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Pharmacokinetics and Safety of Fevipiprant in Patients With Renal Impairment Compared to Matched Healthy Subjects

Phase 1
Completed
Conditions
Renal Insufficiency
Interventions
Drug: QAW039
Drug: QAW39A
Drug: QAW39A2107
Registration Number
NCT03087942
Lead Sponsor
Novartis Pharmaceuticals
Brief Summary

The aim of the study is to assess whether renal impairment could affect fevipiprant pharmacokinetics (PK) to the extent that dosage adjustment is appropriate for this patient population.

The study also aims to determine the effect of dialysis on the fevipiprant pharmacokinetic profile as the procedure might remove a significant fraction of the drug.

Detailed Description

The purpose of this study is to determine if the pharmacokinetic profile of fevipiprant is different in patients with renal impariment compared to healthy matched volunteers to an extent that would require an adjustment of the dosage. Data from this study will be used to guide enrollment criteria in future clinical trials and to support regulatory submission and labeling information

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
45
Inclusion Criteria
  • Healthy subjects must satisfy the criteria for normal renal function as evidenced by normal Glomerular Filtration Rate (GFR): eGFR ≥ 90 mL/min/1.73m2; each healthy subject must match in age (+/- 10years), gender, smoking status, and weight (+/- 15%), a patient from the renail impaired patient groups:
  • A body mass index (BMI) within the range of 18 - 36 kg/m2
  • ESRD patients on hemodialysis: an glomerulo filtration rat GFR of < 15 mL/min/1.73 m2
  • patients with severe renal impairment: GFR of< 30 mL/min/1.73m2 (without need of hemodialysis);
  • patients with moderate renal impairment: 30 mL/min/1.73m2 ≤ eGFR < 60 mL/min/1.73m2;
  • patients with mild impairment: 60 mL/min/1.73m2 ≤ eGFR < 90 mL/min/1.73m2
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Exclusion Criteria
  • Pregnant or nursing (lactating) women
  • History or evidence of any inherited bilirubin disease or disorder
  • subjects participating in another study
  • malignancies in the past
  • Hemoglobin levels below 10 g/dL at screening
  • HIV positiv
  • Heavy smokers (≥20 cigarettes per day)
  • Liver disease, as indicated by ALT, γ-GT, AST and alkaline phosphatase which should not exceed twice the upper limit of normal and should be stable (e.g. increased liver values known from previous patient records). Serum bilirubin > 27 μmol/L (1.6 mg/dL)
  • Clinically significant ECG changes and/or arrhythmias
  • Chronic infection with Hepatitis B (HBV) or Hepatitis C (HCV)
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Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Group 1QAW039ESRD patients
Group 2QAW39Ahealthy volunteers
Group 3QAW39A2107severe and moderate renal impaired patients
Group 4QAW39A2107mild renal impaired patients
Primary Outcome Measures
NameTimeMethod
Pharmacokinetics: Plasma concentration of fevipiprant by AUClast68 hours post dose

AUClast is the area under the plasma concentration-time curve from time zero to the time of the last quantifiable concentration

Pharmacokinetics: Plasma concentration of fevipiprant by AUCinf68 hours post dose

AUCinf is the area under the plasma concentration-time curve from time zero to infinity

Pharmacokinetics: Plasma concentration of fevipiprant by Cmax68 hours post dose

Cmax is the observed maximum plasma concentration following drug administration

Pharmacokinetics: Plasma contentration of fevipiprant by AUC0-68h68 hours post dose

AUC0-68h is the area under the plasma concentration from time zero to time 68 hours of the last measured concentration above the limit of quantification after dosing

Secondary Outcome Measures
NameTimeMethod
urinary excretion of fevipiprant and metabolite in patients with renal impairment compared to healthy controls24 hours post dose

Renal clearance (CLr) and fraction of dose excreted in urine for fevipiprant and metabolite

Relationship between plasma pharmacokinetics of fevipiprant by AUClast and between eGFR as well as creatinine clearance68 hours post dose

AUClast (the area under the plasma concentration time curve from time zero to the time of the last quantifiable concentration ) related to eGFR estimated by the Modification of Diet in Renal Disease (MDRD) formula, and Cockcroft-Gault (C-G) estimated creatinine clearance

Pharmacokinetics of the metabolite CCN362 by AUCinf68 hours post dose

AUCinf is the area under the plasma concentration time curve from time zero to infinity

Pharmacokinetics of the metabolite CCN362 by Cmax68 hours post dose

Cmax is the observed maximum plasma concentration following drug administration

Pharmacokinetics: plasma concentration of fevipiprant in patients with End Stage Renal Disease (ESRD)68 hours post dose

Partial AUCs (AUCt1-t2) covering the time interval of dialysis, Cmax and total AUCs (AUC0-68h and/or AUCinf) will be compared

Pharmacokinetics of the metabolite CCN362 by AUClast68 hours post dose

AUClast is the area under the plasma concentration time curve from time zero to the time of the last quantifiable concentration

Relationship between plasma pharmacokinetics of fevipiprant by AUCinf and between eGFR as well as creatinine clearance68 hours post dose

AUCinf (the area under the plasma concentration time curve from time zero to infinity) related to eGFR estimated by the Modification of Diet in Renal Disease (MDRD) formula, and Cockcroft-Gault (C-G) estimated creatinine clearance

Relationship between plasma pharmacokinetics of fevipiprant by Cmax and between eGFR as well as creatinine clearance68 hours post dose

Cmax (observed maximum plasma concentration following drug administration) related to eGFR estimated by the Modification of Diet in Renal Disease (MDRD) formula, and Cockcroft-Gault (C-G) estimated creatinine clearance

Trial Locations

Locations (1)

Novartis Investigative Site

🇩🇪

Grunstadt, Germany

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