Pharmaceutical profile

Wang B, editors. Pharmaceutical profiling in drug discovery for lead selection. Arlington, VA AAPS Press, 2004. p. 69-80. 

Kerns, E. H., Di, L., Pemsky, S., Kleintop, T., Huryn, D., McConnell, O., Carter, G. Pharmaceutical profiling method for lipophilidty and integrity using liquid chromatography-mass spectrometry. 

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. 

White, R.E., in Pharmaceutical Profiling in Drug Discovery for Lead Selection, Borchardt, R.T., Ed., 2004, American Association of Pharmaceutical Scientists Press, p. 431. 

Kerns, E.H. et al. 2004. Integrated high capacity solid phase extraction-MS/MS system for pharmaceutical profiling in drug discovery. J. Pharm. Biomed. Anal. 34 1. 

Weinstein K, Kardos P, Strab R, Hidalgo U (2004) Cultured epithelial cell assays used to estimate intestinal absorption potential. In Borchardt RT, Kerns EH, Lipinski CA, Thakker DR, Wang B (Eds) Biotechnology Pharmaceutical Aspects Vol I Pharmaceutical Profiling in Drug Discovery for Lead Selection. AAPS Press, Arlington, pp 197-216. 

Volume I Pharmaceutical Profiling in Drug Discovery for Lead Selection... 

High-throughput drug-like property profiling is increasingly used during lead identification and candidate selection. HTS pharmaceutical profiling may include ... 

Kerns, E.H. and Li, D., Pharmaceutical profiling in drug discovery, Drug Disc. Today, 8, 316, 2003. 

Predicting Bioavailability Pharmaceutical Profiling to Assess Absorption,... 

To further strengthen decision-making, it is helpful to use statistical clustering to place each experimental compound in the context of a database created from the pharmaceutical profiling of compounds with well-characterized human PK. In the absence of... 

A variety of in vitro assays are available to assess important parameters that impact bioavailability and these pharmaceutical profiling assays are commonly run to support drug discovery efforts. The major challenge is the interpretation of these results. Misinterpretation can lead to dropping promising compounds or alternatively taking... 

The authors thank Cheryl Wu for her contribution to the pharmaceutical profile part Marie-Christine Bodinier, Emmanuelle Guillaume, Philippe Dupuis, and Gervais Neliat for their contributions to Table 6.4 Catherine Moreau, Cecile Diet, and Loi c Dorgeret for technical assistance. 

During the early discovery phase, the primary function of stability studies is to determine the stability characteristics of the drug. Knowing these characteristics helps researchers select and design the most satisfactory chemical or molecular entity for the desired pharmaceutical profile and indication. The pharmaceutical profile focus on obtaining... 

Hamon V, Crawford M, Jean T. Pharmacological and pharmaceutical profiling New trends. In O Dormell, Smith (eds), The Process of New Drug Discovery and Development, 2nd ed, Taylor and Francis/CRC Press, 2006. 

Zopiclone is a chiral cyclopyrrolone with hypnotic properties, possessing a pharmaceutical profile of high efficacy and low toxicity, similar to that of benzodiazepines. Zopiclone has been commercialized as a racemic mixture however, the (S)-enantiomer is more active and less toxic than the (R)-enantiomer [11]. Although enzymatic hydrolysis of esters or transesteriflcation processes of alcohols have been widely applied for enzymatic resolution or desymmetrization... 

Since the first series of compounds were poorly soluble in water, the next crucial phase of the project set out to increase the water solubility of the drug candidates in order to increase absorption from the gastrointestinal tract. Further refinements led to a candidate that was not only well absorbed when administered orally to animals, but also had outstanding antimalarial profiles both in vitro and in vivo. In comparison to available semi-synthetic artemisinins, the drug candidate OZ 277 (Scheme 27) exhibits structural simplicity, an economically feasible and scalable synthesis, superior antimalarial activity and an improved pharmaceutical profile. The toxicological profiles are also acceptable and this drug candidate entered first into man studies during 2004. 

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