Guanfacine (Intuniv® XR) extended release (GXR) is an orally administered, selective alpha2A-adrenergic receptor agonist, non-stimulant treatment for children and adolescents with attention deficit/hyperactivity disorder (ADHD). Guanfacine is primarily metabolized by the CYP3A4 enzyme. Thus, it was important to evaluate the drug-drug interaction (DDI) liability perpetrated by strong inhibitors and inducers of CYP3A4. Using data from clinical pharmacokinetics (PK) studies in which GXR was administered as a monotherapy, or co-administered with strong CYP3A4 inhibitors or inducers, physiologically-based pharmacokinetic (PBPK) modeling using the Simcyp Simulator was employed for DDI evaluation.
Based on these predictions using Simcyp, dosing recommendations for GXR were approved by the US FDA without the need to conduct further clinical studies, which is beneficial for both patients and the sponsor with obtaining access to GXR more quickly.
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