IN VITRO TESTING Flashcards
Using cell-based models and advanced organ-on-a-chip systems provides an essential foundation for understanding a drug’s potential toxicity before further clinical trials.
IN VITRO TESTING
Advantages of In vitro Testing
• Rapid Screening
• Cost-Effectiveness
• Controlled Environment
• Ethical Considerations
Are a crucial part of the drug development process, allowing researchers to evaluate the potential efficacy and safety of drug candidates before moving to animal and human trials.
IN VITRO DRUG STUDIES
Cell-based Assays:
• Cell Line Selection
• Functional Readouts
• Toxicity Evaluation
In vitro studies provide a fast and efficient way to screen potential drug candidates, enabling a quicker identification of promising leads.
RAPID SCREENING
In vitro studies are generally less expensive to conduct than in vivo studies, reducing overall drug development costs.
COST-EFFECTIVENESS
In vitro studies allow for precise control of variables, minimizing external factors that can influence experimental outcomes.
CONTROLLED ENVIRONMENT
In vitro studies do not involve living organisms, eliminating potential ethical outcomes associated with animal welfare.
ETHICAL CONSIDERATIONS
Choosing the appropriate cell line is crucial, as it should be representative of the target tissue ot disease state.
CELL LINE SELECTION
Cell-based assays can measure various cellular response, such as proliferation, differentiation, or signaling pathway activation.
FUNCTIONAL READOUT
These assays can assess the cytotoxic effects of a drug candidates on cells, helping identify potential safety concerns.
TOXICITY EVALUATION
Genotoxicity and Mutagenicity Testing
• Ames Test
• Micronucleus Assay
• Comet Assay
Evaluating chromosomal damage and aneuploidy in ___?
MAMMALIAN CELLS
Evaluating chromosomal damage and aneuploidy in mammalian cells.
MICRONUCLEUS ASSAY
Detecting mutagenic potential using bacterial reverse mutation assays.
AMES TEST
Measuring DNA strand breaks and alkaline-labile sites in individual cells.
COMET ASSAY
Receptor Binding Assays
• Receptor Specificity
• Binding Affinity
• Functional Activation
These assays determine the selectivity of a drug candidate for its intended receptor target, versus off-target receptors
RECEPTOR SPECIFICITY
quantify the strength of the interaction between a drug candidate and its target receptor.
BINDING AFFINITY
Some receptor binding assays also measure the ability of a drug candidate to activate or inhibit the recepto’r downstream signaling pathways:
FUNCTIONAL ACTIVATION
Biochemical/Enzyme Activity Enzyme
• Enzyme Inhibition
• Enzyme Kinetics
• High- Throughput Screening
These assays determine the ability of a drug candidate to inhibit the activity of a target enzyme, which can be a potential mechanism of action.
ENZYME INHIBITION
Enzyme activity assays can provide information on the kinetic parameters of an enzyme-drug interaction, such as the rate of catalysis or inhibition.
ENZYME KINETICS
Measuring DNA strand breaks and alkaline-labile sites in?
INDIVIDUAL CELLS
Enzyme activity assays are well-suited for high throughput screening of large chemical libraries to identify potential drug candidate.
HIGH-THROUGHPUT SCREENING
Permeability Studies:
• Passive Diffusion
• Active Transport
• Blood-Brain Barrier
Measures the ability of a drug candidate to passively diffuse across cell membranes, which is crucial for oral bioavailability.
PASSIVE DIFFUSION
Evaluates the potential for a drug candidate to be a substrate or inhibitor of membrane transporter proteins.
ACTIVE TRANSPORT
Assess the likelihood of a drug candidate to cross the ____ and reach the central nervous system.
BLOOD-BRAIN BARRIER
Assess the likelihood of a drug candidate to cross the Blood Brain Barrier and reach the _______.
CENTRAL NERVOUS SYSTEM
Metabolic Stability Studies
• Metabolism Pathways
• Metabolite Profiling
• Half-Life Determination
These studies identify the major metabolic pathways and enzymes involved in the biotransformation of a drug candidate.
METABOLISM PATHWAY
Metabolic stability assays can provide a comprehensive understanding of the drug’s metabolic fate and potential metabolite-mediated effects.
METABOLITE PROFILING
The rate if drug metabolism is crucial for determining the appropriate dosing regimen and predicting in vivo pharmacokinetics.
HIGH-LIFE DETERMINATION
Are a vital part of the drug development process, providing valuable insights into the potential efficacy, safety and pharmacokinetic properties of a drug candiates.
IN VITRO DRUG STUDIES
