Identification
- Summary
Cariprazine is an atypical antipsychotic used to treat schizophrenia and acute manic or mixed episodes due to bipolar I disorder.
- Brand Names
- Vraylar
- Generic Name
- Cariprazine
- DrugBank Accession Number
- DB06016
- Background
Cariprazine is an atypical antipsychotic agent and a piperazine derivative that was first developed in Hungary.6 It works as a partial agonist at central dopamine D2, dopamine D3, and serotonin 5-HT1A receptors and as an antagonist at serotonin 5-HT2A receptors.10 Cariprazine has been investigated in a variety of psychiatric disorders, including schizophrenia, bipolar disorders, and major depressive disorder. Cariprazine gained its first global approval in the US in September 2015 2 and was later approved by Health Canada in April 2022.11 It is currently used to treat schizophrenia, and manic or mixed episodes and depressive episodes associated with bipolar I disorder.9,10
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Cariprazine (DB06016)
- Weight
- Average: 427.41
Monoisotopic: 426.1953171 - Chemical Formula
- C21H32Cl2N4O
- Synonyms
- Cariprazine
- trans-N-{4-[2-[4-(2,3-dichlorophenyl)piperazine-1-yl]ethyl]cyclohexyl}-N’,N’-dimethylurea hydrochloride
- External IDs
- MP-214
- RGH-188
Pharmacology
- Indication
Cariprazine is indicated for the treatment of schizophrenia in adults to manage both positive and negative symptoms. It is also indicated to monotherapy for acute management of manic or mixed episodes associated with bipolar I disorder (bipolar mania) in adults, and acute management of depressive episodes associated with bipolar I disorder (bipolar depression) in adults.9,10
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Cariprazine is an antipsychotic agent. In clinical trials, it reduced positive and negative symptoms in patients with schizophrenia and acute mania in patients with bipolar I disorder. In animal models, cariprazine showed therapeutic benefits against cognitive deficits, mania, and catalepsy.2 In a meta-analysis study, cariprazine was shown to improve anxiety and depressed mood in patients with psychosis.3
As cariprazine is a partial agonist at dopamine D2 and D3 receptors, it produces an apparent lower blockade level than other antipsychotic agents that block dopamine receptors. This receptor binding profile is advantageous as dopamine receptor blockade is associated with extrapyramidal symptoms as side effects. Partial agonism would allow the dopamine receptor to be stimulated even at maximal receptor occupancy by the drug.6 Antagonism at 5-HT1A 6 and 5-HT2A receptors by cariprazine can increase dopaminergic neurotransmission in the nigrostriatal pathway, thereby further reducing the risk of extrapyramidal symptoms.3 However, cariprazine is still associated with a risk of akathisia, extrapyramidal disorder, restlessness, and tremor.2,10
- Mechanism of action
While recent research points to the involvement of multiple neurotransmitters in the development and maintenance of schizophrenia and bipolar disorders, the dopamine hypothesis has been and continues to be a key theory in understanding the pathophysiology of these psychiatric disorders. Dopamine is a neurotransmitter that plays several important roles in cells, and most importantly, it is a crucial neurotransmitter involved in reward processing and motivation. The nigrostriatal, mesolimbic, and mesocortical systems consist of dopaminergic projections. The dopamine hypothesis states that dopaminergic aberrations are observed in schizophrenia and bipolar disorders.7,8 For example, hyperactive dopamine D2 receptor activity has been associated with positive symptoms of schizophrenia, such as hallucinations and delusions. On the other hand, alterations in dopamine D3 receptors may be involved in producing negative symptoms of schizophrenia.7 It was stated that hyperdopaminergia, caused by elevations in D2/3 receptor availability and a hyperactive reward processing network, underlies the development of mania in bipolar disorder.8
The exact mechanism of action of cariprazine is not fully elucidated. Cariprazine potently binds to both of these receptors, more preferably to D3 receptors with higher affinity.2 Preclinical studies suggest that D3 receptor blockade is associated with exerting pro-cognitive and antidepressant effects and attenuating negative symptoms in schizophrenia.5 This unique mechanism of action differs from that of other antipsychotic agents that mostly target D2 and 5-HT2A receptors.3 Cariprazine is also a partial agonist at 5-HT1A receptors, an antagonist at 5-HT2B and 5-HT2A receptors, an antagonist at histamine H1 receptors. It also binds to 5-HT2C, alpha (α)-1A adrenergic, and alpha (α)-1B adrenergic receptors with low affinity.2,5
