Development of an Oral Analgesic for Neuropathic Pain

慢性疼痛是一种使人衰弱的健康状况，目前可用的疗法治疗不足。那里 越来越需要开发替代品来治疗慢性疼痛，特别是糖尿病神经病变， 在全球范围内增加，50%的糖尿病患者发生疼痛性神经病变。最近， 脂质作为信号介质及其在伤害感受中的功能意义已被阐明。环氧脂肪 细胞色素P450产生的酸性代谢产物介导镇痛，我们合成了小分子 其代谢酶可溶性环氧化物水解酶（sEH）的抑制剂，以提高其体内水平。与 本研究旨在开发一种新型安全的口服sEH抑制剂，用于治疗周围神经病变 在糖尿病患者中。我们的候选药物EC 5026的临床前研究证明其疗效超过目前 治疗糖尿病神经病变。基于疗效、良好的PK/ADME特性和稳定性，EicOsis具有 选择EC 5026进入进一步的开发阶段。EicOsis将与蓝图开发团队合作， 制定开发计划并启动研究，以测试EC 5026在1期临床试验中的安全性。

Chronic pain is a debilitating health condition that is currently insufficiently treated by available therapies. There is a growing need to develop alternatives to treat chronic pain and specifically diabetic neuropathy as diabetes is increasing worldwide and painful neuropathy occurs in 50% of diabetic patients. Recently, the importance of lipids as signaling mediators and their functional significance in nociception has been elucidated. Epoxy-fatty acid metabolites generated by cytochrome P450s mediate analgesia, and we have synthesized small molecule inhibitors of their metabolizing enzyme, the soluble epoxide hydrolase (sEH), to elevate their levels in vivo. With this proposal, we aim to develop a novel and safe oral inhibitor of sEH for the treatment of peripheral neuropathy in diabetic patients. Preclinical studies with our candidate, EC5026, demonstrate efficacy that exceeds current therapies for diabetic neuropathy. Based on efficacy, good PK/ADME properties and stability, EicOsis has selected EC5026 to enter further development stages. EicOsis will work with Blueprint Development Teams to create a development plan and initiate studies to test the safety of EC5026 in Phase 1 clinical trials.