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Lurasidone

PubChem CID
213046
Structure
Lurasidone_small.png
Lurasidone_3D_Structure.png
Molecular Formula
Synonyms
  • Lurasidone
  • 367514-87-2
  • lurasidona
  • (3aR,4S,7R,7aS)-2-((1R,2R)-2-(4-(1,2-Benzothiazol-3-yl)piperazin-1-ylmethyl)cyclohexylmethyl)hexahydro-4,7-methano-2H-isoindole-1,3-dione
  • Lurasidone [INN]
Molecular Weight
492.7 g/mol
Computed by PubChem 2.2 (PubChem release 2021.10.14)
Dates
  • Create:
    2005-08-09
  • Modify:
    2025-01-18
Description
Lurasidone is an N-arylpiperazine that is (3aR,4S,7R,7aS)-2-{[(1R,2R)-2-(piperazin-1-ylmethyl)cyclohexyl]methyl}hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione in which position N4 of the piperazine ring is substituted by a 1,2-benzothiazol-3-yl group. Lurasidone is used (generally as the hydrochloride salt) as an atypical antipsychotic for the treatment of schizophrenia. It has a role as an adrenergic antagonist, a dopaminergic antagonist, a serotonergic antagonist and a second generation antipsychotic. It is a 1,2-benzisothiazole, a N-arylpiperazine, a bridged compound and a dicarboximide. It is functionally related to a maleimide. It is a conjugate base of a lurasidone(1+).
Lurasidone is an atypical antipsychotic developed by Dainippon Sumitomo Pharma. It was approved by the U.S. Food and Drug Administration (FDA) for treatment of schizophrenia on October 29, 2010 and is currently pending approval for the treatment of bipolar disorder in the United States.
Lurasidone is an Atypical Antipsychotic.

1 Structures

1.1 2D Structure

Chemical Structure Depiction
Lurasidone.png

1.2 3D Conformer

2 Names and Identifiers

2.1 Computed Descriptors

2.1.1 IUPAC Name

(1S,2R,6S,7R)-4-[[(1R,2R)-2-[[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]methyl]cyclohexyl]methyl]-4-azatricyclo[5.2.1.02,6]decane-3,5-dione
Computed by Lexichem TK 2.7.0 (PubChem release 2021.10.14)

2.1.2 InChI

InChI=1S/C28H36N4O2S/c33-27-24-18-9-10-19(15-18)25(24)28(34)32(27)17-21-6-2-1-5-20(21)16-30-11-13-31(14-12-30)26-22-7-3-4-8-23(22)35-29-26/h3-4,7-8,18-21,24-25H,1-2,5-6,9-17H2/t18-,19+,20-,21-,24+,25-/m0/s1
Computed by InChI 1.0.6 (PubChem release 2021.10.14)

2.1.3 InChIKey

PQXKDMSYBGKCJA-CVTJIBDQSA-N
Computed by InChI 1.0.6 (PubChem release 2021.10.14)

2.1.4 SMILES

C1CC[C@H]([C@@H](C1)CN2CCN(CC2)C3=NSC4=CC=CC=C43)CN5C(=O)[C@H]6[C@@H]7CC[C@@H](C7)[C@H]6C5=O
Computed by OEChem 2.3.0 (PubChem release 2024.12.12)

2.2 Molecular Formula

C28H36N4O2S
Computed by PubChem 2.2 (PubChem release 2021.10.14)

2.3 Other Identifiers

2.3.1 CAS

2.3.2 European Community (EC) Number

2.3.3 UNII

2.3.4 ChEBI ID

2.3.5 ChEMBL ID

2.3.6 DrugBank ID

2.3.7 DSSTox Substance ID

2.3.8 Metabolomics Workbench ID

2.3.9 NCI Thesaurus Code

2.3.10 Nikkaji Number

2.3.11 PharmGKB ID

2.3.12 Pharos Ligand ID

2.3.13 RXCUI

2.3.14 Wikidata

2.3.15 Wikipedia

2.4 Synonyms

2.4.1 MeSH Entry Terms

  • 13496, SM
  • HCl, Lurasidone
  • Hydrochloride, Lurasidone
  • latuda
  • lurasidone
  • Lurasidone HCl
  • Lurasidone Hydrochloride
  • N-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinylmethyl)-1-cyclohexylmethyl)-2,3-bicyclo(2.2.1)heptanedicarboximide
  • SM 13,496
  • SM 13496
  • SM-13,496
  • SM-13496
  • SM13,496
  • SM13496

2.4.2 Depositor-Supplied Synonyms

3 Chemical and Physical Properties

3.1 Computed Properties

Property Name
Molecular Weight
Property Value
492.7 g/mol
Reference
Computed by PubChem 2.2 (PubChem release 2021.10.14)
Property Name
XLogP3-AA
Property Value
5.4
Reference
Computed by XLogP3 3.0 (PubChem release 2021.10.14)
Property Name
Hydrogen Bond Donor Count
Property Value
0
Reference
Computed by Cactvs 3.4.8.18 (PubChem release 2021.10.14)
Property Name
Hydrogen Bond Acceptor Count
Property Value
6
Reference
Computed by Cactvs 3.4.8.18 (PubChem release 2021.10.14)
Property Name
Rotatable Bond Count
Property Value
5
Reference
Computed by Cactvs 3.4.8.18 (PubChem release 2021.10.14)
Property Name
Exact Mass
Property Value
492.25589758 Da
Reference
Computed by PubChem 2.2 (PubChem release 2021.10.14)
Property Name
Monoisotopic Mass
Property Value
492.25589758 Da
Reference
Computed by PubChem 2.2 (PubChem release 2021.10.14)
Property Name
Topological Polar Surface Area
Property Value
85 Ų
Reference
Computed by Cactvs 3.4.8.18 (PubChem release 2021.10.14)
Property Name
Heavy Atom Count
Property Value
35
Reference
Computed by PubChem
Property Name
Formal Charge
Property Value
0
Reference
Computed by PubChem
Property Name
Complexity
Property Value
804
Reference
Computed by Cactvs 3.4.8.18 (PubChem release 2021.10.14)
Property Name
Isotope Atom Count
Property Value
0
Reference
Computed by PubChem
Property Name
Defined Atom Stereocenter Count
Property Value
6
Reference
Computed by PubChem
Property Name
Undefined Atom Stereocenter Count
Property Value
0
Reference
Computed by PubChem
Property Name
Defined Bond Stereocenter Count
Property Value
0
Reference
Computed by PubChem
Property Name
Undefined Bond Stereocenter Count
Property Value
0
Reference
Computed by PubChem
Property Name
Covalently-Bonded Unit Count
Property Value
1
Reference
Computed by PubChem
Property Name
Compound Is Canonicalized
Property Value
Yes
Reference
Computed by PubChem (release 2021.10.14)

3.2 Experimental Properties

3.2.1 Flash Point

9.7 °C (49.5 °F) - closed cup
Sigma-Aldrich; Material Safety Data Sheet for Lurasidone hydrochloride solution, Product Number: L-030, Version 5.3 (Revision Date 08/14/2014). Available from, as of September 1, 2015: https://www.sigmaaldrich.com/safety-center.html

