biostudies-literatureUnknown12(1)Naganawa MUCB Pharma<h4>Background</h4>Antiepileptic drugs, levetiracetam (LEV) and brivaracetam (BRV), bind to synaptic vesicle glycoprotein 2A (SV2A). In their anti-seizure activity, speed of brain entry may be an important factor. BRV showed faster entry into the human and non-human primate brain, based on more rapid displacement of SV2A tracer ¹¹C-UCB-J. To extract additional information from previous human studies, we developed a nonlinear model that accounted for drug entry into the brain and binding to SV2A using brain ¹¹C-UCB-J positron emission tomography (PET) data and the time-varying plasma drug concentration, to assess the kinetic parameter K₁ (brain entry rate) of the drugs.<h4>Method</h4>Displacement (LEV or BRV p.i. 60 min post-tracer injection) and post-dose sEJNMMI research71https://www.ebi.ac.uk/biostudies/studies/S-EPMC9643320biostudies-literatureDrug characteristics derived from kinetic modeling: combined ¹¹C-UCB-J human PET imaging with levetiracetam and brivaracetam occupancy of SV2A.PMC9643320Hannestad JKervyn SChen MKMercier JNaganawa MStockis ANabulsi NBGallezot JDHuang YHenry SCarson REFinnema SJMaguire RPNicolas JMKlitgaard HfalseDrug characteristics derived from kinetic modeling: combined ¹¹C-UCB-J human PET imaging with levetiracetam and brivaracetam occupancy of SV2A.<h4>Background</h4>Antiepileptic drugs, levetiracetam (LEV) and brivaracetam (BRV), bind to synaptic vesicle glycoprotein 2A (SV2A). In their anti-seizure activity, speed of brain entry may be an important factor. BRV showed faster entry into the human and non-human primate brain, based on more rapid displacement of SV2A tracer ¹¹C-UCB-J. To extract additional information from previous human studies, we developed a nonlinear model that accounted for drug entry into the brain and binding to SV2A using brain ¹¹C-UCB-J positron emission tomography (PET) data and the time-varying plasma drug concentration, to assess the kinetic parameter K₁ (brain entry rate) of the drugs.<h4>Method</h4>Displacement (LEV or BRV p.i. 60 min post-tracer injection) and post-dose s2022-01-01T00:00:00Z2022 Nov2025-04-04T19:27:46.036Z2025-02-19T01:57:15.144ZS-EPMC96433203634651310.1186/s13550-022-00944-5