KAINATE RECEPTOR ANTAGONISTS TO TREAT NEUROPATHIC PAIN

Bearsden Bio，Inc.的一个部门Arna X已经开发出新的化合物 选择性调节谷氨酸受体亚型用于治疗 中枢神经系统紊乱。在第一阶段，我们演示了SYM 2081，一种强大的 红藻氨酸受体(KAR)的选择性拮抗剂，可以减少 建立的两种急性心肌梗死动物模型对疼痛刺激的敏感性 慢性神经性疼痛的剂量不会损害运动能力。 已确定在SYM 2081之前对KAR进行调制 治疗活体神经性疼痛，我们正在寻求第二阶段资金 开发SYM 2081或另一种KAR选择性拮抗剂，作为领先 治疗这种疾病的候选人。这样的治疗剂将会 满足巨大的未得到满足的需求，因为鸦片类药物和氯胺酮(通过不断 静脉注射。输液)是唯一可用的化合物 神经性疼痛。 候选领先者的其他标准是：(A)体内T1/2&>1.8小时 以及(B)没有形成容忍。在确定了领先的候选人后， 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资金将对确保 其他资金和/或企业合作伙伴将我们的产品商业化 治疗神经病理性疼痛的新型治疗剂。 建议的商业应用： 该项目的目标是将新型化合物商业化 选择性调节红藻氨酸受体的活性作为治疗 用于治疗因损伤引起的疼痛、糖尿病神经病变和 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.