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Phase 1 N=32 Basic Science

Pharmacokinetics of LCZ696 in Subjects With Mild and Moderate Renal Impairment Compared to Healthy Subjects With Normal Renal Function

Mild and Moderate Renal Impairment

Enrolled (actual)
32
Serious AEs
0.0%
Results posted
Aug 2015
Primary outcome: Primary: Time to Reach Maximum Peak Plasma Concentration (Tmax) After Single Dose (Day 1), and After Multiple Dose Administration (Day 5) — 1; 0.5; 0.5; 0.5 hr

Study Design & Population

Study type
Interventional
Phase
Phase 1
Interventions
LCZ696 (Drug)
Age
Adult, Older Adult · 18+ yrs
Sex
All
Sponsor
Novartis Pharmaceuticals
Primary completion
Aug 2014

Outcome Measures

OutcomeResultp-value
PRIMARY
Time to Reach Maximum Peak Plasma Concentration (Tmax) After Single Dose (Day 1), and After Multiple Dose Administration (Day 5)
1; 0.5; 0.5; 0.5; 1; 0.5
PRIMARY
Maximum Peak Plasma Concentration (Cmax) Observed After Single Dose (Day 1), and After Multiple Dose Administration (Day 5)
4220; 3995; 3539; 3743; 3904; 3125
PRIMARY
Area Under the Concentration-time Curve (AUC0-24) From Time Zero to 24- Hour Post-dose (Day 1), and After Multiple Dose Administration (Day 5)
5679; 5396; 5359; 5963; 5656; 5221
PRIMARY
Elimination Half-life (t1/2) After Multiple Dose (Day 5) Administration
1.6; 4.7; 2.9; 1.8; 21.1; 12.6
PRIMARY
Systemic Clearance From Plasma Following Extravascular Administration (CL/F) After Multiple Dose Administration (Day 5)
38261; 39137; 42704; 37902; NA; NA
PRIMARY
Accumulation Ratio (Racc) After Multiple Dose Administration (Day 5)
1.0; 1.0; 1.0; 1.0; 1.64; 1.19
PRIMARY
Renal Clearance From Plasma (CLr) After Multiple Dose Administration (Day 5)
81.2; 129.1; 48.9; 143.9; 253.1; 499.0
PRIMARY
Amount of Drug Excreted Into the Urine From Time Zero to 24-hours Post-dose (Ae0-24) After Single Dose (Day 1), and After Multiple Dose Administration (Day 5)
360.2; 1560; 419.4; 2083; 426.2; 734.5
SECONDARY
Change in Mean 24-hours Sodium Clearance From Baseline to Day 7
107.13; 150.25; 110.65; 158.38; 143.24; 185.75

Summary

The purpose of this study is to determine the multiple dose pharmacokinetics of LCZ696 and its metabolites in subjects with mild to moderate renal impairment and to evaluate the safety of LCZ696 in this population.

Eligibility Criteria

Inclusion Criteria

  • Male, and female subjects of non-child bearing potential,
  • Subjects were to weigh at least 50 kg to participate in the study,
  • and body mass index 80 mL/min
  • Vital signs:
  • oral body temperature between 35.0-37.2 °C
  • systolic blood pressure, 95-140 mm Hg
  • diastolic blood pressure, 60-100 mm Hg
  • pulse rate, 45-90 bpm

Exclusion Criteria

  • Current use of ACE inhibitors, valsartan, and drugs that were known as CYP2C9 substrates, potassium-sparing diuretics;
  • Smokers;
  • History of renal transplant at any time in the past and on immunosuppressant therapy;
  • Dialysis patients;
  • Medical history of clinically significant ECG abnormalities or a family history of a prolonged QT-interval syndrome;
  • Any surgical or medical condition which may significantly alter the absorption, distribution, metabolism or excretion of any drug substance; Other protocol defined inclusion/exclusion criteria may apply
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT01569815). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.

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