Related Experiment Video
Updated: Mar 5, 2026
04:52
Author Spotlight: Discovering New Biopesticides from Bioactive Soil Microbe-Derived Natural Products
Published on: July 26, 2024
2.4K
Why Prodrugs and Propesticides Succeed
1Environmental Chemistry and Toxicology Laboratory, Department of Environmental Science, Policy, and Management, University of California , Berkeley, California 94720, United States.
Chemical Research in Toxicology
|March 24, 2017
Summary
Bioactivation creates effective prodrugs and propesticides by improving drug delivery and specificity. This strategy enhances pharmacokinetic properties, leading to more selective pharmaceutical and pest control agents.
Area of Science:
- Pharmaceutical Chemistry
- Agrochemical Science
- Medicinal Chemistry
Background:
- Many drugs and pesticides require bioactivation to exert their effects.
- Prodrugs and propesticides are designed to overcome pharmacokinetic limitations of parent compounds.
Purpose of the Study:
- To examine the advantages of bioactivation in optimizing drugs and pesticides.
- To understand the prevalence and design principles of prodrugs and propesticides based on market success in 2015.
Main Methods:
- Analysis of major drugs (100) and pesticides (90) from 2015 based on economic value or market success.
- Categorization of compounds into directly acting and those requiring bioactivation.
- Review of specific prodrugs and propesticides, their targets, and bioactivation pathways.
Main Results:
- Established or candidate prodrugs accounted for 19% of total drug sales; proinsecticides (20%), proherbicides (37%), and profungicides (17%).
- Prodrugs generally exhibited improved pharmacodynamic/pharmacokinetic properties, including enhanced specificity, due to optimized physical characteristics.
- Bioactivation commonly involved hydrolases or cytochrome P450 enzymes.
Conclusions:
- The prodrug and propesticide concept is widely applicable, yielding highly selective pharmaceutical and pest control agents.
- Bioactivation strategies effectively address pharmacokinetic limitations, enhancing potency and selectivity.
- Molecular design for bioactivatable precursors is crucial for developing advanced therapeutic and crop protection agents.
More Related Videos
08:03Unveiling Xenobiotic Transport and Effects in Isolated Mitochondria: Insights from Respirometric and Enzymatic Assays
Published on: March 7, 2025
998
10:10Mass Production of Entomopathogenic Fungi, Metarhizium robertsii and Metarhizium pinghaense, for Commercial Application Against Insect Pests
Published on: March 31, 2022
8.3K
Related Concept Videos
01:30Prodrugs
4.5K
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...
Prodrugs help overcome...
4.5K
01:16Drug Biotransformation: Overview
4.0K
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...
4.0K
01:28Drug Biotransformation: Overview
4.4K
Biotransformation, also known as drug metabolism, is a vital physiological process that chemically alters drugs, facilitating their elimination from the body and terminating their action. This process involves two main phases: phase I and phase II reactions. Phase I reactions, including oxidation, reduction, and hydrolysis, introduce or unmask polar functional groups on the drug molecule, thereby increasing its water solubility. By enhancing water solubility, the drug becomes more hydrophilic...
4.4K
01:14Drug Metabolism: Phase II Reactions
5.4K
Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be...
5.4K
01:24Principles of Drug Action
9.2K
Drugs are chemical substances that modify biological responses by interacting with macromolecular targets such as receptors, ion channels, transporters, and enzymes. Pharmacodynamics describes the course of action of drugs leading to the physiological effect at a specific site in the body.
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
9.2K
01:20Modified-Release Drug Delivery Systems: Influencing Factors
87
Modified-release drug delivery systems are designed to optimize the therapeutic effect of drugs by minimizing side effects, reducing the dosage required, and controlling drug release to align with pharmacokinetic and pharmacodynamic needs. The system depends on two key factors: the drug's release from the formulation and its movement through the body to the target site. Unlike conventional dosage forms, where absorption is the limiting step, the rate of drug release is the key determinant in...
87