KAINATE RECEPTOR ANTAGONISTS TO TREAT NEUROPATHIC PAIN

ArnaX是Bearsden Bio，Inc.的一个部门，开发了新的化合物 选择性调节谷氨酸受体亚型， CNS疾病。在第一阶段，我们证明了SYM 2081，一种有效的， 红藻氨酸受体（KAR）的选择性拮抗剂，可以减少 在建立的动物模型中， 和慢性神经性疼痛。 已经确定SYM 2081对KAR的调制是可行的， 在体内治疗神经性疼痛，我们正在寻求第二阶段的资金， 开发SYM 2081或另一种KAR选择性拮抗剂作为先导 治疗这种情况的候选人。这种治疗剂将 满足自阿片类药物和氯胺酮以来尚未满足的巨大需求（通过持续 静脉输注）是唯一可用的化合物， 神经性疼痛 候选先导化合物的其他标准是：（a）体内t1/2>1.8小时 和（B）不产生耐受性。在确定了主要候选人之后， 我们将启动FDA要求的临床前研究。数据 在第二阶段项目期间收集的信息对于确保 额外的资金和/或企业合作伙伴，以商业化我们的 用于神经性疼痛的新治疗剂。 拟议的商业应用： 该项目的目标是将新化合物商业化， 选择性调节红藻氨酸受体的活性作为治疗剂 用于治疗损伤引起的疼痛、糖尿病性神经病变的药物，以及 其他神经系统疾病。

ArnaX, a division of Bearsden Bio, Inc., has developed novel compounds that selectively regulate glutamate receptor subtypes for treatment of CNS disorders. In Phase I, we demonstrated that SYM 2081, a potent and selective antagonist of the kainic acid receptor (KAR), can reduce sensitivity to painful stimuli in established animal models of both acute and chronic neuropathic pain at doses that do not impair motor activity. Having established that KAR modulation by SYM 2081 is feasible for treating neuropathic pain in vivo, we are seeking Phase II funding to develop SYM 2081, or another KAR-selective antagonist, as a lead candidate for treatment of this condition. Such a therapeutic agent would fulfill a tremendous unmet need since opiates and ketamine (by continuous i.v. infusion) are the only available compounds that can alleviate neuropathic pain. Additional criteria for a lead candidate are: (a) t1/2>1.8 hours in vivo and (b)no development of tolerance. Having identified a lead candidate, we will initiate the preclinical studies required by the FDA. Data collected during the Phase II project will be invaluable for securing the additional funding and/or a corporate partner for commercializing our novel therapeutic agent for neuropathic pain. PROPOSED COMMERCIAL APPLICATIONS: The goal of this project is to commercialize the novel compounds that selectively modulate activity of the kainate receptor as therapeutic agents for the treatment of pain due to injury, diabetic neuropathy, and other neurological disorders.