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Web:Biosynthesis of Drug Metabolites for Use in DMPK Experiments and Late-Stage Lead Diversification
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Web:Biosynthesis of Drug Metabolites for Use in DMPK Experiments and Late-Stage Lead Diversification

The ISSX Webinar Series is available to all current ISSX Members as a free membership benefit! Hosted by R. Scott Obach of Pfizer, Inc., this webinar, Biosynthesis of Metabolites for Use in Drug Metabolism Studies and Lead Diversification, will be offered at two different times on Wednesday, July 27, 2016. Select the time that works best for your schedule when you register.

7/27/2016
When: Wednesday, July 27, 2016
10:00 PM
Where: Webinar

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Biosynthesis of Metabolites for Use in Drug Metabolism Studies and Lead Diversification

First Session: 10:00 - 11:00 pm EDT

Authentic standards of drug metabolites are valuable reagents for carrying out experiments aimed toward understanding the disposition, efficacy, and safety of drugs.  However, obtaining metabolite standards by conventional organic synthesis can frequently be challenging, expensive, and they can take weeks to months to prepare.  In this webinar, laboratory procedures used to generate drug metabolites at nanomole scale will be described, and the application of quantitative NMR spectroscopy to determine the amount of product will be shared.  These are activities that can be carried out in most drug metabolism laboratories and require only a couple of days.  Metabolites obtained using these approaches can be used to test target activity, they can be used as authentic standards for quantitative bioanalysis of in vivo and in vitro samples by HPLC-MS, and they can also be used in other in vitro drug metabolism experiments (e.g. metabolism of the metabolite, plasma protein binding, etc).  Interestingly, this approach can be used to make new compounds (i.e. “lead diversification), to bolster the SAR knowledge of a particular target-ligand interaction, and these new compounds could even replace the lead compound as a potentially better drug candidate.  Finally, if time permits, we will share our procedure that leverages this biosynthetic procedure for the replacement of aliphatic hydrogen with fluorine, a frequently sought after modification that can block cytochrome P450 catalyzed  hydroxylation reactions and reduce drug clearance.

The objective of the webinar is that attendees should gain enough knowledge so as to be able to carry out these procedures in their own laboratories.  Using this procedure, it is possible that the next great new medicine could be ‘discovered’ in a drug metabolism laboratory.  

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