drug metabolism blog posts

03 November, 2017

Metabolites in safety testing - the ultimate guide

By Guy Webber

Over the past two decades considerable industry and regulatory discussion has focused around the importance of drug metabolites as potential sources of drug toxicity.

The issue of metabolite-mediated toxicity, and when it should be assessed, has become known as metabolites in safety testing (MIST). Essentially, it tackles the following question: When does a human metabolite become important? It is crucial to MIST to identify the major circulating human metabolites and ensure the species used in safety assessment are exposed to the same metabolites, at similar levels of exposure.

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03 November, 2017

6 crucial facts about DILI you ought to know

By Guy Webber

Drug induced liver injury (DILI) is a major cause of safety-related drug withdrawal and black box warnings post-market. It is also a major cause of drug attrition during development. One of the main concerns about DILI is that it is often undetected until clinical development and/or post-market approval, when the molecule is exposed to larger populations. 

So what do you need to know about DILI that will help you to reduce the risk of hepatotoxicity in humans?  Here are six facts to keep in mind.

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04 October, 2017

Shining the light on drug-drug interactions (DDI)

By Guy Webber

Advancements in in vitro technologies and analytical instrumentation over the past decade allows scientists to apply a variety of in vitro based assays designed to rapidly assess risk-liability, such as drug-drug interactions (DDI), one of the factors contributing to both current high attrition rates and delays in development.

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04 October, 2017

How in vitro assays and drug metabolism are being used to de-risk drug development

By Guy Webber

If all molecules in discovery and development were added together over recent years and compared to the number of successful drug approvals each year, the ratio is (approximately) 10,000:1. In other words, for every 10,000 molecules entering drug discovery, 9,999 will fail during some stage of the development process. Evidently, developing a molecule that has a desired, efficacious yet safe effect in humans is a remarkable achievement considering the lengthy, complex and expensive process.

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