MedPath

Effect of Copanlisib on Metformin Pharmacokinetics and Pharmacodynamics

Phase 1
Completed
Conditions
Healthy Volunteers
Interventions
Registration Number
NCT03655301
Lead Sponsor
Bayer
Brief Summary

The purpose of this study is to learn about a drug-drug interaction. When two medications are taken together at the same time, one medication may change the activity of the other medication in the body - this is called a drug-drug interaction. This study is looking at the effect the Bayer study drug, copanlisib, has on metformin, a commonly used medication to treat diabetes. During the study, blood and urine samples will be collected and analyzed to learn about pharmacokinetics (how copanlisib changes metformin levels in the body) and pharmacodynamics (the effect metformin has on the body when taken together with copanlisib) when someone takes both copanlisib and metformin together.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
13
Inclusion Criteria
  • Healthy male or female subjects - as determined by the investigator or medically qualified designee based on medical evaluations, including medical history, physical examination, laboratory tests and cardiac monitoring
  • Aged 18 to 45 years at the first screening visit
  • Body Mass Index (BMI) of 18.0 - 34 kg / m*2 , with body weight ≥ 50 kg
  • Creatinine clearance ≥ 90 mL/min using the Modification of Diet in Renal Disease
  • Adequate end organ and bone marrow function
Read More
Exclusion Criteria
  • Existing relevant diseases of vital organs (e.g. liver diseases, heart diseases), central nervous system (for example seizures) or other organs (e.g. diabetes mellitus)
  • Incompletely cured pre-existing diseases for which it can be assumed that the absorption, distribution, metabolism, elimination and effects of the study drugs will not be normal
  • Relevant respiratory insufficiency / disorder
  • Administration of strong CYP3A4 inhibitors or inducers within 2 weeks prior to dosing
  • Known history of hypersensitivity (or known allergic reaction) to copanlisib, metformin, related compounds, or any components of the formulation
Read More

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
Copanlisib (Aliqopa, BAY80-6946)Copanlisib (Aliqopa, BAY80-6946)All subjects will receive a single dose of metformin 1000 mg on Days 1 and 8 in a fasting state. Subjects will also receive a single i.v. dose of 60 mg copanlisib on Day 8 as part of the combination with metformin.
Copanlisib (Aliqopa, BAY80-6946)MetforminAll subjects will receive a single dose of metformin 1000 mg on Days 1 and 8 in a fasting state. Subjects will also receive a single i.v. dose of 60 mg copanlisib on Day 8 as part of the combination with metformin.
Primary Outcome Measures
NameTimeMethod
Maximum Drug Concentration of Metformin in Plasma After Single Dose Administration (Cmax)Pre-dose and up to 24 hours after drug administration on Day 1 and Day 8

Maximum observed drug concentration of metformin in plasma after single dose administration without copanlisib (Day 1) and in combination with copanlisib (Day 8) were measured.

Area Under the Plasma Concentration Versus Time Curve From Zero to 24 Hours of Metformin After Single Dose Administration (AUC[0-24])Pre-dose and up to 24 hours after drug administration on Day 1 and Day 8

Area under the concentration versus time curve from zero to 24 hours of metformin after single dose administration without copanlisib (Day 1) and in combination with copanlisib (Day 8) were measured.

Area Under the Plasma Concentration Versus Time Curve From Zero to Infinity of Metformin After Single Dose Administration (AUC)Pre-dose and extrapolated up to infinity after drug administration on Day 1 and Day 8

Area under the concentration verus time curve from zero to infinity of metformin after single dose without copanlisib (Day 1) and in combination with copanlisib (Day 8) were measured.

Secondary Outcome Measures
NameTimeMethod
Number of Participants With Treatment-Emergent Adverse EventsFrom start of study medication until 30 days after end of treatment with study medication.

An adverse event (AE) was any untoward medical occurrence in a subject who received study drug without regard to possibility of causal relationship. Treatment-emergent adverse events (TEAEs) were defined as adverse events that started or worsened after the start of study drug administration up to 30 days after last administration of the study medication.

Number of Participants With Treatment-Emergent Adverse Events by SeverityFrom start of study medication until 30 days after end of treatment with study medication.

An adverse event (AE) was any untoward medical occurrence in a subject who received study drug without regard to possibility of causal relationship. Treatment-emergent adverse events (TEAEs) were defined as adverse events that started or worsened after the start of study drug administration up to 30 days after last administration of the study medication. TEAEs per severity were reported.

Plasma Lactate LevelsUp to 24 hours after study drug administration on Day 1 and Day 8

Lactate levels were analyzed in plasma samples collected during metformin alone or in combination with copanlisib. Plasma lactate levels were summarized by treatment conditions (Day 1 and Day 8).

Maximum Change From Baseline in Plasma Lactate LevelsFrom pre-dose up to 24 hours after study drug administration on Day 1 and Day 8

Lactate levels were analyzed in plasma samples collected during metformin alone or in combination with copanlisib. Maximum change from baseline on Day 1 and Day 8 was summarized.

Trial Locations

Locations (1)

Pharmaceutical Product Development (PPD), LLC

🇺🇸

Austin, Texas, United States

© Copyright 2025. All Rights Reserved by MedPath