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Within Subject Variability Study of ER Torsemide 20 mg Tablet in Healthy Subjects

Phase 1
Completed
Conditions
Congestive Heart Failure
Chronic Kidney Diseases
Interventions
Drug: ER Torsemide 20mg Tablet
Registration Number
NCT03214874
Lead Sponsor
Sarfez Pharmaceuticals, Inc.
Brief Summary

The study will evaluate the within-subject variability of 20mg ER torsemide as compared to 20mg IR torsemide (Demadex) in fully replicate double-crossover trial in healthy volunteers, who are consuming a high-salt diet (300 mmol/day). The study will also evaluate the effects of ER torsemide and IR torsemide on 24h sodium excretion and total urinary excretion.

Detailed Description

Immediate Release (IR) Torsemide is a highly effective natriuretic drug but its short duration of action is a major drawback, which allows significant post-dose sodium retention, and as consequence, limits salt loss in patients with heart failure, unless dietary salt intake is severely restricted. Extended Release (ER) torsemide is being developed to address the drawback by prolonging the duration of action to increase sodium excretion even in patients who consume high salt diet (300 mmol/day).

In addition, IR torsemide induces large and abrupt urination that, in some patients, causes incontinence, and as a result, compliance becomes challenging. ER torsemide is formulated to cause robust but gradual urination over an extended period to reduce accidental wetting and improve compliance.

In this study, ER torsemide is tested for within-subject variability in fully replicate design double-crossover trial in healthy volunteers who are on a 300 mmol/day sodium diet (high salt diet). The primary endpoint of the study is full pharmacokinetics measurements after a single dose of either ER torsemide or IR torsemide (Demadex). The secondary endpoints are 24h sodium excretion and total urinary excretion.

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
24
Inclusion Criteria
  • Healthy male or female, non-smoker, weight 50 kg for male and 45 kg for female, clinically acceptable laboratory profiles with ECG and chest X-ray performed within 6 months
Exclusion Criteria
  • participation in bioavailability/bioequivalence studies,
  • history of drug abuse or alcohol dependence,
  • history of allergies including drug allergies,
  • known hypersensitivity to Torsemide or related drugs,
  • presence of clinically significant disorder,
  • systolic blood pressure <90 mm Hg or > 140 mm Hg diastolic blood pressure,
  • history of incontinence,
  • positive urine drug screening etc.

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Demadex 20mg TabletDemadex 20mg TabletDemadex (IR Torsemide) 20mg tablet once daily is the reference listed drug (RLD) and is marketed for decades to treat edema in Chronic Congestive Heart Failure (CHF) and Chronic Kidney Disease (CKD) patients
ER Torsemide 20mg TabletER Torsemide 20mg TabletER Torsemide 20mg tablet once daily is is the new formulation that will release the active ingredient over an extended period
Primary Outcome Measures
NameTimeMethod
Peak plasma concentration24 hour

Peak tosremide plasma concentration (Cmax) (ng/ml)

Total plasma concentration24 hour

Area under the plasma concentration versus time curve (AUC) (hr/ng/ml)

Urinary excretion24 hour

Torsemide excretion in urine (microgram/min) over 24h post dose

Secondary Outcome Measures
NameTimeMethod
Urinary sodium excretion24 hour

24h sodium (mmol/min)

Urine output24 hour

24h total urinary output (l/day)

Trial Locations

Locations (1)

I.E.C. Consultants

🇮🇳

Bangalore, India

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