Target Actions Organism UDopamine D3 receptor partial agonistHumans UDopamine D2 receptor partial agonistHumans U5-hydroxytryptamine receptor 1A partial agonistHumans U5-hydroxytryptamine receptor 2B antagonistHumans U5-hydroxytryptamine receptor 2A antagonistHumans UHistamine H1 receptor antagonistHumans U5-hydroxytryptamine receptor 2C antagonistHumans UAlpha-1A adrenergic receptor antagonistHumans - Absorption
The most clinically relevant drug concentration equates to the combined systemic concentration of cariprazine plus desmethyl cariprazine (DCAR) and didesmethyl cariprazine (DDCAR), the two main pharmacologically active metabolites of cariprazine.2 After single dose administration of cariprazine, the peak plasma cariprazine concentration occurred in approximately three to six hours.10 In healthy volunteers, the Tmax following oral administration was 3.6 hours for cariprazine, 6.5 hours for DCAR, and 18.1 hours for DDCAR. The steady-state was reached dose-proportionally within three weeks for cariprazine, DCAR, and DDCAR in patients with schizophrenia.2
Administration of a single dose of 1.5 mg cariprazine capsule with a high-fat meal did not significantly affect the Cmax and AUC of cariprazine or its metabolite, desmethyl cariprazine (DCAR).10
- Volume of distribution
Not Available
- Protein binding
Cariprazine and its major active metabolites are highly bound (91 to 97%) to plasma proteins.10
- Metabolism
Cariprazine is extensively metabolized by CYP3A4 and, to a lesser extent, by CYP2D6 to form two major metabolites, desmethyl cariprazine (DCAR) and didesmethyl cariprazine (DDCAR). DCAR and DDCAR are pharmacologically active metabolites with in vitro receptor binding profiles similar to the parent drug. DCAR is further metabolized into DDCAR by CYP3A4 and CYP2D6. DDCAR can be metabolized by CYP3A4 to form a hydroxylated metabolite.1,2,10
Hover over products below to view reaction partners
- Route of elimination
Following administration of 12.5 mg/day cariprazine to patients with schizophrenia for 27 days, about 21% of the daily dose was found in urine, with approximately 1.2% of the daily dose being excreted in urine as unchanged parent drug.10
- Half-life
Cariprazine and its active metabolites have long half lives.5 Terminal half-lives of cariprazine, DCAR, and DDCAR ranged from 31.6 to 68.4, 29.7 to 37.5, and 314 to 446 hours, respectively. The effective half-life, calculated from time to steady state, or the functional half-life of total active moieties was approximately one week.4
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
In pre-marketing clinical trials, an accidental acute overdosage (48 mg/day) was reported in one patient who experienced orthostasis and sedation. The patient fully recovered the same day. As there are no specific antidotes for cariprazine, supportive care, including close medical supervision and monitoring, is advised to manage overdose. The possibility of multiple drug involvement should also be considered.10
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of adverse effects can be increased when Cariprazine is combined with 1,2-Benzodiazepine. Abametapir The serum concentration of Cariprazine can be increased when it is combined with Abametapir. Acebutolol Cariprazine may decrease the antihypertensive activities of Acebutolol. Aceclofenac The risk or severity of hypertension can be increased when Cariprazine is combined with Aceclofenac. Acemetacin The risk or severity of hypertension can be increased when Cariprazine is combined with Acemetacin. Acenocoumarol The risk or severity of adverse effects can be increased when Cariprazine is combined with Acenocoumarol. Acetazolamide The risk or severity of adverse effects can be increased when Acetazolamide is combined with Cariprazine. Acetophenazine The risk or severity of adverse effects can be increased when Acetophenazine is combined with Cariprazine. Acetylsalicylic acid The risk or severity of hypertension can be increased when Acetylsalicylic acid is combined with Cariprazine. Aclidinium Cariprazine may increase the central nervous system depressant (CNS depressant) activities of Aclidinium. 
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- Avoid excessive or chronic alcohol consumption. Given the primary central nervous system effects of cariprazine, cariprazine should be used with caution in combination with alcohol.
- Avoid grapefruit products. Grapefruit is a known CYP3A4 inhibitor. It may increase drug levels and elevate the risk of drug adverse effects.
- Avoid St. John's Wort. St John’s Wort is a known CYP3A4 inducer. It may significantly decrease drug exposure and alter drug efficacy.
