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This study is conducted to determine whether the test product (GW483100 10 mg containing montelukast sodium equivalent to 10 mg of montelukast) is bioequivalent to the reference montelukast sodium 10 mg tablets (innovator product) in healthy adult volunteers under fasting conditions. This is an open-label, balanced, randomized, single dose, two-way crossover study, enrolling 32 healthy human subjects to ensure at least 28 subjects complete the study. Each subject enrolled will participate in two treatment periods separated by a washout period of at least 7 days and no more than 14 days between dosing occasions. Total duration in the study for each subject will be approximately 7 weeks from screening to the subject's last visit.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Sequence A-B (Test Montelukast then Reference Montelukast) | Experimental | Subjects will receive Treatment A- Test montelukast sodium 10 mg tablets (GW483100) in Treatment Period 1 and then Treatment B - Reference montelukast sodium 10 mg tablets (innovator product) in Treatment Period 2. |
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| Sequence B-A (Reference Montelukast then Test Montelukast) | Experimental | Subjects will receive Treatment B- Reference montelukast sodium 10 mg tablets (innovator product) in Treatment Period 1 and then Treatment A Test montelukast sodium 10 mg tablets (GW483100) in Treatment Period 2. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Test Montelukast | Drug | Test Montelukast (GW483100) is available as round, biconvex, pink 10 mg film-coated tablet (containing montelukast sodium equivalent to 10 mg of montelukast) and is administered as a single dose with 240 mL of water. |
| Measure | Description | Time Frame |
|---|---|---|
| Area under the concentration versus time from time zero to infinity (AUC(0 ∞)) for montelukast in relevant treatments | Blood samples will be withdrawn on Day 1 and Day 2, and concentrations of montelukast will be determined in plasma samples. Plasma montelukast concentration-time will be analyzed by non-compartmental method and the PK parameters will be derived. | Samples will be collected at Pre-dose, 0.50, 1.00, 1.50, 2.00, 2.33, 2.67, 3.00, 3.33, 3.67, 4.00, 4.50, 5.00, 6.00, 8.00, 10.00, 12.00, 16.00 and 24.00 hours post-dose in each treatment period |
| AUC from time zero to last time point with measurable concentration (AUC(0-t)) for montelukast in relevant treatments | Blood samples will be withdrawn on Day 1 and Day 2, and concentrations of montelukast will be determined in plasma samples. Plasma montelukast concentration-time will be analyzed by non-compartmental method and the PK parameters will be derived. | Samples will be collected at Pre-dose, 0.50, 1.00, 1.50, 2.00, 2.33, 2.67, 3.00, 3.33, 3.67, 4.00, 4.50, 5.00, 6.00, 8.00, 10.00, 12.00, 16.00 and 24.00 hours post-dose in each treatment period |
| Maximum observed concentration (Cmax) for montelukast in relevant treatments | Blood samples will be withdrawn on Day 1 and Day 2, and concentrations of montelukast will be determined in plasma samples. Plasma montelukast concentration-time will be analyzed by non-compartmental method and the PK parameters will be derived. | Samples will be collected at Pre-dose, 0.50, 1.00, 1.50, 2.00, 2.33, 2.67, 3.00, 3.33, 3.67, 4.00, 4.50, 5.00, 6.00, 8.00, 10.00, 12.00, 16.00 and 24.00 hours post-dose in each treatment period |
| Measure | Description | Time Frame |
|---|---|---|
| Time of occurrence of Cmax (tmax) for montelukast in relevant treatments | Blood samples will be withdrawn on Day 1 and Day 2, and concentrations of montelukast will be determined in plasma samples. Plasma montelukast concentration-time will be analyzed by non-compartmental method and the PK parameters will be derived. | Samples will be collected at Pre-dose, 0.50, 1.00, 1.50, 2.00, 2.33, 2.67, 3.00, 3.33, 3.67, 4.00, 4.50, 5.00, 6.00, 8.00, 10.00, 12.00, 16.00 and 24.00 hours post-dose in each treatment period. |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| GSK Clinical Trials | GlaxoSmithKline | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| GSK Investigational Site | Telangana | 500 013 | India |
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| Label | URL |
|---|---|
| Results for study 201681 can be found on the GSK Clinical Study Register. | View source |
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| ID | Term |
|---|---|
| D012120 | Respiration Disorders |
| D001249 | Asthma |
| D012220 | Rhinitis |
| ID | Term |
|---|---|
| D012140 | Respiratory Tract Diseases |
| D001982 | Bronchial Diseases |
| D008173 | Lung Diseases, Obstructive |
| D008171 | Lung Diseases |
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| Reference Montelukast | Drug | Reference Montelukast (innovator product) is available as pale beige, rounded square shaped,10 mg film-coated tablet (containing montelukast sodium equivalent to 10 mg of montelukast) and is administered as a single dose with 240 mL of water. Singular is the innovator product used for this study, which is a trade name owned by Merck Sharp and Dohme Corporation. |
|
| Percentage of AUC(0-∞) obtained by extrapolation (%AUCex) for montelukast in relevant treatments | Blood samples will be withdrawn on Day 1 and Day 2, and concentrations of montelukast will be determined in plasma samples. Plasma montelukast concentration-time will be analyzed by non-compartmental method and the PK parameters will be derived. | Samples will be collected at Pre-dose, 0.50, 1.00, 1.50, 2.00, 2.33, 2.67, 3.00, 3.33, 3.67, 4.00, 4.50, 5.00, 6.00, 8.00, 10.00, 12.00, 16.00 and 24.00 hours post-dose in each treatment period. |
| Terminal phase half-life (t½) for montelukast in relevant treatments | Blood samples will be withdrawn on Day 1 and Day 2, and concentrations of montelukast will be determined in plasma samples. Plasma montelukast concentration-time will be analyzed by non-compartmental method and the PK parameters will be derived. | Samples will be collected at Pre-dose, 0.50, 1.00, 1.50, 2.00, 2.33, 2.67, 3.00, 3.33, 3.67, 4.00, 4.50, 5.00, 6.00, 8.00, 10.00, 12.00, 16.00 and 24.00 hours post-dose in each treatment period. |
| Blood pressure (BP) as a measure of safety and tolerability | Systolic and diastolic BP will be measured in supine position after 5 minutes rest. | 3 days in each treatment period (assessed up to 3 weeks) |
| Pulse rate measurements as a measure of safety and tolerability | Pulse rate measurements will be measured in supine position after 5 minutes rest. | 3 days in each treatment period (assessed up to 3 weeks) |
| Number of participants with adverse events (AEs) | AEs will be collected from the start of study treatment until the subject's last visit. | Up to 7 weeks |
| Composite of hematology parameters as a measure of safety | 1 day in Treatment Period 1 and 2 days in Treatment Period 2 (assessed up to 3 weeks) |
| Composite of clinical chemistry parameters as a measure of safety | 1 day in Treatment Period 1 and 2 days in Treatment Period 2 (assessed up to 3 weeks) |
| Composite of urinalysis parameters as a measure of safety | 1 day in Treatment Period 1 and 2 days in Treatment Period 2 (assessed up to 3 weeks) |
| D012130 |
| Respiratory Hypersensitivity |
| D006969 | Hypersensitivity, Immediate |
| D006967 | Hypersensitivity |
| D007154 | Immune System Diseases |
| D012141 | Respiratory Tract Infections |
| D007239 | Infections |
| D009668 | Nose Diseases |
| D010038 | Otorhinolaryngologic Diseases |