3.2.2 Stability / Shelf Life

Stable under recommended storage conditions.
Sigma-Aldrich; Material Safety Data Sheet for Lurasidone hydrochloride solution, Product Number: L-030, Version 5.3 (Revision Date 08/14/2014). Available from, as of September 1, 2015: https://www.sigmaaldrich.com/safety-center.html

3.2.3 Other Experimental Properties

White to off-white powder; MP 215-217 °C; sparingly soluble in methanol; slightly soluble in ethanol; very slightly soluble in acetone, water; practically insoluble in 0.1 N HCl, toluene /Lurasidone hydrochloride/
O'Neil, M.J. (ed.). The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. Cambridge, UK: Royal Society of Chemistry, 2013., p. 1044

3.3 Chemical Classes

3.3.1 Drugs

Pharmaceuticals -> Listed in ZINC15
S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
3.3.1.1 Human Drugs
Breast Feeding; Lactation; Milk, Human; Antipsychotic Agents
Human drugs -> Psycholeptics -> Human pharmacotherapeutic group -> EMA Drug Category

5 Chemical Vendors

6 Drug and Medication Information

6.1 Drug Indication

Lurasidone is indicated for the treatment of schizophrenia in patients ≥13 years old. It is also indicated as a monotherapy for the treatment of bipolar depression in patients ≥10 years old, or in combination with lithium or valproate for the treatment of bipolar depression in adults.
Treatment of schizophrenia in adults aged 18 years and over.

6.2 LiverTox Summary

Lurasidone is a second generation (atypical) antipsychotic agent that is used in the treatment of schizophrenia and bipolar depression. Lurasidone is associated with a low rate of serum aminotransferase elevations during therapy but has not been linked to instances of clinically apparent acute liver injury.

6.3 Drug Classes

Breast Feeding; Lactation; Milk, Human; Antipsychotic Agents
Antipsychotic Agents

6.4 Clinical Trials

6.4.1 ClinicalTrials.gov

6.4.2 EU Clinical Trials Register

6.4.3 NIPH Clinical Trials Search of Japan

6.5 EMA Drug Information

Medicine
Category
Human drugs
Therapeutic area
Schizophrenia
Active Substance
lurasidone
INN/Common name
lurasidone
Pharmacotherapeutic Classes
Psycholeptics
Status
This medicine is authorized for use in the European Union
Company
Aziende Chimiche Riunite Angelini Francesco S.p.A.
Market Date
2014-03-21

6.6 Therapeutic Uses

Latuda is indicated for the treatment of patients with schizophrenia. /Included in US product label/
NIH; DailyMed. Current Medication Information for Latuda (Lurasidone Hydrochloride) Tablet, Film Coated (Revised: July 2013). Available from, as of December 31, 2014: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=afad3051-9df2-4c54-9684-e8262a133af8
Latuda is indicated as monotherapy for the treatment of patients with major depressive episodes associated with bipolar I disorder (bipolar depression). /Included in US product label/
NIH; DailyMed. Current Medication Information for Latuda (Lurasidone Hydrochloride) Tablet, Film Coated (Revised: July 2013). Available from, as of December 31, 2014: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=afad3051-9df2-4c54-9684-e8262a133af8
Latuda is indicated as adjunctive therapy with either lithium or valproate for the treatment of patients with major depressive episodes associated with bipolar I disorder (bipolar depression). /Included in US product label/
NIH; DailyMed. Current Medication Information for Latuda (Lurasidone Hydrochloride) Tablet, Film Coated (Revised: July 2013). Available from, as of December 31, 2014: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=afad3051-9df2-4c54-9684-e8262a133af8
The efficacy of Latuda in the treatment of mania associated with bipolar disorder has not been established.
NIH; DailyMed. Current Medication Information for Latuda (Lurasidone Hydrochloride) Tablet, Film Coated (Revised: July 2013). Available from, as of December 31, 2014: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=afad3051-9df2-4c54-9684-e8262a133af8
The effectiveness of Latuda for longer-term use, that is, for more than 6 weeks, has not been established in controlled studies. Therefore, the physician who elects to use Latuda for extended periods should periodically re-evaluate the long-term usefulness of the drug for the individual patient
NIH; DailyMed. Current Medication Information for Latuda (Lurasidone Hydrochloride) Tablet, Film Coated (Revised: July 2013). Available from, as of December 31, 2014: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=afad3051-9df2-4c54-9684-e8262a133af8

6.7 Drug Warnings

/BOXED WARNING/ WARNINGS: INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS; AND SUICIDAL THOUGHTS AND BEHAVIORS. Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Latuda is not approved for use in patients with dementia-related psychosis. Antidepressants increased the risk of suicidal thoughts and behavior in children, adolescents, and young adults in short-term studies. These studies did not show an increase in the risk of suicidal thoughts and behavior with antidepressant use in patients over age 24; there was a reduction in risk with antidepressant use in patients aged 65 and older. In patients of all ages who are started on antidepressant therapy, monitor closely for worsening, and for emergence of suicidal thoughts and behaviors. Advise families and caregivers of the need for close observation and communication with the prescriber.
NIH; DailyMed. Current Medication Information for Latuda (Lurasidone Hydrochloride) Tablet, Film Coated (Revised: July 2013). Available from, as of December 31, 2014: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=afad3051-9df2-4c54-9684-e8262a133af8
Contraindications: Known hypersensitivity to lurasidone hydrochloride or any components in the formulation. Angioedema has been reported. Concurrent administration of strong cytochrome P-450 (CYP) isoenzyme 3A4 (CYP3A4) inhibitors (e.g., ketoconazole) or strong CYP3A4 inducers (e.g., rifampin).
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2457
Geriatric patients with dementia-related psychosis treated with antipsychotic drugs appear to be at an increased risk of death. Analyses of 17 placebo-controlled trials (modal duration of 10 weeks) revealed an approximate 1.6- to 1.7-fold increase in mortality among geriatric patients receiving atypical antipsychotic drugs (i.e., aripiprazole, olanzapine, quetiapine, risperidone) compared with that observed in patients receiving placebo. Over the course of a typical 10-week controlled trial, the rate of death in drug-treated patients was about 4.5% compared with a rate of about 2.6% in the placebo group. Although the causes of death were varied, most of the deaths appeared to be either cardiovascular (e.g., heart failure, sudden death) or infectious (e.g., pneumonia) in nature. Observational studies suggest that, similar to atypical antipsychotics, treatment with conventional (first-generation) antipsychotics may increase mortality; the extent to which the findings of increased mortality in observational studies may be attributed to the antipsychotic drug as opposed to some characteristic(s) of the patients remains unclear. The manufacturer states that lurasidone is not approved for the treatment of patients with dementia-related psychosis.
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2457
An increased incidence of adverse cerebrovascular events (cerebrovascular accidents and transient ischemic attacks), including fatalities, has been observed in geriatric patients with dementia-related psychosis treated with certain atypical antipsychotic agents (aripiprazole, olanzapine, risperidone) in placebo-controlled studies. The manufacturer states that lurasidone is not approved for the treatment of patients with dementia-related psychosis.
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2457
For more Drug Warnings (Complete) data for Lurasidone (27 total), please visit the HSDB record page.

