The double prodrug concept and its applications
1989; Elsevier BV; Volume: 3; Issue: 1 Linguagem: Inglês
10.1016/0169-409x(89)90004-5
ISSN1872-8294
Autores Tópico(s)Pharmaceutical studies and practices
ResumoAlthough the prodrug approach has been generally appreciated as a most useful means to improve the delivery of various drugs, the usual prodrug strategy of preparing a bioreversible derivative or transport form may sometimes fail. In many cases it may be difficult to obtain a prodrug with ideal properties in all respects such as a combination of adequate stability in vitro with a high susceptibility to regenerate the parent drug in vivo. The use of cascade latentiation or the double prodrug concept, i.e., making a prodrug of a prodrug, is suggested as a promising means of overcoming various draw backs of usual prodrugs. A number of specific examples are reviewed with the aim of illustrating the utility of this approach. In addition, various types of bioreversible derivatives from which the regeneration of the parent drug occurs via two or more sequential reactions are discussed.
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