Aripiprazole

Highest phase reached

Approved

www.ebi.ac.uk

Drug type

Small molecule

www.ebi.ac.uk

First approval year

2002

www.ebi.ac.uk

First approval year: 2002
www.ebi.ac.uk

Listing at source: Listed

Highest phase reached: Approved
www.ebi.ac.uk

Drug type: Small molecule
www.ebi.ac.uk

Drug name: Aripiprazole
www.ebi.ac.uk

Molecular weight: 448.39
www.ebi.ac.uk

Structure (SMILES): O=C1CCc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1
www.ebi.ac.uk

abilify
Abilify
abilify asimtufii
Abilify asimtufii
abilify maintena
Abilify maintena
abilify maintena kit
Abilify maintena kit
abilify mycite kit
Abilify mycite kit
aripiprazole
Aripiprazole
aripiprazole accord
Aripiprazole accord
Aripiprazole mylan pharma (previously aripiprazole pharmathen)
aripiprazole mylan pharma previously aripiprazole pharmathen
aripiprazole sandoz
Aripiprazole sandoz
aripiprazole zentiva
Aripiprazole zentiva
opipza
Opipza

7 4 4 2 3 dichlorophenyl 1 piperazinyl butoxy 3 4 dihydrocarbostyril
7-[4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydrocarbostyril
abilify
Abilify
Abilify (aripiprazole)
Abilify (Aripiprazole10 mg)
abilify maintena
Abilify maintena
Abilify Maintena
abilify mycite
Abilify mycite
ABILIFY MYCITE
Abilify MyCite®
Abilify prolonged release aqueous suspension for IM injection (Aripiprazole)
Abilify(aripiprazole)
Abilify(Aripiprazole)
Abilify® 10 mg tablet
Apipe (Aripiprazole10 mg)
aripiprazol
Aripiprazol
aripiprazole
Aripiprazole
aripiprazole (Abilify)
Aripiprazole (Abilify®) IM Depot Injection
Aripiprazole (BMS-337039)

And 51 more, listed on the interactive page.

ATC classification codes

N05AX12

Sources for recorded values

www.ebi.ac.uk

CAS registry numbers

129722-12-9

ChEMBL ID: CHEMBL1112
www.ebi.ac.uk

InChIKey: CEUORZQYGODEFX-UHFFFAOYSA-N
www.ebi.ac.uk

PubChem compound IDs

60795

RxNorm IDs (RxCUI)

89013

FDA ingredient codes (UNII)

82VFR53I78

Applicant: OTSUKA
Approval date: 15 Nov 2002
Application number: NDA021436

Status: Authorised
Status date: 4 Jun 2004
Authorisation date: 4 Jun 2004
Approved indications: Abilify is indicated for the treatment of schizophrenia in adults and in adolescents aged 15 years and older. Abilify is indicated for the treatment of moderate to severe manic episodes in Bipolar I Disorder and for the prevention of a new manic episode in adults who experienced predominantly manic episodes and whose manic episodes responded to aripiprazole treatment. Abilify is indicated for the treatment up to 12 weeks of moderate to severe manic episodes in Bipolar I Disorder in adolescents aged 13 years and older.
Product number: EMEA/H/C/000471
Authorisation holder: Otsuka Pharmaceutical Netherlands B.V.
Priority medicines scheme: No
Generic: No
Biosimilar: No
Generic medicines: 4
Biosimilar medicines: 0
Advanced therapy: No
Conditional approval: No
Additional monitoring: No
Accelerated assessment: No
Exceptional circumstances: No

Therapeutic areas

Bipolar Disorder
Schizophrenia

European medicines record

www.ema.europa.eu

Patents: 45
Designations: 2
Earliest recorded loss of exclusivity: 15 Dec 2041
First in class: No
Fast track: No
Breakthrough designation: No
Orphan designation: No
Priority review: No
Orphan exclusivity: No
Accelerated approval: No
Availability: Prescription only
Boxed warning: Yes

