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Pharmacodynamic and Pharmacokinetic Dose Ranging Study of Tiotropium Bromide Administered Via Inhalation Solution in Patients With Chronic Obstructive Pulmonary Disease (COPD)

Phase 2
Completed
Conditions
Mild to Moderate Chronic Obstructive Pulmonary Disease (COPD)
Interventions
Drug: GSP304 Placebo Inhalation Solution
Drug: GSP304 (tiotropium bromide) Inhalation Solution
Registration Number
NCT03118765
Lead Sponsor
Glenmark Specialty S.A.
Brief Summary

Pharmacodynamic and Pharmacokinetic Dose Ranging Study of Tiotropium Bromide Administered Via Inhalation Solution in Patients With Chronic Obstructive Pulmonary Disease (COPD).

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
155
Inclusion Criteria
  • Male and female subjects ≥40 years and ≤85 years of age at the time of consent.
  • Subject must have a primary diagnosis of mild or moderate COPD defined as post-bronchodilator FEV1/FVC ratio of <70% and FEV1 of ≥50% of predicted normal value as per the NHANES III predicted normal values at screening.
  • Willing to stop all other COPD medications or other medications which will interfere with the study results for the entire duration of the study, except albuterol/salbutamol as needed.
  • Current or ex-smoker with ≥10 pack-year smoking history.
Exclusion Criteria
  • Subjects with a chest x-ray/CT scan that suggests a diagnosis other than COPD (eg, pneumonia, other infection, atelectasis, or pneumothorax or other active/ongoing pulmonary conditions) and taken within 6 months prior to study start. If there is no chest x-ray or CT scan taken within 6 months prior to study start, or if recent results are unavailable for review, a chest x-ray must be performed.
  • Use of oral/parenteral corticosteroids or antibiotics for COPD within 6 weeks or depot corticosteroids within 3 months prior to screening or subject has had a change in dose or type of any medications for COPD within 14 days before screening.
  • Hospitalization for COPD exacerbation or pneumonia within 3 months prior to screening.
  • Subjects with a history of asthma, with the exception of outgrown childhood asthma, defined as transient wheezers outgrown by 5 years of age.
  • Subject has a known history of alpha 1 antitrypsin deficiency-related emphysema.
  • Subject requires nocturnal oxygen or continuous supplemental oxygen therapy.
  • Subject with history of a positive result for HBsAg or HCV antibody.
  • Subject is known to be seropositive for human immunodeficiency virus.
  • Female subject is pregnant or lactating.
  • Subject has a history of allergic reaction to the anti-cholinergic or any components of the study medications.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Test Treatment T4: GSP304 Placebo Inhalation SolutionGSP304 Placebo Inhalation Solution-
Test Treatment T1: GSP304 Inhalation SolutionGSP304 (tiotropium bromide) Inhalation Solution-
Test Treatment T2: GSP304 Inhalation SolutionGSP304 (tiotropium bromide) Inhalation Solution-
Test Treatment T3: GSP304 Inhalation SolutionGSP304 (tiotropium bromide) Inhalation Solution-
Test Treatment T5: Spiriva® Respimat® inhalation spraySpiriva® Respimat® inhalation spray-
Primary Outcome Measures
NameTimeMethod
Relative Bioavailability of Tiotropium With GSP304 in Comparison to SPIRIVA RESPIMAT 5 μg Based on CmaxSSPlasma concentrations on day 21 according to the below schedule: Pre-dose (0 hour), and at 2, 4, 6, 10, 15, 30, and 45, 60, 75, and 90 minutes post-dose, as well as 2, 4, 6, 8, 12, 16, 20 and 24 hours post-dose.

The PK endpoint in plasma to assess the relative bioavailability was peak concentrations of tiotropium during the dosing interval at steady-state (CmaxSS)

Relative Bioavailability of Tiotropium With GSP 304 in Comparison to SPIRIVA RESPIMAT 5 μg Based on AUC0-tauSSPlasma concentrations on day 21 according to the below schedule: Pre-dose (0 hour), and at 2, 4, 6, 10, 15, 30, and 45, 60, 75, and 90 minutes post-dose, as well as 2, 4, 6, 8, 12, 16, 20 and 24 hours post-dose.

