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Review

Current Trends in Clinical Trials of Prodrugs

by
Diogo Boreski
1,
Valentine Fabienne Schmid
2,
Priscila Longhin Bosquesi
1,3,
Jean Leandro dos Santos
1,
Cauê Benito Scarim
1,
Viktor Reshetnikov
4 and
Chung Man Chin
1,3,*
1
Laboratory for Drug Design (LAPDESF), School of Pharmaceutical Sciences, University of São Paulo State (UNESP), Araraquara 14800-903, Brazil
2
Departement Pharmazeutische Wissenschaften, Philosophisch-Naturwissenschaftliche Fakultät, Universität Basel, 4003 Basel, Switzerland
3
Advanced Research Center in Medicine (CEPAM), School of Medicine, Union of the Colleges of the Great Lakes (UNILAGO), Sao Jose do Rio Preto 15030-070, Brazil
4
Department Chemistry and Pharmacy, Organic Chemistry II, Friedrich-Alexander-Universität Erlangen-Nürnberg, Henkestrasse 42, 91301 Erlangen, Germany
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2025, 18(2), 210; https://doi.org/10.3390/ph18020210
Submission received: 16 January 2025 / Revised: 30 January 2025 / Accepted: 2 February 2025 / Published: 4 February 2025
(This article belongs to the Special Issue Prodrugs: Design and Development)

Abstract

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.
Keywords: prodrugs; clinical trials; prodrug design; drug discovery prodrugs; clinical trials; prodrug design; drug discovery

Share and Cite

MDPI and ACS Style

Boreski, D.; Schmid, V.F.; Bosquesi, P.L.; dos Santos, J.L.; Scarim, C.B.; Reshetnikov, V.; Chin, C.M. Current Trends in Clinical Trials of Prodrugs. Pharmaceuticals 2025, 18, 210. https://doi.org/10.3390/ph18020210

AMA Style

Boreski D, Schmid VF, Bosquesi PL, dos Santos JL, Scarim CB, Reshetnikov V, Chin CM. Current Trends in Clinical Trials of Prodrugs. Pharmaceuticals. 2025; 18(2):210. https://doi.org/10.3390/ph18020210

Chicago/Turabian Style

Boreski, Diogo, Valentine Fabienne Schmid, Priscila Longhin Bosquesi, Jean Leandro dos Santos, Cauê Benito Scarim, Viktor Reshetnikov, and Chung Man Chin. 2025. "Current Trends in Clinical Trials of Prodrugs" Pharmaceuticals 18, no. 2: 210. https://doi.org/10.3390/ph18020210

APA Style

Boreski, D., Schmid, V. F., Bosquesi, P. L., dos Santos, J. L., Scarim, C. B., Reshetnikov, V., & Chin, C. M. (2025). Current Trends in Clinical Trials of Prodrugs. Pharmaceuticals, 18(2), 210. https://doi.org/10.3390/ph18020210

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