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References

Trials

Economics

Properties

Spectra

Taxonomy

Lurasidone

Targets (6)Enzymes (1)Biointeractions (6)

Identification

Name

Lurasidone

Accession Number

DB08815

Type

Small Molecule

Groups

Approved, Investigational

Description

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. (Wikipedia)

Structure

Similar Structures

Synonyms

Lurasidona
Lurasidone
Lurasidonum

External IDs

SM-13496

Product Ingredients

Ingredient	UNII	CAS	InChI Key
Lurasidone Hydrochloride	O0P4I5851I	367514-88-3	NEKCRUIRPWNMLK-SCIYSFAVSA-N

Product Images

Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Latuda	Tablet	20 mg	Oral	Sunovion	2014-04-09	Not applicable
Latuda	Tablet, film coated	60 mg/1	Oral	Sunovion Pharmaceuticals Inc.	2013-07-12	Not applicable
Latuda	Tablet	120 mg	Oral	Sunovion	2012-09-06	Not applicable
Latuda	Tablet, film coated	20 mg/1	Oral	Sunovion Pharmaceuticals Inc.	2011-12-07	Not applicable
Latuda	Tablet	40 mg	Oral	Sunovion	2012-09-06	Not applicable
Latuda	Tablet, film coated	80 mg/1	Oral	Bushu Pharmaceutical, LTD.	2010-10-28	Not applicable
Latuda	Tablet, film coated	120 mg/1	Oral	Sunovion Pharmaceuticals Inc.	2012-04-26	Not applicable
Latuda	Tablet	80 mg	Oral	Sunovion	2012-09-05	Not applicable
Latuda	Tablet, film coated	40 mg/1	Oral	Avera McKennan Hospital	2015-03-02	2018-06-07
Latuda	Tablet, film coated	40 mg/1	Oral	Bushu Pharmaceutical, LTD.	2010-10-28	Not applicable

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Lurasidone Hydrochloride	Tablet, coated	120 mg/1	Oral	Amneal Pharmaceuticals LLC	2019-01-03	Not applicable
Lurasidone Hydrochloride	Tablet, coated	60 mg/1	Oral	Amneal Pharmaceuticals LLC	2019-01-03	Not applicable
Lurasidone Hydrochloride	Tablet, coated	20 mg/1	Oral	Amneal Pharmaceuticals LLC	2019-01-03	Not applicable
Lurasidone Hydrochloride	Tablet, coated	40 mg/1	Oral	Amneal Pharmaceuticals LLC	2019-01-03	Not applicable
Lurasidone Hydrochloride	Tablet, coated	80 mg/1	Oral	Amneal Pharmaceuticals LLC	2019-01-03	Not applicable

Categories

UNII

22IC88528T

CAS number

367514-87-2

Weight

Average: 492.676
Monoisotopic: 492.255897106

Chemical Formula

C₂₈H₃₆N₄O₂S

InChI Key

PQXKDMSYBGKCJA-CVTJIBDQSA-N

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

IUPAC Name

(1R,2S,6R,7S)-4-{[(1R,2R)-2-{[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]methyl}cyclohexyl]methyl}-4-azatricyclo[5.2.1.0²,⁶]decane-3,5-dione

SMILES

O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1C[C@@H]1CCCC[C@H]1CN1CCN(CC1)C1=NSC2=CC=CC=C12

Pharmacology

Indication

Treatment of schizophrenia.

Associated Conditions

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.

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.

Target	Actions	Organism
AD(2) dopamine receptor	antagonist	Humans
A5-hydroxytryptamine receptor 2A	antagonist	Humans
U5-hydroxytryptamine receptor 7	antagonist	Humans
U5-hydroxytryptamine receptor 1A	antagonist	Humans
UAlpha-2C adrenergic receptor	antagonist	Humans
UAlpha-2A adrenergic receptor	Not Available	Humans

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%.

Volume of distribution

6173 L

Protein binding

~99% bound to serum proteins.

Metabolism

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.