The PK endpoint in plasma to assess the relative bioavailability was area under the plasma concentration-time curve of tiotropium over the dosing interval at steady state (AUC0-tauSS)

Change From Baseline (Day 1) in Trough FEV1 at 24 Hours After the Last Dose of Treatment on Day 21 in Comparison to Placebo.21 days (Pre- dose trough FEV1 is mean FEV1 at -45 mins and -15 mins pre-morning dose at Day 1. Trough FEV1 is mean FEV1 obtained 23 hrs 15 mins and 23 hrs 45 mins post-morning dose of day 21).

Change from baseline (Day 1) at Day 21 (Week 3) in trough FEV1 response at approximately 24 hours after the last dose (average of 23 hours 15 minutes and 23 hours 45 minutes postdose measurements), in comparison with placebo.

Secondary Outcome Measures
NameTimeMethod
Amount (Aetau) of Tiotropium Excreted in Urine Over the Dosing Interval on Day 21Day 21

Descriptive statistics for tiotropium urine PK parameter - Amount (Aetau) of Tiotropium Excreted in Urine Over the Dosing Interval on Day 21

Fraction of Dose (Fe) of Tiotropium Excreted in Urine Over the Dosing Interval on Day 1Day 1

Descriptive statistics for tiotropium urine PK parameter - Fraction of dose (Fe) of tiotropium excreted in urine over the dosing interval on Day 1

Amount (Aetau) (Cumulative Amount of Unchanged Drug Excreted Into the Urine Over the Dosing Interval) of Tiotropium Excreted in Urine Over the Dosing Interval on Day 1Day 1

Descriptive statistics for tiotropium urine PK parameter - Amount (Aetau) of tiotropium excreted in urine over the dosing interval on Day 1

Fraction of Dose (Fe) of Tiotropium Excreted in Urine Over the Dosing Interval on Day 21Day 21

Descriptive statistics for tiotropium urine PK parameter-Fraction of Dose (Fe) of Tiotropium Excreted in Urine Over the Dosing Interval on Day 21

Time of Peak Drug Concentration Over the Dosing Interval (Tmax) on Day 1Day 1

Descriptive statistics for tiotropium plasma PK parameter - Time of peak drug concentration over the dosing interval (tmax) on Day 1

Peak Concentrations During the Dosing Interval (Cmax) on Day 1Day 1

Descriptive statistics for tiotropium plasma PK parameters - (Cmax) on Day 1

Accumulation Ratio Rac(Auc)Day 21

Descriptive statistics for tiotropium plasma PK parameter-Accumulation ratio Rac(auc). Rac(auc) was calculated as AUC0-tauSS/AUC0-tau.

Change From Baseline in Time-normalized Area Under the Curve for FEV1 Measured Over 12 Hours on Day 1Day 1 (Pre-dose FEV1 at -45 mins and 15 mins prior to dosing on Day 1. On Day 1 FEV1 at post-dose at 5 mins ±3, 15 mins ±2, 30 mins ±5, 60 mins, 90 mins, and 2 hours; and post-dose at 4, 6, 8, 10, 12 hours after the morning dose).

Least Square Mean (SE) change from baseline in time-normalized area under the curve for FEV1 measured over 12 hours on Day 1.

Change From Baseline in Time-normalized Area Under the Curve for FEV1 Measured Over 12 Hours on Day 21Day 21(Pre-dose FEV1 at -45 mins and 15 mins prior to dosing on Day 21. On Day 21, FEV1 at post-dose at 5 mins ±3, 15 mins ±2, 30 mins ±5, 60 mins, 90 mins, and 2 hours; and post-dose at 4, 6, 8, 10, 12 hours after the morning dose).

Least Square Mean (SE) change from baseline in time-normalized area under the curve for FEV1 Measured Over 12 Hours on Day 21.

Change From Baseline in Forced Vital Capacity (FVC) on Day 1Day 1 (Pre-dose FVC at -45 mins and 15 mins prior to dosing on Day 1. Postdose timing were relative to the end of dosing.The window for 1 hour spirometry and thereafter was ±5 minutes).

Least Square Mean change from baseline in forced vital capacity (FVC) to end of Day 1.

