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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...

Targeted Cancer Therapies

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...

Targeted Cancer Therapies

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...

Modified-Release Drug Delivery Systems: Site-Targeted

Modified-Release Drug Delivery Systems: Site-Targeted

Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.

Targets for Drug Action: Overview

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...

Pharmacogenomics: Identification of New Drug Targets

Pharmacogenomics: Identification of New Drug Targets

Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...

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High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

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Targeted enzyme prodrug therapies.

N Schellmann¹, P M Deckert, D Bachran

¹Zentralinstitut für Laboratoriumsmedizin und Pathobiochemie, Charité - Universitätsmedizin Berlin, Campus Benjamin Franklin, Hindenburgdamm 30, D-12200 Berlin, Germany.

Mini Reviews in Medicinal Chemistry

|June 22, 2010

Summary

Targeted cancer therapies, including enzyme prodrug strategies, offer new hope for difficult-to-treat tumors. These innovative treatments aim to specifically activate drugs at the tumor site, improving efficacy and reducing side effects.

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Area of Science:

Oncology
Biochemistry
Pharmacology

Background:

Cancer treatment faces challenges with invasive, metastatic, and inaccessible tumors despite traditional methods like surgery, chemotherapy, and radiotherapy.
Targeted therapies have emerged over the last three decades to specifically locate, detect, and eliminate tumor cells.
Tumor site-specific prodrug activation is a promising two-step targeted therapy approach.

Purpose of the Study:

To provide a concise overview of the history and latest developments in targeted cancer therapies.
To review key technologies in targeted cancer treatment, focusing on enzyme prodrug strategies.
To highlight advancements in prodrug-converting enzymes, prodrugs, and drugs for cancer therapy.

Main Methods:

Review of historical and recent scientific literature on targeted cancer therapies.
Analysis of enzyme prodrug therapy concepts and their evolution since 1974.
Examination of various targeting systems including antibody-directed enzyme prodrug therapy (ADEPT), gene-directed enzyme prodrug therapy (GDEPT), clostridial- (CDEPT), and polymer-directed enzyme prodrug therapy (PDEPT).

Main Results:

Significant progress has been made in developing targeted therapies, particularly those involving enzyme-mediated prodrug activation.
Various targeting systems, enzymes, and prodrugs have been investigated and refined over the years.
The review covers a range of enzyme prodrug therapy approaches and their components.

Conclusions:

Enzyme prodrug therapy represents a significant advancement in the quest for more effective and specific cancer treatments.
Continued research and development in targeting systems, enzymes, and prodrugs are crucial for overcoming challenges in cancer cure.
Targeted therapies, especially ADEPT and GDEPT, offer a promising alternative for treating difficult cancers.