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CYP2C8 is involved in the metabolism of many drugs. So, it is important to assess in vivo the inhibitory 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 CYP2C8 probe substrate montelukast.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Montelukast | Other | 10mg montelukast alone followed by 10mg montelukast + 400mg ASP2151 |
|
| ASP2151 | Other | 10mg montelukast + 400mg ASP2151 followed by 10mg montelukast alone |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Montelukast | Drug |
|
| |
| ASP2151 |
| Measure | Description | Time Frame |
|---|---|---|
| Peak Plasma Concentration (Cmax) of Montelukast | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention | |
| Time of Peak Concentration (Tmax) of Montelukast | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention | |
| Area Under the Curve (AUC) of Montelukast | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention | |
| Half-Life (t1/2) of Montelukast | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention | |
| Apparent Volume of Distribution (Vd/f) of Montelukast | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention | |
| Apparent Total Body Clearance (CL/f) of Montelukast | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention |
| 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 Methyl Hydroxymontelukast | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention | |
| Time of Peak Concentration (Tmax) of Methyl Hydroxymontelukast |
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-December 2014 to 01-April 2015
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| ID | Title | Description |
|---|---|---|
| FG000 | Montelukast, Then Montelukast + ASP2151 | 10mg montelukast alone followed by 10mg montelukast + 400mg ASP2151 Montelukast ASP2151 |
| FG001 | Montelukast + ASP2151, Then Montelukast | 10mg montelukast + 400mg ASP2151 followed by 10mg montelukast alone Montelukast ASP2151 |
| Title | Milestones | Reasons Not Completed | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study |
|
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| ID | Title | Description |
|---|---|---|
| BG000 | Montelukast, Then Montelukast + ASP2151 | 10mg montelukast alone followed by 10mg montelukast + 400mg ASP2151 Montelukast ASP2151 |
| BG001 | Montelukast + ASP2151, Then Montelukast |
| 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 Montelukast | Posted | Geometric Mean | Geometric Coefficient of Variation | ng/mL | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention |
|
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 | Montelukast | Participants received montelukast 10 mg alone in first or second intervention |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Oropharyngeal pain | Respiratory, thoracic and mediastinal 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 |
|---|---|
| C093875 | montelukast |
| C568714 | ASP2151 |
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| Drug |
|
| Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention |
| Area Under the Curve (AUC) of Methyl Hydroxymontelukast | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention |
| Half-Life (t1/2) of Methyl Hydroxymontelukast | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention |
| Peak Plasma Concentration (Cmax) of ASP2151 | Blood samples were taken at pre-dose of Day 1 and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24h after post doses in first or second intervention |
| Time of Peak Concentration (Tmax) of ASP2151 | Blood samples were taken at pre-dose of Day 1 and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24h after post doses in first or second intervention |
| Area Under the Curve (AUC) of ASP2151 | Blood samples were taken at pre-dose of Day 1 and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24h after post doses in first or second intervention |
| Half-Life (t1/2) of ASP2151 | Blood samples were taken at pre-dose of Day 1 and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24h after post doses in first or second intervention |
| Apparent Volume of Distribution (Vd/f) of ASP2151 | Blood samples were taken at pre-dose of Day 1 and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24h after post doses in first or second intervention |
| Apparent Total Body Clearance (CL/f) of ASP2151 | Blood samples were taken at pre-dose of Day 1 and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24h after post doses in first or second intervention |
10mg montelukast + 400mg ASP2151 followed by 10mg montelukast alone
Montelukast
ASP2151
| BG002 | Total | Total of all reporting groups |
| 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 | Count of Participants | Participants |
|
| Units |
|---|
| Counts |
|---|
| Participants |
|
|
| Primary | Time of Peak Concentration (Tmax) of Montelukast | Posted | Median | Full Range | h | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention |
|
|
|
| Primary | Area Under the Curve (AUC) of Montelukast | Posted | Geometric Mean | Geometric Coefficient of Variation | h*ng/mL | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention |
|
|
|
| Primary | Half-Life (t1/2) of Montelukast | Posted | Geometric Mean | Geometric Coefficient of Variation | h | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention |
|
|
|
| Primary | Apparent Volume of Distribution (Vd/f) of Montelukast | Posted | Mean | Standard Deviation | L | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention |
|
|
|
| Primary | Apparent Total Body Clearance (CL/f) of Montelukast | Posted | Mean | Standard Deviation | L/h | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention |
|
|
|
| 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 Methyl Hydroxymontelukast | Posted | Geometric Mean | Geometric Coefficient of Variation | ng/mL | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention |
|
|
|
| Other Pre-specified | Time of Peak Concentration (Tmax) of Methyl Hydroxymontelukast | Posted | Median | Full Range | h | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention |
|
|
|
| Other Pre-specified | Area Under the Curve (AUC) of Methyl Hydroxymontelukast | Posted | Geometric Mean | Geometric Coefficient of Variation | h*ng/mL | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention |
|
|
|
| Other Pre-specified | Half-Life (t1/2) of Methyl Hydroxymontelukast | Posted | Geometric Mean | Geometric Coefficient of Variation | h | Blood samples were taken at pre-dose of Day 1 and 0.5, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 30, 36, 48 and 72h after post doses in first or second intervention |
|
|
|
| Other Pre-specified | Peak Plasma Concentration (Cmax) of ASP2151 | Posted | Geometric Mean | Geometric Coefficient of Variation | ng/mL | Blood samples were taken at pre-dose of Day 1 and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24h after post doses in first or second intervention |
|
|
|
| Other Pre-specified | Time of Peak Concentration (Tmax) of ASP2151 | Posted | Median | Full Range | h | Blood samples were taken at pre-dose of Day 1 and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24h after post doses in first or second intervention |
|
|
|
| Other Pre-specified | Area Under the Curve (AUC) of ASP2151 | Posted | Geometric Mean | Geometric Coefficient of Variation | h*ng/mL | Blood samples were taken at pre-dose of Day 1 and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24h after post doses in first or second intervention |
|
|
|
| Other Pre-specified | Half-Life (t1/2) of ASP2151 | Posted | Geometric Mean | Geometric Coefficient of Variation | h | Blood samples were taken at pre-dose of Day 1 and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24h after post doses in first or second intervention |
|
|
|
| Other Pre-specified | Apparent Volume of Distribution (Vd/f) of ASP2151 | Posted | Mean | Standard Deviation | L | Blood samples were taken at pre-dose of Day 1 and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24h after post doses in first or second intervention |
|
|
|
| Other Pre-specified | Apparent Total Body Clearance (CL/f) of ASP2151 | Posted | Mean | Standard Deviation | L/h | Blood samples were taken at pre-dose of Day 1 and 0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24h after post doses in first or second intervention |
|
|
|
| 0 |
| 24 |
| 0 |
| 24 |
| 7 |
| 24 |
| EG001 | ASP2151 | Participants received montelukast 10 mg with ASP2151 400mg in first or second intervention | 0 | 24 | 0 | 24 | 2 | 24 |
| Cough | Respiratory, thoracic and mediastinal disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Nasal congestion | Respiratory, thoracic and mediastinal disorders | MedDRA/18.0 | Non-systematic Assessment |
|
| Gingivitis | Infections and infestations | MedDRA/18.0 | Non-systematic Assessment |
|
| Nasopharyngitis | Infections and infestations | MedDRA/18.0 | Non-systematic Assessment |
|
| Rhinitis | Infections and infestations | MedDRA/18.0 | Non-systematic Assessment |
|
| Headache | Nervous system 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 |