The main purpose of this study is to assess how selpercatinib gets into the blood stream and how long it takes the body to remove it when administered to participants with impaired hepatic function compared to healthy participants. Information about safety and tolerability will be collected. The study will last up to about 7 weeks, inclusive of screening period.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
36
Administered orally.
Orange County Research Institute
Anaheim, California, United States
National Institute of Clinical Research
Monterey Park, California, United States
Orange County Research Center
Tustin, California, United States
Riverside Clinical Research
Edgewater, Florida, United States
Pharmacokinetics (PK): Maximum Concentration (Cmax) of Selpercatinib
PK: Cmax of selpercatinib was reported.
Time frame: Predose (within 30 minutes), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, and 240 hours postdose
PK: Time to Reach Cmax (Tmax) of Selpercatinib
PK: Tmax of Selpercatinib was reported.
Time frame: Predose (within 30 minutes), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, and 240 hours postdose
PK: Area Under the Concentration-time Curve (AUC), From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib
PK: AUC0-t was calculated using the linear trapezoidal rule for increasing and decreasing concentrations.
Time frame: Predose (within 30 minutes), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, and 240 hours postdose
PK: AUC Extrapolated to Infinity (AUC0-∞) of Selpercatinib
PK: Area under the plasma concentration time curve extrapolated to infinity, calculated as AUC(0-t) + Ct/λZ, where Ct is the last measurable concentration and λZ is the apparent terminal elimination rate constant.
Time frame: Predose (within 30 minutes), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, and 240 hours postdose
PK: Percentage Extrapolation for AUC (%AUCextrap) of Selpercatinib
PK: %AUCextrap of Selpercatinib was reported.
Time frame: Predose (within 30 minutes), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, and 240 hours postdose
PK: Apparent Terminal Elimination Rate Constant (λz) of Selpercatinib
PK: Apparent terminal elimination rate constant, where λZ is the magnitude of the slope of the linear regression of the log concentration versus-time profile during the terminal phase.
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Clinical Pharmacology of Miami
Miami, Florida, United States
Orlando Clinical Research Center
Orlando, Florida, United States
The Texas Liver Institute
San Antonio, Texas, United States
Time frame: Predose (within 30 minutes), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, and 240 hours postdose
PK: Apparent Terminal Elimination Half-life (t1/2) of Selpercatinib
PK: Apparent terminal elimination half-life (whenever possible), where t1/2 = natural log (ln)(2)/λZ.
Time frame: Predose (within 30 minutes), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, and 240 hours postdose
PK: Apparent Systemic Clearance (CL/F) of Selpercatinib
CL/F is apparent clearance of the drug from the plasma, calculated as the drug dose divided AUC (0-inf), expressed in liter/hour (L/hr).
Time frame: Predose (within 30 minutes), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, and 240 hours postdose
PK: Apparent Volume of Distribution During the Terminal Phase (Vd/F) of Selpercatinib
PK: Vd/F was calculated as CL/F/λZ.
Time frame: Predose (within 30 minutes), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, and 240 hours postdose
PK: Mean Residence Time (MRT) of Selpercatinib
PK: MRT represents the average time the drug (selpercatinib) stays in the body.
Time frame: Predose (within 30 minutes), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, and 240 hours postdose
Number of Participants With One or More Serious Adverse Event(s) (SAEs) Considered by the Investigator to be Related to Study Drug Administration
Data presented are the number of participants who experienced SAEs considered by the investigator to be related to study drug administration. A summary of SAEs and all other non-serious Adverse Event(s) (AEs), regardless of causality, is located in the Reported Adverse Event module.
Time frame: Baseline up to Week 7