This study is being conducted in order to assess the need for dose adjustment for elafibranor in patients with hepatic impairment. Pharmacokinetic parameters of elafibranor and its active metabolite (GFT1007) will be compared in hepatic impaired patients (mild, moderate and severe according to Child-Pugh categories) versus healthy participants after a single oral administration of elafibranor 120 mg.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
30
120mg oral single dose
Division of Clinical Pharmacology, University of Miami
Miami, Florida, United States
inVentiv Health Clinical Research
Miami, Florida, United States
Area under curve from dosing time to last measurement (AUC(0-t)) of elafibranor and active metabolite
In participants with mild, moderate and severe hepatic impairment compared to healthy volunteers
Time frame: pre-dose and at 0.17, 0.33, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 and 216 hours post-dose. Additionally, after elafibranor administration at 288 and 384 hours for hepatic impaired patients
Area under curve from dosing time to infinity (AUC(0-∞)) of elafibranor and active metabolite
In participants with mild, moderate and severe hepatic impairment compared to healthy volunteers
Time frame: pre-dose and at 0.17, 0.33, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 and 216 hours post-dose. Additionally, after elafibranor administration at 288 and 384 hours for hepatic impaired patients
Plasma pharmacokinetics: maximum plasma drug concentration (Cmax)
for elafibranor and metabolites
Time frame: pre-dose and at 0.17, 0.33, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 and 216 hours post-dose. Additionally, after elafibranor administration at 288 and 384 hours for hepatic impaired participants
Plasma pharmacokinetics: elimination half-life (t1/2)
for elafibranor and metabolites
Time frame: pre-dose and at 0.17, 0.33, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 and 216 hours post-dose. Additionally, after elafibranor administration at 288 and 384 hours for hepatic impaired participants
Plasma pharmacokinetics: apparent volume of distribution (Vd/F)
for elafibranor
Time frame: pre-dose and at 0.17, 0.33, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 and 216 hours post-dose. Additionally, after elafibranor administration at 288 and 384 hours for hepatic impaired participants
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
Plasma pharmacokinetics: renal clearance (CLr)
for elafibranor and metabolites
Time frame: pre-dose and at 0.17, 0.33, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 and 216 hours post-dose. Additionally, after elafibranor administration at 288 and 384 hours for hepatic impaired participants
Plasma pharmacokinetics: apparent non renal clearance (CLnr/F)
for elafibranor
Time frame: pre-dose and at 0.17, 0.33, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 and 216 hours post-dose. Additionally, after elafibranor administration at 288 and 384 hours for hepatic impaired participants
Plasma pharmacokinetics: apparent total clearance (CL/F)
for elafibranor
Time frame: pre-dose and at 0.17, 0.33, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 and 216 hours post-dose. Additionally, after elafibranor administration at 288 and 384 hours for hepatic impaired participants
Plasma pharmacokinetics: area under the plasma concentration-time curve extrapolated from time t to infinity as a percentage of total area under the plasma concentration-time curve (%AUCextra)
for elafibranor and metabolites
Time frame: pre-dose and at 0.17, 0.33, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 and 216 hours post-dose. Additionally, after elafibranor administration at 288 and 384 hours for hepatic impaired participants
Plasma pharmacokinetics: area under curve from dosing time to last measurement (AUC(0-t)) of glucuronide metabolites and corresponding aglycones
for the glucuronide metabolites of elafibranor and corresponding aglycones
Time frame: pre-dose and at 0.17, 0.33, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 and 216 hours post-dose. Additionally, after elafibranor administration at 288 and 384 hours for hepatic impaired participants
Plasma pharmacokinetics: area under curve from dosing time to infinity (AUC(0-∞)) of glucuronide metabolites and corresponding aglycones
for the glucuronide metabolites of elafibranor and corresponding aglycones
Time frame: pre-dose and at 0.17, 0.33, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 and 216 hours post-dose. Additionally, after elafibranor administration at 288 and 384 hours for hepatic impaired patients
Urine pharmacokinetics: amount excreted (Ae)
for elafibranor and metabolites, if applicable. 24 hours urine collection from dosing to 216 hours post-dose
Time frame: pre-dose and then 24, 48, 72, 96, 120, 144, 168, 192, 216 hours post-dose
Urine pharmacokinetics: cumulative amount excreted (Ae0-t)
for elafibranor and metabolites, if applicable. 24 hours urine collection from dosing to 216 hours post-dose
Time frame: pre-dose and then 24, 48, 72, 96, 120, 144, 168, 192, 216 hours post-dose
Urine pharmacokinetics: percentage of dose excreted (Fe)
for elafibranor and metabolites, if applicable. 24 hours urine collection from dosing to 216 hours post-dose
Time frame: pre-dose and then 24, 48, 72, 96, 120, 144, 168, 192, 216 hours post-dose
Urine pharmacokinetics: cumulative percent of dose excreted (Fe0-t)
for elafibranor and metabolites, if applicable. 24 hours urine collection from dosing to 216 hours post-dose
Time frame: pre-dose and then 24, 48, 72, 96, 120, 144, 168, 192, 216 hours post-dose
Urine pharmacokinetics: renal clearance (CLR)
for elafibranor and metabolites, if applicable. 24 hours urine collection from dosing to 216 hours post-dose
Time frame: pre-dose and then 24, 48, 72, 96, 120, 144, 168, 192, 216 hours post-dose