Prodrug research: futile or fertile?

The objective of this Commentary is to help clarify and illustrate what prodrugs are, what they are not, which benefits they can offer, and what their limits are. To this end, a number of criteria of classification and evaluation are presented. This is followed by a discussion of the pharmaceutical,...

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Bibliographic Details
Published in:Biochemical pharmacology 2004-12, Vol.68 (11), p.2097-2106
Main Author: Testa, Bernard
Format: Article
Language:English
Subjects:
Absorption
Animals
Biological and medical sciences
Chemistry, Pharmaceutical
Commentary
Drug Delivery Systems
Drug Design
Drug metabolism
General pharmacology
Humans
In situ activation
Medical sciences
Miscellaneous
Pharmaceutical objectives
Pharmacodynamic objectives
Pharmacokinetic objectives
Pharmacology. Drug treatments
Prodrug design
Prodrugs - pharmacokinetics
Prodrugs - pharmacology
Solubility
Tissue-selective delivery
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Summary:The objective of this Commentary is to help clarify and illustrate what prodrugs are, what they are not, which benefits they can offer, and what their limits are. To this end, a number of criteria of classification and evaluation are presented. This is followed by a discussion of the pharmaceutical, pharmacokinetic and pharmacodynamic objectives of prodrug research. Recent examples (e.g. oseltamivir, bambuterol, capecitabine, clopidogrel and tirapazamine) are discussed in a biochemical perspective to illustrate these objectives and to demonstrate some of the therapeutic benefits afforded by successful prodrugs. Attention is also called to the fact that the in vitro and in vivo behavior of prodrug candidates may differ from that of the parent drug in ways that go beyond the original pharmaceutical, pharmacokinetic or pharmacodynamic objective being pursued. We conclude that prodrugs offer a viable strategy to disentangle pharmacodynamic and pharmacokinetic optimization.
ISSN:0006-2952
1873-2968
DOI:10.1016/j.bcp.2004.07.005