7 Pharmacology and Biochemistry

7.1 Pharmacodynamics

Lurasidone is a benzothiazol derivative that is an antagonist and binds with high affinity to Dopamine-2 (D2) (Ki = 0.994 nM), 5-HT2A (Ki = 0.47 nM) receptors, and 5-HT7 receptors (Ki = 0.495 nM). It also binds with moderate affinity to alpha-2C adrenergic receptors (Ki = 10.8 nM) and is a partial agonist at 5-HT1A receptors (Ki = 6.38 nM). Its actions on histaminergic and muscarinic receptors are negligible.

7.2 MeSH Pharmacological Classification

Serotonin 5-HT2 Receptor Antagonists
Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes. (See all compounds classified as Serotonin 5-HT2 Receptor Antagonists.)
Antipsychotic Agents
Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus. (See all compounds classified as Antipsychotic Agents.)
Dopamine D2 Receptor Antagonists
Compounds and drugs that bind to and inhibit or block the activation of DOPAMINE D2 RECEPTORS. (See all compounds classified as Dopamine D2 Receptor Antagonists.)
Adrenergic alpha-2 Receptor Antagonists
Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS. (See all compounds classified as Adrenergic alpha-2 Receptor Antagonists.)

7.3 FDA Pharmacological Classification

FDA UNII
22IC88528T
Active Moiety
LURASIDONE
Pharmacological Classes
Established Pharmacologic Class [EPC] - Atypical Antipsychotic
FDA Pharmacology Summary
Lurasidone is an Atypical Antipsychotic.

7.4 ATC Code

N05AE05

N - Nervous system

N05 - Psycholeptics

N05A - Antipsychotics

N05AE - Indole derivatives

N05AE05 - Lurasidone

7.5 Absorption, Distribution and Excretion

Absorption
Lurasidone is readily absorbed and quickly reaches maximal concentrations (Cmax) within 1-4 hours. When taken with food, there is a two-fold increase in exposure and time to maximal concentration is increased by 0.5-1.5 hours. This occurs regardless of fat or caloric content. Bioavailability = 9-19%.
Route of Elimination
Urine (~9%) and feces (~80%)
Volume of Distribution
6173 L
Clearance
3902 mL/min
Following administration of a single radiolabeled dose of lurasidone, approximately 80 and 9% of the dose is excreted in feces and urine, respectively.
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2459
Lurasidone is rapidly absorbed following oral administration and reaches peak serum concentrations within about 1-3 hours. Approximately 9-19% of an administered dose is absorbed orally. Steady-state concentrations of the drug are achieved within 7 days.
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2459

7.6 Metabolism / Metabolites

Lurasidone is metabolized by CYP3A4 in which its major active metabolite is referred to as ID-14283 (25% of parent exposure). Its two minor metabolites are referred to as ID14326 and ID11614 which make up 3% and 1% of parent exposure respectively. Its two non-active metabolites are referred to as ID-20219 and ID-20220.
Lurasidone is highly bound (99.8%) to serum proteins, including albumin and alpha1-acid glycoprotein. The drug is metabolized mainly via CYP3A4. The major biotransformation pathways are oxidative N-dealkylation, hydroxylation of the norbornane ring, and S-oxidation. Lurasidone is metabolized into 2 active metabolites (ID-14283 and ID-14326) and 2 major inactive metabolites (ID-20219 and ID-20220).
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2459

7.7 Biological Half-Life

40 mg dose= 18 hours 120 mg - 160 mg dose = 29-37 hours

7.8 Mechanism of Action

Lurasidone is an atypical antipsychotic that is a D2 and 5-HT2A (mixed serotonin and dopamine activity) to improve cognition. It is thought that antagonism of serotonin receptors can improve negative symptoms of psychoses and reduce the extrapyramidal side effects that are often associated with typical antipsychotics.
Lurasidone is a benzisothiazol-derivative antipsychotic agent and has been referred to as an atypical or second-generation antipsychotic agent. Lurasidone has also been described as an azapirone-derivative. Although the exact mechanism of action of lurasidone and other antipsychotic agents in schizophrenia is unknown, it has been suggested that the efficacy of lurasidone is mediated through a combination of antagonist activity at central dopamine type 2 (D2) and serotonin type 2 (5-hydroxytryptamine [5-HT2A]) receptors. Lurasidone is an antagonist that exhibits high affinity for D2, 5-HT2A, and 5-HT7 receptors and moderate affinity for a2C-adrenergic receptors in vitro. The drug acts as a partial agonist at 5-HT1A receptors and is an antagonist at alpha2A-adrenergic receptors in vitro. Lurasidone exhibits weak affinity for alpha1-adrenergic receptors and little or no affinity for histamine (H1) receptors and muscarinic (M1) receptors.
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2459

8 Use and Manufacturing

8.1 Uses

THERAPEUTIC CATEGORY: Antipsychotic
O'Neil, M.J. (ed.). The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. Cambridge, UK: Royal Society of Chemistry, 2013., p. 1044
MEDICATION

8.1.1 Use Classification

Human drugs -> Psycholeptics -> Human pharmacotherapeutic group -> EMA Drug Category

8.2 Methods of Manufacturing

Preparation: I. Saji et al., European Patent Office patent 464846; eidem, United States of America patent 5532372 (1992, 1996 both to Sumitomo).
O'Neil, M.J. (ed.). The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. Cambridge, UK: Royal Society of Chemistry, 2013., p. 1044

8.3 Formulations / Preparations

Table: Lurasidone Hydrochloride Preparations
Route of Administration
Oral
Dosage Form
Tablets
Strength
40 mg
Brand or Generic Name (Manufacturer)
Latuda (Sunovion)
Route of Administration
Oral
Dosage Form
Tablets
Strength
80 mg
Brand or Generic Name (Manufacturer)
Latuda (Sunovion)
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2460

9 Safety and Hazards

9.1 Hazards Identification

9.1.1 GHS Classification

1 of 2
View All
Pictogram(s)
Irritant
Health Hazard
Signal
Warning
GHS Hazard Statements

H302+H332 (33.3%): Harmful if swallowed or if inhaled [Warning Acute toxicity, oral; acute toxicity, inhalation]

H302 (33.3%): Harmful if swallowed [Warning Acute toxicity, oral]

H317 (66.7%): May cause an allergic skin reaction [Warning Sensitization, Skin]

H332 (33.3%): Harmful if inhaled [Warning Acute toxicity, inhalation]

H336 (33.3%): May cause drowsiness or dizziness [Warning Specific target organ toxicity, single exposure; Narcotic effects]

H351 (66.7%): Suspected of causing cancer [Warning Carcinogenicity]

H361 (33.3%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]

H413 (33.3%): May cause long lasting harmful effects to aquatic life [Hazardous to the aquatic environment, long-term hazard]

Precautionary Statement Codes

P203, P261, P264, P270, P271, P272, P273, P280, P301+P317, P302+P352, P304+P340, P317, P318, P319, P321, P330, P333+P317, P362+P364, P403+P233, P405, and P501

(The corresponding statement to each P-code can be found at the GHS Classification page.)