Route of elimination

Urine (~9%) and feces (~80%)

Half life

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

Clearance

3902 mL/min

Toxicity

Not Available

Affected organisms

Humans and other mammals

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

Drug	Interaction
(R)-warfarin	The metabolism of Lurasidone can be decreased when combined with (R)-warfarin.
(S)-Warfarin	The metabolism of Lurasidone can be decreased when combined with (S)-Warfarin.
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid	The risk or severity of hypertension can be increased when 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid is combined with Lurasidone.
1-benzylimidazole	The risk or severity of hypertension can be increased when 1-benzylimidazole is combined with Lurasidone.
2,4-thiazolidinedione	The therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Lurasidone.
2,5-Dimethoxy-4-ethylamphetamine	The therapeutic efficacy of Lurasidone can be decreased when used in combination with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine	The therapeutic efficacy of Lurasidone can be decreased when used in combination with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-Methylenedioxyamphetamine	The therapeutic efficacy of Lurasidone can be decreased when used in combination with 3,4-Methylenedioxyamphetamine.
3,5-diiodothyropropionic acid	The metabolism of Lurasidone can be decreased when combined with 3,5-diiodothyropropionic acid.
3,5-Dinitrocatechol	The therapeutic efficacy of 3,5-Dinitrocatechol can be decreased when used in combination with Lurasidone.

Food Interactions

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.

References

General References

George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA: Newer antipsychotics and upcoming molecules for schizophrenia. Eur J Clin Pharmacol. 2013 Aug;69(8):1497-509. doi: 10.1007/s00228-013-1498-4. Epub 2013 Apr 2. [PubMed:23545936]
Tarazi FI, Stahl SM: Iloperidone, asenapine and lurasidone: a primer on their current status. Expert Opin Pharmacother. 2012 Sep;13(13):1911-22. doi: 10.1517/14656566.2012.712114. Epub 2012 Jul 31. [PubMed:22849428]

External Links

KEGG Drug: D04820
PubChem Compound: 213046
PubChem Substance: 175427100
ChemSpider: 184739
BindingDB: 85222
ChEBI: 70735
ChEMBL: CHEMBL1237021
PharmGKB: PA166129557
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Lurasidone

