Sponsored Showcases
12:00 - 12:30 | Monday, June 12
Admescope
In vitro and in vivo Metabolism Studies with New Drug Modalities
Ari Tolonen, Ph.D., Admescope
This presentation will introduce basic tools for investigating metabolism of new modalities, together with some new findings and examples concerning correlations between various models employed in metabolism research.
Learning Objectives
1) Metabolism assays with new modalities;
2) Correlation of in vitro systems;
3) In vitro – in vivo correlation.
Target Audience: Professionals interested in metabolism & biotransformation research of new drug modalities.
Over the last decade or two, the role of new modalities in the development pipelines of pharmaceutical industry has been strongly increasing, introducing structures based on natural and modified peptides, oligonucleotides, antibodies and antibody-drug conjugates. However, on the contrary to the well-established methods that are available for investigation of traditional small molecule drugs, no clear consensus has been obtained regarding the biological in vitro systems to be used in their research. The presentation shows some experiences and findings from the authors’ lab, related to the use of in vitro models for studies with new modalities.
12:00 - 12:30 | Tuesday, June 13
Pharmaron
Application of Determined Apparent Permeability to Predict Disposition of Drugs
Katherine Fenner, Pharmaron
The talk is intended to discuss the impact of determined apparent permeability on predicting the ADME properties of small molecules.
Learning Objectives
1) Overview of the current literature position of how the ADME properties of small molecules can be predicted by applying computed properties and measured in vitro properties;
2) Understanding of considerations of experimental protocols of in vitro ADME assays including apparent permeability, solubility, log D and intrinsic clearance parameters;
3) Understanding the relationships between both computed and measured properties of small drug molecules with different aspects of drug disposition.
Target Audience: Anyone working in drug discovery in the pharmaceutical industry.
Over the past decade or so the impact of measured apparent permeability (Papp) to estimate the disposition of small molecule drugs has become apparent (Benet et al 2013). The availability of these data to enable the initial understanding of the likely disposition characteristics is vital in early drug discovery. Here, the application of measured Papp values of a range of well-characterised drug molecules is correlated with a wide range of ADME properties, including fraction absorbed, fraction metabolised, non-metabolic clearance and brain penetration. Predictions applying permeability data are compared to predictions applying other simply determined parameters from in vitro assays such as solubility and log D. Additionally the application of physiochemical parameters to predict disposition properties will also be discussed.
12:00 - 12:15 | Wednesday, June 14
SOLVO Biotechnology - A Charles River Company
Transporter Assays - DDI and Beyond
Noémi Szili, Ph.D., SOLVO Biotechnology - A Charles River Company
This talk is intended to provide an overview of the in vitro transporter interaction landscape and future perspectives.
Learning Objectives
1) Provide an overview of the place of in vitro drug-transporter interactions in the current drug development practice;
2) Show examples of transporters as drug targets or mediators of drug targeting;
3) Highlight the role of automated transporter interaction assays in early development;
4) Show examples as emerging transporters involved in toxicity risks and drug interactions – beyond the regulatory Guidelines;
5) Provide an update on new developments by SOLVO, the leader in transporter assays.
Target Audience: Anyone working on drug development from pharmaceutical companies, academia and CROs.
As the pioneering provider of in vitro transporter-interaction assays, we at SOLVO Biotechnology – a Charles River company, provide an overview of the current transporter landscape and newest developments. Beyond the now standardized in vitro transporter-mediated drug-drug interaction assays required by regulatory agencies for new drug submissions, the importance of transporters is widely recognized in multiple areas of drug development. Modulation of the transport of an endogenous substrate can be a mechanism of action for multiple therapeutic areas, while leveraging drug transporters has also gained traction as a mechanism for targeted delivery. Via a few examples, we showcase how automated in vitro transporter assays can support drug development in earlier phases where engaging transporters is key for candidate or lead selection. The involvement of transporters in potential unwanted effects beyond drug-drug interactions has also been recognized by both developers and the regulatory agencies. In addition to the mandatory list of in vitro tests to be run, now new transporters are explicitly recommended for consideration by the international harmonized draft guidelines and the importance of emerging new transporters is systematically highlighted in the literature. A number of these emerging transporters as well as the new in vitro assays recently developed for their study will be described in more detail.
