Join us our next Webinar on 28 January!
January 20, 2021
ECCS Class 3A: Interaction of Gabapentin and its Analogues with Transporters - a Love-hate Relationship
28 January, 2021
Presenter: Ayman El-Kattan, B. Pharm., PhD, Executive Director and DMPK LEAD Head, Drug Metabolism and Pharmacokinetics, IFM Therapeutics, Cambridge, Massachusetts, USA
Time: 8 am (PT), 11 am (ET), 4 pm (GMT), 5 pm (CET)
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.
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