Friday 12 September 2014
Drug metabolism is
also noted as xenobiotic metabolism is
the biochemical modification of pharmaceutical substances or xenobiotics
respectively by living organisms, usually through unique enzymatic
systems. The increasing
costs and time associated with bringing latest medicines to the market have
developed a need for a fresh paradigm for decreasing the attrition rates of
drug candidates in both preclinical and clinical upbringing stages.
Early
appraisal of drug metabolism and pharmacokinetic (DMPK)
parameters is lately possible due to several higher throughput in vitro and in
vivo screens. This information of DMPK properties should not only lessen the
timelines for the selection of drug candidates but also increase the
probability of their success for development.
The role
of DMPK researchers in the drug research paradigm should not be limited to
screening a great array of compounds during the lead optimization process but
should involve a strive for an understanding of the engagement,
circulation, metabolism, excretion, and possible drug-related toxicities of a
chemical series.
A
specific DMPK research screening paradigm narrates a case study using the
Thrombin Receptor Adversary program. This screening paradigm followed by the
extensive lead optimization process culminated in the selection of SCH 530348,
a potent, careful and orally active thrombin receptor antagonist for the
treatment of thrombosis.
For a complete list, click on Bentham Science Publishers’ Journals Impacting Science
