Abstract:
:Described in this article are strategies implemented to increase the throughput of in vivo rodent pharmacokinetic (PK) studies using the snapshot PK study design and automated methods for compound submission, sample processing, data analysis and reporting. Applying snapshot PK studies to categorize the oral exposure of >1300 discovery compounds as low, moderate or high resulted in an attrition rate of 86%. The follow up full PK studies on the remaining compounds found that 98% of the compounds were predicted in the correct (69%) or adjacent (29%) oral exposure category by the snapshot PK studies. These results demonstrate that the snapshot PK screen in rodents can serve as an effective and efficient in vivo tool in the compound selection process in drug discovery.
journal_name
Drug Discov Todayjournal_title
Drug discovery todayauthors
Liu B,Chang J,Gordon WP,Isbell J,Zhou Y,Tuntland Tdoi
10.1016/j.drudis.2007.10.014subject
Has Abstractpub_date
2008-04-01 00:00:00pages
360-7issue
7-8eissn
1359-6446issn
1878-5832pii
S1359-6446(07)00428-Xjournal_volume
13pub_type
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