Science Pool

Pre-incubating with inhibitor can influence inhibitory potency for some drug transporters such as OATP1B1. It is thought that this phenomenon is a consequence of the time taken for some inhibitors to accumulate inside the cell.

In this poster, we focus on:

• a comparison of a 30 min pre-incubation time with a 15 min pre-incubation time for OATP1B1
• the impact of inhibitor pre-incubation on P-gp and BCRP inhibition in a polarised cell monolayer

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Incubation times for in vitro hepatocyte stability assays are usually relatively short in order to maintain cell viability and enzymatic activity. This can limit the accuracy of clearance prediction for stable compounds. 

In this poster, we focus on:

• a comparison of three human models of in vitro clearance; the HμREL coculture model, 2D hepatocyte monoculture model and suspension hepatocyte model 
• data were scaled to predict in vivo human clearance
• the suitability of each system to accurately predict the clearance of stable compounds was assessed

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Rosuvastatin is used in the treatment of dyslipidemia. The drug transporter BCRP (breast cancer resistant protein) has been identified as the rate limiting barrier to rosuvastatin absorption.

In this poster, we focus on:

• whether estrone 3-sulfate can be applied as a surrogate in vitro BCRP probe substrate for predicting rosuvastatin DDI 
• a comparison of BCRP inhibition assessment using rosuvastatin or estrone 3-sulfate as probe substrate for six established BCRP inhibitors for which a clinical DDI with rosuvastatin has been characterised

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Download this fact sheet to learn more about thermodynamic solubility including:

• Background information
• Assay details and protocol summary
• Data generated in the thermodynamic solubility assay

Download this fact sheet to learn more about turbidimetric solubility including:

• Background information
• Assay details and protocol summary
• Data generated in the turbidimetric solubility assay

Download this fact sheet to learn more about the chemical stability assay including:

• Background information
• Assay details and protocol summary
• Data generated in the chemical stability assay

Learn more about the preclinical hepatic Oatp transporter substrate identification assay including:

• Background information
• Assay details and protocol summary
• Data generated in the preclinical hepatic Oatp transporter substrate identification assay

Learn more about the preclinical hepatic Oatp inhibition assay including:

• Background information
• Assay details and protocol summary
• Data generated in the preclinical Oatp  transporter inhibition assay