden. Tel: +46-18-611-55-13; Fax: +46-18-611-10-27; E-mail: bengt.glimelius{at}onkologi.uu.se

Background: Preclinically, protein kinase C and AKT activation can be inhibited by enzastaurin and reduce tumor growth of colorectal cancer cells. In asymptomatic patients with metastatic colorectal cancer (mCRC), enzastaurin activity was evaluated by measuring the 6-month progression-free survival (PFS) rate in a window study design.

Patients and methods: Chemonaive patients with asymptomatic mCRC who did not require immediate chemotherapy-induced tumor reduction received a 400-mg thrice daily loading dose of enzastaurin on day 1 of cycle 1, followed by 500 mg once daily for the remaining 28-day cycles. Progression was assessed on the basis of radiographic imaging, rise in carcinoembryonic antigen or lactate dehydrogenase (LDH) levels or by appearance of clinical symptoms.

Results: Twenty-eight patients received daily enzastaurin. The 6-month PFS rate was 28% [95% confidence interval (CI) 13%–45%] and median PFS was 1.9 months (95% CI 1.8–4.5 months). Twelve (43%) patients had stable disease with a median duration of 6.1 months. The survival rate at 20 months was 77% (95% CI 47%–92%). No grade 4 toxicity was reported and grade 3 toxic effects were observed in three patients with one patient showing probable drug-related elevation of liver transaminases.

Conclusion: The window design in asymptomatic patients with mCRC can be safely applied to assess the activity and safety of novel cytostatic agents like enzastaurin.

asymptomatic, chemonaive, enzastaurin, metastatic colorectal cancer, window study

Received for publication March 26, 2009. Revision received October 12, 2009. Accepted for publication October 14, 2009.


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