Healthy VolunteerPhase 1NCT01197911
A Study of The Effect of Hepatic Impairment on The Pharmacokinetics of Aleglitazar
A Phase 1 study testing aleglitazar in people with Healthy Volunteer, run by Hoffmann-La Roche at 2 sites in United States.
Trial summary
This open-label study will assess the effects of hepatic impairment on the pharmacokinetics of a single oral dose of aleglitazar in subjects with mild or moderate hepatic impairment (Child-Pugh class A or B) and in matched control subjects with normal hepatic function. Read more about this study
- Who is it for?
- Ages 18 to 70 yearsHealthy volunteers can take part
- Conditions the study is for
- Healthy Volunteer
- What is being tested?
- aleglitazar
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 38 participants
- Where
- 2 sitesUnited States
- Study dates
- Sep 2010to Aug 2011
- Phase
- Phase 1
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 70 years
- All sexes
- Healthy volunteers accepted
- Adult, Older adult
Who may be able to join
- Male and female adults, 18-70 years of age inclusive
- Normal hepatic function or mild to moderate impaired liver function (Child-Pugh class A or B)
- Body mass index (BMI) 18 to 40 kg/m2 inclusive
- Females must be either surgically sterile, postmenopausal, or willing to use two reliable methods of contraception for the duration of the study and started 3 months before study start
Who cannot join
- For subjects with hepatic impairment: evidence of progressive liver disease within the last 4 weeks, or biliary liver cirrhosis or other causes of hepatic impairment not related to parenchymal disorder and/or disease
- For healthy volunteers: positive test for hepatitis B or C, alcohol intake of more than 14 units per week, or history of clinically significant alcohol or drug abuse
- Acute infection or current malignancy requiring treatment
- History of clinically significant allergic disease or drug hypersensitivity
- Positive test for HIV-1 or HIV-2 at screening
- Participation in a clinical study with an investigational drug or new chemical entity within 2 months prior to screening
- Females who are pregnant or lactating
Trial locations and contacts
2 sites in 1 country.
United States2 sites
Study site
Knoxville, Tennessee, 37920
Study site
Orlando, Florida, 32809
About this study
Official title: The Effect of Hepatic Impairment on the Pharmacokinetics of Aleglitazar: A Multiple-centre, Open-label Study Following a Single Oral Dose of Aleglitazar to Subjects With Mild or Moderate Hepatic Impairment and Healthy Subjects With Normal Hepatic Function.
This open-label study will assess the effects of hepatic impairment on the pharmacokinetics of a single oral dose of aleglitazar in subjects with mild or moderate hepatic impairment (Child-Pugh class A or B) and in matched control subjects with normal hepatic function. Subjects will receive a single oral dose of aleglitazar, with assessment of the pharmacokinetics of aleglitazar on Days 1-5. Anticipated duration of study for each enrolled subject is approximately 6 weeks.
- Conditions
- Healthy Volunteer
- Being tested
- aleglitazar
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
aleglitazarDrug
single oral dose
| Study group | Role | What they receive |
|---|---|---|
| Mild impairment | Experimental | Not described Receives: Drug: aleglitazar |
| Moderate impairment | Experimental | Not described Receives: Drug: aleglitazar |
| Normal HF | Experimental | Not described Receives: Drug: aleglitazar |
What is being measured
The primary outcome is the main question the study is designed to answer.
Area Under the Plasma Concentration-time Curve From Time Zero to Infinity (AUCinf) of Aleglitazar
AUCinf was calculated by non-compartmental analysis using the linear trapezoidal rule, using relative actual time values.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose
Maximum Plasma Concentration (Cmax) of Aleglitazar
Cmax was obtained directly from the concentration-time data.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose
Secondary outcomes (24)
AUCinf of M1 (RO4408754) and M6 (RO4583746)
M1 and M6 are pharmacologically inactive metabolites of aleglitazar. AUCinf represents the area under the concentration-time curve of the analyte in plasma over the time interval from zero extrapolated to infinity. AUCinf was calculated by non-compartmental analysis using the linear trapezoidal rule, using relative actual time values.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose
Cmax of M1 and M6
M1 and M6 are pharmacologically inactive metabolites of aleglitazar. Cmax was obtained directly from the concentration-time data.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose
Area Under the Plasma Concentration-time Curve From Time 0 to 48 Hours Post-dose (AUC0-48) of Aleglitazar, M1, and M6