ECHA C&L Notifications Summary

Aggregated GHS information provided per 3 reports by companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.

9.1.2 Hazard Classes and Categories

Acute Tox. 4 (33.3%)

Skin Sens. 1 (66.7%)

Acute Tox. 4 (33.3%)

STOT SE 3 (33.3%)

Carc. 2 (66.7%)

Repr. 2 (33.3%)

Aquatic Chronic 4 (33.3%)

9.2 Fire Fighting

9.2.1 Fire Fighting Procedures

Advice for firefighters: Wear self-contained breathing apparatus for firefighting if necessary. Use water spray to cool unopened containers.
Sigma-Aldrich; Material Safety Data Sheet for Lurasidone hydrochloride solution, Product Number: L-030, Version 5.3 (Revision Date 08/14/2014). Available from, as of September 1, 2015: https://www.sigmaaldrich.com/safety-center.html
Suitable extinguishing media: Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide.
Sigma-Aldrich; Material Safety Data Sheet for Lurasidone hydrochloride solution, Product Number: L-030, Version 5.3 (Revision Date 08/14/2014). Available from, as of September 1, 2015: https://www.sigmaaldrich.com/safety-center.html

9.3 Accidental Release Measures

9.3.1 Cleanup Methods

ACCIDENTAL RELEASE MEASURES. Personal precautions, protective equipment and emergency procedures: Wear respiratory protection. Avoid breathing vapours, mist or gas. Ensure adequate ventilation. Remove all sources of ignition. Evacuate personnel to safe areas. Beware of vapours accumulating to form explosive concentrations. Vapours can accumulate in low areas.; Environmental precautions: Prevent further leakage or spillage if safe to do so. Do not let product enter drains.; Methods and materials for containment and cleaning up: Contain spillage, and then collect with an electrically protected vacuum cleaner or by wet-brushing and place in container for disposal according to local regulations.
Sigma-Aldrich; Material Safety Data Sheet for Lurasidone hydrochloride solution, Product Number: L-030, Version 5.3 (Revision Date 08/14/2014). Available from, as of September 1, 2015: https://www.sigmaaldrich.com/safety-center.html

9.3.2 Disposal Methods

SRP: At the time of review, regulatory criteria for small quantity disposal are subject to significant revision, however, household quantities of waste pharmaceuticals may be managed as follows: Mix with wet cat litter or coffee grounds, double bag in plastic, discard in trash.
SRP: Expired or waste pharmaceuticals shall carefully take into consideration applicable DEA, EPA, and FDA regulations. It is not appropriate to dispose by flushing the pharmaceutical down the toilet or discarding to trash. If possible return the pharmaceutical to the manufacturer for proper disposal being careful to properly label and securely package the material. Alternatively, the waste pharmaceutical shall be labeled, securely packaged and transported by a state licensed medical waste contractor to dispose by burial in a licensed hazardous or toxic waste landfill or incinerator.

9.3.3 Preventive Measures

Gloves must be inspected prior to use. Use proper glove removal technique (without touching glove's outer surface) to avoid skin contact with this product. Dispose of contaminated gloves after use in accordance with applicable laws and good laboratory practices. Wash and dry hands.
Sigma-Aldrich; Material Safety Data Sheet for Lurasidone hydrochloride solution, Product Number: L-030, Version 5.3 (Revision Date 08/14/2014). Available from, as of September 1, 2015: https://www.sigmaaldrich.com/safety-center.html
Appropriate engineering controls: Avoid contact with skin, eyes and clothing. Wash hands before breaks and immediately after handling the product.
Sigma-Aldrich; Material Safety Data Sheet for Lurasidone hydrochloride solution, Product Number: L-030, Version 5.3 (Revision Date 08/14/2014). Available from, as of September 1, 2015: https://www.sigmaaldrich.com/safety-center.html
Precautions for safe handling: Avoid contact with skin and eyes. Avoid inhalation of vapour or mist. Use explosion-proof equipment.Keep away from sources of ignition - No smoking.Take measures to prevent the build up of electrostatic charge.
Sigma-Aldrich; Material Safety Data Sheet for Lurasidone hydrochloride solution, Product Number: L-030, Version 5.3 (Revision Date 08/14/2014). Available from, as of September 1, 2015: https://www.sigmaaldrich.com/safety-center.html

9.4 Handling and Storage

9.4.1 Storage Conditions

Conditions for safe storage, including any incompatibilities: Keep container tightly closed in a dry and well-ventilated place. Containers which are opened must be carefully resealed and kept upright to prevent leakage. Recommended storage temperature -20 °C
Sigma-Aldrich; Material Safety Data Sheet for Lurasidone hydrochloride solution, Product Number: L-030, Version 5.3 (Revision Date 08/14/2014). Available from, as of September 1, 2015: https://www.sigmaaldrich.com/safety-center.html

9.5 Exposure Control and Personal Protection

9.5.1 Personal Protective Equipment (PPE)

Respiratory protection: Where risk assessment shows air-purifying respirators are appropriate use a full-face respirator with multipurpose combination (US) or type ABEK (EN 14387) respirator cartridges as a backup to engineering controls. If the respirator is the sole means of protection, use a full-face supplied air respirator. Use respirators and components tested and approved under appropriate government standards such as NIOSH (US) or CEN (EU).
Sigma-Aldrich; Material Safety Data Sheet for Lurasidone hydrochloride solution, Product Number: L-030, Version 5.3 (Revision Date 08/14/2014). Available from, as of September 1, 2015: https://www.sigmaaldrich.com/safety-center.html
Body Protection: Complete suit protecting against chemicals, Flame retardant antistatic protective clothing., The type of protective equipment must be selected according to the concentration and amount of the dangerous substance at the specific workplace.
Sigma-Aldrich; Material Safety Data Sheet for Lurasidone hydrochloride solution, Product Number: L-030, Version 5.3 (Revision Date 08/14/2014). Available from, as of September 1, 2015: https://www.sigmaaldrich.com/safety-center.html
Skin protection: Handle with gloves.
Sigma-Aldrich; Material Safety Data Sheet for Lurasidone hydrochloride solution, Product Number: L-030, Version 5.3 (Revision Date 08/14/2014). Available from, as of September 1, 2015: https://www.sigmaaldrich.com/safety-center.html
Eye/face protection: Face shield and safety glasses Use equipment for eye protection tested and approved under appropriate government standards such as NIOSH (US) or EN 166(EU).
Sigma-Aldrich; Material Safety Data Sheet for Lurasidone hydrochloride solution, Product Number: L-030, Version 5.3 (Revision Date 08/14/2014). Available from, as of September 1, 2015: https://www.sigmaaldrich.com/safety-center.html

