ArticleEJNMMI research2022
Drug characteristics derived from kinetic modeling: combined
Article in EJNMMI research, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 11 citations in OpenAlex.
- HIV-1 Tat expression drives progressive synaptic decline: evidence from longitudinal [NeuroImmune pharmacology and therapeutics · 2026Article
- Brivaracetam monotherapy in juvenile myoclonic epilepsy: a safety and efficacy evaluation.Therapeutic advances in neurological disorders · 2026Article
- Review
- Assessment of cerebral drug occupancy in humans using a single PET-scan: A [European journal of nuclear medicine and molecular imaging · 2024Observational
- Narrative Review of Brivaracetam: Preclinical Profile and Clinical Benefits in the Treatment of Patients with Epilepsy.Advances in therapy · 2024Review
- Evaluation of [EJNMMI research · 2024Article
- The impact of brivaracetam on cognitive processes and anxiety in various experimental models.Pharmacological reports : PR · 2024Article
- Kinetic models for estimating occupancy from single-scan PET displacement studies.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2023Article
Corrections and comments
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Authors and funding
15 authors at 2 institutions in 2 countries.
Funding
Abstract
backgroundAntiepileptic 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
methodDisplacement (LEV or BRV p.i. 60 min post-tracer injection) and post-dose scans were conducted in five healthy subjects. Blood samples were collected for measurement of drug concentration and the tracer arterial input function. Fitting of nonlinear differential equations was applied simultaneously to time-activity curves (TACs) from displacement and post-dose scans to estimate 5 parameters: K
resultsThe proposed model described well the TACs in all subjects; however, estimates of drug K
conclusionsUnder appropriate conditions, this advanced nonlinear model can directly estimate entry rates of drugs into tissue by analysis of PET TACs. Using a conservative statistical cutoff, BRV enters the brain at least sevenfold faster than LEV.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.