The objective of this study is to determine the mass balance and routes of excretion of total radioactivity after a single oral 200 mg dose of \[14C\]rogaratinib given as a solution. For further clinical development, human mass balance data are required to elucidate the absorption, distribution, metabolism, and excretion (ADME) of rogaratinib.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
6
Single dose, intake orally, 200 mg
PRAHealthSciences
Groningen, Netherlands
Cmax of rogaratinib in plasma
Cmax: maximum drug concentration in the measured matrix, directly taken from analytical data
Time frame: At pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h post-dose. Collection will be extended depending on the radioactivity recovery.
AUC(0-tlast) of rogaratinib in plasma
AUC(0-tlast): area under the measured matrix concentration versus time curve to the last data point above the lower limit of quantitation
Time frame: At pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h post-dose. Collection will be extended depending on the radioactivity recovery.
AUC of rogaratinib in plasma
AUC: area under the measured matrix concentration versus time curve from the first time point (t=0) extrapolated to infinity
Time frame: At pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h post-dose. Collection will be extended depending on the radioactivity recovery.
Cmax of total radioactivity in plasma and whole blood
Time frame: At pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h post-dose. Collection will be extended depending on the radioactivity recovery.
AUC(0-tlast) of total radioactivity in plasma and whole blood
Time frame: At pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h post-dose. Collection will be extended depending on the radioactivity recovery.
AUC of total radioactivity in plasma and whole blood
Time frame: At pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h post-dose. Collection will be extended depending on the radioactivity recovery.
AE,ur (%) of rogaratinib and its metabolites
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AE,ur: amount excreted into urine from 0 to infinity
Time frame: In intervals of 12h from Day -1 till Day 2 and in intervals of 24h afterwards: at pre-dose (-12-0h), 0-12, 12-24, 24-48, 48-72, 72-96,96-120, 120-144 and 144-168 hours post dose. Collection will be extended depending on the radioactivity recovery.
AE,fec (%) of rogaratinib and its metabolites
AE,fec: amount excreted into feces from 0 to infinity
Time frame: In intervals of 24h at pre dose (-18-0h), 0-24, 24-48, 48-72, 72-96, 96-120, 120-144 and 144-168 hours post dose. Collection will be extended depending on the radioactivity recovery.
AE,vom (%) of rogaratinib and its metabolites, if applicable
AE,vom: amount excreted into vomit
Time frame: During the first 6 hours after dosing