L-Nucleosides as Chemotherapeutic Agents

  • Giuseppe Gumina
  • Youhoon Chong
  • Chung K. Chu
Part of the Cancer Drug Discovery and Development book series (CDD&D)


Nucleoside analogs have been a major class of chemotherapeutic agents. Currently, more than 30 commercially available antiviral and antitumor nucleosides and nucleoside analogs are available. Among nucleoside analogs, nonnatural L-enantiomers have been particularly interesting. The most notable example is lamivudine, which has been playing an important role in the treatment of human immunodeficiency virus and hepatitis B virus infections. The reason for their high therapeutic potential is that, when biologically active, L-nucleosides have proven to possess favorable toxicological, chemical, and biochemical profiles, such as potency, low toxicity, and high metabolic stability. These characteristics have been the key factors in their success as drugs. Currently, two L-nucleosides, lamivudine and emtricitabine, are available for the treatment of human immunodeficiency virus and hepatitis B virus infections, and several other analogs, such as clevudine and troxacitabine, are in advanced clinical trial development stages. Among these, troxacitabine, a true chain terminator, is the first L-nucleoside endowed with promising antitumor activity against leukemia as well as solid tumors. This chapter reviews the important L-nucleosides used in therapy as well as compounds in development.

Key Words

Anticancer agents antiviral agents deoxycytidine kinase L-nucleosides troxacitabine. 


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Copyright information

© Humana Press Inc., Totowa, NJ 2006

Authors and Affiliations

  • Giuseppe Gumina
    • 1
  • Youhoon Chong
    • 2
  • Chung K. Chu
    • 3
  1. 1.Department of Pharmaceutical SciencesMedical University of South CarolinaCharleston
  2. 2.Department of Pharmaceutical and Biomedical SciencesCollege of Pharmacy, University of GeorgiaAthens
  3. 3.Department of Pharmaceutical and Biomedical SciencesCollege of Pharmacy, University of GeorgiaAthens

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