To investigate the effect of neomycin on the pharmacokinetics (PK) of regorafenib in healthy male subjects
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Masking
NONE
Enrollment
27
single oral dose (s.d.) 160 mg (four 40 mg tablets) of regorafenib on two occasions (Day 1, Period 1, and Day 1, Period 2) separated by a washout period of at least 14 days
1 g tid (three times a day) regimen of Neomycin (oral) on five days in Period 2 starting 4 days before regorafenib intake on day 1 in period 2.
Unnamed facility
Berlin, State of Berlin, Germany
AUC (area under the plasma concentration vs. time curve) for regorafenib
Time frame: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168 and 192 hours post-dose
Cmax (maximum drug concentration) for regorafenib
Time frame: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168 and 192 hours post-dose
AUC(0-24) (area under the plasma concentration vs. time curve) for regorafenib
Time frame: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose
AUC(0-tlast) (area under the plasma concentration vs. time curve) for regorafenib
Time frame: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168 and 192 hours post-dose
AUC (area under the plasma concentration vs. time curve) for BAY75-7495 (M-2) and BAY81-8752 (M-5)
Time frame: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168 and 192 hours post-dose
Cmax (maximum drug concentration) for M-2 and M-5
Time frame: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168 and 192 hours post-dose
tmax (time to reach maximum drug concentration in plasma after single dose) for regorafenib, M-2 and M-5
Time frame: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168 and 192 hours post-dose
tlast (time of last concentration above lower limit of quantification) for regorafenib, M-2 and M-5
Time frame: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168 and 192 hours post-dose
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t1/2 (half-life associated with the terminal slope) for regorafenib, M-2 and M-5
Time frame: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168 and 192 hours post-dose
AE,ur(0-72) (amount of drug excreted via urine during the collection interval 0-72 hours post administration) for metabolites BAY86-6651 (M-7) and BAY86-6652 (M-8)
Time frame: 0-72 hours post dose
Number of participants with adverse events as a measure of safety and tolerability
Time frame: Up to 30 days after last dose