【摘 要】
:
One of the most critical drug evaluation systems is a pre-clinical evaluation for absorption, distribution, metabolism and elimination and toxicity (ADMET), which has been demonstrated to cause approx
【机 构】
:
President & CEO, Shanghai Medicilon Inc.China
【出 处】
:
2005 WHTS3rd Annual Congress of International Drug Discovery
论文部分内容阅读
One of the most critical drug evaluation systems is a pre-clinical evaluation for absorption, distribution, metabolism and elimination and toxicity (ADMET), which has been demonstrated to cause approximately over 40% new drug development failure.Pharmacokinetic criteria have to be considered as a clinical strategy to increase the accuracy when making decisions for go/no go.The ability to be administered by the oral route is a highly desirable property for new drugs because it is the safest, most convenient and economic method.Appropriate oral bioavailability is good as long as plasma drug levels can be reached the therapeutic concentrations.This characteristic is indeed a demand in drugs destined for the long-term treatment.Chemical structural criteria for selecting NCE (i.e Lipinski rule of 5) has been proposed and has been applied in drug development, however pharmacokinetic criteria has not been defined.There are several methods for predicting DMPK profiles including OraSpotterTM99, IDEA and GastroPlus.Application of GastroPlus in simulating GI absorption and pharmacokinetics for orally dosed drugs will be discussed.
其他文献
Flos Carthami, the dried flower petals of safflower, Carthamus tinctorius is an important crude drug in traditional Chinese medicine for promoting blood circulation and removing blood stasis, with the
The c-Jun N-terminal kinase (JNK), also called stress-activated protein kinase (SAPK), belongs to the mitogen-activated protein kinase (MAPK) superfamily.JNK plays a crucial role in cell proliferation
P.C.Kothary, A.Britton, N.Lewis, V.Patel, D.Rivers, and M.A.Del Monte, Department of Ophthalmology, University of Michigan Medical Center, Ann Arbor, MI Introduction: Insulin, the most common therapy
Today the number of unique chemical compounds available for screening on the commercial basis is about twenty millions.The number of potential pharmacological targets is quickly growing due to the ach
Osteoporosis is a bone disease most commonly found amongst the elderly females than in males.In the affected patients the amount of bone destruction is higher than its formation.This leads to bone los
Modulation of signaling pathways and gene expression is an important approach in the treatment of autoimmune and inflammatory disorders.This presentation will focus on the development of drugs that in
To develop new antibiotics, evaluation of their therapeutic effect using animal model is essential.Mice have been used for decades, however, the use of mice creates ethical and cost problems.To overco
Resistance of bacteria to antibiotics has become one of the main problems in human health.The discovery of new antibiotic families is a way to circumvent such problems and antimicrobial peptides may r
We have developed a technical platform composing a high density peptide array and a computer algorithms that can be used to screen, identify, and design peptides for specific targeting in a high throu
The presentation will be focused on application of advanced in vitro technologies, especially in vitro models based on human and animal tissues, and strategies into new discovery and development of ne