Prodrugs. Do they have advantages in clinical practice?

  title={Prodrugs. Do they have advantages in clinical practice?},
  author={Valentino J. Stella and William N. Charman and Vijay H. Naringrekar},
  volume={29 5},
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… 

Prodrugs: design and clinical applications

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.


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

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

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

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

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.


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

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

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



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

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.

Molecular pharmacology, a basis for drug design.

  • E. J. Ariëns
  • Biology
    Fortschritte der Arzneimittelforschung. Progress in drug research. Progres des recherches pharmaceutiques
  • 1966
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.

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.

The disposition of sulindac

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.

Chemical modification of lincomycin: synthesis and bioactivity of selected 2,7-dialkylcarbonate esters.

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.

Chemical Aspects of Selective Toxicity

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

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

Phenytoin prodrugs V: In vivo evaluation of some water-soluble phenytoin prodrugs in dogs.

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.