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Quetiapine, formulation

Phase 3

Bipolar Disorder | Small molecule | Psychiatry |Johnson & Johnson|Last Updated: Jun 20, 2014

Target and mechanism

Molecular targetHTR2A, DRD2, HTR2C
Target classAntagonist
ModalitySmall molecule
ChEMBLCHEMBL716

Also known as Quetiapine, oral formulation, Quetiapine, Quetiapine XR

Success Probability

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Market & Valuation

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Trial Design

RandomizedDouble-BlindPLACEBO_CONTROLLED
Total Trials1
Total Enrollment493

FDA Designations

No designations recorded

Clinical trial landscape

Quetiapine, formulation · 2 trials · 3 indications

Phase 3 1Phase 1 1
NCT00309699A Study to Evaluate the Efficacy and Safety of Flexible Doses of Extended-release (ER) Paliperidone Compared With Flexible Doses of Quetiapine and Placebo in Patients With Bipolar I DisorderBipolar Disorder
COMPLETED493 Analytics
PHASE3COMPLETED
A Study to Evaluate the Efficacy and Safety of Flexible Doses of Extended-release (ER) Paliperidone Compared With Flexible Doses of Quetiapine and Placebo in Patients With Bipolar I Disorder
Bipolar DisorderUnlock trial analytics

Study Endpoints

Primary Endpoints

The primary effectiveness outcome is the change in the total YMRS score from baseline to the last assessment during the acute treatment phase.
3 weeks
Aripiprazole concentration in venous and capillary plasma, venous and capillary whole blood
16 time points over 408 hours postdose
Quetiapine concentration in venous and capillary plasma, venous and capillary whole blood
12 time points over 108 hours postdose
Olanzapine concentration in venous and capillary plasma, venous and capillary whole blood
12 time points over 108 hours postdose
Risperidone concentration in venous and capillary plasma, venous and capillary whole blood
12 time points over 108 hours postdose
Paliperidone concentration in venous and capillary plasma, venous and capillary whole blood
12 time points over 108 hours postdose
Dehydroaripiprazole concentration in venous and capillary plasma, venous and capillary whole blood
16 time points over 408 hours postdose
9 hydroxy-risperidone concentration in venous and capillary plasma, venous and capillary whole blood
12 time points over 108 hours postdose

Secondary Endpoints

The secondary effectiveness outcomes are the change in GAF from baseline to endpoint or the last assessment during the acute treatment phase and the change in total YMRS score from baseline to endpoint or the last assessment during the maintenance phase.
12 weeks
Incidence of adverse events as a measure of safety and tolerability
Approximately 26 days (Cohorts B, C, D, E), and approximately 39 days (Cohort A)
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Study Design & Arms

AllocationRANDOMIZED
MaskingQUADRUPLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
003PLACEBO_COMPARATORPlacebo Daily for 3 weeks
002ACTIVE_COMPARATORQuetiapine 400 to 800 mg daily, initially titrated and flexibly dosed, for 12 weeks
001EXPERIMENTALPaliperidone ER 3 to 12 mg daily, flexibly dosed, for 12 weeks
Cohort A: AripiprazoleEXPERIMENTAL -
Cohort B: QuetiapineEXPERIMENTAL -
Cohort C: OlanzapineEXPERIMENTAL -
Cohort D: RisperidoneEXPERIMENTAL -
Cohort E: PaliperidoneEXPERIMENTAL -

Interventions

NameTypeDescription
PlaceboDRUGDaily for 3 weeks
QuetiapineDRUG400 to 800 mg daily, initially titrated and flexibly dosed, for 12 weeks
Paliperidone ERDRUG3 to 12 mg daily, flexibly dosed, for 12 weeks
AripiprazoleDRUGType= exact number, unit= mg, number= 5, form= tablet, route= oral administration. A single oral dose of a 5-mg aripiprazole tablet will be administered after an overnight fast.
OlanzapineDRUGType= exact number, unit= mg, number= 5, form= tablet, route= oral administration. A single oral dose of a 5-mg olanzapine tablet will be administered after an overnight fast.
RisperidoneDRUGType= exact number, unit= mg, number= 1, form= tablet, route= oral administration. A single oral dose of a 1-mg risperidone tablet will be administered after an overnight fast.
PaliperidoneDRUGType= exact number, unit= mg, number= 3, form= tablet, route= oral administration. A single oral dose of a 3-mg paliperidone tablet will be administered after an overnight fast.
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Eligibility Criteria

Age Range18 Years to 65 Years
SexALL
Healthy VolunteersNo
Study Sites47

Inclusion Criteria: * Meets Diagnostic and Statistical Manual of Mental Disorders-Fourth Edition (DSM IV) criteria for Bipolar I Disorder, Most Recent Episode Manic or Mixed (with or without psychotic features) * history of at least 1 previously documented manic or mixed episode requiring medical t...

Countries:United StatesGreeceLithuaniaRussiaSouth KoreaTaiwanTurkey (Türkiye)UkraineBelgium
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Frequently asked questions about Quetiapine, formulation

What is quetiapine used for?

Quetiapine is an oral antipsychotic medicine studied and used in psychiatry, including for bipolar disorder. In the clinical program described here it was evaluated in patients with bipolar I disorder and mood disorders, and separately in healthy volunteers for blood concentration comparisons. It is available in immediate-release and extended-release oral formulations, including a 50 mg extended-release strength.

What does quetiapine target?

Quetiapine targets the serotonin 2A receptor (HTR2A), the dopamine D2 receptor (DRD2), and the serotonin 2C receptor (HTR2C). It acts as an antagonist at these receptors. This receptor binding profile underlies its activity as a small-molecule antipsychotic agent used in psychiatric conditions such as bipolar disorder.

Who makes quetiapine?

Quetiapine is developed by Johnson & Johnson, which trades under the ticker JNJ. The company is associated with the oral quetiapine formulations, including immediate-release quetiapine and the extended-release version known as quetiapine XR, which is also available in a 50 mg strength.

What phase is quetiapine in?

Quetiapine has been studied in Phase 3 clinical development for bipolar disorder. The Phase 3 trial in this program is completed, and no trials are currently active. A separate Phase 1 study in healthy volunteers has also been completed. Quetiapine is an established oral small-molecule antipsychotic available in immediate-release and extended-release formulations.

What clinical trials is quetiapine in?

Quetiapine has been evaluated in two completed trials. NCT00309699 was a Phase 3, randomized, double-blind, placebo-controlled study of flexible-dose extended-release paliperidone compared with flexible-dose quetiapine and placebo in 493 patients with bipolar I disorder across multiple countries. NCT01607762 was a Phase 1 study comparing capillary and venous whole blood and plasma concentrations of five antipsychotics in 31 healthy volunteers in Belgium.

Is quetiapine the same as quetiapine XR?

Quetiapine XR is an extended-release oral formulation of quetiapine, so the two names refer to related forms of the same medicine rather than different drugs. Quetiapine XR is also available in a 50 mg strength. Other names used for this asset include quetiapine oral formulation and quetiapine XR 50 mg.