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Lurasidone
Systematic (IUPAC) name
(3aR,4S,7R,7aS)-2-[((1 R,2R)-2-{[4-(1,2-benzisothiazol-3-yl)-piperazin-1-yl]methyl}cyclohexyl)methyl]hexahydro-1 H-4,7-methanisoindol-1,3-dione
Identifiers
CAS number  ?
ATC code none
PubChem 213046
Chemical data
Formula C 28H36N4O2S 
Mol. mass 492.676 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status Uncontrolled
Routes Oral

Lurasidone (SM-13,496) is a psychoactive drug and research chemical under development as an atypical antipsychotic for the treatment of schizophrenia and bipolar disorder by Dainippon Sumitomo Pharma.[1] It is currently in Phase III clinical trials.[2]

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.[3] It has only weak or negligible actions at the 5-HT2C, α1-adrenergic, H1, and mACh receptors.[3]

In clinical studies, lurasidone alleviates both positive (e.g., hallucations, delusions) and negative (e.g., apathy, emotional withdrawal) symptoms of schizophrenia without inducing extrapyramidal side effects, despite its potent D2 antagonistic actions.[3][4] 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.[3][4] 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.[3][5]

References

  1. ^ Meyer JM, Loebel AD, Schweizer E (September 2009). "Lurasidone: a new drug in development for schizophrenia". Expert Opinion on Investigational Drugs. doi:10.1517/13543780903286388. PMID 19780705. http://www.informapharmascience.com/doi/abs/10.1517/13543780903286388.  
  2. ^ a b Dainippon Sumitomo Pharma (August 26, 2009). "Lurasidone Demonstrated Efficacy in Treating Patients with Schizophrenia in Pivotal Phase III Study". http://www.ds-pharma.co.jp/english/news/pdf/ne20090826.pdf.  
  3. ^ a b c d e Ishiyama T, Tokuda K, Ishibashi T, Ito A, Toma S, Ohno Y (October 2007). "Lurasidone (SM-13496), a novel atypical antipsychotic drug, reverses MK-801-induced impairment of learning and memory in the rat passive-avoidance test". European Journal of Pharmacology 572 (2-3): 160–70. doi:10.1016/j.ejphar.2007.06.058. PMID 17662268. http://linkinghub.elsevier.com/retrieve/pii/S0014-2999(07)00737-6.  
  4. ^ a b Nakamura M, Ogasa M, Guarino J, et al. (June 2009). "Lurasidone in the treatment of acute schizophrenia: a double-blind, placebo-controlled trial". The Journal of Clinical Psychiatry 70 (6): 829–36. doi:10.4088/JCP.08m04905. PMID 19497249. http://article.psychiatrist.com/?ContentType=START&ID=10004141.  
  5. ^ Enomoto T, Ishibashi T, Tokuda K, Ishiyama T, Toma S, Ito A (January 2008). "Lurasidone reverses MK-801-induced impairment of learning and memory in the Morris water maze and radial-arm maze tests in rats". Behavioural Brain Research 186 (2): 197–207. doi:10.1016/j.bbr.2007.08.012. PMID 17881065. http://linkinghub.elsevier.com/retrieve/pii/S0166-4328(07)00423-8.  







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