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A Study to Investigate the Pharmacodynamic and Pharmacokinetic Interaction Between Aliskiren and Furosemide in Patients With Heart Failure

Registration Number
NCT01125514
Lead Sponsor
Novartis Pharmaceuticals
Brief Summary

This study assessed the interaction between single and multiple doses of aliskiren (150 mg and 300 mg) and furosemide (60 mg) in patients with heart failure.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
37
Inclusion Criteria
  • Systolic or diastolic heart failure, diagnosed with either NYHA functional class II to III at least 3 months prior to screening and on stable medication for at least 12 weeks.
  • Patients must have met either of the criteria at screening:
  • Documented left ventricular ejection fraction (LVEF) greater than 20% but lower than 40% OR
  • Patients with a documented LVEF greater than 40% and with a history of NT-pro-BNP> 400pg/mL (or BNP > 100pg/mL) within 12 months of screening.
Exclusion Criteria
  • Treatment with Angiotensin Receptor Blockers (ARBs), aldosterone receptor antagonists and diuretics (other than furosemide) within 3 weeks of first dose and during the study. Beta blockers were permitted provided the dose was stable for at least 3 weeks before the first dose and remains so throughout the study.
  • Hypertrophic cardiomyopathy (HCMP).
  • If a subject is currently treated with furosemide, the dose must be stable for at least 3 weeks before the first dose and the dose must not exceed 60 mg daily
  • Stable heart failure requiring treatment with both an ACE inhibitor and an ARB or Current acute decompensated heart failure.
  • Mean sitting systolic blood pressure ≥160 mmHg and/or mean sitting diastolic blood pressure ≥ 100mmHg and/or secondary forms of hypertension.
  • Persistent sitting systolic blood pressure <90 mmHg.
  • History of angioedema.

Other protocol-defined inclusion/exclusion criteria may apply

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
Furosemide 60 mgPlacebo for AliskirenTreatment period 1 (Day 1 to Day 7): All eligible patients received 60 mg furosemide, 150 mg placebo of aliskiren, and 300 mg placebo aliskiren once daily.
Furosemide 60 mgFurosemide 60 mgTreatment period 1 (Day 1 to Day 7): All eligible patients received 60 mg furosemide, 150 mg placebo of aliskiren, and 300 mg placebo aliskiren once daily.
Furosemide 60 mg + Aliskiren 150 mgAliskiren 150 mgTreatment Period 2 (Day 8 to day 17): Patients received 60 mg furosemide, 150 mg aliskiren and 300 mg placebo once daily.
Furosemide 60 mg + Aliskiren 150 mgPlacebo for AliskirenTreatment Period 2 (Day 8 to day 17): Patients received 60 mg furosemide, 150 mg aliskiren and 300 mg placebo once daily.
Furosemide 60 mg + Aliskiren 300 mgPlacebo for AliskirenTreatment Period 3 (Day 18 to day 27): Patients received 60 mg furosemide, 300 mg aliskiren and 150 mg placebo of aliskiren once daily.
Furosemide 60 mg + Aliskiren 300 mgAliskiren 300 mgTreatment Period 3 (Day 18 to day 27): Patients received 60 mg furosemide, 300 mg aliskiren and 150 mg placebo of aliskiren once daily.
Furosemide 60 mg + Aliskiren 150 mgFurosemide 60 mgTreatment Period 2 (Day 8 to day 17): Patients received 60 mg furosemide, 150 mg aliskiren and 300 mg placebo once daily.
Furosemide 60 mg + Aliskiren 300 mgFurosemide 60 mgTreatment Period 3 (Day 18 to day 27): Patients received 60 mg furosemide, 300 mg aliskiren and 150 mg placebo of aliskiren once daily.
Primary Outcome Measures
NameTimeMethod
Diuretic Efficacy Index 1 for Sodium Excretion0 to 24 hours

Efficacy of furosemide for sodium excretion (efficacy index 1) was defined by dividing urinary sodium excretion by the urinary excretion of furosemide. Diuretic index 1 for sodium was calculated for the for the total 0 to 24 hour urine collection.

Diuretic Efficacy Index 2 for Water Excretion0 to 24 hours

Efficacy of furosemide for water excretion (efficacy index 2) was defined by dividing urine volume by the urinary excretion of furosemide.Diuretic index 2 for water was calculated for the 0 to 4 hour fraction and for the total 0 to 24 hour urine collection.

