开发治疗肾纤维化的新型药物-猫眼课题宝

开发治疗肾纤维化的新型药物

批准号：

8780197

负责人：

ANIL K KARIHALOO

金额：

$61.63万

依托单位：

EPIGEN BIOSCIENCES, INC.

依托单位国家：

美国

项目类别：

财政年份：

2012

资助国家：

美国

项目状态：

已结题

起止时间：

2012-03-01 至 2016-08-31

来源：

https://reporter.nih.gov/project-details/8780197

关键词：

Achievement Acute Animal Model Area Back Behavior Biological Assay CYP2D6 gene CYP3A4 gene Caco-2 Cells Canis familiaris Cell model Characteristics Chronic Kidney Failure Clinical Development Diabetic Nephropathy Disease model Dose Drug Kinetics End stage renal failure Evaluation Feasibility Studies Fibrosis Goals Grant Human In Vitro Inhibitory Concentration 50 Kidney Lead Letters Liver Microsomes Lysophosphatidic Acid Receptors Medical Metabolic Modeling Mus Oral Administration Permeability Pharmaceutical Preparations Pharmacotherapy Phase Positioning Attribute Preparation Property Rattus Renal Replacement Therapy Research Safety Selection Criteria Series Signal Pathway Small Business Innovation Research Grant Streptozocin Testing Therapeutic Intervention Toxic effect Ureteral obstruction analog clinical efficacy commercialization improved in vivo lead series lipophilicity meetings mortality novel novel therapeutics pre-clinical preclinical study prevent programs public health relevance safety study scale up small molecule standard of care therapy development

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中文摘要

翻译

描述（由申请人提供）：我们项目的最终目标是开发有效治疗慢性肾脏疾病的新型疗法，这些慢性肾脏疾病通常会发展为纤维化，导致终末期肾脏疾病并需要肾脏替代治疗。该SBIR 2期应用建立在1期获得的结果的基础上，其中发现了新型和选择性小分子拮抗剂，可预防单侧输尿管梗阻中肾纤维化的进展 (UUO)动物模型将针对药物样和ADME特性对第1阶段确定的先导化合物进行优化。将评估符合选择标准的候选化合物的体内安全性，并在几种不同的慢性肾脏疾病动物模型中检查最佳化合物，以描绘临床环境中的发展路径。

英文摘要

DESCRIPTION (provided by applicant): The ultimate goal of our project is to develop novel therapeutics effective in chronic kidney diseases that normally develop fibrosis, lead to end stage renal disease and require renal replacement therapy. This SBIR phase 2 application builds on the results obtained in phase 1 where novel and selective small molecule antagonists were discovered that prevent the progression of renal fibrosis in a unilateral ureteral obstruction (UUO) animal model. Leads identified in phase 1 will be optimized for drug-like and ADME properties. Candidate compounds meeting the selection criteria will be assessed for safety in vivo and the best compound will be examined in several different animal models of chronic kidney disease to delineate a development path in the clinical setting.

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