The purpose of the study was to evaluate the pharmacokinetics of a single oral dose of gilteritinib in male and female participants with severe renal impairment compared to healthy male and female participants with normal renal function. This study also evaluated safety and tolerability of a single oral dose of gilteritinib in male and female participants with severe renal impairment and healthy male and female participants with normal renal function. Part 2 of the study (mild and moderate renal impairment) was not conducted based on the final pharmacokinetic findings from part 1 (severe renal impairment).
This study was comprised of participants with severe renal impairment and normal renal function. Participants were residential for a single period of 14 days/13 nights. Participants were discharged from the clinical unit on day 14 on the condition that all required assessments had been performed and that there were no medical reasons for a longer stay in the clinical unit.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
17
Oral
National Institute of Clinical Research
Garden Grove, California, United States
Orange County Research Institute
Tustin, California, United States
Orlando Clinical Research Center
Orlando, Florida, United States
Site BG35901
Sofia, Bulgaria
Pharmacokinetics (PK) of gilteritinib in plasma: Area under the concentration-time curve (AUC) from the time of dosing extrapolated to time infinity (AUCinf)
Area under the concentration-time curve from the time of dosing extrapolated to time infinity was derived from the plasma samples.
Time frame: Predose on day 1 and at the following postdose time points on 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24,48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312 hour(s) and at the end of study (maximum: day 23)
PK of gilteritinib in plasma: Area under the concentration-time curve from the time of dosing to the last measurable concentration (AUClast)
Area under the concentration-time curve from the time of dosing to the last measurable concentration was derived from the plasma samples.
Time frame: Predose on day 1 and at the following postdose time points on 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24,48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312 hour(s) and at the end of study (maximum: day 23)
PK of gilteritinib in plasma: Maximum concentration (Cmax)
Maximum plasma concentration of gilteritinib was derived from the plasma samples.
Time frame: Predose on day 1 and at the following postdose time points on 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24,48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312 hour(s) and at the end of study (maximum: day 23)
PK of gilteritinib in plasma: Apparent clearance (CL/F)
CL/F derived from plasma samples.
Time frame: Predose on day 1 and at the following postdose time points on 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24,48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312 hour(s) and at the end of study (maximum: day 23)
Pk of gilteritinib in plasma: Area under the concentration-time curve from the time of dosing extrapolated to the time infinity (unbound)(AUCinf,u)
Area under the concentration-time curve from the time of dosing extrapolated to time infinity (unbound) was derived from plasma samples.
Time frame: Predose on day 1 and at the following postdose time points on 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24,48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312 hour(s) and at the end of study (maximum: day 23)
PK of gilteritinib in plasma: Area under the concentration-time curve from the time of dosing to the last measurable concentration (unbound) (AUClast, u)
Area under the concentration-time curve from the time of dosing to the last measurable concentration (unbound) was derived from plasma samples.
Time frame: Predose on day 1 and at the following postdose time points on 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24,48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312 hour(s) and at the end of study (maximum: day 23)
PK of gilteritinib in plasma: Maximum concentration (unbound) (Cmax,u)
Maximum concentration of gilteritinib (unbound) was derived from plasma samples.
Time frame: Predose on day 1 and at the following postdose time points on 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24,48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312 hour(s) and at the end of study (maximum: day 23)
Number of participants with Treatment Emergent Adverse Events (TEAEs)
An AE is any untoward medical occurrence in a participant administered a study drug, which does not necessarily have to have a causal relationship with this treatment. It can, therefore, be any unfavorable and unintended sign, symptom or disease (new or exacerbated) temporally associated with the use of a medicinal product whether considered related to the medicinal product. Treatment Emergent Adverse Event defined as an AE observed after starting administration of the study drug till 23 days.
Time frame: Up to Day 23
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