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Drug Metab Rev. 2021 Aug;53(3):384-433. doi: 10.1080/03602532.2021.1916028. Epub 2021 Jun 24.

Novel advances in biotransformation and bioactivation research - 2020 year in review.

Drug metabolism reviews

S Cyrus Khojasteh, Upendra A Argikar, James P Driscoll, Carley J S Heck, Lloyd King, Klarissa D Jackson, Wenying Jian, Amit S Kalgutkar, Grover P Miller, Valerie Kramlinger, Ivonne M C M Rietjens, Aaron M Teitelbaum, Kai Wang, Cong Wei

Affiliations

  1. Department of Drug Metabolism and Pharmacokinetics, Genentech, Inc., South San Francisco, CA, USA.
  2. Translational Medicine, Novartis Institutes for Biomedical Research, Inc., Cambridge, MA, USA.
  3. Department of Drug Metabolism and Pharmacokinetics, MyoKardia, Inc., South San Francisco, CA, USA.
  4. Medicine Design, Pfizer Worldwide Research, Development and Medical, Groton, CT, USA.
  5. Department of DMPK, UCB Biopharma, Slough, UK.
  6. Division of Pharmacotherapy and Experimental Therapeutics, UNC Eshelman School of Pharmacy, Chapel Hill, NC, USA.
  7. Drug Metabolism and Pharmacokinetics, Janssen Research & Development, Spring House, PA, USA.
  8. Medicine Design, Pfizer Worldwide Research, Development and Medical, Cambridge, MA, USA.
  9. Department of Biochemistry and Molecular Biology, University of Arkansas for Medical Sciences, Little Rock, Arkansas, USA.
  10. Division of Toxicology, Wageningen University, Wageningen, The Netherlands.
  11. Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, CT, USA.
  12. Drug Metabolism and Pharmacokinetics, Janssen Research & Development, San Diego, CA, USA.
  13. Drug Metabolism & Pharmacokinetics, Biogen Inc., Cambridge, MA, USA.

PMID: 33910427 DOI: 10.1080/03602532.2021.1916028

Abstract

This annual review is the sixth of its kind since 2016 (see references). Our objective is to explore and share articles which we deem influential and significant in the field of biotransformation and bioactivation. These fields are constantly evolving with new molecular structures and discoveries of corresponding pathways for metabolism that impact relevant drug development with respect to efficacy and safety. Based on the selected articles, we created three sections: (1) drug design, (2) metabolites and drug metabolizing enzymes, and (3) bioactivation and safety (Table 1). Unlike in years past, more biotransformation experts have joined and contributed to this effort while striving to maintain a balance of authors from academic and industry settings.[Table: see text].

Keywords: Drug metabolism; bioactivation; biotransformation; nonp450 enzymes; p450 enzymes

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