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Effect of Neomycin on the Pharmacokinetics of Regorafenib

Single-center, Open-label, Non-randomized, Two-period Sequential Treatment Study to Assess the Effect of Neomycin on the Pharmacokinetics of Regorafenib in Healthy Male Subjects

Status
Completed
Phases
Phase 1
Study type
Interventional
Source
ClinicalTrials.gov
Registry ID
NCT02001909
Enrollment
27
Registered
2013-12-05
Start date
2013-12-31
Completion date
2014-04-30
Last updated
2015-08-13

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Neoplasms

Keywords

Regorafenib, Neomycin, Cancer, Pharmacokinetics, Safety

Brief summary

To investigate the effect of neomycin on the pharmacokinetics (PK) of regorafenib in healthy male subjects

Interventions

DRUGRegorafenib (Stivarga, BAY73-4506)

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.

Sponsors

Bayer
Lead SponsorINDUSTRY

Study design

Allocation
NON_RANDOMIZED
Intervention model
PARALLEL
Masking
NONE

Eligibility

Sex/Gender
MALE
Age
18 Years to 45 Years
Healthy volunteers
Yes

Inclusion criteria

Inclusion: * Healthy male subjects * Age: 18 to 45 years (inclusive) at the first screening examination/visit * Body mass index (BMI): above/equal 18 and below 30 kg / m² * Confirmation of the subject's health insurance coverage prior to the first screening examination/visit * Subjects enrolled in this study must use adequate barrier birth control measures prior to, during the course of the study, and 3 months after the last administration of regorafenib. An adequate contraception includes the use of condoms or a vasectomy. In addition, adequate birth control measures for the subject's partner is required, such as a hormonal contraception with implants or combined oral contraceptives, certain intrauterine devices, bilateral tubal ligation, or hysterectomy. Exclusion: * Known or suspected hypersensitivity to regorafenib and/or neomycin * Any illness or medical condition that is unstable or could jeopardize the safety of the subject and his compliance in the study * Clinically significant illness within 30 days prior to Day 1, Period 1. * Regular use of medicines at the time of screening, including herbal supplements and high dose vitamins * Smoking; however, former smokers who have stopped smoking at least 3 months before the first study drug administration may be included * Clinically relevant findings in the electrocardiogram (ECG) * Clinically relevant findings in the complete physical examination * Positive results for hepatitis B virus surface antigen (HBsAg), hepatitis C virus antibodies (anti-HCV), human immune deficiency virus antibodies (anti-HIV 1+2) at screening. * Positive urine drug screening

Design outcomes

Primary

MeasureTime frame
AUC (area under the plasma concentration vs. time curve) for regorafenibPre-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 regorafenibPre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168 and 192 hours post-dose

Secondary

MeasureTime frame
AUC (area under the plasma concentration vs. time curve) for BAY75-7495 (M-2) and BAY81-8752 (M-5)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-5Pre-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-5Pre-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 regorafenibPre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose
t1/2 (half-life associated with the terminal slope) for regorafenib, M-2 and M-5Pre-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)0-72 hours post dose
Number of participants with adverse events as a measure of safety and tolerabilityUp to 30 days after last dose
tlast (time of last concentration above lower limit of quantification) for regorafenib, M-2 and M-5Pre-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-tlast) (area under the plasma concentration vs. time curve) for regorafenibPre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168 and 192 hours post-dose

Countries

Germany

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026