Search research articles

ABOUT JoVE

Overview Leadership Blog JoVE Help Center

AUTHORS

Publishing Process Editorial Board Scope & Policies Peer Review FAQ Submit

LIBRARIANS

Testimonials Subscriptions Access Resources Library Advisory Board FAQ

RESEARCH

JoVE Journal Methods Collections JoVE Encyclopedia of Experiments Archive

EDUCATION

JoVE Core JoVE Business JoVE Science Education JoVE Lab Manual Faculty Resource Center Faculty Site

Terms & Conditions of Use

Related Concept Videos

Prodrugs

Prodrugs

Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
Prodrugs help overcome...

Drug Regulation

Drug Regulation

Drug regulation encompasses the management of drug usage by evaluating its safety and efficacy through assessments conducted by regulatory authorities. Regrettably, the history of drug regulation is marred by several catastrophic events. One such incident is the Elixir Sulfanilamide tragedy, in which the toxic compound diethyl glycol was included in a sweet-tasting medication, leading to numerous fatalities. This event prompted the enactment of the Food, Drug, and Cosmetic Act in 1938. Under...

Prescription, Nonprescription and Orphan Drugs

Prescription, Nonprescription and Orphan Drugs

Prescription drugs require a prescription from a medical practitioner and can only be obtained from a pharmacy. They have many applications, including treating pain, anxiety, and hypertension.
The misuse and addiction to prescription drugs is a growing problem that can affect people of all age groups, specifically teenagers. This can happen when prescription medications are used in ways not intended by the prescriber, such as taking someone else's prescription or using medication for...

Drug Administration and Therapy Phases: Overview

Drug Administration and Therapy Phases: Overview

Drugs, the chemical agents used in diagnosing, treating, or preventing diseases, undergo a four-phase process of development: pharmaceutic, pharmacokinetics, pharmacodynamics, and therapeutic.
The pharmaceutical phase focuses on leveraging the physicochemical properties of the drug to design and manufacture an effective product. Variants include orally administered tablets or capsules, topical creams or ointments, and parenteral-delivery solutions or emulsions.
The pharmacokinetic phase...

Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence

Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence

Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...

Drug Biotransformation: Overview

Drug Biotransformation: Overview

Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by

Same author

Bortezomib Aqueous Solubility in the Presence and Absence of D-Mannitol: A Clarification With Formulation Implications.

Journal of pharmaceutical sciences·2020

Same author

Prodrugs: My Initial Exploration and Where It Led.

Journal of pharmaceutical sciences·2020

Same author

Sulfobutylether-β-cyclodextrin.

International journal of pharmaceutics·2020

Same author

Boric Acid, a Lewis Acid With Unique and Unusual Properties: Formulation Implications.

Journal of pharmaceutical sciences·2020

Same author

Some Preformulation Studies of Pyruvic Acid and Other α-Keto Carboxylic Acids in Aqueous Solution: Pharmaceutical Formulation Implications for These Peroxide Scavengers.

Journal of pharmaceutical sciences·2019

Same author

Origins, and formulation implications, of the pK<sub>a</sub> difference between boronic acids and their esters: A density functional theory study.

European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences·2018

Same journal

Green, renewable, or low-carbon? A framework for informed solvent selection in pharmaceutical sciences.

Journal of pharmaceutical sciences·2026

Same journal

Theranostic potential of ramucirumab functionalized magnetoliposomes for targeted delivery of sorafenib and MRI.

Journal of pharmaceutical sciences·2026

Same journal

Intranasal mucoadhesive chitosan microspheres of ranolazine: Formulation, design, and pharmacokinetic evaluation.

Journal of pharmaceutical sciences·2026

Same journal

Evolving landscape of drug development for pediatric rare diseases-from successes to strategies for addressing unmet needs.

Journal of pharmaceutical sciences·2026

Same journal

A mathematical framework for predicting tablet weight variability from blend particle size distribution and tooling geometry.

Journal of pharmaceutical sciences·2026

Same journal

Recrystallization can stop nitrosamine formation in ranitidine hydrochloride.

Journal of pharmaceutical sciences·2026

See all related articles

Search research articles

Related Experiment Video

Updated: Jun 9, 2026

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies

Published on: February 17, 2023

Prodrugs: Some thoughts and current issues.

Valentino J Stella¹

¹Department of Pharmaceutical Chemistry, The University of Kansas, Lawrence, Kansas 66047, USA. stella@ku.edu

Journal of Pharmaceutical Sciences

|September 8, 2010

Summary

This summary is machine-generated.

Prodrugs, used in 20% of new drugs, offer solutions for complex molecule delivery challenges but have limitations. Their role in drug discovery and commercialization is growing, despite ongoing research issues.

More Related Videos

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System

Published on: December 11, 2016

Related Experiment Videos

Last Updated: Jun 9, 2026

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies

Published on: February 17, 2023

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System

Published on: December 11, 2016

Area of Science:

Medicinal Chemistry
Pharmaceutical Sciences
Drug Delivery

Background:

The prodrug strategy addresses formulation, delivery, and toxicity issues with problematic drugs.
Approximately 20% of new small molecule New Chemical Entities (NCEs) over the past decade have utilized the prodrug approach.
Increasing molecular complexity in drug discovery necessitates advanced delivery solutions.

Purpose of the Study:

To discuss the challenges and limitations associated with the prodrug approach.
To highlight the growing integration of prodrugs in pharmaceutical research and development.
To explore issues in prodrug research and commercialization.

Main Methods:

Literature review and analysis of prodrug trends in pharmaceutical research.
Discussion of the strategic application of prodrugs in overcoming drug candidate limitations.
Examination of commercialization challenges and research hurdles in the prodrug field.

Main Results:

Prodrugs are increasingly vital in overcoming drug delivery challenges posed by complex molecules.
A significant percentage (approx. 20%) of recent New Chemical Entities (NCEs) are prodrugs, indicating their rising importance.
Despite their benefits, prodrugs present inherent limitations and research/commercialization challenges.

Conclusions:

The prodrug approach is an integral part of modern drug discovery, particularly for complex molecules.
Continued research and strategic development are crucial to address prodrug limitations and enhance commercial viability.
The increasing prevalence of prodrugs underscores their value in pharmaceutical innovation.