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01-12-2014 | PRECLINICAL STUDIES

CG100649, a novel COX-2 inhibitor, inhibits colorectal adenoma and carcinoma growth in mouse models

Authors: Sun-Hee Kim, Ofer Margalit, Hiroshi Katoh, Dingzhi Wang, Hong Wu, Dianren Xia, Vijaykumar R. Holla, Peiying Yang, Raymond N. DuBois

Published in: Investigational New Drugs | Issue 6/2014

Summary

Nonsteroidal anti-inflammatory drugs (NSAIDs) and selective cyclooxygenase-2 (COX-2) inhibitors (COXIBs) can reduce the risk of developing colorectal cancer (CRC) and are being considered for use as adjuvant therapy for treatment of CRC patients. However, long-term use of most NSAIDs, except aspirin, increases cardiovascular risk, hampering use of these drugs in CRC prevention and possibly for treatment. CG100649 is a new member of the COXIB family, which is proposed to inhibit both COX-2 and carbonic anhydrase-I/-II (CA-I/-II) activity. Using mouse models, we show here that CG100649 inhibits premalignant and malignant colorectal lesions in mouse models, partly through inhibiting tumor cell proliferation. These pre-clinical findings suggest a need for further exploration of CG100649 for CRC prevention and treatment. The long-term safety profile of CG100649, particularly regarding its effect on cardiovascular risk, is yet to be determined.

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Title: CG100649, a novel COX-2 inhibitor, inhibits colorectal adenoma and carcinoma growth in mouse models
Authors: Sun-Hee Kim
Ofer Margalit
Hiroshi Katoh
Dingzhi Wang
Hong Wu
Dianren Xia
Vijaykumar R. Holla
Peiying Yang
Raymond N. DuBois
Publication date: 01-12-2014
Publisher: Springer US
Published in: Investigational New Drugs / Issue 6/2014
Print ISSN: 0167-6997
Electronic ISSN: 1573-0646
DOI: https://doi.org/10.1007/s10637-014-0144-z

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