Lessons Learned from Marketed and Investigational Prodrugs

Author:

Ettmayer Peter1,Amidon Gordon L.1,Clement Bernd1,Testa Bernard1

Affiliation:

1. Novartis Institute for BioMedical Research, Brunnerstrasse 59, A-1235 Vienna, Austria, College of Pharmacy, The University of Michigan, Ann Arbor, Michigan 48109-1065, Pharmaceutical Institute, University of Kiel, D-24118 Kiel, Germany, and Department of Pharmacy, University Hospital Centre (CHUV), CH-1011 Lausanne, Switzerland

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Reference82 articles.

1. Rote Liste; Editio Cantor Verlag:  Aulendorf, Germany, 2002. This is a list of nearly all marketed drugs in Germany containing 1562 different active substances. Of these, 108 could definitely be classified as prodrugs (6.9%), 53 of which are activated by hydrolysis (49%) and 25 (23%) are bioprecursors (i.e., lacking a promoiety) activated by a biosynthetic reaction. In addition, 62 (4%) can be considered as limited prodrugs (i.e., active substances forming one or more active metabolites).

2. Prodrugs

3. Chemical Aspects of Selective Toxicity

4. Soft drug design: General principles and recent applications

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