Pharmacologically Active Drug Metabolites: Impact on Drug Discovery and Pharmacotherapy

  title={Pharmacologically Active Drug Metabolites: Impact on Drug Discovery and Pharmacotherapy},
  author={R. Obach},
  journal={Pharmacological Reviews},
  pages={578 - 640}
  • R. Obach
  • Published 2013
  • Chemistry, Medicine
  • Pharmacological Reviews
  • Metabolism represents the most prevalent mechanism for drug clearance. Many drugs are converted to metabolites that can retain the intrinsic affinity of the parent drug for the pharmacological target. Drug metabolism redox reactions such as heteroatom dealkylations, hydroxylations, heteroatom oxygenations, reductions, and dehydrogenations can yield active metabolites, and in rare cases even conjugation reactions can yield an active metabolite. To understand the contribution of an active… CONTINUE READING
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