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Evaluation of the Pharmacokinetics of Tropifexor in Subjects With Mild, Moderate, or Severe Hepatic Impairment Compared to Healthy Control Subjects

Phase 1
Completed
Conditions
Non-alcoholic Fatty Liver Disease
Interventions
Drug: LJN452
Registration Number
NCT03681457
Lead Sponsor
Novartis Pharmaceuticals
Brief Summary

The primary purpose of this study is to evaluate the effect of hepatic impairment on the systemic exposure of tropifexor and to evaluate the safety of tropifexor in subjects with hepatic impairment. The results of this study will support treatment and dosing decisions for patients with varying degrees of hepatic impairment.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
42
Inclusion Criteria
  • In good health as determined by past medical history, physical examination, ECG, laboratory tests, and urinalysis at Screening.
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Exclusion Criteria
  • Liver disease or liver injury
  • Chronic infection with Hepatitis B or Hepatitis C
  • History or presence of impaired renal function

Hepatically Impaired Subjects:

Inclusion Criteria:

  • Hepatic impairment as defined by the Child-Pugh classification for severity of liver disease

Exclusion Criteria:

  • Severe complications of liver disease within the preceding 3 months
  • Emergency room visit or hospitalization due to liver disease within the preceding 3 months for mildly and moderately hepatically impaired subjects, and within the preceding 1 month for severely hepatically impaired subjects
  • Subject has received liver transplant at any time in the past and is on immunosuppressant therapy
  • Acute Hepatitis B or Hepatitis C infection

Other protocol-defined inclusion/exclusion criteria may apply.

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Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Group 1 - Normal Hepatic FunctionLJN452Normal hepatic function - Control - control group
Group 2 - Mild Hepatic ImpairmentLJN452Mild hepatic impairment - Child-Pugh A (Score 5-6)
Group 3 - Moderate Hepatic ImpairmentLJN452Moderate hepatic impairment - Child-Pugh B (Score 7-9)
Group 4 - Severe Hepatic ImpairmentLJN452Severe hepatic impairment - Child-Pugh C (score 10-15)
Primary Outcome Measures
NameTimeMethod
CmaxUp to 8 days

The maximum (peak) observed drug concentration after single dose administration (mass x volume-1)

TmaxUp to 8 days

Time to reach the maximum (peak) plasma drug concentration after single dose administration (time)

AUClastUp to 8 days

The area under the concentration-time curve from time zero to the time of the last quantifiable concentration sampling time (mass x time x volume-1)

AUCinfUp to 8 days

The area under the concentration-time curve from time zero to infinity (mass x time x volume-1)

T1/2Up to 8 days

The elimination half-life associated with the terminal slope of a semi-logarithmic concentration-time curve

CL/FUp to 8 days

The apparent total body clearance of the drug from plasma (volume x time-1)

Vz/FUp to 8 days

The apparent volume of distribution during the terminal phase

Secondary Outcome Measures
NameTimeMethod
fuDay 1

Fraction of analyte unbound calculated in-vitro

Cmax,uDay 1

The maximum (peak) observed plasma drug concentration after single dose administration (Cmax) of unbound drug (mass x time x volume-1), calculated as Cmax\*fu

AUClast,uDay 1

The area under the concentration-time curve from time zero to the last quantifiable concentration sampling time of unbound drug (mass x time x volume-1), calculated as AUClast\*fu

AUCinf,uDay 1

The area under the concentration-time curve from time zero to infinity of unbound drug (mass x time x volume-1), calculated as AUCinf\*fu

CL/F,uDay 1

The apparent total body clearance of drug from the plasma of unbound drug (volume x time-1), calculated as CL/F/fu

Trial Locations

Locations (1)

Novartis Investigative Site

🇺🇸

Knoxville, Tennessee, United States

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