Developing a new antifungal drug is a complex process with a high failure rate. Our in vitro Drug Metabolism and Pharmacokinetics (DMPK) services are designed to help you de-risk your antifungal drug discovery programs by providing critical insights into how your compounds behave in a biological system. We offer a comprehensive suite of services to accelerate your research from hit-to-lead to preclinical candidate selection, giving you the data you need to make informed decisions and move your project forward with confidence. Contact Us for a Customized Quote
Overview
In vitro DMPK studies are an essential part of drug discovery and development. DMPK is a field that studies the Absorption, Distribution, Metabolism, and Excretion (ADME) properties of a drug candidate. By using in vitro methods, we can evaluate a compound's ADME properties early in the discovery process, helping to identify and optimize compounds with favorable profiles while eliminating those with potential liabilities. For antifungal drugs, this is particularly crucial as you must find a compound that effectively targets the fungus without causing unacceptable toxicity to the human host.
Detailed Scope of Services
We provide a full range of in vitro DMPK services tailored specifically for antifungal drug candidates. Our assays help you characterize your compounds and select the best candidates for further development.
Workflow
Service Details
Absorption & Permeability Studies
Metabolism & Stability Studies
Distribution Studies
Physicochemical Properties
Samples
Deliverables
Turnaround Time
Absorption & Permeability Studies
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Caco-2 Permeability Assay: Measures a compound's ability to cross the intestinal membrane, predicting oral absorption. We offer both apical-to-basolateral and basolateral-to-apical transport studies.
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MDCK & PAMPA Assays: Provides rapid, high-throughput screening for permeability.
Metabolism & Stability Studies
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Metabolic Stability in Microsomes & Hepatocytes: Determines the rate at which your compound is metabolized by liver enzymes from different species (human, rat, dog, etc.). This data is crucial for predicting in vivo clearance.
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Metabolite Identification & Profiling: Using high-resolution mass spectrometry, we identify the specific metabolites formed, providing valuable information for safety and toxicology studies.
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Cytochrome P450 (CYP) Inhibition & Induction Studies: Assesses the potential for drug-drug interactions. We evaluate your compound's ability to inhibit or induce major human CYP isoforms.
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Reaction Phenotyping: Identifies which specific CYP enzymes are responsible for the metabolism of your compound.
Distribution Studies
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Plasma Protein Binding (PPB): Determines the fraction of your compound that is free (unbound) in plasma. Only the unbound drug is available to diffuse into tissues and interact with its target.
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Blood-to-Plasma Ratio: Measures the compound's partitioning between red blood cells and plasma.
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Tissue Binding: Evaluates the compound's binding to various tissue homogenates.
Physicochemical Properties
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Aqueous Solubility (Kinetic & Thermodynamic): Determines how well your compound dissolves in water, a key factor for formulation and absorption.
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LogD/LogP: Measures the lipophilicity of your compound, which influences its absorption, distribution, and permeability.
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pKa Determination: Identifies the compound's acid-base properties, which are crucial for predicting ionization at different pH values.
Sample Information
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Compound Name & CAS Number
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Molecular Weight & Formula
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Purity (>95% required)
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Solubility Information
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Safety Data Sheet (SDS)
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Target Concentration for Assays
Deliverables
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Comprehensive Study Report
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Raw Data Files
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Analysis of Results & Interpretation
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Recommendations for Next Steps
Turnaround Time
Most standard assays are completed within 3-6 weeks from sample receipt. Rush services are available upon request.
Ready to discuss your project? Let us get in touch and explore how our consulting services can help you achieve your goals.
Mechanism of Action & The Need for In Vitro DMPK
Antifungal drugs typically work by targeting unique structures or processes in fungal cells that are absent or significantly different in human cells. Common targets include:
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Cell Wall: Antifungals like echinocandins inhibit the synthesis of (1→3)-β-D-glucan, a key component of the fungal cell wall that is not present in human cells.
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Cell Membrane: Polyenes and azoles target ergosterol, the primary sterol in fungal membranes, which is a structural analog of cholesterol in human cells.
While these targets are selective, the drug's journey through the body—its absorption, distribution to the site of infection, metabolism, and excretion—can be impacted by its physicochemical properties and interactions with human systems. For instance, some antifungals can interact with mammalian cytochrome P450 (CYP) enzymes, leading to potential drug-drug interactions (DDI). Our in vitro DMPK services help you understand and predict these behaviors early on.
Our Advantages
Expertise
Our team has extensive experience in antifungal drug discovery and DMPK.
Integrated Approach
We can design a complete DMPK package from early-stage screening to IND-enabling studies.
Customization
We don't just offer off-the-shelf solutions; we work with you to tailor studies to your specific project needs.
High-Quality Data
Our labs are equipped with the latest technology and follow strict quality control standards to ensure accurate and reliable data.
Cost-Effective
Early in vitro screening helps you save time and money by identifying and culling poor-performing candidates before moving to expensive in vivo studies.
Target Customer Groups
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Biotech & Pharmaceutical Companies: From small startups to large pharma, we support all stages of antifungal drug discovery and development.
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Academic & Research Institutions: We partner with university and government labs to help translate promising research into viable drug candidates.
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Other CROs: We can serve as a specialized partner for specific DMPK assays.
Your next breakthrough is just a conversation away. Let's talk about your challenges and find a custom solution together.
FAQs
Why are in vitro DMPK studies so important for antifungal drugs?
Fungi are eukaryotes, just like humans. This genetic similarity makes finding a selective drug target challenging. In vitro DMPK studies allow us to quickly assess a compound's potential toxicity and predict its behavior in the human body, helping to identify candidates that are both potent against the fungus and safe for the patient.
What is the most critical in vitro DMPK assay for an antifungal drug?
Metabolic stability in human microsomes is often a top priority. A compound with poor metabolic stability will be cleared from the body too quickly to be effective.
Can you help with custom assay development?
Absolutely! We have extensive experience developing custom assays for unique compounds or specific project requirements. Contact us to discuss your needs.