ATC Codes

N05AE05 — Lurasidone

AHFS Codes

28:16.08.04 — Atypical Antipsychotics

FDA label

Download (452 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
1	Completed	Not Available	Male, Healthy Normal Subjects	1
1	Completed	Not Available	Metabolism / Pharmacokinetics	1
1	Completed	Not Available	Pharmacokinetics	1
1	Completed	Not Available	Schizophrenia Patients	1
1	Completed	Not Available	Schizophrenic Disorders	3
1	Completed	Basic Science	Schizophrenic Disorders	1
1	Completed	Treatment	Autism, Early Infantile / Schizophrenic Disorders	1
1	Recruiting	Treatment	Schizophrenic Disorders	1
2	Completed	Treatment	Affective Disorders / Asperger's Syndrome / Autistic Disorder / Bipolar I Disorder / Bipolar II Disorder / Child Development Disorders, Pervasive / Psychotic Disorder NOS / Schizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorder / Severe Major Depression With Psychotic Features / Severe Mood Disorder With Psychotic Features / Single Episode Major Depression Without Psychotic Symptoms	1
2	Completed	Treatment	Depression, Bipolar / Suicidal Thoughts / Suicide, Attempted	1
2	Completed	Treatment	Schizophrenic Disorders	4
2	Recruiting	Treatment	Schizophrenic Disorders	1
2, 3	Not Yet Recruiting	Treatment	Depression, Bipolar / Suicidal Thoughts	1
3	Active Not Recruiting	Treatment	Depression, Bipolar	1
3	Completed	Treatment	Autism, Early Infantile	1
3	Completed	Treatment	Autism, Early Infantile / Depression, Bipolar / Schizophrenic Disorders	1
3	Completed	Treatment	Bipolar Disorder (BD) / Schizophrenic Disorders	1
3	Completed	Treatment	Bipolar I Disorder	4
3	Completed	Treatment	Depression, Bipolar	5
3	Completed	Treatment	Major Depressive Disorder (MDD)	1
3	Completed	Treatment	Major Depressive Disorder With Mixed Features	1
3	Completed	Treatment	Schizoaffective Disorders / Schizophrenic Disorders	1
3	Completed	Treatment	Schizophrenic Disorders	10
3	Recruiting	Treatment	Bipolar Disorder (BD)	1
3	Withdrawn	Treatment	Major Depressive Disorder (MDD)	1
4	Completed	Treatment	Psychotic Disorder NOS	1
4	Completed	Treatment	Schizoaffective Disorders / Schizophrenic Disorders	1
4	Completed	Treatment	Schizophrenic Disorders	2
4	Recruiting	Treatment	Schizophrenic Disorders	2
4	Withdrawn	Treatment	Bipolar Disorder (BD) / Bipolar I / Bipolar II / Bipolar Spectrum Disorder / Mania	1
Not Available	Completed	Not Available	Bipolar Disorder (BD)	1
Not Available	Completed	Treatment	Depression, Bipolar	1
Not Available	Enrolling by Invitation	Not Available	Bipolar Disorder (BD)	1
Not Available	Recruiting	Not Available	Acute Bacterial Exacerbation of Chronic Bronchitis (ABECB) / Acute Bacterial Sinusitis (ABS) / Acute Decompensated Heart Failure (ADHF) / Acute Pyelonephritis / Adenovirus / Adjunct to general anesthesia therapy / Adrenal Insufficiency / Airway Swelling / Anaesthesia therapy / Anxiolysis / Arterial Hypotension / Autism, Early Infantile / Autistic Disorder / Bartonellosis / Benzodiazepine Withdrawal / Benzodiazepines / Bipolar Disorder (BD) / Bloodstream Infections / Bone and Joint Infections / Brain Swelling / Bronchospasm / Brucellosis / Cardiac Arrest / Central Nervous System Infections / Cholera / Chronic Bacterial Prostatitis / Community Acquired Pneumonia (CAP) / Complicated Urinary Tract Infections / Convulsions / Cytomegalovirus Retinitis / Drug hypersensitivity reaction / Early-onset Schizophrenia Spectrum Disorders / Edema / Epilepsies / Feeling Anxious / Flu caused by Influenza / Gastroparesis / Gynaecological infection / Headaches / Herpes Simplex Virus / High Blood Pressure (Hypertension) / High Cholesterol / Hospital-acquired bacterial pneumonia / Hyperlipidemias / Infantile Hemangiomas / Infection NOS / Inflammatory Conditions / Inflammatory Reaction / Influenza Treatment or Prophylaxis / Inhalational Anthrax (Post-Exposure) / Intra-Abdominal Infections / Life-threatening Fungal Infections / Lower Respiratory Tract Infection (LRTI) / Meningitis, Bacterial / Migraines / Muscle Spasms / Nausea / Opioid Addiction / Pain NOS / Plague / Pneumonia / Prophylaxis / Psittacosis / Q Fever / Reflux / Relapsing Fever / Rocky Mountain Spotted Fever / Schizophrenic Disorders / Sedation therapy / Seizures / Sepsis / Skeletal Muscle Spasms / Skin and Subcutaneous Tissue Bacterial Infections / Skin Structures and Soft Tissue Infections / Stable Angina (SA) / Thromboprophylaxis / Thrombotic events / Toxic effect of hydrocyanic acid and cyanides / Trachoma / Treatment-resistant Schizophrenia / Tularemia / Typhus Fever / Uncomplicated Skin and Skin Structure Infections / Uncomplicated Urinary Tract Infections / Urinary Tract Infections (UTIs) / Vomiting / Withdrawal	1
Not Available	Unknown Status	Not Available	Schizophrenic Disorders	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage forms

Form	Route	Strength
Tablet	Oral	120 mg
Tablet	Oral	20 mg
Tablet	Oral	40 mg
Tablet	Oral	60 mg
Tablet	Oral	80 mg
Tablet, film coated	Oral	120 mg/1
Tablet, film coated	Oral	20 mg/1
Tablet, film coated	Oral	40 mg/1
Tablet, film coated	Oral	60 mg/1
Tablet, film coated	Oral	80 mg/1
Tablet, coated	Oral	120 mg/1
Tablet, coated	Oral	20 mg/1
Tablet, coated	Oral	40 mg/1
Tablet, coated	Oral	60 mg/1
Tablet, coated	Oral	80 mg/1

