Effect of Ketoconazole on Regorafenib (BAY73-4506) Pharmacokinetics

A Phase I, Non-Randomized, Open Label Study to Determine the Effetc of Ketoconazole on the Pharmacokinetics of a Single Oral Dose of Regorafenib (BAY73-4506) in Healthy Volunteers

The purpose of this study is to estimate the effect of multiple doses of ketoconazole on the pharmacokinetics of a single dose of BAY73-4506 in healthy male volunteers.

Study Overview

• Status: Completed
• Conditions: Pharmacokinetics
• Intervention / Treatment: Drug: Regorafenib (BAY73-4506); Regorafenib (BAY73-4506) plus ketoconazole

• Study Type: Interventional
• Enrollment (Actual): 24
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Massachusetts
    • Brighton, Massachusetts, United States, 02135

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 45 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Healthy male subjects between 18 and 45 years of age, inclusive
• BMI between 18 and 32 kg/m2 inclusive

Exclusion Criteria:

• Subjects with evidence of disease, conditions affecting drug absorption or metabolism
• Treatment with other investigational drug within 30 days
• History of regular alcohol or recreational drug consumption
• Use of prescription drugs within 14 days
• Use of nonprescription drugs and dietary supplement within 7 days
• Blood donation within 30 days

Study Plan

How is the study designed?

Design Details

• Allocation: Non-Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Arm1	Drug: Regorafenib (BAY73-4506); Regorafenib (BAY73-4506) plus ketoconazole; Treatment 1: A single 160 mg dose of BAY73-4506. Treatment 2: Ketoconazole 400 mg once daily from Day -4 to Day 3. A single 160 mg dose of BAY73-4506 on Day 1.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Area under the plasma concentration versus time curve from zero to infinity ( Plasma AUCinf) of BAY73-4506 given alone or with ketoconazole.	1 month
Peak plasma concentration (Cmax) of BAY73-4506 given alone or with ketoconazole	1 month

Secondary Outcome Measures

Outcome Measure	Time Frame
Plasma AUCinf of metabolites of a single oral dose BAY73-4506 given alone or with ketoconazole.	1 month
Plasma Cmax of metabolites of a single oral dose BAY73-4506 given alone or with ketoconazole.	1 month
Number of subjects with adverse events following a single oral dose of BAY73-4506, adminstered alone and concomitantly with ketoconazole.	1 month

Collaborators and Investigators

• Sponsor: Bayer

Study record dates

Study Major Dates

• Study Start: March 1, 2011
• Primary Completion (Actual): July 1, 2011
• Study Completion (Actual): July 1, 2011

Study Registration Dates

• First Submitted: February 18, 2011
• First Submitted That Met QC Criteria: March 16, 2011
• First Posted (Estimate): March 18, 2011

Study Record Updates

• Last Update Posted (Estimate): November 2, 2014
• Last Update Submitted That Met QC Criteria: October 31, 2014
• Last Verified: October 1, 2014

More Information

Terms related to this study

• Keywords: pharmacokinetics; drug interactions; ketoconazole; human volunteers
• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Molecular Mechanisms of Pharmacological Action; Anti-Infective Agents; Enzyme Inhibitors; Hormones, Hormone Substitutes, and Hormone Antagonists; Cytochrome P-450 CYP3A Inhibitors; Cytochrome P-450 Enzyme Inhibitors; Hormone Antagonists; Antifungal Agents; Steroid Synthesis Inhibitors; 14-alpha Demethylase Inhibitors; Ketoconazole
• Other Study ID Numbers: 12435