Secondary Outcome Measures
NameTimeMethod
Plasma Pharmacokinetics (PK) of Furosemide: Area Under the Plasma Concentration-time Curve (AUC)pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 and 24 hours post dose

Pharmacokinetic (PK) parameters were determined from the plasma concentration time profile of furosemide using a non-compartmental method:

AUCtau: Area under the plasma concentration-time curve from time zero to the end of the dosing interval

AUC (0-24): Area under the plasma concentration-time curve from time zero to 24 hours

AUClast: Area under the plasma concentration-time curve from time zero to the time of the last quantifiable concentration. AUClast was calculated as the sum of linear trapezoids using non-compartmental analysis.

AUCinf: Area under the plasma concentration-time curve from time zero to infinity. AUCinf was calculated by adding AUClast and the value obtained from dividing the last measurable plasma concentration by λz, where λz was determined from automated linear regression of the last three time points with non-zero concentrations in the terminal phase of the log-transformed concentration-time profile

Urine Pharmacokinetics (PK) of Furosemide: Renal Clearance (CLR)0 to 4, 4 to 8, 8 to 12 and 12 to 24 hours post dose

The renal clearance of drug \[volume x time-1\]

Plasma Pharmacokinetics (PK) of Furosemide: Observed Maximum Plasma Concentration Following Drug Administration at Steady State (Cmax, ss)pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 and 24 hours post dose

Cmax,ss was directly determined from the raw plasma concentration-time data.

Plasma Pharmacokinetics (PK) of Furosemide: Time to Reach the Maximum Concentration After Drug Administration (Tmax)pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 and 24 hours post dose

Tmax was directly determined from the raw plasma concentration-time data.

Plasma Pharmacokinetics (PK) of Furosemide: Average Steady State Plasma Concentration During Multiple Dosing (Cav,ss)pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 and 24 hours post dose

The average steady-state drug concentration in the plasma, blood, serum, or other body fluids during multiple dosing \[amount x volume-1\]. This was estimated as AUCτ/τ

Plasma Pharmacokinetics (PK) of Furosemide: Lowest Plasma Concentration Observed During a Dosing Interval at Steady State (Cmin, ss)pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 24 hours post dose

The minimum observed steady-state drug concentration in the plasma, blood, serum, or other body fluids at the end of the dosing interval during multiple dosing \[amount x volume-1\]

Urine Pharmacokinetics (PK) of Furosemide: Amount of Drug Excreted Into the Urine From Time Zero to 24 Hours After Administration (Ae0-24)0 to 4, 4 to 8, 8 to 12 and 12 to 24 hours post dose

The area under the plasma (or serum or blood) concentration-time curve from time zero to 24 h \[mass × time × volume-1\]

Creatinine Clearance0 to 4, 4 to 8, 8 to 12 and 12 to 24 hours post dose

Creatinine clearance= (Urine creatinine/Serum creatinine) x (Urine volume/(24\*60)).

Urine Sodium and Potassium Excretion Per Treatment at 4 Hours Postdose4 hours postdose

Urine was collected 4 hours postdose in all treatment groups for sodium and potassium analysis. Each patient was required to void their bladder before drug administration and at the end 4 hours.

Urine Sodium and Potassium Excretion Per Treatment at 8 Hours Postdose8 hours postdose

Urine was collected 8 hours postdose in all treatment groups for sodium and potassium analysis. Each patient was required to void their bladder before drug administration and at the end 8 hours.

Urine Sodium and Potassium Excretion Per Treatment at 12 Hours Postdose12 hours postdose

Urine was collected 12 hours postdose in all treatment groups for sodium and potassium analysis. Each patient was required to void their bladder before drug administration and at the end 12 hours.

Urine Sodium and Potassium Excretion Per Treatment at 24 Hours Postdose24 hours postdose

Urine was collected 24 hours postdose in all treatment groups for sodium and potassium analysis. Each patient was required to void their bladder before drug administration and at the end 24 hours.

Mean Sitting Systolic Blood Pressure (msSBP)and Mean Sitting Diastolic Blood Pressure (msDBP)0.5 hour pre-dose, 0.5, 1, 2, 4, 8, 12 and 24 hours post dose.

Sitting blood pressure was measured three times at 1 to 2-minute intervals. The mean of the three sitting blood pressure measurements was used as the average of the sitting office blood pressure. The msSBP and msDBP data were analyzed using a mixed effect model with fixed effects from treatment and treatment\*time; random effect from patients and predose as covariate.

Trial Locations

Locations (1)

Novartis Investigative Site

🇱🇹

Vilnius, Lithuania

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