M1 and M6 are pharmacologically inactive metabolites of aleglitazar. AUC0-48 was calculated by non-compartmental analysis using the linear trapezoidal rule, using relative actual time values.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose
Area Under the Plasma Concentration-time Curve From 0 to the Last Quantifiable Time-point Post-dose (AUClast) of Aleglitazar, M1, and M6
AUClast was calculated by non-compartmental analysis using the linear trapezoidal rule, using relative actual time values.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose
Apparent Total Body Clearance (CL/F) of Aleglitazar
CL/F was calculated as dose/AUCinf, where AUCinf represents the area under the concentration-time curve of the analyte in plasma over the time interval from zero extrapolated to infinity.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose
Renal Clearance (CLR) of Aleglitazar, M1, and M6
CLR was calculated as Ae0-48/AUC0-48, where Ae0-48 as amount excreted in urine from time 0 to 48 hours post-dose and AUC0-48 represents area under the concentration-time curve of the analyte in plasma over the time interval from zero to the 48 hours post-dose.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72, and 96 hours post-dose for plasma; 0-4, 4-8, 8-12, 12-24, and 24-48 hours post-dose for urine
Apparent Non-renal Clearance (CLNR/F) of Aleglitazar
Plasma and urine samples were collected for this PK parameter. CLNR/F was estimated as CL/F, based on the approximated formula of CLNR/F = (CL-CLR)/F with CLR of aleglitazar being equal to zero. CL/F was calculated as dose/AUCinf, where AUCinf represents the area under the concentration-time curve of the analyte in plasma over the time interval from zero extrapolated to infinity. CLR was calculated as Ae0-48/AUC0-48, where Ae0-48 as amount excreted in urine from time zero to 48 hours post-dose and AUC0-48 represents area under the concentration-time curve of the analyte in plasma over the time interval from zero to the 48 hours post-dose.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose for plasma; 0-4, 4-8, 8-12, 12-24, and 24-48 hours post-dose for urine
Time of Maximum Plasma Concentration (Tmax) of Aleglitazar, M1, and M6
M1 and M6 are pharmacologically inactive metabolites of aleglitazar. Tmax was measured as time to reach the maximum concentration in the plasma after post-dose.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose
Apparent Terminal Half-life (t½) of Aleglitazar, M1, and M6
M1 and M6 are pharmacologically inactive metabolites of aleglitazar. T1/2 is the time required for a given drug concentration in the plasma to decrease by 50%.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose
Elimination Rate Constant (Kel) of Aleglitazar
The kel is fraction of a substance that is removed per unit time measured at any particular instant. It was calculated using at least 3 concentration-time points and ideally covered more than 2 half-lives.
Measured: 0-4, 4-8, 8-12, 12-24, and 24-48 hours post-dose
Apparent Volume of Distribution (Vz/F) of Aleglitazar
Vz/F is the apparent volume of distribution during terminal phase after non-intravenous administration. It was calculated as CL/F/kel, where CL/F was calculated as dose/AUCinf, where AUCinf represents the area under the concentration-time curve of the analyte in plasma over the time interval from zero extrapolated to infinity and kel as constant elimination rate of aleglitazar.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose for plasma; 0-4, 4-8, 8-12, 12-24, and 24-48 hours post-dose for urine
Amount Excreted in Urine From Time 0 to 48 Hours Post-dose (Ae0-48) of Aleglitazar, M1, and M6
The cumulative amount excreted in urine Ae0-48 over the entire collection interval of 48 hours was calculated by adding the Ae of the intervals 0-4, 4-8, 8-12, 12-24, and 24-48 hours, where Ae was calculated by multiplying the urine volume within the collection interval by the associated drug concentration.
Measured: 0-4, 4-8, 8-12, 12-24, and 24-48 hours post-dose
Fraction of Drug Excreted in Urine From Time 0 to 48 Hours Post-dose (fe0-48) of Aleglitazar
fe0-48 was calculated as Ae0-48/dose. The cumulative amount excreted in urine Ae0-48 over the entire collection interval of 48 hours was calculated by adding the Ae of the intervals 0-4, 4-8, 8-12, 12-24, and 24-48 hours. Ae was calculated by multiplying the urine volume within the collection interval by the associated drug concentration.
Measured: 0-4, 4-8, 8-12, 12-24, and 24-48 hours post-dose
Mean of Fraction of Unbound Aleglitazar (fu)
fu was calculated using the mean of the 2-hour (reflecting Cmax) and 24-hour (reflecting Ctrough) values for each participant or, if the result of only one time-point was available, fu was the result of the available time-point. Ctrough) is a measured concentration at the end of a dosing interval at steady state.
