2011
DOI: 10.1007/s13318-011-0035-z
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The rationality for using prodrug approach in drug discovery programs for new xenobiotics: opportunities and challenges

Abstract: The concept of prodrugs has been successfully executed for life cycle management options of several approved drugs and drugs in development. In addition to imparting ideal biopharmaceutical properties, such as solubility, permeability and lipophilicity, some prodrug concepts have also enabled site-specific drug delivery, prolonged the duration of therapeutic effect and improved therapeutic index. The strategic inclusion of prodrug concept during drug discovery and early development process brings in some uniqu… Show more

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Cited by 11 publications
(5 citation statements)
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References 55 publications
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“…Other xenobiotics need assistance to obtain similar effects. 104 For the sake of this review, both assistance with xenobiotic delivery and activity will be summarized with one indicator on the chart, although the two categories “aid” quite differently. “Delivery aids” encompass structural modifications ( i.e.…”
Section: Recent Studies On Botanical Nps and Associated Drug Developm...mentioning
confidence: 99%
“…Other xenobiotics need assistance to obtain similar effects. 104 For the sake of this review, both assistance with xenobiotic delivery and activity will be summarized with one indicator on the chart, although the two categories “aid” quite differently. “Delivery aids” encompass structural modifications ( i.e.…”
Section: Recent Studies On Botanical Nps and Associated Drug Developm...mentioning
confidence: 99%
“…For example, a broad-spectrum herbicide, such as isoxaflutole, does not have a promoiety or carrier, but after biotransformation, diketonitrile is the metabolite of isoxaflutole which is the actual inhibitor and herbicide (Figure 7). For the carrier-linked prodrug, once it enters the organism, it undergoes enzymatic or non-enzymatic cleavage to release the originally active agent and carrier [82,88,89]. Types of carrier-linked prodrugs include esters, amides, phosphates, carbamates, carbonates, oximes, imines, and N-Mannich bases.…”
Section: Targeted Herbicide Discovery and Developmentmentioning
confidence: 99%
“…12). No carrier is present in this type of example, but the molecule must be metabolized to undergo functional group transformation [37][38][39] . Some examples include nabumetone (relafen), prontosil (Fig.…”
Section: Sultamicillinmentioning
confidence: 99%