Maximizing Use of in Vitro ADMET Tools to Predict in Vivo Bioavailability and Safety

来源 :中国上海第七届国际新药发明科技年会 | 被引量 : 0次 | 上传用户:crazyasp
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
  The demands to reduce R&D costs in of new drugs and to improve the high attrition rate of drug candidates in development have shifted to early discovery phase the profiling activities to assess absorption,distribution metabolism,elimination and toxicity (ADMET) properties,along with the efficacy of drug candidates.Multiple predictive filters of ADMET properties (such as in silico,high-throughput in vitro and tailored mechanistic assays) are established in the various cascades of drug discovery and development process to flag and address the potential ADME and liability issues of new chemical entities (NCEs).An organization needs to establish a powerful landscape will lead to the most efficient and reliable prediction of in vivo ADMET matters in a timely and cost effective fashion.It is critical that,despite limited resource,increase in capacity should not be capitalized at the expense of deteriorated predictive power of the in vitro assays in early discovery.Meanwhile,collective utilization of those predictive tools will improve the productivity of drug discovery and development by prioritizing the drug-like NCEs,allowing candidates with poor drugability to be killed early and cheap.In this presentation,case studies will also be presented to demonstrate the impacts of those early in vitro predictive tools on the success of drug discovery projects.
其他文献
在大陆做成功的企业,不管是哪个行业,他们若能最快地了解中国文化,能够抓到重点,能够真正从心里认同一些差异性,最后能够创造出自己的特色,就能成功。相对来说,财务实力和专
通常一个人被雷电劈中的概率微乎其微,但美国南卡罗莱纳纠·158岁男子梅尔文·罗伯兹过去几十年来竟已经被雷电击中过5次。不可思议的是,6月27日,“霹雳哥”梅尔文竟在一场暴风
  A combined strategy based on the development of pharmacophore hypotheses and NMR approaches is reported for the identification of novel inhibitors of hepara
会议
  Calcium channel blockers (CCBs) have got potential therapeutic uses against several cardiovascular and non-cardiovascular diseases,such as angina,hypertensi
会议
刘蓓早就是大红大紫的影视明星了。《过把瘾》中的出镜使她获得第十二届大众电视金鹰奖最佳女配角奖:《甲方乙方》的上映让她赢得第十二届大众电影百花奖最佳女主角奖等等。在
  Peptides derived from the venoms of marine cone snails have attracted recent attention as potential therapeutic agents for the treatment of chronic pain.Alt
会议
地膜西瓜后期早衰的主要表现是,长势减弱,生长缓慢,上部叶片瘦小,叶色淡绿,叶片变薄,下部叶片变黄或褐,瓜重、品质下降和大面积减产。早衰的原因1、脱肥种西瓜一般基肥施的较
在移动A d hoc网络研究中,路由协议的研究一直都是学术界广泛关注的焦点,围绕A d hoc网络的路由协议,已经开展了大量的研究工作,具有成果性的协议主要有DSR,AODV,DSDV和TORA
  We are developing an alternative approach to siRNA,which may be designated as siDNA,small interfering DNA,by using hairpin-loop-structured DNA oligodeoxynuc
会议
近年来,随着城市绿化对草坪需求的增加,培育草坪已成为一条新的致富门路,市场前景看好。在沿海一些城市,草坪的覆盖率正以每年30%左右的速度递增。这些城市对草坪的需求旺盛,在绿化中