Related Experiment Video
Updated: Aug 3, 2026
08:09
Gene-environment Interaction Models to Unmask Susceptibility Mechanisms in Parkinson's Disease
Published on: January 7, 2014
PD-140248 (Parke-Davis & Co)
1Institute for Medical Microbiology and Virology, University Hospital Düsseldorf, Germany.
Idrugs : the Investigational Drugs Journal
|August 19, 2005
Summary
PD-140248, a novel pyrrolidinyl naphthyridine, shows potent antibacterial activity against Gram-positive and quinolone-resistant bacteria. Its specific enantiomer exhibits enhanced efficacy, targeting further preclinical development for bacterial infections.
Area of Science:
- Microbiology
- Medicinal Chemistry
- Pharmacology
Background:
- PD-140248 is an investigational isomerase and topoisomerase II inhibitor developed for bacterial infections.
- It belongs to the pyrrolidinyl naphthyridine class, designed to combat quinolone-resistant bacteria.
Purpose of the Study:
- To evaluate the antibacterial spectrum and potency of PD-140248.
- To compare the activity of different stereoisomers of PD-140248.
Main Methods:
- In vitro susceptibility testing (MIC90) against various Gram-positive and Gram-negative bacteria.
- In vitro and in vivo comparison of PD-140248 enantiomers against stereoisomers.
Main Results:
- PD-140248 demonstrated broad-spectrum activity, particularly against Gram-positive bacteria like Staphylococcus and Streptococcus species.
- It showed significant activity against quinolone-resistant strains, including methicillin- and ciprofloxacin-resistant S. aureus.
- The (3R,1S) enantiomer of PD-140248 displayed 1- to 10-fold enhanced activity compared to its stereoisomers.
Conclusions:
- PD-140248 exhibits potent in vitro antibacterial activity, especially against Gram-positive pathogens.
- The specific enantiomer, (3R,1S)-PD-140248, warrants further preclinical investigation due to its superior efficacy.
Related Concept Videos
01:15Parkinson's Disease: Overview
Neurodegenerative disorders are progressive diseases that cause irreversible damage and loss to neurons in specific brain areas. Examples of these disorders include Parkinson's disease, Alzheimer's disease, Multiple Sclerosis (MS), and Amyotrophic Lateral Sclerosis (ALS). These disorders share characteristics such as proteinopathies, selective neuronal vulnerability, and a complex interplay between genetic and environmental factors. The primary therapeutic goal for these conditions is to...
01:24Parkinson's Disease: Treatment
Neurodegenerative disorders, such as Parkinson's Disease (PD), involve the gradual and irreversible destruction of neurons in particular brain areas. These disorders exhibit standard features like proteinopathies, selective vulnerability of some neurons, and an interaction of intrinsic properties, genetics, and environmental influences in neural injury.
Parkinson's Disease is primarily a result of the loss of dopaminergic neurons in the substantia nigra pars compacta. The cornerstone of its...
Parkinson's Disease is primarily a result of the loss of dopaminergic neurons in the substantia nigra pars compacta. The cornerstone of its...
01:24Dosage Regimen: Individualization
Individualization in dosing regimens is the customization of medication doses for individual patients. Its necessity arises from the goal of maximizing therapeutic benefits while minimizing risks. This approach is pivotal because human responses to drugs can vary widely; what is effective for one person may be inadequate or excessive for another. Interpatient (intersubject) variability refers to differences in drug responses between individuals, while intrapatient (intrasubject) variability...
01:15Impact of Pharmacokinetic–Pharmacodynamic Models: Regulatory Decisions
PK–PD modeling has significantly influenced FDA regulatory decisions, particularly drug approval, dosage optimization, and labeling. These models integrate pharmacokinetics (PK) and pharmacodynamics (PD) to predict drug behavior and effects, aiding in optimizing dosing regimens and enhancing the probability of clinical trial success.One notable example is Nesiritide (Natrecor®), a recombinant human brain natriuretic peptide for treating acute decompensated congestive heart failure (CHF).
01:24Parkinson Disease l: Introduction
Parkinson’s disease is a chronic, progressive neurodegenerative disorder that primarily affects movement. It is characterized by motor symptoms such as resting tremors, muscle rigidity, bradykinesia (slowness of movement), and postural instability. Patients may notice hand tremors at rest, stiffness during movement, or a shuffling gait. In addition to motor features, non-motor symptoms include sleep disturbances, mood and behavioral changes, constipation, and cognitive impairment, all of which...