Vitro Drug Screening

Alternative approaches that feature in vitro methodologies for drug screening have been incorporated into drug development schemes. Due to the wealth of samples resulting from high-throughput events 

Summary of the data obtained for 30 compounds screened using the CARRS assay  

Source Reprinted with permission from Korfmacher et al., 2001. Copyright 2001 John Wiley Sons. a Dose PO lOmg/kg in the rat. 

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In vitro drug screening Metabolic stability Membrane permeability Drug-drug interaction Automated metabolite identification Ackerman et al., 1998 Caldwell et al., 1998 Bu et al., 2000 Ayrton et al., 1998a Lopez et al., 1998... 

Holbeck SL. Update on NCI in vitro drug screen utilities. Eur J Cancer 2004 40 785-93. 

H.F. Cui, J.S. Ye, Y. Chen, S.C. Chong and F.S. Sheu, Microelectrode array biochip Tool for in vitro drug screening based on the detection of a drag effect on dopamine release from pcl2 cells. Analytical Chemistry, 78(18), 6347-6355 (2006). 

To date, a typical drug development flow contains pre-clinical, clinical and postmarketing phases [ ]./ vitro drug screening (bench test) and drug delivery test (currently, mostly animal test) are the two most important pre-clinical phase steps [1, 2]. Those steps aims to select the drugs most likely to work in humans via... 

Valko, K., Reynolds, D. P. High-throughput physicochemical and in vitro ADMET screening a role in pharmaceutical profiling. Am. J. Drug Deliv. 2005, 3, 83-100. 

Astashkina, A., Mann, B. Grainger, D. W. A critical evaluation of in vitro cell culture models for high-throughput drug screening and toxicity. Pharmacol. Ther. 134, 82-106 (2012). 

Trubetskoy, O.V., Gibson, J.R., and Marks, B.D. 2005. Highly miniaturized formats for in vitro drug metabolism assays using vivid fluorescent substrates and recombinant human cytochrome P450 enzymes. J. Biomol. Screen. 10 56. 

LC/MS/MS with selected reaction monitoring (SRM) offers a fast and simple means to analyze biological matrices, which is a key factor in high-throughput CYP inhibition screens using liver microsomes. Potentially, the LC/MS/MS technique is suitable for analyses of cocktail substrates in other in vitro drug metabolism evaluations such as CYP induction/activation assays, rapid analysis of pooled liver microsomes, rapid reaction phenotyping of tissue (hepatic and extrahepatic) samples, as well as evaluation of hepatocytes/tissue slice CYP activity. ° ... 

Hsu, S. et al. A mechanism-based in vitro anticancer drug screening approach for phenolic phytochemicals. Assay Drug Dev Technol. 1, 611, 2003. 

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