Pharmacology name: aripiprazole
Type: Synthetic organic
Drug name stem: -prazole
Approval recorded by Guide to Pharmacology: Yes

Administration routes

Oral
Parenteral

Action
Antagonist
Action type
Antagonist
Target
H1 receptor
Gene symbol
HRH1
Protein identifier
P35367
Median affinity
7.5
Affinity units
pKi
Mechanism
Serotonin 2a (5-HT2a) receptor antagonist
Action type
Antagonist
Target
5-hydroxytryptamine receptor 2A
Protein identifier
P28223
Action
Full agonist
Action type
FULL_AGONIST
Target
5-HT1D receptor
Gene symbol
HTR1D
Protein identifier
P28221
Median affinity
7.2
Affinity units
pKi
Action
Full agonist
Action type
FULL_AGONIST
Target
5-HT1B receptor
Gene symbol
HTR1B
Protein identifier
P28222
Median affinity
6.1
Affinity units
pKi
Action
Partial agonist
Action type
PARTIAL_AGONIST
Target
5-HT1A receptor
Gene symbol
HTR1A
Protein identifier
P08908
Median affinity
8.2
Affinity units
pKi
Action
Partial agonist
Action type
PARTIAL_AGONIST
Target
D2 receptor
Gene symbol
DRD2
Protein identifier
P14416
Median affinity
9.1
Affinity units
pKi
Primary target
Yes
Action
Partial agonist
Action type
PARTIAL_AGONIST
Target
5-HT2A receptor
Gene symbol
HTR2A
Protein identifier
P28223
Affinity units
pKi
Action
Partial agonist
Action type
PARTIAL_AGONIST
Target
5-HT2C receptor
Gene symbol
HTR2C
Protein identifier
P28335
Median affinity
7.6
Affinity units
pKi
Mechanism
Dopamine D2 receptor partial agonist
Action type
PARTIAL_AGONIST
Target
D(2) dopamine receptor
Protein identifier
P14416
Mechanism
Serotonin 1a (5-HT1a) receptor partial agonist
Action type
PARTIAL_AGONIST
Target
5-hydroxytryptamine receptor 1A
Protein identifier
P08908

Mechanism
Serotonin 2a (5-HT2a) receptor antagonist
Action type
Antagonist
Target
5-hydroxytryptamine receptor 2A
Mechanism
Dopamine D2 receptor partial agonist
Action type
PARTIAL AGONIST
Target
D(2) dopamine receptor
Mechanism
Serotonin 1a (5-HT1a) receptor partial agonist
Action type
PARTIAL AGONIST
Target
5-hydroxytryptamine receptor 1A

Action type
Antagonist
Gene symbol
HTR2A
Protein identifier
P28223
Organism
Homo sapiens
Target development level
Clinical
Action type
PARTIAL AGONIST
Gene symbol
HTR1A
Protein identifier
P08908
Organism
Homo sapiens
Target development level
Clinical
Action type
PARTIAL AGONIST
Gene symbol
DRD2
Protein identifier
P14416
Organism
Homo sapiens
Target development level
Clinical