- Take with or without food. A high-fat, high-calorie meal may delay Tmax, but food generally has no significant effect on drug exposure.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Cariprazine hydrochloride KQD7C255YG 1083076-69-0 GPPJWWMREQHLQT-BHQIMSFRSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Reagila Capsule 1.5 mg Oral Gedeon Richter 2020-12-16 Not applicable EU 
Reagila Capsule 4.5 mg Oral Gedeon Richter 2020-12-16 Not applicable EU Reagila Capsule 4.5 mg Oral Gedeon Richter 2020-12-16 Not applicable EU Reagila Capsule 3 mg Oral Gedeon Richter 2020-12-16 Not applicable EU Reagila Capsule 4.5 mg Oral Gedeon Richter 2020-12-16 Not applicable EU Reagila Capsule 6 mg Oral Gedeon Richter 2020-12-16 Not applicable EU Reagila Capsule 3 mg Oral Gedeon Richter 2020-12-16 Not applicable EU Reagila Capsule 4.5 mg Oral Gedeon Richter 2020-12-16 Not applicable EU Reagila Capsule 1.5 mg Oral Gedeon Richter 2020-12-16 Not applicable EU Reagila Capsule 6 mg Oral Gedeon Richter 2020-12-16 Not applicable EU - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Vraylar Cariprazine (1.5 mg/1) + Cariprazine (3 mg/1) Kit Oral Allergan, Inc. 2015-09-17 Not applicable US 
Vraylar Cariprazine (1.5 mg/1) + Cariprazine (3 mg/1) Kit Oral Allergan, Inc. 2015-09-17 Not applicable US
Categories
- ATC Codes
- N05AX15 — Cariprazine
- Drug Categories
- Agents that produce hypertension
- Antidepressive Agents
- Antipsychotic Agents
- Antipsychotic Agents (Second Generation [Atypical])
- Central Nervous System Agents
- Central Nervous System Depressants
- Chlorobenzenes
- Cyclohexanes
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (weak)
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 Inhibitors (weak)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (weak)
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (weak)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP2E1 Inhibitors
- Cytochrome P-450 CYP2E1 Inhibitors (weak)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (weak)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Inducers
- Cytochrome P-450 CYP3A5 Inducers (strength unknown)
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Dopamine Agonists
- Dopamine D2/D3 receptor modulators
- Histamine Antagonists
- Histamine H1 Antagonists
- Nervous System
- Neurotoxic agents
- P-glycoprotein inhibitors
- Piperazines
- Psycholeptics
- Psychotropic Drugs
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin 5-HT1 Receptor Agonists
- Serotonin 5-HT2 Receptor Antagonists
- Serotonin 5-HT2A Receptor Antagonists
- Serotonin 5-HT2C Receptor Antagonists
- Serotonin Agents
- Serotonin Receptor Agonists
- Serotonin Receptor Antagonists
- Tranquilizing Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenylpiperazines. These are compounds containing a phenylpiperazine skeleton, which consists of a piperazine bound to a phenyl group.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Diazinanes
- Sub Class
- Piperazines
- Direct Parent
- Phenylpiperazines
- Alternative Parents
- N-arylpiperazines / Dichlorobenzenes / Dialkylarylamines / Aniline and substituted anilines / N-alkylpiperazines / Aryl chlorides / Ureas / Trialkylamines / Azacyclic compounds / Organopnictogen compounds show 4 more
- Substituents
- 1,2-dichlorobenzene / Amine / Aniline or substituted anilines / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / Carbonic acid derivative / Carbonyl group show 20 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- F6RJL8B278
- CAS number
- 839712-12-8
- InChI Key
- KPWSJANDNDDRMB-QAQDUYKDSA-N
- InChI
- InChI=1S/C21H32Cl2N4O/c1-25(2)21(28)24-17-8-6-16(7-9-17)10-11-26-12-14-27(15-13-26)19-5-3-4-18(22)20(19)23/h3-5,16-17H,6-15H2,1-2H3,(H,24,28)/t16-,17-
