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Drug Discovery: Overview

Drug Discovery: Overview

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...

Structure-Activity Relationships and Drug Design

Structure-Activity Relationships and Drug Design

Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...

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...

Preclinical Development: Overview

Preclinical Development: Overview

Preclinical development consists of a series of tests that ensure the safety and efficacy of a new therapeutic compound before it is tested in humans. There are four main phases to this process. First, safety pharmacology tests are conducted to ensure the drug does not produce any acutely harmful effects. These tests examine parameters such as bronchoconstriction, cardiac dysrhythmias, blood pressure changes, and ataxia. Next, preliminary toxicological testing is performed to determine the...

Biopharmaceutical Factors Influencing Drug Product Design: Overview

Biopharmaceutical Factors Influencing Drug Product Design: Overview

Rational drug product design integrates knowledge of the drug’s physicochemical properties, formulation components, manufacturing techniques, and intended route of administration. Each factor influences the drug’s performance, including how it is released, absorbed, and eliminated in the body.The physicochemical properties of a drug—such as solubility, stability, and particle size—affect its compatibility with excipients and the choice of dosage form. Excipients, though pharmacologically...

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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Updated: May 27, 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

Re-engineering drug discovery and development.

Garret A FitzGerald¹

¹Clinical & Translational Science Award (CTSA), University of Pennsylvania, Philadelphia, Pennsylvania, USA.

LDI Issue Brief

|November 5, 2011

Summary

This summary is machine-generated.

Drug development costs are rising dramatically while new drug approval rates remain stagnant. This unsustainable model necessitates changes in regulatory science and translational medicine for safer, more effective therapeutics.

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Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery

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Last Updated: May 27, 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

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery

Published on: May 16, 2021

Area of Science:

Pharmaceuticals
Drug Development
Regulatory Science

Background:

The rate of new drug approvals in the US has been constant since 1950.
Drug development costs have significantly increased over the same period.
This trend raises concerns about the sustainability of the current pharmaceutical development model.

Purpose of the Study:

To summarize the challenges in current drug development.
To describe governmental initiatives aimed at improving the process.
To suggest advancements in regulatory science and translational medicine.

Main Methods:

Analysis of historical drug approval rates and development costs.
Review of governmental policies and interventions.
Identification of potential improvements in regulatory science and translational medicine.

Main Results:

Drug approval rates have not kept pace with escalating development costs.
Governmental efforts are underway to address the issue.
Proposed changes focus on enhancing regulatory science and translational medicine.

Conclusions:

The current drug development model faces sustainability challenges due to rising costs and stagnant approval rates.
Implementing changes in regulatory science and translational medicine is crucial.
These changes aim to foster the development of safer and more effective therapeutics.