Book description
The goal of this book is to improve the readers' knowledge of
metabolite elucidation in drug metabolism by exposing them to in depth
coverage of the biotransformation of xenobiotics, strategies for
identifying and characterizing metabolites, FDA guidelines, and case
studies on how to improve the decision-making process in structural
modification of drug candidates to reduce toxicity.
The book consists of 8 chapters; it first provides an introduction on
biotransformation of xenobiotics, and then presents modern approaches
and strategies for dealing with metabolite characterization, using
tools such as LC-MS, H-D exchange, stable isotopes LC-MS-NMR, and
radiolabeled compounds. Also, strategies for dealing with reactive
intermediates in drug discovery and development are presented as well
as case studies on improving the decision-making process in the
structural modification of drug candidates. The last chapter discusses
the regulatory perspectives of safety testing of drug metabolites and
why, how, and when to test their safety.
ALA F. NASSAR, PHD, has worked in the
pharmaceutical industry for more than ten years. For over five years,
Dr. Nassar oversaw the drug metabolism and bioanalytical department at
Vion Pharmaceuticals, working in these key areas of drug discovery and
development. One principal area of his research involved understanding
how structure modification can improve the ADME profile for new
chemical entities as they advance toward clinical candidacy. He
identified and subsequently patented pharmacologically active
metabolites of Nexavar (sorafenib), and recently identified the
pharmacologically active metabolite of Onrigin (laromustine), and is
in the process of seeking a patent on this discovery. Dr. Nassar has
more than fifty publications in journal articles and book chapters;
and has taught and coordinated several courses on bioanalytical
chemistry, LC-MS, and drug metabolism to share his experience with
other scientists in the field. Currently, he is the Director of the
Mass Spectrometry Facility and Research Assistant Professor at
Brandeis University.