- IUPAC Name
- 3,3-dimethyl-1-[(1r,4r)-4-{2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl}cyclohexyl]urea
- SMILES
- CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCN(CC2)C2=C(Cl)C(Cl)=CC=C2)CC1
References
- Synthesis Reference
Agai-Csongor E, Domany G, Nogradi K, Galambos J, Vago I, Keseru GM, Greiner I, Laszlovszky I, Gere A, Schmidt E, Kiss B, Vastag M, Tihanyi K, Saghy K, Laszy J, Gyertyan I, Zajer-Balazs M, Gemesi L, Kapas M, Szombathelyi Z: Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors. Bioorg Med Chem Lett. 2012 May 15;22(10):3437-40. doi: 10.1016/j.bmcl.2012.03.104. Epub 2012 Apr 4. Pubmed
- General References
- Citrome L: Cariprazine: chemistry, pharmacodynamics, pharmacokinetics, and metabolism, clinical efficacy, safety, and tolerability. Expert Opin Drug Metab Toxicol. 2013 Feb;9(2):193-206. doi: 10.1517/17425255.2013.759211. [Article]
- McCormack PL: Cariprazine: First Global Approval. Drugs. 2015 Nov;75(17):2035-43. doi: 10.1007/s40265-015-0494-7. [Article]
- Cooper H, Mishriky R, Reyad AA: Efficacy and Safety of Cariprazine in Acute Management of Psychiatric Disorders: a Meta-Analysis of Randomized Controlled Trials. Psychiatr Danub. 2020 Spring;32(1):36-45. doi: 10.24869/psyd.2020.36. [Article]
- Nakamura T, Kubota T, Iwakaji A, Imada M, Kapas M, Morio Y: Clinical pharmacology study of cariprazine (MP-214) in patients with schizophrenia (12-week treatment). Drug Des Devel Ther. 2016 Jan 14;10:327-38. doi: 10.2147/DDDT.S95100. eCollection 2016. [Article]
- Stahl SM: Mechanism of action of cariprazine. CNS Spectr. 2016 Apr;21(2):123-7. doi: 10.1017/S1092852916000043. Epub 2016 Mar 9. [Article]
- Roberts RJ, Findlay LJ, El-Mallakh PL, El-Mallakh RS: Update on schizophrenia and bipolar disorder: focus on cariprazine. Neuropsychiatr Dis Treat. 2016 Jul 25;12:1837-42. doi: 10.2147/NDT.S97616. eCollection 2016. [Article]
- Brisch R, Saniotis A, Wolf R, Bielau H, Bernstein HG, Steiner J, Bogerts B, Braun K, Jankowski Z, Kumaratilake J, Henneberg M, Gos T: The role of dopamine in schizophrenia from a neurobiological and evolutionary perspective: old fashioned, but still in vogue. Front Psychiatry. 2014 May 19;5:47. doi: 10.3389/fpsyt.2014.00047. eCollection 2014. [Article]
- Ashok AH, Marques TR, Jauhar S, Nour MM, Goodwin GM, Young AH, Howes OD: The dopamine hypothesis of bipolar affective disorder: the state of the art and implications for treatment. Mol Psychiatry. 2017 May;22(5):666-679. doi: 10.1038/mp.2017.16. Epub 2017 Mar 14. [Article]
- Health Canada Approved Drug Products: VRAYLAR (Cariprazine) Oral Capsules [Link]
- FDA Approved Drug Products: VRAYLAR (cariprazine) capsules, for oral use [Link]
- Cision PR Newswire: Health Canada Approves VRAYLAR® (cariprazine) for the Treatment of Bipolar l Disorder and Schizophrenia in Adults [Link]
- External Links
- KEGG Drug
- D09997
- PubChem Compound
- 11154555
- PubChem Substance
- 310264859
- ChemSpider
- 25999972
- BindingDB
- 50443101
- 1667655
- ChEBI
- 90933
- ChEMBL
- CHEMBL2028019
- ZINC
- ZINC000100907004
- PDBe Ligand
- 7RU
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Cariprazine
- PDB Entries
- 7vod
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Not Yet Recruiting Basic Science Depression, Bipolar 1 4 Not Yet Recruiting Treatment Social Anxiety Disorder (SAD) 1 4 Recruiting Treatment Attention Deficit Hyperactivity Disorder (ADHD) 1 3 Active Not Recruiting Treatment Bipolar 1 Disorder / Depression / Mania 1 3 Completed Prevention Schizophrenia 1 3 Completed Treatment Bipolar 1 Disorder 1 3 Completed Treatment Bipolar 1 Disorder / Mania 1 3 Completed Treatment Bipolar Disorder (BD) / Depression 2 3 Completed Treatment Bipolar Disorder (BD) / Mania 1 3 Completed Treatment Major Depressive Disorder (MDD) 4
