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File:Lurasidone structure.svg
Systematic (IUPAC) name
Clinical data
Routes of
Legal status
Legal status
  • Uncontrolled
CAS Number 367514-87-2
ATC code none
PubChem CID 213046
Chemical data
Formula C28H36N4O2S
Molar mass 492.676 g/mol[[Script error: No such module "String".]]
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Lurasidone (SM-13,496) is an atypical antipsychotic developed by Dainippon Sumitomo Pharma which is currently pending approval for the treatment of schizophrenia and bipolar disorder in the United States.[1] It has completed Phase III clinical trials[2] and an NDA was recently (as of December 30, 2009) submitted to the FDA.[3]

Lurasidone acts as a D2 (Ki = 1.68 nM), 5-HT2A (Ki = 2.03 nM), 5-HT7 (Ki = 0.495 nM), and α2C-adrenergic (Ki = 10.8 nM) receptor antagonist, and 5-HT1A (Ki = 6.75 nM) receptor agonist.[4] It has only weak or negligible actions at the 5-HT2C, α1-adrenergic, H1, and mACh receptors.[4]

In clinical studies, lurasidone alleviates both positive (e.g., hallucinations, delusions) and negative (e.g., apathy, emotional withdrawal) symptoms of schizophrenia without inducing extrapyramidal side effects except for akathisia, despite its potent D2 antagonistic actions.[4][5] It has a relatively well-tolerated side effect profile, with low propensity for extrapyramidal symptoms, QTc interval changes, and weight-, lipid-, and glucose-related adverse effects. Side effects reported in at least 5% of subjects and at least twice the frequency of placebo include akathisia (17.6% vs 3.1% placebo), somnolence (11.7% vs 5.5%), parkinsonism (6.8% vs 0%), and weight gain (5.1% vs 2.4%).[2]

Lurasidone may be exceptionally useful for treating cognitive and memory deficits seen in schizophrenia for several reasons: 1) unlike many other antipsychotics, lurasidone does not block the muscarinic acetylcholine receptors, an action well-known to impair learning and memory; 2) lurasidone has prominent activity at 5-HT1A, 5-HT2A, 5-HT7, and α2C-adrenergic receptors, all of which have been implicated in enhancement of cognitive function if modulated properly; 3) due to its low liability for extrapyramidal symptoms, lurasidone is unlikely to require coadministration of anticholinergics, which impair cognition in their own right.[4][5] Indeed, in animal studies, lurasidone was found to be superior to all of the other antipsychotics examined in reversing dizocilpine-induced learning and memory impairment, including risperidone, olanzapine, quetiapine, clozapine, aripiprazole, and haloperidol.[4][6]

See also


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de:Lurasidon ja:ルラシドン
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  2. 2.0 2.1 Dainippon Sumitomo Pharma (August 26, 2009). "Lurasidone Demonstrated Efficacy in Treating Patients with Schizophrenia in Pivotal Phase III Study" (PDF). 
  3. "lurasidone New Drug Application". 
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