NRTS AS THERAPEUTICS FOR INFLAMMATORY BOWEL DISEASE

描述（改编自应用程序）：治疗和预防 炎症性肠病（IBD）的衰弱症状代表了一种主要的 未满足的医疗需求本提案旨在支持第II阶段研究， 培养Centaur的主要IBD候选人。在第一阶段赠款期间， 优化了先导候选物CPI-1189的化学结构， 以改善其在IBD的体内大鼠模型中的功效特征， 维持其高口服生物利用度和药代动力学（PK）特征。 从这些研究中，开发了一种新的先导化合物C203;该化合物 其功效是CPI-1189的两倍。在目前的第二阶段 应用，额外的功效和机制研究，建议开发 纳入C203美国IND的药理学包。还计划 原料药生产以及中试安全性和PK研究，以支持28天GLP C203在大鼠和犬中的毒性研究。这些活动都将 支持IND申请。目前的建议是对以前的一项建议的修订。 申请第二阶段资助。 拟议商业应用：不可用

DESCRIPTION (Adapted from the application): The treatment and prevention of the debilitating symptoms of inflammatory bowel disease (IBD) represents a major unmet medical need. This proposal is for support of Phase II studies to further develop Centaur's lead IBD candidate. During the period of the Phase I grant the chemical structure of the lead candidate, CPI-1189 was optimized in order to improve its efficacy characteristics in an in vivo rat model of IBD while maintaining its high oral bioavailability and pharmacokinetic (PK) profile. From these studies a new lead compound, C203, was developed; this compound appears to have twice the efficacy of CPI-1189. In the present Phase II application, additional efficacy and mechanism studies are proposed to develop a pharmacology package for inclusion in a US IND for C203. Also planned are bulk drug production, and pilot safety and PK studies to support 28-day GLP toxicity studies with C203 in the rat and dog. These activities will all support an IND filing. The present proposal is a revision of a previous application for Phase II funding. PROPOSED COMMERCIAL APPLICATION: NOT AVAILABLE