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Development of novel agents for the treatment of renal fibrosis

Development of novel agents for the treatment of renal fibrosis
开发治疗肾纤维化的新型药物
批准号：
8917935
负责人：
Michael J. Caplan
金额：
$83.53万
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 2017-08-31
来源：
https://reporter.nih.gov/project-details/8917935
关键词：
AchievementAcuteAnimal ModelAreaBackBehaviorBiological AssayCYP2D6 geneCYP3A4 geneCaco-2 CellsCanis familiarisCell modelCharacteristicsChronic Kidney FailureClinicalDevelopmentDiabetic NephropathyDisease modelDoseDrug KineticsEnd stage renal failureEvaluationFeasibility StudiesFibrosisGoalsGrantHealthHumanIn VitroInhibitory Concentration 50KidneyLeadLettersLiver MicrosomesLysophosphatidic Acid ReceptorsMedicalMetabolicModelingMusOral AdministrationPermeabilityPharmaceutical PreparationsPharmacotherapyPhasePositioning AttributePreparationPropertyRattusRenal Replacement TherapyResearchSafetySelection CriteriaSeriesSignal PathwaySmall Business Innovation Research GrantStreptozocinTestingTherapeutic InterventionToxic effectUreteral obstructionanalogclinical efficacycommercializationimprovedin vivolead serieslipophilicitymeetingsmortalitynovelnovel therapeuticspre-clinicalpreclinical studypreventprogramssafety studyscale upsmall moleculestandard of caretherapy development

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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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