ECCS Class 3A: Interaction of Gabapentin and its Analogues with Transporters – a love-hate relationship

Date: January 28 2021
Presenter(s): Ayman El-Kattan, B. Pharm., PhD

Summary of the presentation:

The extended clearance classification system (ECCS) was first reported in the literature in 2016, and since then its utility and use has expanded in the field of drug development. This presentation will focus on ECCS class 3A compounds, specifically gabapentin and its analogues, and the work that was done at various research institutions to understand the disposition of these molecules. Discussions will include the impact of system L transporters on gabapentin and pregabalin oral absorption, and the less-than-proportional increase in exposure noted with gabapentin oral dose increase. Also, we will shed light on the role of system L transporters in the distribution of Gabapentin, and detail how these transporters can be successfully used to affect the half-life of Gabapentin analogs and ensure once-daily dosing by increasing drug renal reabsorption and reducing active intestinal secretion mediated by renal transporters.

About the presenter:


Executive Director and DMPK LEAD Head, Drug Metabolism and Pharmacokinetics, IFM Therapeutics, Cambridge, Massachusetts, USA


Dr. Ayman El-Kattan is Executive Director and DMPK LEAD Head at IFM Therapeutics. Previously, he was Associate Research Fellow at the Pharmacokinetics, Dynamics, and Metabolism Department, Pfizer Inc. Cambridge Laboratories where he worked for 17 years. He earned his bachelor degree in pharmacy with distinction from University of Jordan and a Ph.D. in Basic Pharmaceutical Sciences at University of South Carolina in the US. His main research interests are focused on understanding the role of transporters in influencing drug disposition and oral absorption. Also, it involves studying the utility of physiological based pharmacokinetic modeling (PBPK) tools in projecting drug disposition and drug-drug interaction liabilities in man for new molecular entities (NME). He is also an Adjunct Professor at College of Pharmacy-University of Rhode Island in Rhode Island, US where he lectures in the graduate-level pharmacokinetic courses and serves as external advisor on dissertation committees.  Dr. El-Kattan is active member of the American Association of Pharmaceutical Scientists (AAPS) and serves on the committee of the Drug Transporter community. He has been invited speaker over 50 times at national and international conferences and meetings and has published over 100 papers in peer-reviewed Journals and book chapters. Dr. El-Kattan also published a book by Wiley and titled: Oral Bioavailability Assessment: Basics and Strategies for Drug Discovery and Development (Wiley Series on Pharmaceutical Science and Biotechnology: Practices, Applications and Methods).