9.6 Stability and Reactivity

9.6.1 Hazardous Reactivities and Incompatibilities

Incompatible materials: Acids, Oxidizing agents, Alkali metals, Strong oxidizing agents, Strong acids, Acid chlorides, Acid anhydrides, Reducing agents, Strong reducing agents, Phosphorus halides
Sigma-Aldrich; Material Safety Data Sheet for Lurasidone hydrochloride solution, Product Number: L-030, Version 5.3 (Revision Date 08/14/2014). Available from, as of September 1, 2015: https://www.sigmaaldrich.com/safety-center.html

9.7 Regulatory Information

REACH Registered Substance

9.7.1 FDA Requirements

The Approved Drug Products with Therapeutic Equivalence Evaluations identifies currently marketed prescription drug products, including lurasidone hydrochloride, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act. /Lurasidone hydrochloride/
DHHS/FDA; Electronic Orange Book-Approved Drug Products with Therapeutic Equivalence Evaluations. Available from, as of March 6, 2015: https://www.fda.gov/cder/ob/

9.8 Other Safety Information

9.8.1 Other Hazardous Reactions

Possibility of hazardous reactions: Vapours may form explosive mixture with air.
Sigma-Aldrich; Material Safety Data Sheet for Lurasidone hydrochloride solution, Product Number: L-030, Version 5.3 (Revision Date 08/14/2014). Available from, as of September 1, 2015: https://www.sigmaaldrich.com/safety-center.html

10 Toxicity

10.1 Toxicological Information

10.1.1 Toxicity Summary

IDENTIFICATION AND USE: Lurasidone is indicated for the treatment of patients with schizophrenia, as monotherapy for the treatment of patients with major depressive episodes associated with bipolar I disorder (bipolar depression), and as adjunctive therapy with either lithium or valproate for the treatment of patients with major depressive episodes associated with bipolar I disorder (bipolar depression). HUMAN EXPOSURE AND TOXICITY: An increased incidence of adverse cerebrovascular events (cerebrovascular accidents and transient ischemic attacks), including fatalities, has been observed in geriatric patients with dementia-related psychosis treated with certain atypical antipsychotic agents (aripiprazole, olanzapine, risperidone) in placebo-controlled studies. The manufacturer states that lurasidone is not approved for the treatment of patients with dementia-related psychosis. Neuroleptic malignant syndrome (NMS), a potentially fatal syndrome requiring immediate discontinuance of the drug and intensive symptomatic treatment, has been reported in patients receiving antipsychotic agents, including lurasidone. Rash and pruritus have been reported frequently and angioedema has been reported rarely in patients receiving lurasidone. Adverse effects occurring in 5% or more of patients receiving lurasidone for schizophrenia and at a frequency at least twice that reported with placebo include somnolence (including hypersomnia, hypersomnolence, and sedation), akathisia, nausea, parkinsonism, and agitation. Akathisia and somnolence appear to be dose-related adverse effects.The effect of lurasidone on labor and delivery is unknown. It is not known whether lurasidone and/or its metabolites are distributed into milk in humans. In geriatric patients (65-85 years of age) with psychosis, serum lurasidone concentrations were similar to those observed in younger adults. Geriatric patients with dementia-related psychosis treated with lurasidone are at an increased risk of death compared with those treated with placebo. Safety and effectiveness of lurasidone in pediatric and adolescent patients have not been established. ANIMAL STUDIES: Lurasidone increased the incidence of mammary gland carcinomas in females rats orally dosed at 12 and 36 mg/kg/day: the lowest dose; 3 mg/kg/day is the no-effect dose which produced plasma levels (AUC) 0.4-times those in humans receiving the MRHD. No increases in tumors were seen in male rats up to the highest dose tested, which produced plasma levels (AUC) 6-times those in humans receiving the MRHD. Lurasidone is distributed into milk in rats. Estrus cycle irregularities were seen in rats orally administered lurasidone at 1.5, 15 and 150 mg/kg/day for 15 consecutive days prior to mating, during the mating period, and through day 7 of gestation. The no-effect dose is 0.1 mg/kg which is approximately 0.006-times the MRHD of 160 mg/day based on body surface area. Fertility was reduced only at the highest dose, which was reversible after a 14-day drug-free period. The no-effect dose for reduced fertility was 15 mg/kg, which is approximately equal to the MRHD based on body surface area. Lurasidone had no effect on fertility in male rats treated orally with lurasidone for 64 consecutive days prior to mating and during the mating period at doses up to 150 mg/kg/day (9-times the MRHD based on mg/m sq body surface area). The drug did not cause mutation or chromosomal aberration when tested in vitro and in vivo. It was negative in the Ames gene mutation test, the Chinese Hamster Lung (CHL) cells, and in the in vivo mouse bone marrow micronucleus test up to 2000 mg/kg (61 times the MRHD of 160 mg/day based on mg/ sq m body surface area).

10.1.2 Hepatotoxicity

Liver test abnormalities occur in 1% to 3% of patients on long term therapy with lurasidone, but similar rates have been reported with placebo therapy and with comparator agents. The ALT elevations are usually mild, transient and often resolve even without dose modification or drug discontinuation. There have been no published reports of clinically apparent liver injury with symptoms or jaundice attributed to lurasidone therapy.

Likelihood score: E (unlikely cause of clinically apparent liver injury).

10.1.3 Effects During Pregnancy and Lactation

◉ Summary of Use during Lactation

Lurasidone is more than 99% bound to plasma proteins, so it is unlikely that the drug would be excreted into milk in sufficient amounts to affect a breastfed infant. Data from one mother-infant pair appears to support the poor excretion into milk and lack of effect on the breastfed infant. Until more data are available, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.

◉ Effects in Breastfed Infants

A woman with depressive type schizoaffective disorder was taking lurasidone 40 mg at night and desvenlafaxine 50 mg daily after giving birth. She exclusively breastfed her infant. The infant’s growth and development was good during a follow-up period of 39 days.

Patients enlisted in the National Pregnancy Registry for Atypical Antipsychotics who were taking a second-generation antipsychotic drug while breastfeeding (n = 576) were compared to control breastfeeding patients who were not treated with a second-generation antipsychotic (n = 818). Of the patients who were taking a second-generation antipsychotic drug, 60.4% were on more than one psychotropic. A review of the pediatric medical records, no adverse effects were noted among infants exposed or not exposed to second-generation antipsychotic monotherapy or to polytherapy. The number of women taking lurasidone was not reported.

◉ Effects on Lactation and Breastmilk

Increases in serum prolactin with lurasidone are generally infrequent, small and less than risperidone. A woman with elevated serum prolactin, breast tenderness and galactorrhea while taking risperidone improved when lurasidone was substituted for risperidone and these side effects subsided completely when the lurasidone dose was increased from 20 mg to 40 mg daily. The prolactin level in a mother with established lactation may not affect her ability to breastfeed.