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US9174975	Yes	2015-11-03	2026-12-25
US9259423	Yes	2016-02-16	2031-11-23
US8729085	Yes	2014-05-20	2026-11-26
US5532372	Yes	1996-07-02	2019-01-02
US8883794	Yes	2014-11-11	2026-11-26
USRE45573	Yes	2015-06-23	2025-12-23
US9555027	No	2017-01-31	2026-05-26
US9815827	No	2017-11-14	2024-02-20
US9827242	No	2017-11-28	2031-05-23
US9907794	No	2018-03-06	2026-05-26

Properties

State

Solid

Experimental Properties

Not Available

Predicted Properties

Property	Value	Source
Water Solubility	0.00789 mg/mL	ALOGPS
logP	5.25	ALOGPS
logP	4.56	ChemAxon
logS	-4.8	ALOGPS
pKa (Strongest Basic)	8.5	ChemAxon
Physiological Charge	1	ChemAxon
Hydrogen Acceptor Count	5	ChemAxon
Hydrogen Donor Count	0	ChemAxon
Polar Surface Area	56.75 Å²	ChemAxon
Rotatable Bond Count	5	ChemAxon
Refractivity	139.33 m³·mol^-1	ChemAxon
Polarizability	56.2 Å³	ChemAxon
Number of Rings	7	ChemAxon
Bioavailability	1	ChemAxon
Rule of Five	Yes	ChemAxon
Ghose Filter	No	ChemAxon
Veber's Rule	No	ChemAxon
MDDR-like Rule	No	ChemAxon

Predicted ADMET features

Property	Value	Probability
Human Intestinal Absorption	+	1.0
Blood Brain Barrier	+	0.9907
Caco-2 permeable	+	0.5257
P-glycoprotein substrate	Substrate	0.6029
P-glycoprotein inhibitor I	Inhibitor	0.6713
P-glycoprotein inhibitor II	Inhibitor	0.73
Renal organic cation transporter	Inhibitor	0.5487
CYP450 2C9 substrate	Non-substrate	0.7897
CYP450 2D6 substrate	Substrate	0.8918
CYP450 3A4 substrate	Substrate	0.5922
CYP450 1A2 substrate	Non-inhibitor	0.677
CYP450 2C9 inhibitor	Inhibitor	0.6714
CYP450 2D6 inhibitor	Non-inhibitor	0.8292
CYP450 2C19 inhibitor	Inhibitor	0.7439
CYP450 3A4 inhibitor	Non-inhibitor	0.7835
CYP450 inhibitory promiscuity	High CYP Inhibitory Promiscuity	0.8126
Ames test	Non AMES toxic	0.6477
Carcinogenicity	Non-carcinogens	0.8986
Biodegradation	Not ready biodegradable	0.9959
Rat acute toxicity	2.4051 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.6636
hERG inhibition (predictor II)	Inhibitor	0.5858

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available

Taxonomy

Description: This compound belongs to the class of organic compounds known as n-arylpiperazines. These are organic compounds containing a piperazine ring where the nitrogen ring atom carries an aryl group.
Kingdom: Organic compounds
Super Class: Organoheterocyclic compounds
Class: Diazinanes
Sub Class: Piperazines
Direct Parent: N-arylpiperazines
Alternative Parents: Aromatic monoterpenoids / Isoindolones / Benzothiazoles / Dialkylarylamines / N-alkylpiperazines / Aminothiazoles / Benzenoids / Pyrrolidine-2-ones / Imidolactams / N-substituted carboxylic acid imides
show 11 more
Substituents: N-arylpiperazine / Aromatic monoterpenoid / Monoterpenoid / Norbornane monoterpenoid / Isoindolone / 1,2-benzothiazole / Isoindoline / Isoindole or derivatives / Dialkylarylamine / N-alkylpiperazine
show 29 more
Molecular Framework: Aromatic heteropolycyclic compounds
External Descriptors: N-arylpiperazine, dicarboximide, bridged compound, 1,2-benzisothiazole (CHEBI:70735)

