ArticlePsychopharmacology2013
Determination of dopamine D₂ receptor occupancy by lurasidone using positron emission tomography in healthy male subjects.
Article in Psychopharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers, 1 of them a synthesis that pooled it.
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Who cites it
9 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Pharmacokinetics and Pharmacodynamics of Lurasidone Hydrochloride, a Second-Generation Antipsychotic: A Systematic Review of the Published Literature.Clinical pharmacokinetics · 2017Pooled it
- Clinical efficacy and safety of vortioxetine as an adjuvant drug for patients with bipolar depression.Journal of Zhejiang University. Science. B · 2025Trial
- Dopamine DNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2019Trial
- Estimation of target occupancy in repeated dosing design studies using positron emission tomography: Biases due to target upregulation.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2024Article
- Can Isolated Head Tremors Be an Extrapyramidal Symptom Associated with Lurasidone?-A Case Series.Indian journal of psychological medicine · 2021Article
- Current Limitations and Candidate Potential of 5-HT7 Receptor Antagonism in Psychiatric Pharmacotherapy.Frontiers in psychiatry · 2021Review
- Dopamine Targeting Drugs for the Treatment of Schizophrenia: Past, Present and Future.Current topics in medicinal chemistry · 2016Review
- ITI-007 demonstrates brain occupancy at serotonin 5-HT₂A and dopamine D₂ receptors and serotonin transporters using positron emission tomography in healthy volunteers.Psychopharmacology · 2015Article
- Management of bipolar I depression: clinical utility of lurasidone.Therapeutics and clinical risk management · 2015Review
Corrections and comments
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Authors and funding
7 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
rationaleA positron emission tomography (PET) study of dopamine D₂ receptor occupancy was conducted to support a rational dose selection for clinical efficacy studies with lurasidone, an atypical antipsychotic that was approved for the treatment of schizophrenia by the FDA in late 2010.
objectivesTo determine the dopamine D₂ receptor occupancy of lurasidone in the ventral striatum, putamen and caudate nucleus, and to characterize the relationship between lurasidone serum concentration and D₂ receptor occupancy.
methodsA single oral dose of lurasidone (10, 20, 40, 60, or 80 mg) was administered sequentially to healthy male subjects (n = 4 in each cohort). Two PET scans were performed. For each scan, 20 mCi of [¹¹C]raclopride was administered intravenously as a bolus injection, followed immediately by 90 min of PET scan acquisitions.
resultsThe D₂ receptor occupancy levels were 41-43% for 10 mg, 51-55% for 20 mg, 63-67% for 40 mg, 77-84% for 60 mg, and 73-79% for 80 mg of lurasidone. The relationship between D₂ receptor occupancy and the mean serum lurasidone concentration during the PET scan (C PET) was similar for the putamen, caudate nucleus, and ventral striatum regions. Mean D₂ receptor occupancy levels correlated well with average peak serum concentration of lurasidone.
conclusionsIn healthy volunteers, single doses of lurasidone 40-80 mg resulted in D₂ receptor occupancy levels of >60%, a level of receptor occupancy previously associated with clinical response for atypical antipsychotics.
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