동향
동향 내용
How to report and discuss ADME data in medicinal chemistry publications: in vitro data or in vivo extrapolations?
분류 ADME 조회 1592
발행년도 2015 등록일 2015-07-21
출처 J Pharm Sci (바로가기)
Early drug discovery projects often utilize data from ADME (absorption, distribution, metabolism, elimination) assays to benchmark data and guide discussion, rather than the predicted in vivo consequences of these data. Here, the two paradigms are compared, using evaluations of metabolic stability based on either microsomal clearance assay data or from the predicted in vivo hepatic clearance and half-life calculated through the combination of the venous well-stirred model and Øie-Tozer's model. The need for a shift in paradigm is presented, and its implications discussed. It is suggested that discussions about ADME data should revolve around potential clinical problems that are most likely to surface during the development phase, each benchmarked with a suitable variable derived from the assay data.

목록



[추천 메일 발송]
추천 메일 발송
받는 분 이메일 @
추천인
리스트 이전글과 다음글
이전글이전글 Drug Distribution to Human Tissues: Prediction and Examination of the Basic Assumption in In Vivo Pharmacokinetics-Pharmacodynamics (PK/PD) Research.
다음글다음글 The Affymetrix DMET Plus Platform Reveals Unique Distribution of ADME-Related Variants in Ethnic Arabs.