Patients enlisted in the National Pregnancy Registry for Atypical Antipsychotics who were taking a second-generation antipsychotic drug while breastfeeding (n = 576) were compared to control breastfeeding patients who had primarily diagnoses of major depressive disorder and anxiety disorders, most often treated with SSRI or SNRI antidepressants, but not with a second-generation antipsychotic (n = 818). Among women on a second-generation antipsychotic, 60.4% were on more than one psychotropic compared with 24.4% among women in the control group. Of the women on a second-generation antipsychotic, 59.3% reported “ever breastfeeding” compared to 88.2% of women in the control group. At 3 months postpartum, 23% of women on a second-generation antipsychotic were exclusively breastfeeding compared to 47% of women in the control group. The number of women taking lurasidone was not reported.

A 14-year-old girl with hallucinatory schizophrenia was treated inadequately with aripiprazole, then paliperidone. As she was transitioned from paliperidone to lurasidone at age 16 years, her serum prolactin increased to 4240 mIU/L (normal range 60-400 mIU/L). As the lurasidone dose was titrated to a maximum of 111 mg daily, prolactin levels continued to increase and the patient experienced breast fullness and galactorrhea. Six of 7 serum prolactin measurements were in the range of 4240 to 6140 mIU/L. Once lurasidone was discontinued, her serum prolactin normalized.

In an Italian study of treatment of schizophrenic patients with lurasidone, 2.4% of patients developed hyperprolactinemia and galactorrhea.

◈ What is lurasidone?

Lurasidone is an antipsychotic medication that has been used to treat schizophrenia and bipolar depression. It is sold under the brand name Latuda®.Sometimes when people find out they are pregnant, they think about changing how they take their medication, or stopping their medication altogether. However, it is important to talk with your healthcare providers before making any changes to how you take this medication. Your healthcare providers can talk with you about the benefits of treating your condition and the risks of untreated illness during pregnancy.

◈ I take lurasidone. Can it make it harder for me to get pregnant?

Studies have not been done in humans to see if lurasidone can make it harder to get pregnant.

◈ Does taking lurasidone increase the chance for miscarriage?

Miscarriage can occur in any pregnancy. Studies have not been done to see if lurasidone can increase the chance for miscarriage.

◈ Does taking lurasidone increase the chance of birth defects?*

Every pregnancy starts out with a 3-5% chance of having a birth defect. This is called the background risk. Information on the use of lurasidone in pregnancy is limited. Animal studies in rats and rabbits have not shown an increased chance of birth defects. In a case report of a person taking lurasidone throughout pregnancy, the baby was born healthy and without birth defects. A study looking at 134 people who used lurasidone in pregnancy found no specific patterns of birth defects.

◈ Does taking lurasidone in pregnancy increase the chance of other pregnancy-related problems?

Studies have not been done to see if lurasidone use in pregnancy increases the chance for pregnancy-related problems such as preterm delivery (birth before week 37) or low birth weight (weighing less than 5 pounds, 8 ounces [2500 grams] at birth).

◈ I need to take lurasidone throughout my entire pregnancy. Will it cause symptoms in my baby after birth?

Product labels written by the U.S. Food and Drug Administration (FDA) note a chance for symptoms in newborns exposed to antipsychotic drugs in the third trimester of pregnancy. Symptoms may include uncontrolled muscle movements, changes in muscle tone, being too sleepy, trouble with breathing, and/or trouble with feeding. Not all babies who are exposed to antipsychotic drugs during pregnancy will have these symptoms. These symptoms can be temporary and can go away on their own. Treatment of symptoms can be started, if needed.These symptoms have not been reported with exposure to lurasidone during pregnancy. The available information on the use of lurasidone in pregnancy is so limited that it is hard to know if these symptoms might happen. Let your healthcare providers know before delivery if you are taking lurasidone. If needed, babies can be monitored for symptoms.

◈ Does taking lurasidone in pregnancy affect future behavior or learning for the child?

Studies have not been done to see if lurasidone use in pregnancy can cause behavior or learning issues for the child.

◈ Breastfeeding while taking lurasidone:

Information on the use of lurasidone while breastfeeding is limited. There is a report of one person who was taking lurasidone while breastfeeding. No negative effects were reported in the nursing child. The benefit of using lurasidone may outweigh possible risks. Your healthcare providers can talk with you about using lurasidone and what treatment is best for you. Be sure to talk to your healthcare provider about all your breastfeeding questions.

◈ If a male takes lurasidone, could it affect fertility (ability to get partner pregnant) or increase the chance of birth defects?

Studies have not been done in humans to see if lurasidone could affect fertility or increase the chance of birth defects above the background risk. In general, exposures that fathers or sperm donors have are unlikely to increase the risks to a pregnancy. For more information, please see the MotherToBaby fact sheet Paternal Exposures at https://mothertobaby.org/fact-sheets/paternal-exposures-pregnancy/.

10.1.4 Interactions

Lurasidone is not a substrate for CYP1A2 in vitro; therefore, smoking should not alter the pharmacokinetics of the drug.
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2459
Concomitant administration of rifampin (600 mg daily for 8 days), a strong CYP3A4 inducer, and lurasidone (single 40-mg dose) decreased peak serum lurasidone concentrations and AUCs by approximately 86 and 80%, respectively. Rifampin should not be concurrently administered with lurasidone.
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2459
Concomitant administration of lurasidone (40 mg daily at steady state) with an oral contraceptive containing ethinyl estradiol and norgestimate resulted in equivalent peak plasma concentrations and AUCs of ethinyl estradiol and norgestimate relative to oral contraceptive administration alone. Sex hormone binding globulin concentrations also were not substantially affected by concurrent administration of the drugs. Oral contraceptive dosage adjustment is not required in patients receiving lurasidone concurrently.
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2459
Concomitant administration of lurasidone (120 mg daily at steady state) with a single 5-mg dose of midazolam, a CYP3A4 substrate, increased peak plasma concentrations and AUCs of midazolam by approximately 21 and 44%, respectively. Midazolam dosage adjustment is not required in patients receiving lurasidone concurrently.
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2459
For more Interactions (Complete) data for Lurasidone (11 total), please visit the HSDB record page.