Targets

Details1. D(2) dopamine receptor

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Antagonist

General Function: Potassium channel regulator activity
Specific Function: Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name: DRD2
Uniprot ID: P14416
Uniprot Name: D(2) dopamine receptor
Molecular Weight: 50618.91 Da

References

George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA: Newer antipsychotics and upcoming molecules for schizophrenia. Eur J Clin Pharmacol. 2013 Aug;69(8):1497-509. doi: 10.1007/s00228-013-1498-4. Epub 2013 Apr 2. [PubMed:23545936]

Details2. 5-hydroxytryptamine receptor 2A

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Antagonist

General Function: Virus receptor activity
Specific Function: G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name: HTR2A
Uniprot ID: P28223
Uniprot Name: 5-hydroxytryptamine receptor 2A
Molecular Weight: 52602.58 Da

References

George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA: Newer antipsychotics and upcoming molecules for schizophrenia. Eur J Clin Pharmacol. 2013 Aug;69(8):1497-509. doi: 10.1007/s00228-013-1498-4. Epub 2013 Apr 2. [PubMed:23545936]

Details3. 5-hydroxytryptamine receptor 7

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Antagonist

General Function: Serotonin receptor activity
Specific Function: This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name: HTR7
Uniprot ID: P34969
Uniprot Name: 5-hydroxytryptamine receptor 7
Molecular Weight: 53554.43 Da

References

George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA: Newer antipsychotics and upcoming molecules for schizophrenia. Eur J Clin Pharmacol. 2013 Aug;69(8):1497-509. doi: 10.1007/s00228-013-1498-4. Epub 2013 Apr 2. [PubMed:23545936]

Details4. 5-hydroxytryptamine receptor 1A

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Antagonist

General Function: Serotonin receptor activity
Specific Function: G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Gene Name: HTR1A
Uniprot ID: P08908
Uniprot Name: 5-hydroxytryptamine receptor 1A
Molecular Weight: 46106.335 Da

References

George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA: Newer antipsychotics and upcoming molecules for schizophrenia. Eur J Clin Pharmacol. 2013 Aug;69(8):1497-509. doi: 10.1007/s00228-013-1498-4. Epub 2013 Apr 2. [PubMed:23545936]

Details5. Alpha-2C adrenergic receptor

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Antagonist

General Function: Protein homodimerization activity
Specific Function: Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name: ADRA2C
Uniprot ID: P18825
Uniprot Name: Alpha-2C adrenergic receptor
Molecular Weight: 49521.585 Da

References

George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA: Newer antipsychotics and upcoming molecules for schizophrenia. Eur J Clin Pharmacol. 2013 Aug;69(8):1497-509. doi: 10.1007/s00228-013-1498-4. Epub 2013 Apr 2. [PubMed:23545936]

Details6. Alpha-2A adrenergic receptor

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Thioesterase binding
Specific Function: Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Gene Name: ADRA2A
Uniprot ID: P08913
Uniprot Name: Alpha-2A adrenergic receptor
Molecular Weight: 48956.275 Da

References

Tarazi FI, Stahl SM: Iloperidone, asenapine and lurasidone: a primer on their current status. Expert Opin Pharmacother. 2012 Sep;13(13):1911-22. doi: 10.1517/14656566.2012.712114. Epub 2012 Jul 31. [PubMed:22849428]

Enzymes

Details1. Cytochrome P450 3A4

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Vitamin d3 25-hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name: CYP3A4
Uniprot ID: P08684
Uniprot Name: Cytochrome P450 3A4
Molecular Weight: 57342.67 Da

References

George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA: Newer antipsychotics and upcoming molecules for schizophrenia. Eur J Clin Pharmacol. 2013 Aug;69(8):1497-509. doi: 10.1007/s00228-013-1498-4. Epub 2013 Apr 2. [PubMed:23545936]
Lurasidone HCl FDA Label [Link]

Drug created on July 24, 2011 11:04 / Updated on January 18, 2019 21:51

Lurasidone

Identification

Structure for Lurasidone (DB08815)

Pharmacology

Interactions

References

Clinical Trials

Pharmacoeconomics

Properties

Spectra

Taxonomy

Targets

References

References

References

References

References

References

Enzymes

References