Candidate screening

Automated online SPE systems have been applied to various phases of drug discovery. McLoughlin et al. (1997) utilized the Prospekt system in pharmacokinetic animal studies for rapid drug candidate screening. Up to 10 compounds were simultaneously monitored. The lower limits of detection were... 

Zhang, H., Pan, Y Affinity ultrafiltration of DNA topoisomerases-targeted compounds determined with HPLC/ESI-MS for drug candidate screening. J. Zhqiang Univ. Sci. 2004, 5, 900-905. 

The job analysis provides useful information for both employees and managers. For managers, information from the job analysis is used in writing job descriptions, interviewing job candidates, screening candidates, and setting performance criteria. For employees, information from the job analysis tells employees how work is to be done and the outcomes expected. 

Drug discovery Lead candidate Screening Protein identification natural products identification metabolic stability profiles molecular weight determination for combinatorial/ medicinal chemistry support. 

Fortunately, robot-based drug candidate screening systems represent a success story for time-to-market and labour- and time-saving reasons, these systems are making a comeback in this specific pharmaceutical field. 

Analytical documentation requirements during the life cycle of a pharmaceutical product—from initial candidate screening and selection, through entry into humans/IND, to NDA and postapproval marketed product support—are discussed in this book. Most of the information is based on US FDA and ICFF guidelines EU requirements are not substantially different. 

This chapter describes analytical documentation needs during the life cycle of a pharmaceutical product—from initial candidate screening and selection,... 

The primary goal during candidate screening is to rank a large number of compounds based on efficacy in animal models, biopharmaceutical properties (such as solubility and permeability in caco-2 cells), preliminary pharmacokinetic profile in animals, and potential for metabolic and toxicity liability. A non-good laboratory practice (GLP) Ames test may be performed to screen for potential mutagenicity. 

The analysis of a molecule with one site of action is a good indicator for the LD50, such as in phenacyl alcohol derivatives. Steroids, however, are complex molecules, and their metabolites contribute to the experimentally measured LD50 values. If the toxicity can be related to superoxide, the measurement of chemiluminescence intensity can be used for a drug candidate screening. Further studies of the substituent effect of steroids are required before LD50 values can be estimated from computational chemical calculations. 

Case Study 1 Drug Candidate-Induced Direct Acinar Cell Toxicity In Vivo with Confirmation of Toxicity and Drug Candidate Screening In Vitro... 

Dmg discovery Lead candidate Screening 1- PiDtein identification 2- Metabolic stability profiles 3- Molecular weight determination for medicinal chemistry support... 

Table 13.4 Liquid Hydrogen Bubble Point Pressure Computed at the Normal Boiling Point for Candidate Screens for the Fuel Depot...

Usually, one or two compounds are selected from the candidate screening and evaluated further in at least one rodent and one nonrodent species for gross toxicity (i.e., 1-2 weeks dosing). 

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