Phase I, Randomized, Double-Blind, Placebo Controlled, Dose Escalation,Single Dose, Safety, Tolerance, and Pharmacokinetic Study of CXB909 in Healthy Male Volunteers

The primary objective of this dose escalation study is to examine the safety, tolerability, and pharmacokinetic properties of single-doses of CXB909, compared to placebo, in healthy male volunteers. This study may evaluate five (5) dose levels of CXB909; however, the number of dose levels, as well as the dosages, may be adjusted after evaluation of in-study analysis of the safety, tolerability, and pharmacokinetic data. This study will attempt to identify the maximum tolerated single dose of CXB909.

开始日期2012-12-01

申办/合作机构

CeNeRx BioPharma, Inc.

100 项与 CXB-909 相关的临床结果

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100 项与 CXB-909 相关的转化医学

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100 项与 CXB-909 相关的专利（医药）

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项与 CXB-909 相关的文献（医药）

2007-04-16·Neuroreport4区 · 医学

Wide spectrum modulation by KP-544 in models relevant for neuronal survival

4区 · 医学

Article

作者: Geist, Marie A. ; Volbracht, Christiane ; Podhorna, Jana ; Falsig, Jeppe ; Leist, Marcel

Reduced neurotrophic signalling has been proposed as a part of the pathophysiology behind neuronal death and dysfunction. The small molecule KP-544 was developed with the intention to enhance nerve growth factor signalling. To characterize the actions of KP-544 pharmacologically, we used four diverse models with relevance for neuronal function and survival. We found that 300-1000 nM KP-544 enhanced the neurite outgrowth in PC12 cells in response to a suboptimal concentration of nerve growth factor. KP-544 also protected the cerebellar granule cells from excitotoxicity apoptosis induced by the mitochondrial toxin methyl-phenyl-pyridinium, and modulated inflammation by inhibiting interleukin-6 production in primary astrocytes. Chronic treatment of rats with KP-544 prevented the hyper-responsiveness to amphetamine of animals treated with methylazoxymethanol acetate, a recently described neurodevelopmental model of schizophrenia.

2007-01-01·Restorative neurology and neuroscience

The novel substituted pyrimidine, KP544, reduces motor deficits in the R6/2 transgenic mouse model of Huntington's disease.

Article

作者: York, Lynae R ; Sandstrom, Michael I ; Myers, Rebecca A ; Lu, Ming ; Dey, Nicholas D ; Boersen, Angela J ; Dunbar, Gary L ; Bombard, Matthew C ; Hulce, Verne D ; Lescaudron, Laurent

PURPOSE:

The purpose of this study was to test the potential therapeutic effects of the substituted pyrimidine, KP544, which has been shown to amplify the effects of nerve growth factor in vitro, on motor deficits in the R6/2 transgenic mouse model of Huntington's disease (HD).

METHODS:

Young, female R6/2 mice were given daily oral intubation of either 10 mg/kg KP544 or vehicle (0.5% methylcellulose) at 6 weeks of age and tested from postnatal weeks 8 through 12 on a battery of motor tasks, including assessments of clasping (drawing of the limbs to the torso when suspended by the tail), motor coordination on the rotarod, and spontaneous motor activity in the open-field. Following testing, the mice were sacrificed and the brains were sectioned and stained with cresyl violet for histological examination.

RESULTS:

KP544 treatment decreased balance deficits on the rotarod task, reduced clasping, delayed the onset of hypoactivity, and reduced enlargement of the lateral ventricles in R6/2 mice.

CONCLUSION:

These results suggest that KP544 can reduce motor deficits and anatomical alterations in R6/2 mice. Further research into the use of KP544 as a potential pharmacotherapy HD is warranted.

100 项与 CXB-909 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
神经系统疾病	临床2期	-	CeNeRx BioPharma, Inc.	-
神经系统疾病	临床2期	-	Keryx Biopharmaceuticals, Inc.	-
神经系统疾病	临床2期	-	Krenitsky Pharmaceuticals, Inc.	-
阿尔茨海默症	临床前	美国	Keryx Biopharmaceuticals, Inc.	-