Clinical trial NCT02119221: Copanlisib Mass Balance Study
Official title: Single Center, Open-label, Non-randomized, Non-placebo-controlled Study to Investigate the Metabolism, Excretion Pattern, Mass Balance, Safety, Tolerability and Pharmacokinetics After Single Intravenous Administration of 12 mg [14C]Copanlisib (BAY 80-6946) in Healthy Male Subjects
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy Volunteers
Lead sponsor: Bayer
Sponsor class: INDUSTRY
First posted: 2014-04-21
Enrollment: 6
Sex: MALE
Minimum age (years): 45
Maximum age (years): 65
Standard ages: ADULT
OLDER_ADULT
Accepts healthy volunteers: yes
Allocation: NA
Intervention model: SINGLE_GROUP
Primary purpose: BASIC_SCIENCE

Brief summary: The study aims to provide understanding of the relative relevance of the different excretion pathways of Copanlisib in humans, as well as to characterize its metabolite profile.


Eligibility criteria: Inclusion Criteria:

* Healthy male subject
* Age: 45 to 65 years
* Body weight greater or equal to 60 kg and body mass index (BMI): above/equal 18 and below/equal 30 kg/m²

Exclusion Criteria:

* Regular use of medicines
* Known recent (last 2 years) abuse of recreational drugs, suspicion of drug or alcohol abuse, or positive results of the drug and alcohol screen tests at screening or baseline
* Use of strong inhibitors of cytochrome P450 (CYP)3A4, as well as use of St John's Wort or strong inducers of CYP3A4 prohibited from 14 days before the administration of study drug until discharge from the clinic
* Smoking
* Average intake of more than 24 units of alcohol per week; Regular daily consumption of more than 1 L of methylxanthine-containing beverages
* Any condition, which may result in longer than usual retention of urine or feces in the body, such as pronounced (less than one defecation in 2 days) constipation or symptomatic prostatic hypertrophy.
* Participation in another mass balance study with a radiation burden \> 0.1 mSv in the period of 1 year before screening

Primary outcomes:
measure: Pharmacokinetics of copanlisib in plasma by maximum concentration (Cmax)
timeFrame: Multiple time points up to 336 hours
measure: Pharmacokinetics of copanlisib in plasma by area under the measured matrix concentration versus time curve from the first time point (t=0) extrapolated to infinity (AUC)
timeFrame: Multiple time points up to 336 hours
measure: Pharmacokinetics of copanlisib in plasma by area under the measured matrix concentration versus time curve to the last data point above the lower limit of quantitation (AUC(0-tlast))
timeFrame: Multiple time points up to 336 hours
measure: Pharmacokinetics of total radioactivity in plasma by Cmax
timeFrame: Multiple time points up to 336 hours
measure: Pharmacokinetics of total radioactivity in plasma by AUC
timeFrame: Multiple time points up to 336 hours
measure: Pharmacokinetics of total radioactivity in plasma by AUC(0-tlast)
timeFrame: Multiple time points up to 336 hours
measure: Pharmacokinetics of total radioactivity in whole blood by Cmax
timeFrame: Multiple time points up to 336 hours
measure: Pharmacokinetics of total radioactivity in whole blood by AUC
timeFrame: Multiple time points up to 336 hours
measure: Pharmacokinetics of total radioactivity in whole blood by AUC(0-tlast)
timeFrame: Multiple time points up to 336 hours
measure: Radioactivity excreted in urine as a percentage of the dose (AE,ur)
timeFrame: Multiple time points up to 336 hours
measure: Radioactivity excreted in feces as a percentage of the dose (AE,fec)
timeFrame: Multiple time points up to 336 hours
measure: Metabolite profile in plasma
timeFrame: Multiple time points up to 336 hours
measure: Metabolite profile in urine
timeFrame: Multiple time points up to 336 hours
measure: Metabolite profile in feces
timeFrame: Multiple time points up to 336 hours
Secondary outcomes:
measure: Number of participants with adverse events as a measure of safety and tolerability
timeFrame: Until 30 days after study drug administration
Other outcomes:
Locations:
city: Zuidlaren
country: Netherlands
Study officials:
affiliation: Bayer
name: Bayer Study Director
role: STUDY_DIRECTOR
References: