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CYP2B6 is involved in the metabolism of many drugs. So, it is important to assess in vivo the effect of ASP2151 on that enzyme to determine any possible drug interactions. The aim of this trial is to investigate the potential for interaction of ASP2151 with the CYP2B6 probe substrate bupropion.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Bupropion + ASP2151 | Other | 400 mg ASP2151 followed by 150 mg Bupropion |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Bupropion | Drug |
|
| |
| ASP2151 |
| Measure | Description | Time Frame |
|---|---|---|
| Peak Plasma Concentration (Cmax) of Bupropion | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 | |
| Area Under the Concentration-time Curve Extrapolated to Infinite Time (AUC0-∞) of Bupropion | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
| Measure | Description | Time Frame |
|---|---|---|
| Number of Participants With Serious and Non-Serious Adverse Events | Refer to the result of adverse event. | Up to 32 days after the last dose |
| Measure | Description | Time Frame |
|---|---|---|
| Peak Plasma Concentration (Cmax) of Hydroxybupropion | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 | |
| Time of Peak Concentration (Tmax) of Hydroxybupropion | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
Inclusion Criteria:
Exclusion Criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Hammersmith Medicines Research Ltd | London | NW10 7EW | United Kingdom |
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Participants took part in the study at one investigative site in United Kingdom from 03-February 2015 to 17-April 2015
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| ID | Title | Description |
|---|---|---|
| FG000 | Bupropion + ASP2151 | 400 mg ASP2151 followed by 150 mg Bupropion Bupropion ASP2151 |
| Title | Milestones | Reasons Not Completed | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study |
|
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| ID | Title | Description |
|---|---|---|
| BG000 | Bupropion + ASP2151 | 400 mg ASP2151 followed by 150 mg Bupropion Bupropion ASP2151 |
| Units | Counts |
|---|---|
| Participants |
|
| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes |
|---|---|---|---|---|---|---|---|---|---|
| Age, Categorical | Count of Participants |
| Type | Title | Description | Population Description | Reporting Status | Anticipated Posting Date | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Time Frame | Units Analyzed | Denominator Units Selected | Arm/Group Information | Denominators | Classes | Analyses | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Primary | Peak Plasma Concentration (Cmax) of Bupropion | Posted | Geometric Mean | Geometric Coefficient of Variation | ng/mL | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
|
Up to 32 days after the last dose
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| ID | Title | Description | Deaths (Affected) | Deaths (At Risk) | Serious Events (Affected) | Serious Events (At Risk) | Other Events (Affected) | Other Events (At Risk) |
|---|---|---|---|---|---|---|---|---|
| EG000 | Bupropion | after dosing with bupropion on Day 1 and before the first dose of ASP2151 on Day 6. |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Headache | Nervous system disorders | MedDRA/18.0 | Non-systematic Assessment |
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| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Maruho Co.,Ltd. Kyoto R&D Center | Clinical Development Dept. | +81-75-325-3255 | ctinfo@mii.maruho.co.jp |
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| ID | Term |
|---|---|
| D006561 | Herpes Simplex |
| ID | Term |
|---|---|
| D006566 | Herpesviridae Infections |
| D004266 | DNA Virus Infections |
| D014777 | Virus Diseases |
| D007239 | Infections |
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| ID | Term |
|---|---|
| D016642 | Bupropion |
| C568714 | ASP2151 |
| ID | Term |
|---|---|
| D011427 | Propiophenones |
| D007659 | Ketones |
| D009930 | Organic Chemicals |
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| Drug |
|
| Area Under Concentration-Time Curve up to Last Non-zero Value (AUC0-tn) of Hydroxybupropion | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
| Area Under the Concentration-time Curve Extrapolated to Infinite Time (AUC0-∞) of Hydroxybupropion | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
| Half-life (t1/2) of Hydroxybupropion | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
| Trough Plasma Concentration (Ctrough) of ASP2151 | Days 6-14 and at pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h after dosing on Day 15 |
| Peak Plasma Concentration (Cmax) of ASP2151 | prior to initial dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h after dosing on Day 15 |
| Time of Peak Concentration (Tmax) of ASP2151 | prior to initial dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h after dosing on Day 15 |
| Area Under the Concentration-time Curve Over the Dosing Interval (AUC0-tau) of ASP2151 | prior to initial dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h after dosing on Day 15 |
| Area Under the Concentration-time Curve Extrapolated to Infinite Time (AUC0-∞) of ASP2151 | prior to initial dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h after dosing on Day 15 |
| Half-life (t1/2) of ASP2151 | prior to initial dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h after dosing on Day 15 |
| Apparent Volume of Distribution (Vd/F) of ASP2151 | prior to initial dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h after dosing on Day 15 |
| Apparent Total Body Clearance (CL/F) of ASP2151 | prior to initial dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h after dosing on Day 15 |
| Time of Peak Concentration (Tmax) of Bupropion | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
| Area Under the Curve Over up to Last No-zero Value (AUC0-tn) of Bupropion | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
| Half-life (t1/2) of Bupropion | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
| Apparent Volume of Distribution (Vd/F) of Bupropion | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
| Apparent Total Body Clearance (CL/F) of Bupropion | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
| Participants |
|
| Age, Continuous | Mean | Standard Deviation | year |
|
| Sex: Female, Male | Count of Participants | Participants |
|
| Ethnicity (NIH/OMB) | Count of Participants | Participants |
|
| Race (NIH/OMB) | Count of Participants | Participants |
|
| Region of Enrollment | Number | participants |
|
| Day 29 |
150 mg bupropion alone |
|
|
| Primary | Area Under the Concentration-time Curve Extrapolated to Infinite Time (AUC0-∞) of Bupropion | Posted | Geometric Mean | Geometric Coefficient of Variation | h*ng/mL | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
|
|
|
| Secondary | Number of Participants With Serious and Non-Serious Adverse Events | Refer to the result of adverse event. | Posted | Number | participants | Up to 32 days after the last dose |
|
|
|
| Other Pre-specified | Peak Plasma Concentration (Cmax) of Hydroxybupropion | Posted | Geometric Mean | Geometric Coefficient of Variation | ng/mL | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
|
|
|
| Other Pre-specified | Time of Peak Concentration (Tmax) of Hydroxybupropion | Posted | Median | Full Range | h | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
|
|
|
| Other Pre-specified | Area Under Concentration-Time Curve up to Last Non-zero Value (AUC0-tn) of Hydroxybupropion | Posted | Geometric Mean | Geometric Coefficient of Variation | h*ng/mL | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
|
|
|
| Other Pre-specified | Area Under the Concentration-time Curve Extrapolated to Infinite Time (AUC0-∞) of Hydroxybupropion | Posted | Geometric Mean | Geometric Coefficient of Variation | h*ng/mL | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
|
|
|
| Other Pre-specified | Half-life (t1/2) of Hydroxybupropion | Posted | Geometric Mean | Geometric Coefficient of Variation | h | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
|
|
|
| Other Pre-specified | Trough Plasma Concentration (Ctrough) of ASP2151 | Posted | Mean | Standard Deviation | ng/mL | Days 6-14 and at pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h after dosing on Day 15 |
|
|
|
| Other Pre-specified | Peak Plasma Concentration (Cmax) of ASP2151 | Posted | Geometric Mean | Geometric Coefficient of Variation | ng/mL | prior to initial dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h after dosing on Day 15 |
|
|
|
| Other Pre-specified | Time of Peak Concentration (Tmax) of ASP2151 | Posted | Median | Full Range | h | prior to initial dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h after dosing on Day 15 |
|
|
|
| Other Pre-specified | Area Under the Concentration-time Curve Over the Dosing Interval (AUC0-tau) of ASP2151 | Posted | Geometric Mean | Geometric Coefficient of Variation | h*ng/mL | prior to initial dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h after dosing on Day 15 |
|
|
|
| Other Pre-specified | Area Under the Concentration-time Curve Extrapolated to Infinite Time (AUC0-∞) of ASP2151 | Posted | Geometric Mean | Geometric Coefficient of Variation | h*ng/mL | prior to initial dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h after dosing on Day 15 |
|
|
|
| Other Pre-specified | Half-life (t1/2) of ASP2151 | Posted | Geometric Mean | Geometric Coefficient of Variation | h | prior to initial dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h after dosing on Day 15 |
|
|
|
| Other Pre-specified | Apparent Volume of Distribution (Vd/F) of ASP2151 | Posted | Mean | Standard Deviation | L | prior to initial dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h after dosing on Day 15 |
|
|
|
| Other Pre-specified | Apparent Total Body Clearance (CL/F) of ASP2151 | Posted | Mean | Standard Deviation | L/h | prior to initial dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h after dosing on Day 15 |
|
|
|
| Other Pre-specified | Time of Peak Concentration (Tmax) of Bupropion | Posted | Median | Full Range | h | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
|
|
|
| Other Pre-specified | Area Under the Curve Over up to Last No-zero Value (AUC0-tn) of Bupropion | Posted | Geometric Mean | Geometric Coefficient of Variation | h*ng/mL | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
|
|
|
| Other Pre-specified | Half-life (t1/2) of Bupropion | Posted | Geometric Mean | Geometric Coefficient of Variation | h | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
|
|
|
| Other Pre-specified | Apparent Volume of Distribution (Vd/F) of Bupropion | Posted | Mean | Standard Deviation | L | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
|
|
|
| Other Pre-specified | Apparent Total Body Clearance (CL/F) of Bupropion | Posted | Mean | Standard Deviation | L/h | prior to initial dose of Day 1 and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 60, 72 and 96 h after dosing on Day 1, Days 15, 22 and 29 |
|
|
|
| 0 |
| 24 |
| 0 |
| 24 |
| 4 |
| 24 |
| EG001 | ASP2151 After Bupropion | after the first dose of ASP2151 on Day 6, and before co-administration of bupropion and ASP2151 on Day 15. | 0 | 24 | 0 | 24 | 5 | 24 |
| EG002 | Bupropion With ASP2151 | after co-administration of bupropion and ASP2151 on Day 15. | 0 | 24 | 0 | 24 | 10 | 24 |
| EG003 | Total | 0 | 24 | 0 | 24 | 12 | 24 |
| Neuralgia | Nervous system disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Catheter site pain | General disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Catheter site haematoma | General disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Catheter site phlebitis | General disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Catheter site related reactions | General disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Vessel puncture site pain | General disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Rhinitis | Infections and infestations | MedDRA/18.0 | Non-systematic Assessment |
|
| Nasopharyngitis | Infections and infestations | MedDRA/18.0 | Non-systematic Assessment |
|
| Otitis media | Infections and infestations | MedDRA/18.0 | Non-systematic Assessment |
|
| Back pain | Musculoskeletal and connective tissue disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Musculoskeletal pain | Musculoskeletal and connective tissue disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Myalgia | Musculoskeletal and connective tissue disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Dry skin | Skin and subcutaneous tissue disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Rash | Skin and subcutaneous tissue disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Skin irritation | Skin and subcutaneous tissue disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Anxiety | Psychiatric disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Insomnia | Psychiatric disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Abdominal | Gastrointestinal disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Concstipation | Gastrointestinal disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Epistaxis | Respiratory, thoracic and mediastinal disorders | MedDRA/18.0 | Non-systematic Assessment |
|
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| D017193 |
| Skin Diseases, Viral |
| D012874 | Skin Diseases, Infectious |
| D012871 | Skin Diseases |
| D017437 | Skin and Connective Tissue Diseases |