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Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...

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Updated: Jun 21, 2026

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

Current prodrug design for drug discovery.

Pei-Wen Hsieh¹, Chi-Feng Hung, Jia-You Fang

¹Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan, Taiwan.

Current Pharmaceutical Design

|July 16, 2009

Summary

Prodrugs are inactive compounds that become active drugs in the body. Recent advancements focus on oral delivery and tumor-specific targeting to improve drug efficacy and reduce side effects.

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Area of Science:

Medicinal Chemistry
Pharmacology
Drug Delivery

Background:

Prodrugs are inactive precursors metabolized to active drugs, offering enhanced therapeutic benefits.
Mechanisms include improved solubility, permeability, bioavailability, half-life, and targeted delivery.
Optimization of vehicles and enhancement techniques are crucial alongside prodrug design.

Purpose of the Study:

To review recent developments in orally administered prodrugs.
To highlight advancements in tumor-targeted prodrug strategies.
To systematically introduce pharmacokinetic and pharmacodynamic evaluations of these prodrugs.

Main Methods:

Review of recent scientific literature on prodrug design and development.
Focus on strategies enhancing oral bioavailability.
Analysis of techniques for achieving tumor-specific targeting.

Main Results:

Significant progress in prodrug strategies for oral administration.
Key developments in achieving targeted delivery to tumors.
Systematic presentation of pharmacokinetic and pharmacodynamic data for novel prodrugs.

Conclusions:

Prodrug design has seen major advancements, particularly in oral bioavailability and tumor targeting.
These strategies offer promising avenues for improved therapeutic efficacy and reduced adverse effects.
Further pharmacokinetic and pharmacodynamic evaluations are essential for clinical translation.