Condition
Mental Disorders
Highest recorded phase
3
Condition identifier
EFO:0000677
Subject identifier
D001523
Condition
Stress Disorders, Post-Traumatic
Highest recorded phase
3
Condition identifier
EFO:0001358
Subject identifier
D013313
Condition
Cocaine-Related Disorders
Highest recorded phase
2
Condition identifier
EFO:0002610
Subject identifier
D019970
Condition
Aggression
Highest recorded phase
4
Condition identifier
EFO:0003015
Subject identifier
D000374
Condition
Child Development Disorders, Pervasive
Highest recorded phase
3
Condition identifier
EFO:0003756
Subject identifier
D002659
Condition
Asperger Syndrome
Highest recorded phase
2
Condition identifier
EFO:0003757
Subject identifier
D020817
Condition
Autistic Disorder
Highest recorded phase
4
Condition identifier
EFO:0003758
Subject identifier
D001321
Condition
Attention Deficit Disorder with Hyperactivity
Highest recorded phase
2
Condition identifier
EFO:0003888
Subject identifier
D001289
Condition
Obsessive-Compulsive Disorder
Highest recorded phase
2
Condition identifier
EFO:0004242
Subject identifier
D009771
Condition
Amphetamine-Related Disorders
Highest recorded phase
1
Condition identifier
EFO:0004701
Subject identifier
D019969
Condition
Tourette Syndrome
Highest recorded phase
4
Condition identifier
EFO:0004895
Subject identifier
D005879
Condition
Anxiety
Highest recorded phase
3
Condition identifier
EFO:0005230
Subject identifier
D001007
Condition
Psychotic Disorders
Highest recorded phase
4
Condition identifier
EFO:0005407
Subject identifier
D011618
Condition
Psychotic Disorders
Highest recorded phase
4
Condition identifier
EFO:0005411
Subject identifier
D011618
Condition
Depression, Postpartum
Highest recorded phase
3
Condition identifier
EFO:0007453
Subject identifier
D019052
Condition
Bipolar Disorder
Highest recorded phase
4
Condition identifier
EFO:0009963
Subject identifier
D001714
Condition
Psychomotor Agitation
Highest recorded phase
4
Condition identifier
HP:0000713
Subject identifier
D011595
Condition
Dementia
Highest recorded phase
3
Condition identifier
HP:0000726
Subject identifier
D003704
Condition
Trichotillomania
Highest recorded phase
2
Condition identifier
HP:0012167
Subject identifier
D014256
Condition
Child Development Disorders, Pervasive
Highest recorded phase
3
Condition identifier
MONDO:0000594
Subject identifier
D002659
Condition
Tic Disorders
Highest recorded phase
3
Condition identifier
MONDO:0001074
Subject identifier
D013981
Condition
Depressive Disorder, Major
Highest recorded phase
4
Condition identifier
MONDO:0002009
Subject identifier
D003865
Condition
Depressive Disorder
Highest recorded phase
4
Condition identifier
MONDO:0002009
Subject identifier
D003866
Condition
Depressive Disorder
Highest recorded phase
4
Condition identifier
MONDO:0002050
Subject identifier
D003866
Condition
Tic Disorders
Highest recorded phase
3
Condition identifier
MONDO:0002420
Subject identifier
D013981

And 7 more, listed on the interactive page.

Condition identifier
EFO_0000195
Condition identifier
EFO_0000677
Highest recorded phase
3
Condition identifier
EFO_0001358
Highest recorded phase
3
Condition identifier
EFO_0002610
Highest recorded phase
2
Condition identifier
EFO_0003015
Condition identifier
EFO_0003015
Highest recorded phase
4
Condition identifier
EFO_0003756
Condition identifier
EFO_0003757
Highest recorded phase
2
Condition identifier
EFO_0003758
Condition identifier
EFO_0003759
Highest recorded phase
2
Condition identifier
EFO_0003888
Highest recorded phase
2
Condition identifier
EFO_0004242
Highest recorded phase
2
Condition identifier
EFO_0004609
Condition identifier
EFO_0004701
Highest recorded phase
1
Condition identifier
EFO_0004714
Condition identifier
EFO_0004895
Condition identifier
EFO_0005407
Condition identifier
EFO_0005411
Highest recorded phase
3
Condition identifier
EFO_0007319
Condition identifier
EFO_0007453
Highest recorded phase
3
Condition identifier
EFO_0007634
Highest recorded phase
3
Condition identifier
EFO_0009963
Condition identifier
EFO_0009963
Highest recorded phase
4
Condition identifier
HP_0000713
Condition identifier
HP_0000713
Highest recorded phase
4

And 46 more, listed on the interactive page.