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule Oral 1.635 MG Capsule Oral 1.5 mg Capsule Oral 3.27 MG Capsule Oral 3 mg Capsule Oral 4.905 MG Capsule Oral 4.5 mg Capsule Oral 6.54 MG Capsule Oral 6 mg Capsule, gelatin coated Oral 1.5 mg Capsule, gelatin coated Oral 3.000 mg Capsule, gelatin coated Oral 4.500 mg Capsule, gelatin coated Oral 6.000 mg Capsule, gelatin coated Oral 1.5 mg/1 Capsule, gelatin coated Oral 3 mg/1 Capsule, gelatin coated Oral 4.5 mg/1 Capsule, gelatin coated Oral 6 mg/1 Kit Oral - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US7737142 No 2010-06-15 2027-03-27 US US7943621 No 2011-05-17 2028-12-16 US USRE47350 No 2019-04-16 2029-07-16 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.0279 mg/mL ALOGPS logP 4.56 ALOGPS logP 4.06 ChemAxon logS -4.2 ALOGPS pKa (Strongest Acidic) 15.68 ChemAxon pKa (Strongest Basic) 7.91 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 3 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 38.82 Å2 ChemAxon Rotatable Bond Count 5 ChemAxon Refractivity 117.81 m3·mol-1 ChemAxon Polarizability 48.36 Å3 ChemAxon Number of Rings 3 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule Yes ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET Features
- Not Available
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
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Partial agonist
- Curator comments
- Inhibition constant (Ki) = 0.085 nmol/L
- General Function
- G-protein coupled amine receptor activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
- Gene Name
- DRD3
- Uniprot ID
- P35462
- Uniprot Name
- D(3) dopamine receptor
- Molecular Weight
- 44224.335 Da
References
- McCormack PL: Cariprazine: First Global Approval. Drugs. 2015 Nov;75(17):2035-43. doi: 10.1007/s40265-015-0494-7. [Article]
- Stahl SM: Mechanism of action of cariprazine. CNS Spectr. 2016 Apr;21(2):123-7. doi: 10.1017/S1092852916000043. Epub 2016 Mar 9. [Article]
- FDA Approved Drug Products: VRAYLAR (cariprazine) capsules, for oral use [Link]
- Health Canada Approved Drug Products: VRAYLAR (Cariprazine) Oral Capsules [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Partial agonist
- Curator comments
- Inhibition constant (Ki) = 0.49 nmol/L for D2L, 0.69 nmol/L for D2S
- 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
- McCormack PL: Cariprazine: First Global Approval. Drugs. 2015 Nov;75(17):2035-43. doi: 10.1007/s40265-015-0494-7. [Article]
- Stahl SM: Mechanism of action of cariprazine. CNS Spectr. 2016 Apr;21(2):123-7. doi: 10.1017/S1092852916000043. Epub 2016 Mar 9. [Article]
- FDA Approved Drug Products: VRAYLAR (cariprazine) capsules, for oral use [Link]
- Health Canada Approved Drug Products: VRAYLAR (Cariprazine) Oral Capsules [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Partial agonist
- Curator comments
- Inhibition constant (Ki) = 2.6 nmol/L
- 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
- McCormack PL: Cariprazine: First Global Approval. Drugs. 2015 Nov;75(17):2035-43. doi: 10.1007/s40265-015-0494-7. [Article]
- Stahl SM: Mechanism of action of cariprazine. CNS Spectr. 2016 Apr;21(2):123-7. doi: 10.1017/S1092852916000043. Epub 2016 Mar 9. [Article]
- FDA Approved Drug Products: VRAYLAR (cariprazine) capsules, for oral use [Link]
- Health Canada Approved Drug Products: VRAYLAR (Cariprazine) Oral Capsules [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- Curator comments
- Inhibition constant (Ki) = 0.58 nmol/L
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation...
