Copanlisib Mass Balance Study

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

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.

Study Overview

• Status: Completed
• Conditions: Healthy Volunteers
• Intervention / Treatment: Drug: Copanlisib (BAY80-6946)

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Contacts and Locations

Study Locations

• Netherlands
  • Zuidlaren, Netherlands, 9471 GP

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 45 years to 65 years (Adult, Older Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

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

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: [14C]Copanlisib	Drug: Copanlisib (BAY80-6946); Intravenous infusion of 12 mg copanlisib labeled with 2.76 MBq (75 μCi) of [14C]

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Pharmacokinetics of copanlisib in plasma by maximum concentration (Cmax)	Multiple time points up to 336 hours
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)	Multiple time points up to 336 hours
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))	Multiple time points up to 336 hours
Pharmacokinetics of total radioactivity in plasma by Cmax	Multiple time points up to 336 hours
Pharmacokinetics of total radioactivity in plasma by AUC	Multiple time points up to 336 hours
Pharmacokinetics of total radioactivity in plasma by AUC(0-tlast)	Multiple time points up to 336 hours
Pharmacokinetics of total radioactivity in whole blood by Cmax	Multiple time points up to 336 hours
Pharmacokinetics of total radioactivity in whole blood by AUC	Multiple time points up to 336 hours
Pharmacokinetics of total radioactivity in whole blood by AUC(0-tlast)	Multiple time points up to 336 hours
Radioactivity excreted in urine as a percentage of the dose (AE,ur)	Multiple time points up to 336 hours
Radioactivity excreted in feces as a percentage of the dose (AE,fec)	Multiple time points up to 336 hours
Metabolite profile in plasma	Multiple time points up to 336 hours
Metabolite profile in urine	Multiple time points up to 336 hours
Metabolite profile in feces	Multiple time points up to 336 hours

Secondary Outcome Measures

Outcome Measure	Time Frame
Number of participants with adverse events as a measure of safety and tolerability	Until 30 days after study drug administration

Collaborators and Investigators

• Sponsor: Bayer

Study record dates

Study Major Dates

• Study Start: February 1, 2014
• Primary Completion (Actual): April 1, 2014
• Study Completion (Actual): October 1, 2014

Study Registration Dates

• First Submitted: April 17, 2014
• First Submitted That Met QC Criteria: April 17, 2014
• First Posted (Estimate): April 21, 2014

Study Record Updates

• Last Update Posted (Estimate): October 28, 2014
• Last Update Submitted That Met QC Criteria: October 27, 2014
• Last Verified: October 1, 2014

More Information

Terms related to this study

• Other Study ID Numbers: 16353; 2013-002544-90 (EudraCT Number)