Warning
Black Box Warning
Warning
Black Box Warning
Effect
psychiatric toxicity

Warning
Black Box Warning
Country
United States
Warning
Black Box Warning
Effect
psychiatric toxicity
Country
United States

Event
abnormal behaviour
Reports
355
Reporting signal score
344.651
Event
aggression
Reports
481
Reporting signal score
490.503
Event
agitation
Reports
547
Reporting signal score
404.872
Event
akathisia
Reports
957
Reporting signal score
2,693.2
Event
anosognosia
Reports
210
Reporting signal score
814.327
Event
anxiety
Reports
811
Reporting signal score
358.279
Event
blood creatine phosphokinase increased
Reports
386
Reporting signal score
311.894
Event
blood prolactin abnormal
Reports
247
Reporting signal score
962.837
Event
delusion
Reports
459
Reporting signal score
914.136
Event
diarrhoea
Reports
210
Reporting signal score
360.847
Event
disturbance in social behaviour
Reports
198
Reporting signal score
615.641
Event
dyskinesia
Reports
726
Reporting signal score
1,233.53
Event
dystonia
Reports
765
Reporting signal score
1,782.23
Event
extrapyramidal disorder
Reports
726
Reporting signal score
1,606.86
Event
gambling disorder
Reports
190
Reporting signal score
690.027
Event
hallucination, auditory
Reports
365
Reporting signal score
631.856
Event
hyperprolactinaemia
Reports
169
Reporting signal score
369.973
Event
mania
Reports
384
Reporting signal score
661.809
Event
metabolic disorder
Reports
211
Reporting signal score
521.04
Event
muscle rigidity
Reports
244
Reporting signal score
366.711
Event
neuroleptic malignant syndrome
Reports
683
Reporting signal score
1,517.35
Event
obsessive-compulsive disorder
Reports
193
Reporting signal score
404.406
Event
oculogyric crisis
Reports
134
Reporting signal score
334.002
Event
parkinsonism
Reports
500
Reporting signal score
1,151.74
Event
personality change
Reports
195
Reporting signal score
346.901

And 13 more, listed on the interactive page.

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And 211 more, listed on the interactive page.

Dose: 10 mg/day
Route: Oral
How often: Once daily

Conditions of use

Take without regard to meals

Hydrogen bond acceptors: 4
Hydrogen bond donors: 1
Polar surface area: 44.81
Calculated partition coefficient (ALogP): 4.86
Calculated partition coefficient (XLogP): 4.6
Prodrug: No
Chirality: Achiral
Inorganic: No
Rule-of-five violations: 0
Rotatable bonds: 7
Heavy atoms: 30
Molecular formula: C23H27Cl2N3O2
Monoisotopic mass: 447.1480325
Natural product: Yes

0615-8375
0615-8524
0615-8525
0904-6656
0904-7366
0904-7367
0904-7368
0904-7369
0904-7370
0904-7371
13668-216
13668-217
13668-218
13668-219
13668-220
13668-221
15370-401
15370-402
15370-403
16714-141
16714-142
16714-143
16714-144
16714-145
16714-146

And 242 more, listed on the interactive page.

Recorded assays: 2,603
Active assays: 562

Confirmatory
Other
Screening
Summary

Antidepressive Agents
id.nlm.nih.gov
Antipsychotic Agents
id.nlm.nih.gov
Dopamine Agonists
id.nlm.nih.gov
Serotonin 5-HT1 Receptor Agonists
id.nlm.nih.gov
Serotonin 5-HT2 Receptor Antagonists
id.nlm.nih.gov
Dopamine D2 Receptor Antagonists
id.nlm.nih.gov

These details could not be displayed.

Related records

Trials (354)