- Gene Name
- HTR2B
- Uniprot ID
- P41595
- Uniprot Name
- 5-hydroxytryptamine receptor 2B
- Molecular Weight
- 54297.41 Da
References
- McCormack PL: Cariprazine: First Global Approval. Drugs. 2015 Nov;75(17):2035-43. doi: 10.1007/s40265-015-0494-7. [Article]
- Stahl SM: Mechanism of action of cariprazine. CNS Spectr. 2016 Apr;21(2):123-7. doi: 10.1017/S1092852916000043. Epub 2016 Mar 9. [Article]
- FDA Approved Drug Products: VRAYLAR (cariprazine) capsules, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- Curator comments
- Inhibition constant (Ki) = 18.8 mmol/L
- 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
- McCormack PL: Cariprazine: First Global Approval. Drugs. 2015 Nov;75(17):2035-43. doi: 10.1007/s40265-015-0494-7. [Article]
- Stahl SM: Mechanism of action of cariprazine. CNS Spectr. 2016 Apr;21(2):123-7. doi: 10.1017/S1092852916000043. Epub 2016 Mar 9. [Article]
- FDA Approved Drug Products: VRAYLAR (cariprazine) capsules, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- Curator comments
- Inhibition constant (Ki) = 23 nmol/L
- General Function
- Histamine receptor activity
- Specific Function
- In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
- Gene Name
- HRH1
- Uniprot ID
- P35367
- Uniprot Name
- Histamine H1 receptor
- Molecular Weight
- 55783.61 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- Curator comments
- Inhibition constant (Ki) = 155 nM
- 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, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
- Gene Name
- HTR2C
- Uniprot ID
- P28335
- Uniprot Name
- 5-hydroxytryptamine receptor 2C
- Molecular Weight
- 51820.705 Da
References
- FDA Approved Drug Products: VRAYLAR (cariprazine) capsules, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- Curator comments
- Inhibition constant (Ki) = 134 nM
- General Function
- Protein heterodimerization activity
- Specific Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
- Gene Name
- ADRA1A
- Uniprot ID
- P35348
- Uniprot Name
- Alpha-1A adrenergic receptor
- Molecular Weight
- 51486.005 Da
References
- FDA Approved Drug Products: VRAYLAR (cariprazine) capsules, for oral use [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitorInducer
- Curator comments
- Based on in vitro results, cariprazine has the potential to act as a CYP3A4/3A5 inducer at the intestinal level. Cariprazine and its major active metabolites were weak inhibitors in vitro.
- 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
- Citrome L: Cariprazine: chemistry, pharmacodynamics, pharmacokinetics, and metabolism, clinical efficacy, safety, and tolerability. Expert Opin Drug Metab Toxicol. 2013 Feb;9(2):193-206. doi: 10.1517/17425255.2013.759211. [Article]
- FDA Approved Drug Products: VRAYLAR (cariprazine) capsules, for oral use [Link]
- Health Canada Approved Drug Products: VRAYLAR (Cariprazine) Oral Capsules [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- Curator comments
- Cariprazine and its major active metabolites were weak inhibitors in vitro.
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Citrome L: Cariprazine: chemistry, pharmacodynamics, pharmacokinetics, and metabolism, clinical efficacy, safety, and tolerability. Expert Opin Drug Metab Toxicol. 2013 Feb;9(2):193-206. doi: 10.1517/17425255.2013.759211. [Article]
- FDA Approved Drug Products: VRAYLAR (cariprazine) capsules, for oral use [Link]
- Health Canada Approved Drug Products: VRAYLAR (Cariprazine) Oral Capsules [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inducer
- Curator comments
- Based on in vitro results, cariprazine has the potential to act as a CYP3A4/3A5 inducer at the intestinal level.
- General Function
- Oxygen binding
- 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 oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Health Canada Approved Drug Products: VRAYLAR (Cariprazine) Oral Capsules [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Cariprazine and its major active metabolites were weak inhibitors in vitro.
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- 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 oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- FDA Approved Drug Products: VRAYLAR (cariprazine) capsules, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Cariprazine and its major active metabolites were weak inhibitors in vitro.
- General Function
- Steroid 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 oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- FDA Approved Drug Products: VRAYLAR (cariprazine) capsules, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Cariprazine, but not its active metabolites, was a weak inhibitor in vitro.
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- FDA Approved Drug Products: VRAYLAR (cariprazine) capsules, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Cariprazine, but not its active metabolites, was a weak inhibitor in vitro.
- General Function
- Steroid hydroxylase activity
- Specific Function
- Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
- Gene Name
- CYP2E1
- Uniprot ID
- P05181
- Uniprot Name
- Cytochrome P450 2E1
- Molecular Weight
- 56848.42 Da
References
- FDA Approved Drug Products: VRAYLAR (cariprazine) capsules, for oral use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- Curator comments
- Based on in vitro results, cariprazine has the potential to act as a weak P-glycoprotein (P-gp) inhibitor at the intestinal level.
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Health Canada Approved Drug Products: VRAYLAR (Cariprazine) Oral Capsules [Link]
Drug created at November 18, 2007 18:29 / Updated at May 03, 2022 17:30