Area Under the Plasma Concentration-time Curve Over the Dosing Interval (AUC0-tau) on Day 1Day 1

Descriptive statistics for tiotropium plasma PK parameter - Area under the plasma concentration-time curve over the dosing interval (AUC0-tau) on Day 1

Change From Baseline in Peak FEV1 Within 12 Hours Post-dose on Day 21Day 21(Pre-dose FEV1 at -45 mins and 15 mins prior to dosing on Day 21. On Day 21, FEV1 at post-dose at 5 mins ±3, 15 mins ±2, 30 mins ±5, 60 mins, 90 mins, and 2 hours; and post-dose at 4, 6, 8, 10, 12 hours after the morning dose).

The least square mean change from baseline to peak FEV1 within 12 hours postdose on Day 21. Change from baseline in peak FEV1 within 12 hours postdose on Day 21 was derived from the serial readings taken through 12 hours postdose and calculating the change from baseline.

Time of Peak Drug Concentration Over the Dosing Interval (Tmax) on Day 21Day 21

Descriptive statistics for tiotropium plasma PK parameter - Time of peak drug concentration over the dosing interval (tmax) on Day 21

Average Concentration During a Dosing Interval at Steady State (CavSS) on Day 21Day 21

Descriptive statistics for tiotropium plasma PK parameter - Average concentration during a dosing interval at steady state (CavSS) on day 21

Accumulation Ratio Rac(Cmax)Day 21

Descriptive statistics for tiotropium plasma PK parameter-Accumulation ratio Rac(cmax). Rac(Cmax) was calculated as CmaxSS/Cmax.

Change From Baseline in Peak FEV1 Within 12 Hours Post-dose on Day 1Day 1 (Pre-dose FEV1 at -45 mins and 15 mins prior to dosing on Day 1. On Day 1 FEV1 at post-dose at 5 mins ±3, 15 mins ±2, 30 mins ±5, 60 mins, 90 mins, and 2 hours; and post-dose at 4, 6, 8, 10, 12 hours after the morning dose).

The least square mean change from baseline to peak FEV1 within 12 hours postdose on Day 1. Change from baseline in peak FEV1 within 12 hours postdose on Day 1 was derived from the serial readings taken through 12 hours postdose and calculating the change from baseline.

Change From Baseline in Forced Vital Capacity (FVC) on Day 21Day 21 (Pre-dose FVC at -45 mins and 15 mins prior to dosing on Day 21. Postdose timing were relative to the end of dosing. The window for 1 hour spirometry and thereafter was ±5 minutes).

Least Square Mean change from baseline in forced vital capacity (FVC) to end of Day 21

Trial Locations

Locations (25)

Glenmark Investigational Site 13

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Winter Park, Florida, United States

Glenmark Investigational Site 22

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Columbus, Ohio, United States

Glenmark Investigational Site 3

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Easley, South Carolina, United States

Glenmark Investigational Site 7

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Spartanburg, South Carolina, United States

Glenmark Investigational Site 10

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Miami Lakes, Florida, United States

Glenmark Investigational Site 24

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Miami, Florida, United States

Glenmark Investigational Site 11

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Medford, Oregon, United States

Glenmark Investigational Site 20

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Ormond Beach, Florida, United States

Glenmark Investigational Site 12

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Phoenix, Arizona, United States

Glenmark Investigational Site 23

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Andalusia, Alabama, United States

Glenmark Investigational Site 14

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Tempe, Arizona, United States

Glenmark Investigational Site 17

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Fullerton, California, United States

Glenmark Investigational Site 16

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Miami, Florida, United States

Glenmark Investigational Site 8

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Dublin, Ohio, United States

Glenmark Investigational Site 25

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Tomball, Texas, United States

Glenmark Investigational Site 19

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Edgewater, Florida, United States

Glenmark Investigational Site 6

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Orlando, Florida, United States

Glenmark Investigational Site 21

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Vero Beach, Florida, United States

Glenmark Investigational Site 18

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Las Vegas, Nevada, United States

Glenmark Investigational Site 15

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Spartanburg, South Carolina, United States

Glenmark Investigational Site 4

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Greenville, South Carolina, United States

Glenmark Investigational Site 1

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Rock Hill, South Carolina, United States

Glenmark Investigational Site 9

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Charlotte, North Carolina, United States

Glenmark Investigational Site 5

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Columbus, Ohio, United States

Glenmark Investigational Site 2

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Greenville, South Carolina, United States

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