Measured: 2 and 24 hours post-dose
Area Under the Unbound Plasma Concentration-time Curve of Aleglitazar From Time 0 to Infinity (AUCu,Inf)
AUCinf represents the area under the concentration-time curve of the analyte in plasma over the time interval from zero extrapolated to infinity. It was calculated by non-compartmental analysis using the linear trapezoidal rule, using relative actual time values. It was assessed using an analysis of variance model on the log-transformed values of AUCinf of aleglitazar with hepatic impairment group as factor.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose
Maximum Unbound Plasma Concentration (Cmax,u) of Aleglitazar
Cmax was obtained directly from the concentration-time data.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose
Area Under the Unbound Plasma Concentration-time Curve of Aleglitazar From 0 to the Last Quantifiable Time-point Post-dose (AUCu,Last)
Plasma samples were collected for this PK parameter. AUClast represents the area under the concentration-time curve of the analyte in plasma over the time interval from zero 0 to the last quantifiable time-point post-dose. It was calculated by non-compartmental analysis using the linear trapezoidal rule, using relative actual time values. AUClast was extrapolated to AUCinf by adding the ratio of Clast/kel to the AUClast, where Clast was the last observed concentration and kel was elimination rate constant.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose
Area Under the Unbound Plasma Concentration-time Curve of Aleglitazar From Time 0 to 48 Hours Post-dose (AUCu,0-48)
AUClast represents the area under the concentration-time curve of the analyte in plasma over the time interval from zero to the 48 hours post-dose. It was calculated by non-compartmental analysis using the linear trapezoidal rule, using relative actual time values.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose
Apparent Unbound Volume of Distribution (Vz/Fu) of Aleglitazar
VzF/u is an apparent volume of Unbound distribution during terminal phase after non-intravenous administration. It was calculated as CL/F/kel, where CL/F was calculated as dose/AUCinf, where AUCinf represents the area under the concentration-time curve of the analyte in plasma over the time interval from zero extrapolated to infinity and kel as constant elimination rate of aleglitazar.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose for plasma; 0-4, 4-8, 8-12, 12-24, and 24-48 hours post-dose for urine
Apparent Unbound Total Body Clearance (CL/Fu) of Aleglitazar
CL/F is an apparent total clearance of the drug from plasma after oral administration. It was calculated as dose/AUCinf. AUCinf represents the area under the concentration-time curve of the analyte in plasma over the time interval from zero extrapolated to infinity.
Measured: Pre-dose, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 15, 24, 36, 48, 72 and 96 hours post-dose for plasma; 0-4, 4-8, 8-12, 12-24, and 24-48 hours post-dose for urine
Number of Participants With Any Adverse Events (AEs), Serious Adverse Events (SAEs), Death, and Study Discontinuation
An AE is defined as any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered to be related to the medicinal product. An SAE is any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or results in a congenital anomaly/birth defect.
Measured: Up to 6 weeks
Number of Participants With Low and High Electrocardiograms (ECGs) Parameter Values
The ECG evaluations were performed after participants were at rest and in supine position for at least 5 minutes before recording and remain resting and supine during the recordings. ECGs parameters included heart rate (HR), RR interval, PR interval, QRS duration, QT interval, QTcB, and QTcF intervals. The normal ranges of ECG parameter values were: HR as 40-100 beats per minute, RR as 600-1500 milliseconds (msec), PR as 120-200 msec, QRS as 80-120 msec, QT as 200-500 msec, QTcB as 350-450 msec, and QTcF as 350-450 msec. Data was reported as the number of participants who had low level values (values less than the normal range) and high level values (values more than the normal range).
Measured: Screening (Days -28 to -2), baseline (Day -1), Days 1 to 5, and follow-up visit (Day 10)
Number of Participants With Low and High Vital Signs Values
Vital signs were assessed after participants had rested in a supine position for no less than 5 minutes. Vital signs included systolic blood pressure, diastolic blood pressure, pulse rate, and oral body temperature. The normal ranges of vital signs were: systolic blood pressure as 90-140 millimeter of Hg (mm Hg), diastolic blood pressure as 50-90 mm Hg, pulse rate as 45-100 beats per minute, and oral body temperature as 36.3-37.5 degree Celsius. Data was reported as the number of participants who had low level values (values less than the normal range) and high level values (values more than the normal range).
Measured: Days -28 to -2, Day -1, Days 1 to 5, and Day 10 for blood pressure and pulse rate; and Days -28 to -2, Day -1, and Day 10 for oral body temperature
Number of Participants With Marked Abnormalities in Clinical Laboratory Parameters
Laboratory parameters included hematology, coagulation, biochemistry, and urinalysis. A marked abnormality was defined as a test result which was outside of the marked abnormality range. Data was reported as the number of participants who had low level values (values less than the normal range) and high level values (values more than the normal range).
Measured: Up to 6 weeks
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted9 Sep 2010 (estimated)
- Study startSep 2010
- Primary completionAug 2011
- Study completionAug 2011
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Posted resultsParticipant flow, outcome measures and adverse events reported by the sponsor.
- Other trials for Healthy VolunteerStudies of the same condition, open and under way.
- More trials run by Hoffmann-La RocheThe sponsor's other registered studies.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Allocation
- Non-randomised
- Intervention model
- Parallel groups
- Masking
- None (open label)
- Enrolment
- 38 participants (actual)
Sponsor and investigators
- Lead sponsor
- Hoffmann-La Roche
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
- Investigators
- Clinical Trials, Study director, Hoffmann-La Roche
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT01197911
- Sponsor's protocol ID
- BP25240
- Status last verified
- Nov 2015
- First submitted
- 8 Sep 2010
- Last updated
- 24 Dec 2015
- Results posted
- Yes, on ClinicalTrials.gov