This will be an open-label, single-center study to evaluate pharmacokinetics and safety of HMPL-013 in approximately 6 healthy male subjects receiving a single oral 5mg dose of HMPL-013 containing approximately 100 microcuries of \[14C\] HMPL-013. This study will investigate the absorption, drug biotransformation and mass balance of HMPL-013, seek to identify the compound's major metabolites and supply information for clinical application.
This study will be an open-label, mass balance study of fruquintinib administered orally at 5mg (100mCi). Subjects will be screened for eligibility up to 14 days prior to entry into the study. For study period, subjects will be admitted to the clinical research unit (CRU) on the day before dosing and fast overnight (approximately 10 hours). On the morning of dosing for study period, subjects will receive a single oral dose of 5 mg fruquintinib in the fasted state. Subjects will remain at the CRU for at least 336 hours after administration of study drug for collection of serial blood samples for pharmacokinetic (PK) analysis and safety monitoring.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
OTHER
Masking
NONE
Enrollment
6
fruquintinib suspension, 5mg ( 100mCi), oral, taken once, fast
Jiangsu Province Hospital
Nanjing, Jiangsu, China
Total radioactivity on blood, urine and faeces (radiocarbon) following oral suspension [14C]HMPL-013 dosing
Total radioactivity in blood to determine Cmax, Tmax, Half-life, AUC0-t, AUC0-∞ Total radioactivity in urine and faeces at each time interval and cumulative radioactivity (mass balance)
Time frame: Up to 14 days
Blood concentrations of HMPL-013 and its metabolites
Blood concentrations of HMPL-013 and its metabolites to determine Cmax, Tmax, Half-life, AUC0-t, AUC0-∞
Time frame: Up to 14 days
Mass balance after a single oral dose of [14C] HMPL-013 as generated from recovery of total radioactivity excreted in urine and faeces.
Time frame: Up to 14 days
Metabolite profililing and identification of metabolites in blood, urine and faeces
Time frame: up to 14 days
Safety and tolerability parameters, including adverse events (AEs), vital signs, ECGs, and clinical laboratory assessments.
safety will assessed by physical exam, clinical laboratory evaluations and ECGs.
Time frame: Up to 14 days
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