10.1.5 Antidote and Emergency Treatment

/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/
Currance, P.L. Clements, B., Bronstein, A.C. (Eds).; Emergency Care For Hazardous Materials Exposure. 3rd revised edition, Elsevier Mosby, St. Louis, MO 2007, p. 160
/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 mL/kg up to 200 mL of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poisons A and B/
Currance, P.L. Clements, B., Bronstein, A.C. (Eds).; Emergency Care For Hazardous Materials Exposure. 3rd revised edition, Elsevier Mosby, St. Louis, MO 2007, p. 160
/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W TKO /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's (LR) if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poisons A and B/
Currance, P.L. Clements, B., Bronstein, A.C. (Eds).; Emergency Care For Hazardous Materials Exposure. 3rd revised edition, Elsevier Mosby, St. Louis, MO 2007, p. 160-1

10.1.6 Human Toxicity Excerpts

/HUMAN EXPOSURE STUDIES/ The effects of LATUDA on the QTc interval were evaluated in a randomized, double-blind, multiple-dose, parallel-dedicated thorough QT study in 43 patients with schizophrenia or schizoaffective disorder, who were treated with LATUDA doses of 120 mg daily, 600 mg daily and completed the study. The maximum mean (upper 1-sided, 95% CI) increase in baseline-adjusted QTc intervals based on individual correction method (QTcI) was 7.5 (11.7) ms and 4.6 (9.5) ms, for the 120 mg and 600 mg dose groups respectively, observed at 2 to 4 hours after dosing. In this study, there was no apparent dose (exposure)-response relationship. In short-term, placebo-controlled studies in schizophrenia and bipolar depression, no post-baseline QT prolongations exceeding 500 msec were reported in patients treated with LATUDA or placebo.
NIH; DailyMed. Current Medication Information for Latuda (Lurasidone Hydrochloride) Tablet, Film Coated (Revised: July 2013). Available from, as of March 30, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=afad3051-9df2-4c54-9684-e8262a133af8
/SIGNS AND SYMPTOMS/ Known hypersensitivity to lurasidone hydrochloride or any components in the formulation. Angioedema has been reported. Concurrent administration of strong cytochrome P-450 (CYP) isoenzyme 3A4 (CYP3A4) inhibitors (e.g., ketoconazole) or strong CYP3A4 inducers (e.g., rifampin).
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2457
/SIGNS AND SYMPTOMS/ An increased incidence of adverse cerebrovascular events (cerebrovascular accidents and transient ischemic attacks), including fatalities, has been observed in geriatric patients with dementia-related psychosis treated with certain atypical antipsychotic agents (aripiprazole, olanzapine, risperidone) in placebo-controlled studies. The manufacturer states that lurasidone is not approved for the treatment of patients with dementia-related psychosis.
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2457
/SIGNS AND SYMPTOMS/ Neuroleptic malignant syndrome (NMS), a potentially fatal syndrome requiring immediate discontinuance of the drug and intensive symptomatic treatment, has been reported in patients receiving antipsychotic agents, including lurasidone.
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2457
For more Human Toxicity Excerpts (Complete) data for Lurasidone (16 total), please visit the HSDB record page.

10.1.7 Non-Human Toxicity Excerpts

/LABORATORY ANIMALS: Chronic Exposure or Carcinogenicity/ LATUDA increased the incidence of mammary gland carcinomas in females rats orally dosed at 12 and 36 mg/kg/day: the lowest dose; 3 mg/kg/day is the no-effect dose which produced plasma levels (AUC) 0.4-times those in humans receiving the MRHD. No increases in tumors were seen in male rats up to the highest dose tested, which produced plasma levels (AUC) 6-times those in humans receiving the MRHD.
NIH; DailyMed. Current Medication Information for Latuda (Lurasidone Hydrochloride) Tablet, Film Coated (Revised: July 2013). Available from, as of March 30, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=afad3051-9df2-4c54-9684-e8262a133af8
/LABORATORY ANIMALS: Chronic Exposure or Carcinogenicity/ LATUDA increased incidences of malignant mammary gland tumors and pituitary gland adenomas in female mice orally dosed with 30, 100, 300, or 650 mg/kg/day. The lowest dose produced plasma levels (AUC) approximately equal to those in humans receiving the MRHD of 160 mg/day. No increases in tumors were seen in male mice up to the highest dose tested, which produced plasma levels (AUC) 14-times those in humans receiving the MRHD.
NIH; DailyMed. Current Medication Information for Latuda (Lurasidone Hydrochloride) Tablet, Film Coated (Revised: July 2013). Available from, as of March 30, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=afad3051-9df2-4c54-9684-e8262a133af8
/LABORATORY ANIMALS: Developmental or Reproductive Toxicity/ Estrus cycle irregularities were seen in rats orally administered LATUDA at 1.5, 15 and 150 mg/kg/day for 15 consecutive days prior to mating, during the mating period, and through day 7 of gestation. The no-effect dose is 0.1 mg/kg which is approximately 0.006-times the MRHD of 160 mg/day based on body surface area. Fertility was reduced only at the highest dose, which was reversible after a 14-day drug-free period. The no-effect dose for reduced fertility was 15 mg/kg, which is approximately equal to the MRHD based on body surface area. LATUDA had no effect on fertility in male rats treated orally with LATUDA for 64 consecutive days prior to mating and during the mating period at doses up to 150 mg/kg/day (9-times the MRHD based on mg/m sq body surface area).
NIH; DailyMed. Current Medication Information for Latuda (Lurasidone Hydrochloride) Tablet, Film Coated (Revised: July 2013). Available from, as of March 30, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=afad3051-9df2-4c54-9684-e8262a133af8
/GENOTOXICITY/ LATUDA did not cause mutation or chromosomal aberration when tested in vitro and in vivo. LATUDA was negative in the Ames gene mutation test, the Chinese Hamster Lung (CHL) cells, and in the in vivo mouse bone marrow micronucleus test up to 2000 mg/kg (61 times the MRHD of 160 mg/day based on mg/sq m body surface area).
NIH; DailyMed. Current Medication Information for Latuda (Lurasidone Hydrochloride) Tablet, Film Coated (Revised: July 2013). Available from, as of March 30, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=afad3051-9df2-4c54-9684-e8262a133af8

10.1.8 Populations at Special Risk

Esophageal dysmotility and aspiration have been associated with the use of antipsychotic agents. Aspiration pneumonia is a common cause of morbidity and mortality in geriatric patients, particularly in those with advanced Alzheimer's dementia. Lurasidone is not approved for the treatment of patients with dementia-related psychosis and should not be used in patients at risk for aspiration pneumonia.
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2458
Neonates exposed to antipsychotic agents during the third trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms following delivery. Symptoms reported to date have included agitation, hypertonia, hypotonia, tardive dyskinetic-like symptoms, tremor, somnolence, respiratory distress, and feeding disorder. Neonates exhibiting such symptoms should be monitored. The complications have varied in severity; some neonates recovered within hours to days without specific treatment while others have required intensive care unit support and prolonged hospitalization. The effect of lurasidone on labor and delivery is unknown.
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2459
Similar to other antipsychotic agents and drugs with dopamine D2 antagonistic activity, lurasidone can elevate serum prolactin concentrations. In short-term clinical trials, the median change from baseline to end point in prolactin concentrations for lurasidone-treated patients was an increase of 1.1 mg/mL compared with a decrease of 0.6 mg/mL in the placebo group. The increase in prolactin was greater in female patients. The proportion of patients with prolactin elevations 5 or more times the upper limit of normal was 3.6% for lurasidone-treated patients compared with 0.7% for placebo recipients. Clinical disturbances such as galactorrhea, amenorrhea, gynecomastia, and impotence have been associated with prolactin-elevating drugs. In addition, chronic hyperprolactinemia associated with hypogonadism may lead to decreased bone density in both female and male patients. If lurasidone therapy is considered in a patient with previously detected breast cancer, clinicians should consider that approximately one-third of human breast cancers are prolactin-dependent in vitro.
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2458
In short-term clinical trials, seizures occurred in less than 0.1% of patients receiving lurasidone compared with 0.2% of patients receiving placebo. As with other antipsychotic agents, lurasidone should be used with caution in patients with a history of seizures or with conditions that may lower the seizure threshold (e.g., dementia of the Alzheimer's type); conditions that lower the seizure threshold may be more prevalent in patients 65 years of age or older.
American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 2458
For more Populations at Special Risk (Complete) data for Lurasidone (7 total), please visit the HSDB record page.

