Daily Archives: October 3, 2012

Can In Vitro Metabolism-Dependent Covalent Binding Data Distinguish Hepatotoxic from Nonhepatotoxic Drugs? An Analysis Using Human Hepatocytes and Liver S-9 Fraction by scientists from Pfizer on CRT 2009

Bauman, J. N., et al. Chem. Res. Toxicol., 2009, 22 (2), pp 332–340 An examination on whether or not that hepatotoxic drugs can be distinguished from nonhepatotoxic ones based on in vitro covalent binding data carried out by researcher from Pfizer.

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Can In Vitro Metabolism-Dependent Covalent Binding Data in Liver Microsomes Distinguish Hepatotoxic from Nonhepatotoxic Drugs? An Analysis of 18 Drugs with Consideration of Intrinsic Clearance and Daily Dose by R. Scott Obach et al on CRT 2008

Obach, R. S., et al. Chem. Res. Toxicol., 2008, 21 (9), pp 1814–1822 A study on assessment of correlation of the amount of covalent binding formation and hepato-toxicity performed by scientists from Pfizer.

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Managing the Challenge of Chemically Reactive Metabolites in Drug Development by scientists from industry on Nat. Rev. Drug Disc. 2011

Park, B. K., et al. Nat. Rev. Drug Discov. 10, 292-306 (April 2011) | doi:10.1038/nrd3408 A review on reactive metabolites from an industry perspective.

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Mechanism-Based Inactivation (MBI) of Cytochrome P450 Enzymes: Structure−Activity Relationships and Discovery Strategies To Mitigate Drug−Drug Interaction Risks by scientists from Pfizer on JMC 2012

 Orr, S. T. M., et al. J. Med. Chem., 2012, 55 (11), pp 4896–4933 A recent review on MBI of cytochrome P450: SAR and mitigating DDI.

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Improving Drug Candidates by Design: A Focus on Physico-chemical Properties As a Means of Improving Compound Disposition and Safety by Nicholas A. Meanwell on CRT 2011

Meanwell, N., Chem. Res. Toxicol., 2011, 24 (9), pp 1420–1456 A review on improving compound disposition and safety by optimizing the physico-chemical properties.

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Mitigating Heterocycle Metabolism in Drug Discovery by scientists from Amgen on JMC 2012

St. Jean Jr., D. J.; Fotsch, C., J. Med. Chem., 2012, 55 (13), pp 6002–6020 A review on how medicinal chemists deal with heterocycle metabolism in drug discovery on JMC 2012.

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Biotransformation Reactions of Five-Membered Aromatic Heterocyclic Rings by scientists from Pfizer on CRT 2002

Dalvie, D. K., et al. Chem. Res. Toxicol., 2002, 15 (3), pp 269–299 A review on biotransformation reactions of five-membered aromatic heterocyclic rings by Deepak K. Dalvie et al on CRT 2002.

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A Comprehensive Listing of Bioactivation Pathways of Organic Functional Groups by scientists from Pfizer on Curr. Drug Metab. 2005

Kalgulkar, A. S., et al. Curr. Drug Metab. 2005, 6(3), pp 161-225 A classic review on bioactivation pathways of organic functional groups by Amit S. Kalgutkar et al on Curr. Drug Metab. 2005.

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Structural Alert/Reactive Metabolite Concept as Applied in Medicinal Chemistry to Mitigate the Risk of Idiosyncratic Drug Toxicity: A Perspective Based on the Critical Examination of Trends in the Top 200 Drugs Marketed in the United States by scientists from Pfizer and Merck on CRT 2011

Stepan, A. F., et al. Chem. Res. Toxicol., 2011, 24 (9), pp 1345–1410 A collection of structural alert/reactive metabolite based on examination of top 200 drugs marketed in the United States.

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Cytochrome P450 and Chemical Toxicology by F. Peter Guengerich on CRT 2008

Guengerich, F. P., Chem. Res. Toxicol., 2008, 21 (1), pp 70–83 A nice review on cytochrome P450 and chemical toxicology by F. Peter Guengerich in 2008 on CRT.

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