Monday, April 22, 2013

Introducing the new MetaboLyte™ Production Platform From Screening To Optimizate Production of Metabolites from Drug Candidates

United States Biological and HepatoChem™ have teamed up to offer a revolutionary way to screen, optimize, and produce metabolites from drug candidates. 

HepatoChem™ technology exploits an optimized panel of catalytic chemical reaction conditions in a multi-well parallel format which, by its diversity, mimics the suite of cytochrome P450 enzymes (CYP) present in human hepatocytes, offering the researcher a unique, synthetic chemical liver.
Exciting New Technology Speeds Up Metabolite Study
  • Produce drug metabolites in days, not months.
  • Exclusive process produces large quantities of metabolites.
  • Rapid, inexpensive scale up for NMR and in vitro testing.
  • Eliminate complex and costly synthetic chemistries.

 

Hepatochem™ Technology

Our innovative approach is based on a diverse set of chemical conditions that mimics the main reactions occurring during drug metabolism. This panel is used to quickly find reaction conditions that generate specific drug metabolites. This HepatoChem™ approach, basically a chemical liver, is analogous to the panel of cytochromes P450 present in the human liver, but with the advantage of the scalability of chemistry. When a reaction condition is identified, it is optimized and scaled up to produce mg to g quantities of metabolites.

HepatoChem™ developed a series of biomimetic panels. These panels are using several kinds of catalysts, including metalloporphyrins, which gives access to a unique set of reaction conditions. This series of easy-to-use kits is suitable for the preparation of metabolites for MSMS and NMR.

 

Applications


Research Stage
Structure elucidation of drug metabolites allows faster metabolic stability optimization and also provides an opportunity to identify unique analogues.

Pre-Clinical Stage
Biological profiling and toxicology studies of lead compound metabolites are critical to improve the quality of the pipeline and reduce attrition rates. Significantly, the FDA published a guidance on safety studies of metabolites in 2008. Guidance for industry, Safety testing of drug metabolites, FDA, February 2008.

Clinical Stage
Quantification studies necessitate access to pure samples of metabolites. Metabolite IP permits full protection of related, marketed drugs.

Key Benefits
  • Direct synthesis of Metabolites from parent drug
  • Authentication with biological reference samples
  • Rapid optimization in hours Milligram to gram scale

Common Biotransformation Reactions
  • Aliphatic Hydroxylation
  • N-Dealkylation
  • O-Dealkyation
  • Cleavage
  • N-Oxidation
  • S-Oxidation
  • Rearrangement Formylation
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