Alvaro-Gracia J M
Servico de Reumatologia, Hospital de la Princesa, Madrid, Spain.
Rheumatology (Oxford). 2004 Feb;43 Suppl 1:i21-5. doi: 10.1093/rheumatology/keh105.
Licofelone, a competitive inhibitor of 5-lipoxygenase, cyclooxygenase (COX)-1 and COX-2, is currently in clinical development for the treatment of osteoarthritis (OA). Licofelone decreases the production of proinflammatory leukotrienes and prostaglandins-which are involved in the pathophysiology of OA and in gastrointestinal (GI) damage induced by NSAIDs-and has the potential to combine good analgesic and anti-inflammatory effects with excellent GI tolerability. Initial endoscopy data in healthy volunteers have demonstrated that licofelone is well tolerated and has a GI safety profile similar to placebo and significantly better than naproxen. These tolerability results were confirmed in patients with OA in two separate randomized studies. Furthermore, a long-term study (52 weeks) has shown that licofelone is at least as effective as naproxen in the treatment of OA. Licofelone also appears to be as effective as the selective COX-2 inhibitor celecoxib in the treatment of the signs and symptoms of OA. Licofelone has a GI safety profile similar to that of celecoxib, but may offer the advantage of fewer incidences or worsening of peripheral oedema. Preliminary data have also shown that licofelone coadministration with low-dose aspirin does not lead to increased GI toxicity. The emerging clinical data for licofelone indicate that it is an effective and well-tolerated therapy that could offer safety advantages over current treatment options, and that it could be suitable for the long-term treatment of a broad spectrum of patients with OA.
利考非洛，一种5-脂氧合酶、环氧化酶（COX）-1和COX-2的竞争性抑制剂，目前正处于治疗骨关节炎（OA）的临床开发阶段。利考非洛可减少促炎白三烯和前列腺素的产生，这些物质参与OA的病理生理过程以及非甾体抗炎药（NSAIDs）引起的胃肠道（GI）损伤，并且有可能将良好的镇痛和抗炎作用与出色的胃肠道耐受性相结合。健康志愿者的初始内镜检查数据表明，利考非洛耐受性良好，其胃肠道安全性与安慰剂相似，且显著优于萘普生。在两项独立的随机研究中，OA患者的这些耐受性结果得到了证实。此外，一项长期研究（52周）表明，利考非洛在治疗OA方面至少与萘普生一样有效。利考非洛在治疗OA的体征和症状方面似乎也与选择性COX-2抑制剂塞来昔布一样有效。利考非洛的胃肠道安全性与塞来昔布相似，但可能具有外周水肿发生率更低或病情恶化更少的优势。初步数据还表明，利考非洛与低剂量阿司匹林联合使用不会导致胃肠道毒性增加。利考非洛新出现的临床数据表明，它是一种有效且耐受性良好的治疗方法，与目前的治疗选择相比可能具有安全性优势，并且可能适用于广泛的OA患者的长期治疗。
