In the ever-evolving landscape of drug discovery, a promising antifungal compound's journey from the lab to a marketable drug hinges on a comprehensive understanding of its ADME (Absorption, Distribution, Metabolism, and Excretion) properties. Early and accurate ADME profiling is critical for identifying potential liabilities and optimizing drug candidates with favorable pharmacokinetic profiles, thereby reducing late-stage failures and accelerating development timelines. Creative Biolabs offers specialized ADME profiling services tailored specifically for antifungal drug candidates. We provide an integrated platform to support your research from hit identification to lead optimization and candidate selection. Contact Us for a Customized Quote
Overview & Mechanism of Action
ADME profiling evaluates how a drug candidate interacts with the body. For antifungal agents, this means understanding their journey from administration to elimination.
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Absorption: How the antifungal drug gets into the bloodstream. This is influenced by factors like solubility, permeability, and the route of administration (e.g., oral, intravenous).
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Distribution: Where the drug goes in the body. Key factors include tissue penetration, protein binding, and accumulation in target organs (e.g., lungs, liver, and central nervous system).
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Metabolism: How the body biochemically transforms the drug. This is primarily handled by enzymes, particularly cytochrome P450 (CYP) enzymes in the liver. Metabolism can activate, inactivate, or generate toxic metabolites.
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Excretion: How the drug and its metabolites are eliminated from the body, typically through the kidneys (renal excretion) or liver (biliary excretion).
Understanding these processes helps us predict a drug's bioavailability, half-life, and potential for drug-drug interactions (DDIs).
Detailed Scope of Services
We offer a comprehensive suite of in vitro and in vivo ADME assays, which can be customized to meet your specific project needs.
Workflow
Service Details
Samples
Deliverables
Turnaround Time
In Vitro ADME Services
Physicochemical Properties
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Aqueous Solubility: Measures a compound's solubility in different media (e.g., physiological buffers) to predict oral absorption.
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LogP/LogD: Determines lipophilicity, which is a key predictor of membrane permeability and tissue distribution.
Absorption & Permeability
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Caco-2 Permeability: A well-established cell-based assay using human colon carcinoma cells to model intestinal permeability and predict oral absorption.
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MDCK Permeability: Uses Madin-Darby canine kidney cells to assess permeability and potential for active transport.
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P-glycoprotein (P-gp) and other transporter assays: Evaluates if a drug is a substrate or inhibitor of key efflux transporters, which can significantly impact bioavailability and tissue penetration.
Metabolism & Stability
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Microsomal Stability: Assesses a compound's metabolic stability and intrinsic clearance using liver microsomes from various species (e.g., human, rat, mouse).
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Hepatocyte Stability: A more physiologically relevant assay using intact hepatocytes to evaluate metabolism and metabolite formation.
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Cytochrome P450 (CYP) Inhibition and Induction: Identifies potential DDIs by assessing a compound's ability to inhibit or induce major CYP enzymes (e.g., CYP3A4, 2D6, 2C9).
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Metabolite Identification and Profiling: Uses high-resolution mass spectrometry to identify and quantify drug metabolites.
In Vivo Pharmacokinetics (PK) Services
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Single-Dose PK: Administers a single dose of the antifungal drug to an animal model (e.g., mouse, rat) to determine key PK parameters like Cmax (maximum concentration), Tmax (time to reach Cmax), and AUC (area under the curve).
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Multiple-Dose PK: Evaluates drug accumulation and steady-state concentration after multiple doses.
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Tissue Distribution: Measures drug concentration in various tissues (e.g., liver, kidney, brain) to assess distribution and potential for accumulation.
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Bioavailability Studies: Compares drug exposure after oral vs. intravenous administration to calculate oral bioavailability (F).
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PK/PD (Pharmacokinetic/Pharmacodynamic) Studies: Links the drug's concentration in the body to its antimicrobial effect against the fungal pathogen in vivo.
Sample Information
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Required amount: Varies by assay. Typically, we require milligrams of a compound for in vitro studies and tens to hundreds of milligrams for in vivo PK studies.
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Purity: Compounds should be ≥95% pure.
Deliverables
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Raw data files from analytical instruments.
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Formatted data tables and graphs.
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A detailed final report including experimental methods, results, data interpretation, and expert recommendations.
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A presentation of the results and a consultation with our scientific team.
Turnaround Time
Turnaround times are project-specific.
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In Vitro Assays: Typically range from 3 to 6 weeks.
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In Vivo PK Studies: Can range from 6 to 10 weeks, depending on the study design and animal model.
Ready to discuss your project? Let us get in touch and explore how our consulting services can help you achieve your goals.
Necessity
The need for robust ADME profiling is paramount in antifungal drug development due to the significant challenges posed by fungal pathogens. Fungal infections are a growing public health concern, often affecting immunocompromised patients. The current antifungal armamentarium is limited, with many existing drugs having poor bioavailability, off-target toxicity, or resistance issues. Early ADME profiling helps mitigate these risks, allowing you to select candidates with a higher probability of success.
Our Advantages
Mycology Expertise
We possess a deep understanding of fungal biology and the unique challenges of antifungal drug development, allowing us to design highly relevant and effective ADME studies.
Integrated Solutions
Our ADME services are seamlessly integrated with our other offerings, including antifungal susceptibility testing, in vitro and in vivo efficacy models, and medicinal chemistry support.
State-of-the-Art Technology
We utilize advanced analytical platforms, including LC-MS/MS and HRMS, to provide precise and sensitive data.
Speed & Quality
Our streamlined processes and automation ensure fast turnaround times without compromising data integrity or regulatory compliance.
Customizable Service
Every project is unique. We offer flexible study designs to meet your specific needs, from single-assay screens to comprehensive IND-enabling packages.
Target Customer Groups
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Pharmaceutical & Biotechnology Companies: Small to mid-sized biotech firms and large pharma companies seeking to outsource a portion of their drug discovery and development pipeline.
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Academic & Research Institutions: University labs and non-profit organizations working on early-stage drug discovery projects.
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Venture Capital Firms: Investors looking to de-risk their portfolio by validating the ADME properties of new drug candidates.
Your next breakthrough is just a conversation away. Let's talk about your challenges and find a custom solution together.
FAQs
Why is early ADME profiling so important for antifungal drugs?
Early profiling helps identify compounds with undesirable properties (e.g., poor oral absorption, rapid metabolism) before significant resources are invested, saving time and money and increasing the chances of clinical success.
Can you work with compounds that are poorly soluble?
Yes, we have specialized techniques and formulations to handle compounds with low solubility, ensuring accurate and reproducible results.
Do you offer GLP-compliant studies?
We can provide non-GLP studies for early discovery and are partnered with a network of GLP-certified labs for later-stage, regulatory-compliant studies.
How do you address drug-drug interactions (DDIs)?
We conduct in vitro assays to screen for potential DDI risks, such as CYP inhibition and induction, and can design custom in vivo DDI studies to further investigate these interactions.
