Current Trends in Clinical Trials of Prodrugs

The development of new drugs is a lengthy and complex process regarding its conception and ideation, passing through in silico studies, synthesis, in vivo studies, clinical trials, approval, and commercialization, with an exceptionally low success rate. The lack of efficacy, safety, and suboptimal p...

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Main Authors: Diogo Boreski, Valentine Fabienne Schmid, Priscila Longhin Bosquesi, Jean Leandro dos Santos, Cauê Benito Scarim, Viktor Reshetnikov, Chung Man Chin
Format: Article
Language:English
Published: MDPI AG 2025-02-01
Series:Pharmaceuticals
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Online Access:https://www.mdpi.com/1424-8247/18/2/210
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author Diogo Boreski
Valentine Fabienne Schmid
Priscila Longhin Bosquesi
Jean Leandro dos Santos
Cauê Benito Scarim
Viktor Reshetnikov
Chung Man Chin
author_facet Diogo Boreski
Valentine Fabienne Schmid
Priscila Longhin Bosquesi
Jean Leandro dos Santos
Cauê Benito Scarim
Viktor Reshetnikov
Chung Man Chin
author_sort Diogo Boreski
collection DOAJ
description The development of new drugs is a lengthy and complex process regarding its conception and ideation, passing through in silico studies, synthesis, in vivo studies, clinical trials, approval, and commercialization, with an exceptionally low success rate. The lack of efficacy, safety, and suboptimal pharmacokinetic parameters are commonly identified as significant challenges in the discovery of new drugs. To help address these challenges, various approaches have been explored in medicinal chemistry, including the use of prodrug strategies. As a well-established approach, prodrug design remains the best option for improving physicochemical properties, reducing toxicity, and increasing selectivity, all while minimizing costs and saving on biological studies. This review article aims to analyze the current advances using the prodrug approach that has allowed the advance of drug candidates to clinical trials in the last 10 years. The approaches presented here aim to inspire further molecular optimization processes and highlight the potential of this strategy to facilitate the advancement of new compounds to clinical study phases.
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spelling doaj-art-c47d43ddc2f54f57994cbdb98d90d9252025-08-20T02:45:01ZengMDPI AGPharmaceuticals1424-82472025-02-0118221010.3390/ph18020210Current Trends in Clinical Trials of ProdrugsDiogo Boreski0Valentine Fabienne Schmid1Priscila Longhin Bosquesi2Jean Leandro dos Santos3Cauê Benito Scarim4Viktor Reshetnikov5Chung Man Chin6Laboratory for Drug Design (LAPDESF), School of Pharmaceutical Sciences, University of São Paulo State (UNESP), Araraquara 14800-903, BrazilDepartement Pharmazeutische Wissenschaften, Philosophisch-Naturwissenschaftliche Fakultät, Universität Basel, 4003 Basel, SwitzerlandLaboratory for Drug Design (LAPDESF), School of Pharmaceutical Sciences, University of São Paulo State (UNESP), Araraquara 14800-903, BrazilLaboratory for Drug Design (LAPDESF), School of Pharmaceutical Sciences, University of São Paulo State (UNESP), Araraquara 14800-903, BrazilLaboratory for Drug Design (LAPDESF), School of Pharmaceutical Sciences, University of São Paulo State (UNESP), Araraquara 14800-903, BrazilDepartment Chemistry and Pharmacy, Organic Chemistry II, Friedrich-Alexander-Universität Erlangen-Nürnberg, Henkestrasse 42, 91301 Erlangen, GermanyLaboratory for Drug Design (LAPDESF), School of Pharmaceutical Sciences, University of São Paulo State (UNESP), Araraquara 14800-903, BrazilThe development of new drugs is a lengthy and complex process regarding its conception and ideation, passing through in silico studies, synthesis, in vivo studies, clinical trials, approval, and commercialization, with an exceptionally low success rate. The lack of efficacy, safety, and suboptimal pharmacokinetic parameters are commonly identified as significant challenges in the discovery of new drugs. To help address these challenges, various approaches have been explored in medicinal chemistry, including the use of prodrug strategies. As a well-established approach, prodrug design remains the best option for improving physicochemical properties, reducing toxicity, and increasing selectivity, all while minimizing costs and saving on biological studies. This review article aims to analyze the current advances using the prodrug approach that has allowed the advance of drug candidates to clinical trials in the last 10 years. The approaches presented here aim to inspire further molecular optimization processes and highlight the potential of this strategy to facilitate the advancement of new compounds to clinical study phases.https://www.mdpi.com/1424-8247/18/2/210prodrugsclinical trialsprodrug designdrug discovery
spellingShingle Diogo Boreski
Valentine Fabienne Schmid
Priscila Longhin Bosquesi
Jean Leandro dos Santos
Cauê Benito Scarim
Viktor Reshetnikov
Chung Man Chin
Current Trends in Clinical Trials of Prodrugs
Pharmaceuticals
prodrugs
clinical trials
prodrug design
drug discovery
title Current Trends in Clinical Trials of Prodrugs
title_full Current Trends in Clinical Trials of Prodrugs
title_fullStr Current Trends in Clinical Trials of Prodrugs
title_full_unstemmed Current Trends in Clinical Trials of Prodrugs
title_short Current Trends in Clinical Trials of Prodrugs
title_sort current trends in clinical trials of prodrugs
topic prodrugs
clinical trials
prodrug design
drug discovery
url https://www.mdpi.com/1424-8247/18/2/210
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AT cauebenitoscarim currenttrendsinclinicaltrialsofprodrugs
AT viktorreshetnikov currenttrendsinclinicaltrialsofprodrugs
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