10.1.9 Protein Binding

~99% bound to serum proteins.

11 Associated Disorders and Diseases

12 Literature

12.1 Consolidated References

12.2 NLM Curated PubMed Citations

12.3 Chemical Co-Occurrences in Literature

12.4 Chemical-Gene Co-Occurrences in Literature

12.5 Chemical-Disease Co-Occurrences in Literature

13 Patents

13.1 Depositor-Supplied Patent Identifiers

13.2 Chemical Co-Occurrences in Patents

13.3 Chemical-Disease Co-Occurrences in Patents

13.4 Chemical-Gene Co-Occurrences in Patents

14 Interactions and Pathways

14.1 Chemical-Target Interactions

14.2 Drug-Drug Interactions

14.3 Drug-Food Interactions

  • Avoid alcohol. The effects of alcohol could be made worse while taking Lurasidone.
  • Avoid grapefruit products. Grapefruit and grapefruit juice may affect the amount of Lurasidone in your blood.
  • Take with food. The manufacturer recommends co-administration with at least 350 calories.

15 Biological Test Results

15.1 BioAssay Results

16 Classification

16.1 MeSH Tree

16.2 NCI Thesaurus Tree

16.3 ChEBI Ontology

16.4 WHO ATC Classification System

16.5 FDA Pharm Classes

16.6 ChemIDplus

16.7 IUPHAR / BPS Guide to PHARMACOLOGY Target Classification

16.8 ChEMBL Target Tree

16.9 UN GHS Classification

16.10 NORMAN Suspect List Exchange Classification

16.11 EPA DSSTox Classification

16.12 MolGenie Organic Chemistry Ontology

17 Information Sources

  1. CAS Common Chemistry
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    https://creativecommons.org/licenses/by-nc/4.0/
  2. ChemIDplus
    ChemIDplus Chemical Information Classification
    https://pubchem.ncbi.nlm.nih.gov/source/ChemIDplus
  3. DrugBank
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    Creative Common's Attribution-NonCommercial 4.0 International License (http://creativecommons.org/licenses/by-nc/4.0/legalcode)
    https://www.drugbank.ca/legal/terms_of_use
  4. EPA DSSTox
    CompTox Chemicals Dashboard Chemical Lists
    https://comptox.epa.gov/dashboard/chemical-lists/
  5. European Chemicals Agency (ECHA)
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    https://echa.europa.eu/web/guest/legal-notice
    (1R,2S,6R,7S)-4-{[(1R,2R)-2-{[4-(1,2-benzothiazol-3- yl)piperazin-1-yl]methyl}-cyclohexyl]methyl}-4- azatricyclo[5.2.1.0^{2,6}]decane-3,5-dione
    https://chem.echa.europa.eu/100.225.187
    (1R,2S,6R,7S)-4-{[(1R,2R)-2-{[4-(1,2-benzothiazol-3- yl)piperazin-1-yl]methyl}-cyclohexyl]methyl}-4- azatricyclo[5.2.1.0^{2,6}]decane-3,5-dione (EC: 696-042-8)
    https://echa.europa.eu/information-on-chemicals/cl-inventory-database/-/discli/details/231388
  6. FDA Global Substance Registration System (GSRS)
    LICENSE
    Unless otherwise noted, the contents of the FDA website (www.fda.gov), both text and graphics, are not copyrighted. They are in the public domain and may be republished, reprinted and otherwise used freely by anyone without the need to obtain permission from FDA. Credit to the U.S. Food and Drug Administration as the source is appreciated but not required.
    https://www.fda.gov/about-fda/about-website/website-policies#linking
  7. Hazardous Substances Data Bank (HSDB)
  8. ChEBI
  9. FDA Pharm Classes
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    Unless otherwise noted, the contents of the FDA website (www.fda.gov), both text and graphics, are not copyrighted. They are in the public domain and may be republished, reprinted and otherwise used freely by anyone without the need to obtain permission from FDA. Credit to the U.S. Food and Drug Administration as the source is appreciated but not required.
    https://www.fda.gov/about-fda/about-website/website-policies#linking
  10. LiverTox
  11. Open Targets
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    Datasets generated by the Open Targets Platform are freely available for download.
    https://platform-docs.opentargets.org/licence
  12. ChEMBL
    LICENSE
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    http://www.ebi.ac.uk/Information/termsofuse.html
  13. ClinicalTrials.gov
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    https://clinicaltrials.gov/ct2/about-site/terms-conditions#Use
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    https://www.ema.europa.eu/en/about-us/legal-notice
  15. IUPHAR/BPS Guide to PHARMACOLOGY
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    https://www.guidetopharmacology.org/about.jsp#license
    Guide to Pharmacology Target Classification
    https://www.guidetopharmacology.org/targets.jsp
  16. Drugs and Lactation Database (LactMed)
  17. Mother To Baby Fact Sheets
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    https://www.ncbi.nlm.nih.gov/books/about/copyright/
  18. EU Clinical Trials Register
  19. WHO Anatomical Therapeutic Chemical (ATC) Classification
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    https://www.whocc.no/copyright_disclaimer/
  20. Japan Chemical Substance Dictionary (Nikkaji)
  21. Metabolomics Workbench
  22. NCI Thesaurus (NCIt)
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    https://www.cancer.gov/policies/copyright-reuse
  23. NIPH Clinical Trials Search of Japan
  24. NLM RxNorm Terminology
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    https://www.nlm.nih.gov/research/umls/rxnorm/docs/termsofservice.html
  25. NORMAN Suspect List Exchange
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    https://creativecommons.org/licenses/by/4.0/
    lurasidone hydrochloride
    NORMAN Suspect List Exchange Classification
    https://www.norman-network.com/nds/SLE/
  26. PharmGKB
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    https://www.pharmgkb.org/page/policies
  27. Pharos
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  28. Wikidata
  29. Wikipedia
  30. Medical Subject Headings (MeSH)
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    Serotonin 5-HT2 Receptor Antagonists
    https://www.ncbi.nlm.nih.gov/mesh/68058830
    Dopamine D2 Receptor Antagonists
    https://www.ncbi.nlm.nih.gov/mesh/68065127
    Adrenergic alpha-2 Receptor Antagonists
    https://www.ncbi.nlm.nih.gov/mesh/68058669
  31. PubChem
  32. GHS Classification (UNECE)
  33. MolGenie
    MolGenie Organic Chemistry Ontology
    https://github.com/MolGenie/ontology/
  34. NCBI
CONTENTS