A Study to Determine the Pharmacokinetics, Pharmacodynamics, and Tolerabiltiy of Betrixaban in Patients With Mild, Moderate, and Severe Renal Impairment

Phase 1

Completed

• Conditions: Renal Impairment
• Interventions: Drug: Betrixaban

• Registration Number: NCT00999336
• Lead Sponsor: Portola Pharmaceuticals

Brief Summary

The purpose of the study is to compare the pharmacokinetics, pharmacodynamics, and tolerability of betrixaban in patients with mild, moderate, and severe renal impairment to healthy volunteers.

Detailed Description

Not available

Study Timeline

• Study Start: 2009-07-31
• Study First Submitted: 2009-10-20
• Study First Submitted QC: 2009-10-20
• Study First Posted: 2009-10-21
• Primary Completion: 2010-02-28
• Study Completion: 2010-02-28
• Results First Submitted: 2022-03-29
• Status Verified: 2022-10
• Results First Submitted QC: 2022-10-13
• Last Update Submitted: 2022-10-13
• Results First Posted: 2023-08-22
• Last Update Posted: 2023-08-22

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 32

Inclusion Criteria

• Able to understand and sign the written informed consent.
• Subjects should have either normal renal function or have stable renal disease

Exclusion Criteria

• Subjects require dialysis
• Evidence of active bleeding or bleeding disorder
• Unstable or clinically significant other disorders such as respiratory, hepatic, metabolic, psychiatric or gastrointestinal disorder

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: PARALLEL

Arm && Interventions

Group	Intervention	Description
Group B	Betrixaban	Patients with moderate renal impairment
Group A	Betrixaban	Patients with mild renal impairment
Group H	Betrixaban	Healthy subjects matched to the renal impairment groups
Group C	Betrixaban	Patients with severe renal impairment

Primary Outcome Measures

Name	Time	Method
Area Under The Plasma Concentration-Time Curve From Time Zero To 24 Hours (AUC0-24) Postdose Of Oral Doses Of Betrixaban On Day 8	Predose up to 168 hours postdose	Blood and urine samples for pharmacokinetic analysis were collected and determined from the plasma and urine concentrations of betrixaban using non-compartmental procedures in WinNonlin Enterprise Version 5.2.; Results were reported in nanogram multiplied by hour per milliliter (ng\*h/mL).
Maximum Observed Plasma Concentration (Cmax) Following Administration Of Oral Doses Of Betrixaban On Day 8	Predose, up to 168 hours postdose	Blood and urine samples for pharmacokinetic analysis were collected and determined from the plasma and urine concentrations of betrixaban using non-compartmental procedures in WinNonlin Enterprise Version 5.2.; Results were reported in nanogram per milliliter (ng/mL).
Plasma Terminal Elimination Half-Life (T½) Following Administration Of Oral Doses Of Betrixaban On Day 8	Predose, up to 168 hours postdose	Blood and urine samples for pharmacokinetic analysis were collected and determined from the plasma and urine concentrations of betrixaban using non-compartmental procedures in WinNonlin Enterprise Version 5.2.; Harmonic mean and Jackknife standard deviation was used to report this outcome and results were reported in hour.
Total Plasma Clearance (CL/F) Following Administration Of Oral Doses Of Betrixaban On Day 8	Predose, up to 168 hours postdose	Blood and urine samples for pharmacokinetic analysis were collected and determined from the plasma and urine concentrations of betrixaban using non-compartmental procedures in WinNonlin Enterprise Version 5.2.; Results were reported in milliliter per minute (mL/min).
Volume Of Distribution During The Terminal Phase (Vz/F) Following Administration Of Oral Doses Of Betrixaban On Day 8	Predose, up to 168 hours postdose	Blood and urine samples for pharmacokinetic analysis were collected and determined from the plasma and urine concentrations of betrixaban using non-compartmental procedures in WinNonlin Enterprise Version 5.2.; Results were reported in liter.
Thrombin Generation Following Administration Of Oral Doses Of Betrixaban On Day 8	Day 1: predose; Day 8: 2, 3, 4, 8, 24, and 48 hours postdose	Blood samples were collected at the protocol-specified time points. Plasma samples were assayed for measurement of thrombin generation for all participants.
Anti-Factor Xa (fXa) Activity Following Administration Of Oral Doses Of Betrixaban On Day 8	Day 8: 2, 3, 4, 8, 24, and 48 hours postdose	Blood samples were collected at the protocol-specified time points. Plasma samples were assayed for measurement of anti-fXa activity at baseline and steady state for all participants.; Results were reported in international units per milliliter (IU/mL).
Percentage Of Dose Excreted In Urine From 0-24 (fe0-24) Postdose Of Oral Doses Of Betrixaban On Day 8	Predose, up to 24 hours postdose	Blood and urine samples for pharmacokinetic analysis were collected and determined from the plasma and urine concentrations of betrixaban using non-compartmental procedures in WinNonlin Enterprise Version 5.2.; Results were reported in percentage.
Percentage Of Betrixaban Bound To Plasma Proteins On Day 8	4 hours Postdose at Day 8	Blood samples were collected for measurement of plasma protein binding for betrixaban for all participants. Results of protein binding assays were summarized by sample time and eGFR group. Results were reported in percent (%).

Trial Locations

Locations (1)

APEX GmbH; 🇩🇪 Munich, Germany