Prodrugs. Do they have advantages in clinical practice?

@article{Stella1985ProdrugsDT,
  title={Prodrugs. Do they have advantages in clinical practice?},
  author={Valentino J. Stella and William N. Charman and Vijay H. Naringrekar},
  journal={Drugs},
  year={1985},
  volume={29 5},
  pages={
          455-73
        }
}
Prodrugs are pharmacologically inactive chemical derivatives of a drug molecule that require a transformation within the body in order to release the active drug. They are designed to overcome pharmaceutical and/or pharmacokinetically based problems associated with the parent drug molecule that would otherwise limit the clinical usefulness of the drug. The scientific rationale, based on clinical, pharmaceutical and chemical experience, for the design of various currently used prodrugs is… 
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188 Citations
Highly Influential Citations
2
Background Citations
32
Methods Citations
3

188 Citations

Prodrugs: design and clinical applications

TLDR
The most common functional groups that are amenable to prodrug design are described, and examples of prodrugs that are either launched or are undergoing human trials are highlighted.

PRODRUGS: A REVIEW

TLDR
Classification, effect of prodrug on solubility, chemical stability, bioavailability, long duration of action and site targeted challenge with examples of pro drug illustrating the role of produg as a better way for the more effective treatment of different diseases are included.

Design and Pharmaceutical Applications of Prodrugs

TLDR
The design and pharmaceutical applications of prodrugs are studied, which aims to overcome limitations of a parent drug that would otherwise hinder its clinical use.

Concept of Prodrug

Prodrug Approach: An Alternative to Improve Pharmacokinetic Properties

TLDR
This review introduces in depth the rationale behind the use of the promoiety, and also considers the possible problems that can arise from inadequate activation of prodrugs.

Prodrug Design by Computation Methods: A New Era

TLDR
Prodrugs, soft drugs, targeted drugs, and metabolites of drugs are common terms that are used in the pharmaceutical field and can be enzymatically or chemically converted in vivo to provide the parent active drug to exert a therapeutic effect.

Highly Efficient Prodrugs: Design and Therapeutic Applications

TLDR
In this review, different types of carriers, which can be used for prodrug synthesis are summarized and both marketed and investigational prodrugs from several promoieties are discussed not only for their advantages and uses but also their prospects.

LATENTIATED PRODRUG APPROACH OF DRUGS: AN OVERVIEW

TLDR
The purpose of this review is to understand the prodrugs, strategies incorporated in designing the proDrugs, applications, their crucial benefits in targeted action at a specific site of the body, their advantageous effects in chemotherapy.

Prodrugs available on the Brazilian pharmaceutical market and their corresponding bioactivation pathways

TLDR
Examination of examples of prodrugs from many important therapeutic classes shows that prodrug design is a very valuable aspect in the research of new drugs and for the pharmaceutical industry as a whole.

Cutting Edge Approach on Prodrug: Contrivance for Target Drug Delivery

TLDR
Prodrugs are the shrouded drugs which are one or two chemical or enzymatic steps away from the active parent drug.
...

References

SHOWING 1-10 OF 101 REFERENCES

Chapter 31. Prodrug Approach in Drug Design

A Physical Chemical Basis for the Design of Orally Active Prodrugs

Phenytoin prodrugs III: water-soluble prodrugs for oral and/or parenteral use.

TLDR
Various bioreversible derivatives of phenytoin, a poorly water soluble and erratically absorbed drug after both oral and parenteral dosing, confirmed that a number of the derivatives did indeed behave as prodrugs.

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TLDR
The design of drugs has been tried for many years but many, if not most, drugs used in these days are not the products but more the by-products of efforts in drug design.

Phenytoin prodrugs IV: Hydrolysis of various 3-(hydroxymethyl)phenytoin esters.

TLDR
The aqueous chemical stability of various bioreversible derivatives or prodrugs of phenytoin, a poorly water-soluble and erratically absorbed drug after both oral and intramuscular parenteral dosing, was evaluated to identify a number of promising candidate pro drugs.

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TLDR
The reversible biotransformation between sulindac and its active sulfide metabolite provides the basis for two therapeutic advantages relating to the gastrointestinal intolerance usually associated with anti‐inflammatory drugs.

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TLDR
Serum hydrolysis studies on certain 2,7-diesters of lincomycin established that a high degree of esterase activity is present in the serum of several different rodent species and appeared to be limited to these species.

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Phenytoin prodrugs VI: In vivo evaluation of a phosphate ester prodrug of phenytoin after parenteral administration to rats.

TLDR
It was concluded that 3-(hydroxymethyl)-5,5-diphenylhydantoin disodium phosphate ester might be useful as a nonirritant phenytoin prodrug suitable for parenteral administration.

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TLDR
It was concluded that one of the amino acyl esters, 3-(hydroxymethyl)-5,5-diphenylhydantoin N,N-dimethylglycine ester methanesulfonate, would be the most useful prodrug for oral administration, while 3-(Hydroxym methyl)-5-5- diphenytoin disodium phosphate ester would beThe most useful for parenteral administration.
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