Hepatic Cellular Models

A wide range of in vitro models are used in preclinical drug testing for the investigation of ADME-Tox (Absorption, Distribution, Metabolism, Excretion and oxicity) properties of New Chemical Entities (NCEs). The liver is the main organ with regards to ADME-Tox, it’s the place of more than 500 different functions, including: metabolism of lipids, carbohydrates, and vitamins, detoxification, production of bile, albumin, fibrinogen, globulin, etc (1). The liver lobule is composed of parenchymal cells (hepatocytes) and nonparenchymal cells (Kupffer cells, hepatic stellate cells, and sinusoidal endothelial cells).

Hepatocytes – the Gold Standard

Hepatocytes represent 80% of liver volume. Hepatocytes are commonly used in drug discovery and preclinical drug development to perform experiments requiring intact cellular systems. Intact hepatocytes contain the major hepatic drug-metabolizing enzymes required to study the four categories of xenobiotic biotransformation: hydrolysis, reduction, oxidation and conjugation.

Because of these enzymes, hepatocytes provide a viable and cost-effective alternative to in vivo testing. [Read more…]

5 most popular posts in ADME-Tox in 2014!

Take a look at the 5 posts on our blog in the field of ADME-Tox that saw the most visits in 2014!

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Predicting CYP induction in stable cell lines

Assessing gene transcription as an endpoint for determining induction of drug metabolizing enzymes and transporters has become the “method of choice” in the FDA’s latest draft Guidance for Industry drug interaction studies. Increased gene transcription due to NCE exposure can be determined by two distinct methods, nuclear receptor activation and changes in mRNA levels in primary hepatocyte cultures.

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20th International Symposium on Microsomes and Drug Oxidations | 18-22 May , 2014

Meet Jean-François Têtu, our “Cells & related Services and Reagents” sales manager at MDO2014. This meeting will take place in Stuttgart at the MDO, an international symposium series for the science of drug metabolism, drug metabolizing enzymes & related areas.

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