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

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

Research output: Contribution to journalArticle

11 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)1105-1112
Number of pages8
JournalInvestigational New Drugs
Volume32
Issue number6
DOIs
StatePublished - Dec 1 2014

Keywords

  • Carbonic anhydrase-I/-II
  • Celecoxib
  • CG100649
  • Colorectal cancer
  • COX-2
  • PGE<inf>2</inf>

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)
  • Oncology

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  • Cite this

    Kim, S. H., Margalit, O., Katoh, H., Wang, D., Wu, H., Xia, D., Holla, V. R., Yang, P., & Dubois, R. N. (2014). CG100649, a novel COX-2 inhibitor, inhibits colorectal adenoma and carcinoma growth in mouse models. Investigational New Drugs, 32(6), 1105-1112. https://doi.org/10.1007/s10637-014-0144-z