Current technologies are designed to identify metabolites but are unable to produce testable quantities of metabolites. Consequently, metabolite studies are delayed in the drug discovery process. Having access to milligram quantities of drug metabolite permits resolution of many of the fundamental questions surrounding small molecule metabolism, including:
Our biomimetic technology will speed up metabolite studies and allow rapid improvement of metabolic properties of drug candidates. Additionally, outsourcing metabolite production will save chemistry resources usually allocated to metabolite synthesis and analytical resources allocated to structure elucidation.
Metabolic stability improvement:
With access to exact structures of metabolites, medicinal chemists can find rapid ways to improve low metabolic stability. One strategy consists of blocking sites of oxidative metabolism with fluorine.
Zetia (Merck) $596 million in 2007
J.W. Clader, J. Med. Chem. 2004, 47, 1-9
Active metabolites and patent protection:
Active metabolites can offer valuable opportunities for new drug discovery and better protection of your IP drugs.
The Clarinex, a metabolite of Claritin, generated $722 million in 2006 while OTC Claritin totaled $356 million that year.
Zyrtec sales were approximately $1.4 billion in 2007 .