1/2-MC4R Genotype and Pediatric Antipsychotic Drug- Induced Weight Gain
12- Week Open Label Treatment of Refractory Bipolar Depression
15 Month Study for Adults Who Have Been Diagnosed With Schizophrenia and Incarcerated
A Comparative Study of Patient Satisfaction Between Continued Administration of Previous Antipsychotics Versus Switched Administration to Paliperidone ER in Non-satisfied Patients With Previous Antipsychotic Drug
A Comparison of Medication Augmentation and PST in the Treatment of Depression in Older Adults
A Comparison of Risperidone and Aripiprazole for Treatment of Patirnts With Methamphetamine-Associated Psychosis
A Comparison Study of LY2140023 and Aripiprazole in Schizophrenia Patients
A Double-Blind, Controlled Study of Aripiprazole in Co-Morbid Schizophrenia and Cocaine Dependence
A Double-Blind, Placebo-Controlled Study of Aripiprazole Adjunctive to Antidepressant Therapy
A Double-Blind, Randomized Comparative Study of Carliprazine and Aripiprazole in Patients with Acute Schizophrenia
A Follow-on Study of the Long-Term Safety of Aripiprazole in Patients With Chronic Schizophrenia
A Long-Term Study of Aripiprazole in Patients With Major Depressive Disorder
A Long-term, Extended Treatment Study of Aripiprazole in Pediatric Patients With Autistic Disorder
A Long-term, Extended Treatment Study of Aripiprazole in Pediatric Patients With Schizophrenia
A Long-Term, Open-Label, Study on Schizophrenia
A Multicenter Investigative Study of the Safety and Efficacy of Long-term Administration of Aripiprazole in Combination With Mood Stabilizer for the Treatment of Patients With Bipolar Disorder Experiencing a Manic or Mixed Episode
A Multicenter Open-label Study Investigating the Pharmacokinetics and Safety of Aripiprazole IM Depot Formulation (OPC-14597 IMD) During Repeated Administration by Injection Into the Deltoid Muscle in Patients With Schizophrenia
A Multicenter Study to Evaluate the Effects of Switching to Aripiprazole 12 Weeks on the Sexual Dysfunction From Risperidone or Paliperidone in Patients With Schizophrenia Spectrum Disorders or Bipolar Spectrum Disorders
A Multicenter, Investigative Study of the Safety and Efficacy of Extended Administration of Aripiprazole in Combination With Mood Stabilizer for the Treatment of Patients With Bipolar Disorder Experiencing a Manic or Mixed Episode
A Multicenter, Placebo-controlled, Double-blind Investigative Extension Trial of the Safety and Efficacy of Aripiprazole in the Treatment of Patients With Bipolar Disorder Experiencing a Manic or Mixed Episode

Approved for (9)

Autism
Bipolar depression
Bipolar disorder
Depressive disorder
Major depressive disorder
Psychotic disorder
Schizoaffective disorder
Schizophrenia
Tourette syndrome

In development for (20)

Alcohol dependence Phase 3
Alzheimer disease Phase 3
Anorexia nervosa Phase 3
Anxiety Phase 3
Attention deficit-hyperactivity disorder Phase 2
Autism spectrum disorder Phase 3
Autism spectrum disorder 1 Phase 2
Chronic tic disorder Phase 3
Cocaine abuse Phase 2
Cocaine dependence Phase 2
Dementia Phase 3
Fragile X syndrome Phase 2
Mental disorder Phase 3
Methamphetamine dependence Phase 1
Obsessive-compulsive disorder Phase 2
Pervasive developmental disorder Phase 3
Post-traumatic stress disorder Phase 3
Postpartum depression Phase 3
Tic disorder Phase 3
Trichotillomania Phase 2

Targets (3)

DRD2 Dopamine D2 receptor partial agonist
HTR1A Serotonin 1a (5-HT1a) receptor partial agonist
HTR2A Serotonin 2a (5-HT2a) receptor antagonist

Aripiprazole

Development status

Names and chemistry

Brand names (22)

Other names (76)

Identifiers

Regulatory information

United States

European Union

Therapeutic areas

Other regulatory facts

Pharmacology

Drug classification

Administration routes

Mechanisms of action (10)

Open Targets mechanisms (3)

DrugCentral mechanisms (3)

Investigated indications (32)

Open Targets indications (71)

Warnings (2)

Open Targets warnings (2)

Reported adverse events (38)

Trial references (236)

Dosing

Conditions of use

Chemical properties

National Drug Codes

Evidence counts

Active assay types (4)

Pharmacologic actions

Biological measurements

Related records

Trials (354)

Approved for (9)

In development for (20)

Other linked conditions (3)

Targets (3)