Skip to main content
OpenTrials
Completed

NCT Number: NCT01529294

Single-dose Iloperidone Pharmacokinetics in Patients With Mild or Moderate Liver Disease, Compared to Healthy Volunteers

This study aims to determine the pharmacokinetic profile and the tolerability of iloperidone in subjects with mild or moderate hepatic impairment comparatively to healthy matched subjects

Completed

Looking for future studies?

Notify Me

Key information

Conditions

Hepatic Impairment

Age range

18 year–65 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

Novartis Investigative Site, Anaheim, California, United States

Loading trial locations.

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • Inclusion criteria (all subjects):
  • Caucasian subjects
  • Inclusion criteria (hepatic impaired subjects):
  • subjects with physical signs consistent with a clinical diagnosis of stable liver disease, which has been confirmed by imaging techniques, ultrasound, Magnetic Resonance Imaging or Computed Tomogram within 3 months of screening, and a creatinine clearance > 50 mL/min (based on Cockroft and Gault formula).
  • Inclusion criteria (healthy volunteers):
  • good general health
  • matched by age, gender, smoking status, Body Mass Index, and CYP2D6 phenotype to hepatic impaired subjects.

Exclusion criteria

  • Exclusion criteria (all subjects):
  • Subjects who report smoking a pipe, cigars or more than 20 cigarettes per day .
  • History of drug abuse as defined in Diagnostic and Statistical Manual of Mental Disorders, Diagnostic Criteria for Drug and Alcohol Abuse, within the 12 months prior to screening
  • History of first-dose response/syncope to alpha1-blocking agents
  • Exclusion criteria (Hepatic impaired subjects):
  • Patients with symptoms or 6 months past history of encephalopathy.
  • Patients with clinical evidence of moderate-severe ascites.
  • Patients having a previous surgical porto-systemic shunt.
  • Exclusion criteria (Healthy volunteers):
  • History of alcohol abuse prior to dosing, or evidence of such abuse during screening.
  • Pulse Rate > 200 msec

Other protocol-defined inclusion/exclusion criteria may apply

Treatment and study plan

iloperidone

Drug

Primary outcomes

  1. Measure: Area Under Curve (AUClast, AUCinf) and maximum concentration (Cmax)

    Time frame: predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose

    Pharmacokinetics of iloperidone in subjects with mild or moderate hepatic impairment, compared to healthy volunteers.

  2. Maximum plasma concentration following drug administration (Cmax) of iloperidone

    Time frame: pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120 hours post-dose, and from pre-dose to 48 hours post-dose

    Blood and urine samples will be collected and plasma and urine concentration will be measured.

  3. Protein binding of iloperidone

    Time frame: pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120 hours post-dose, and from pre-dose to 48 hours post-dose

    Blood samples will be collected and protein binding will be measured .

  4. Area under the plasma concentration-time Curve from time zero to infinity (AUCinf) of iloperidone

    Time frame: pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120 hours post-dose, and from pre-dose to 48 hours post-dose

    Blood and urine samples will be collected and plasma and urine concentration will be measured.

Secondary outcomes

  1. Area Under the plasma Curve (AUC) of iloperidone metabolite P88

    Time frame: pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120 hours post-dose and from pre-dose to 48 hours post-dose

    Blood and urine samples will be collected and plasma and urine concentrations of metabolite 88 will be measured

  2. Area under the plasma concentration-time Curve from time zero to infinity (AUCinf) of iloperidone metabolite P88 records, listed by subject. Summary statistics provided by impairment group and visit/time.

    Time frame: pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120 hours post-dose and from pre-dose to 48 hours post-dose

    Blood and urine samples will be collected and plasma and urine concentrations of metabolite 88 will be measured

  3. Maximum plasma concentration following drug administration (Cmax) of iloperidone metabolites P88

    Time frame: pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120 hours post-dose and from pre-dose to 48 hours post-dose

    Blood and urine samples will be collected and plasma and urine concentrations of metabolite 88 will be measured

  4. Protein binding of iloperidone metabolites P88 (CLr)

    Time frame: pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120 hours post-dose and from pre-dose to 48 hours post-dose

    Blood samples will be collected and protein binding of metabolite 88 will be measured

  5. Area Under the plasma Curve (AUC) of iloperidone metabolite P95

    Time frame: pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120 hours post-dose and from pre-dose to 48 hours post-dose

    Blood and urine samples will be collected and plasma and urine concentrations of metabolite 95 will be measured

  6. Area under the plasma concentration-time Curve from time zero to infinity (AUCinf) of iloperidone metabolite P95

    Time frame: pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120 hours post-dose and from pre-dose to 48 hours post-dose

    Blood and urine samples will be collected and plasma and urine concentrations of metabolite 95 will be measured

  7. Maximum plasma concentration following drug administration (Cmax) of iloperidone metabolites P95

    Time frame: pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120 hours post-dose and from pre-dose to 48 hours post-dose

    Blood and urine samples will be collected and plasma and urine concentrations of metabolite 95 will be measured

  8. Protein binding of iloperidone metabolites P95

    Time frame: pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120 hours post-dose and from pre-dose to 48 hours post-dose

    Blood samples will be collected and protein binding of metabolite 95 will be measured

  9. Number of participants with adverse events

    Time frame: Day 6

    Adverse events will be determined by evaluating clinical, laboratory evaluations, impact on vital signs and impacts on Electrocardiograms (ECGs)

Sponsors and collaborators

Lead sponsor

Novartis Pharmaceuticals

Industry

Registry information

Official study title

Open-label, Single-dose, Parallel-group Study to Compare the PKs of Iloperidone in Subjects With Mild or Moderate Hepatic Impairment With That in Matched Healthy Control Subjects

Important dates

Study start
2010
Primary completion
2012
Study completion
2012
First posted
Feb 8, 2012
Registry last updated
Mar 14, 2013

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

Related clinical trials

Published trials that share one or more normalized conditions with this study.