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Prodrugs pp 1163-1171 | Cite as

Case Study: Amifostine: (Ethyol®)

  • Roger A. Rajewski
Part of the Biotechnology: Pharmaceutical Aspects book series (PHARMASP, volume V)

Abstract

Amifostine is a prodrug of its free thiol, active metabolite, WR-1065. The thiophosphate promoiety protects the free thiol group of WR-1065 from oxidation to the symmetrical disulfide, WR-33278, while providing a handle for high levels of WR-1065 production at the target tissue. The thiophosphate promoiety of amifostine is cleaved by alkaline phosphatase to produce WR-1065, which accumulates in non-cancerous tissues to a greater extent than in cancerous tissues (Capizzi, 1996).

Keywords

Radiat Oncol Biol Phys Product Insert Mixed Disulphide Thiophosphoric Acid Radiation Oncology Biol Phys 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© American Association of Pharmaceutical Scientists 2007

Authors and Affiliations

  • Roger A. Rajewski
    • 1
  1. 1.Center for Drug Delivery ResearchThe University of KansasLawrenceUSA

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