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In Vitro Metabolism

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With extensive knowledge and experience in drug discovery, Creative Bioarray can provide standard, cost-effective in vitro metabolism services including drug metabolic stability services and drug-drug interaction services to support your drug development process.

Drug safety and efficacy, the most important issues in drug discovery, are greatly affected by drug metabolism and drug-drug interactions. Since a drug is eliminated either by excretion or by metabolism to one or more active or inactive metabolites after entering the body, the metabolism rate and the bioactivity of the metabolites generated in the elimination process directly affect the retaining time of the drug in the body in bioactive forms. A high metabolism rate and the generation of active metabolites can produce a blood level that causes unacceptable toxicity. Therefore, it’s very important to understand the metabolizing route of a drug at an early stage of drug development to better predict drug toxicity or side effects, drug-drug interactions, and to obtain information which helps to form dosing strategies.

The major goals1 of in vitro drug metabolism evaluation are:

To identify major metabolic pathways and enzymes that affect the elimination of the test drug and its metabolites;
To evaluates the effects of the test drug on the metabolism of other drugs, or vice versa.

In Vitro Metabolism

Figure 1. Routes of elimination of the top 200 most prescribed drugs in 20022. Metabolism represents the listed clearance mechanism for ~73% of the top 200 drugs. Of the drugs cleared via metabolism, about three-quarters are metabolized by members of the cytochrome P450 (CYP) superfamily. For the CYP-mediated clearance mechanisms, the majority of drug oxidations (46%) were carried out by members of the CYP3A family; followed by 16% by CYP2C9; 12% for both CYP2C19 and CYP2D6; 9% for members of the CYP1A family; and 2% for both CYP2B6 and CYP2E1, UGT, uridine diphosphate glucuronyl transferase.


Creative Bioarray can provide various in vitro metabolism assays, including, but not limited to:

• Hepatocyte stability assay
• S9 stability assay
• Microsomal stability assay
• Plasma stability assay
• Metabolite identification
• Pathway determination assay
• CYP- and UGT-reaction phenotyping
• Cytochrome P450 induction and inhibition assays
• UGT inhibition (and other non-CYP enzymes)
• Drug transporters

Due to the complexity of the drug development process, you need a flexible partner to provide reliable support to your specific needs. With extensive experience and knowledge in the field of drug development, Creative Bioarray can provide various flexible and integrated services for drug discovery. Our experienced scientific team and state-of-the-art facilities enable us to offer our clients the following benefits:

• Flexibility to customize assays
• Reliable data of high consistency and quality
• Highly competitive pricing
• Detailed, concise report of results

Creative Bioarray is dedicated to providing fast and integrated services of the highest quality to accelerate the drug discovery process. If you have any special needs or questions regarding our services, please feel free to contact us at info@creative-bioarray.com or 1-631-626-9181 to get support from our experienced experts. We look forward to working with you in the future.

 

Reference:

1. US Food and Drug Administration. "Guidance for industry: Drug metabolism/drug interaction studies in the drug development process: studies in vitro." US Food and Drug Administration, Rockville, MD (1997).
2. Wienkers, Larry C., and Timothy G. Heath. "Predicting in vivo drug interactions from in vitro drug discovery data." Nature reviews Drug discovery 4.10 (2005): 825-833.

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Contact Us
USA
45-1 Ramsey Road, Shirley, NY 11967, USA
Tel: 1-631-626-9181
Fax: 1-631-614-7828
Email: info@creative-bioarray.com

Europe
Tel: 44-207-048-3343
Email: info@creative-bioarray.com