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  • 02월 23일 15시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

Development of CG100649, a Next Generation NSAID

2009년 2월 16일 17시 05분 30초
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목 14시 : 30분
의약화학 - Drug Discovery for Prevention of Aging and Improvement in Quality of Life
저자 및
크리스탈지노믹스(주), Korea
Many NSAIDs are available for curing arthritic pain through the inhibition of cyclooxygenase-2 (COX-2). However, there is still a large unmet medical need for better antiinflammatory analgesics because adverse effects in the gastrointestinal (GI) track and cardiovascular (CV) system. Adverse effects on GI tract are believed to be due to inhibition of COX-1 that reduces the protective of prostaglandins on gastric and intestinal mucosa. On the other hand, adverse effects on the CV system may be caused by COX-2 inhibition that may result in thrombosis and vasoconstriction. We hypothesized that it may be possible to avoid GI and CV side effects by tissue-specific inhibition of COX-2. CG100649 is an orally available, small molecule that inhibits COX-2 tissue-specifically through dual inhibition of COX-2 and carbonic anhydrase (CA). Oral administration of CG100649 produces significant levels of free active drug in joints, synovial fluid which are devoid of CA activity, but it is sequestered in an inactive form in many other tissues because the drug is tightly bound to CA-I and CA-II, a known family of proteins that are prevalent in the blood and in sites of potential COX-2 toxicity. CG100649 is currently under development for rheumatoid arthritis, osteoarthritis (OA) and acute pain. Specifically, in the phase IIa clinical study carried in Europe with 248 OA patients, strong evidence for the superiority of CG100649 over placebo was provided and there were no withdrawals due to lack of efficacy. There were no serious adverse events, and no indication of a negative effect on heart function, ECG profiles and blood pressure. Moreover, no evidence of gastrointestinal bleeding was found in any group during this study. In this presentation, overall progress of the development of CG100649 will be discussed.