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Pharmacokinetics and Safety of Vilaprisan in Renal Impairment

Primary Purpose

Uterine Fibroids, Endometriosis

Status

Completed

Phase

Phase 1

Locations

United States

Study Type

Interventional

Intervention

Vilaprisan (BAY1002670)

About this trial

This is an interventional other trial for Uterine Fibroids focused on measuring Pharmacokinetics

Eligibility Criteria

18 Years - 79 Years (Adult, Older Adult)All SexesAccepts Healthy Volunteers

Inclusion Criteria:

BMI: 18 to 40 kg/m*2 (inclusive)
Decreased renal function, as assessed at screening, based on serum creatinine and calculated according to the Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI) formula, either:

Moderately impaired renal function: eGFR: 30 to 59 mL/min/1.73 m*2; or Severely impaired renal function: eGFR <30 mL/min/1.73 m*2 but not on dialysis

- Normal renal function, as assessed at screening and based on serum creatinine according to the CKD-EPI formula: eGFR ≥90 mL/min/1.73 m*2

Exclusion Criteria:

Any relevant disease within 4 weeks prior to study drug administration including infections and acute gastrointestinal diseases (vomiting, diarrhea, constipation) requiring medical treatment.
Severe cerebrovascular or cardiac disorders less than 6 months prior to study drug administration, e.g. stroke, myocardial infarction, unstable angina pectoris, percutaneous transluminal coronary angioplasty or coronary artery bypass graft, congestive heart failure of Grade III or IV according to New York Heart Association, or arrhythmia requiring antiarrhythmic treatment.
Malignancy diagnosed or treated within the past 5 years. This does not include adequately treated basal cell carcinoma or localized squamous cell carcinoma of the skin.
Acute renal failure or acute nephritis within the past 2 years.
Pregnancy or lactation.
Use of CYP3A4 inducers from 2 weeks before study drug administration until last day of blood sampling for PK after study drug administration, including grapefruits.
Insufficiently controlled diabetes mellitus with fasting blood glucose >220 mg/dL or HbA1c >10%.

Sites / Locations

Clinical Pharmacology of Miami, Inc.
Orlando Clinical Research Center

Arms of the Study

Arm 1

Arm 2

Arm 3

Arm Type

Experimental

Arm Label

Subjects with moderately decreased renal function

Subjects with severely decreased renal function

Control subjects with normal renal function

Arm Description

Subjects with moderate renal impairment with an estimated glomerular filtration rate (eGFR) of 30 to 59 mL/min/1.73 m*2 according to the Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI) formula.

Subjects with severe renal impairment not on dialysis with an eGFR <30 mL/min/1.73 m*2 (CKD-EPI formula).

Subjects with an eGFR ≥90 mL/min/1.73 m*2 (CKD-EPI formula) who are matched based on sex, age, race and weight.

Outcomes

Primary Outcome Measures

Area under the concentration versus time curve from zero to infinity after single (first) dose (AUC) of BAY1002670

Area under the concentration versus time curve from zero to the last data point above the lower limit of quantitation [AUC(0-tlast)], if AUC cannot be estimated in all subjects. In subjects with normal and moderately reduced renal function.

Maximum observed drug concentration in measured matrix after single dose administration (Cmax) of BAY1002670

In subjects with normal and moderately reduced renal function.

Secondary Outcome Measures

Number of participants with adverse events

In subjects with normal, moderately, and severely reduced renal function.

AUC

In subjects with normal, moderately, and severely reduced renal function.

unbound AUC (AUCu)

In subjects with normal, moderately, and severely reduced renal function.

Cmax

In subjects with normal, moderately, and severely reduced renal function.

Unbound Cmax (Cmax,u)

In subjects with normal, moderately, and severely reduced renal function.

Apparent oral clearance (CL/F)

In subjects with normal, moderately, and severely reduced renal function.

Unbound CL/F (CLu/F)

In subjects with normal, moderately, and severely reduced renal function.

Half-life associated with the terminal slope (t1/2)

In subjects with normal, moderately, and severely reduced renal function.

Renal clearance (CLR)

In subjects with normal, moderately, and severely reduced renal function.

Fraction of free (unbound) drug in plasma (fu)

In subjects with normal, moderately, and severely reduced renal function.

Full Information

NCT ID

NCT03411980

First Posted

January 22, 2018

Last Updated

December 1, 2019

Sponsor

Bayer

1. Study Identification

Unique Protocol Identification Number

NCT03411980

Brief Title

Pharmacokinetics and Safety of Vilaprisan in Renal Impairment

Official Title

An Open-label, Single-dose Study to Evaluate the Pharmacokinetics and Safety of Vilaprisan in Subjects With Decreased Renal Function in Comparison With Matched Subjects With Normal Renal Function

Study Type

Interventional

2. Study Status

Record Verification Date

December 2019

Overall Recruitment Status

Completed

Study Start Date

February 2, 2018 (Actual)

Primary Completion Date

October 10, 2018 (Actual)

Study Completion Date

February 6, 2019 (Actual)

3. Sponsor/Collaborators

Responsible Party, by Official Title

Sponsor

Name of the Sponsor

Bayer

4. Oversight

Studies a U.S. FDA-regulated Drug Product

Yes

Studies a U.S. FDA-regulated Device Product

Data Monitoring Committee

5. Study Description

Brief Summary

The purpose of the study is to evaluate the pharmacokinetics of vilaprisan in subjects with moderate to severe renal impairment compared with matched subjects with normal renal function.

Detailed Description

This is a multiple-center, open-label, non-randomized, single-dose study in 3 parallel groups of subjects with moderately or severely impaired renal function or normal renal function matched with regard to sex, age, race and weight. PK blood and urine sampling for determination of vilaprisan concentrations in plasma and urine, respectively, will be preformed at pre-defined time points up to 14 days post-dose. Safety and tolerability will be assessed through adverse events, clinical laboratory tests, vital signs, 12-lead electrocardiograms and physical examinations.

6. Conditions and Keywords

Primary Disease or Condition Being Studied in the Trial, or the Focus of the Study

Uterine Fibroids, Endometriosis

Keywords

Pharmacokinetics

7. Study Design

Primary Purpose

Other

Study Phase

Phase 1

Interventional Study Model

Parallel Assignment

Masking

None (Open Label)

Allocation

Non-Randomized

Enrollment

26 (Actual)

8. Arms, Groups, and Interventions

Arm Title

Subjects with moderately decreased renal function

Arm Type

Experimental

Arm Description

Arm Title

Subjects with severely decreased renal function

Arm Type

Experimental

Arm Description

Subjects with severe renal impairment not on dialysis with an eGFR <30 mL/min/1.73 m*2 (CKD-EPI formula).

Arm Title

Control subjects with normal renal function

Arm Type

Experimental

Arm Description

Subjects with an eGFR ≥90 mL/min/1.73 m*2 (CKD-EPI formula) who are matched based on sex, age, race and weight.

Intervention Type

Drug

Intervention Name(s)

Vilaprisan (BAY1002670)

Intervention Description

Single oral dose (1 x 2 mg immediate-release, film-coated tablet)

Primary Outcome Measure Information:

Title

Area under the concentration versus time curve from zero to infinity after single (first) dose (AUC) of BAY1002670

Description

Time Frame

-1hour (h), 30minutes (min), 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1day (d), 2d, 3d, 4d, 7d, 10d, 14d

Title

Maximum observed drug concentration in measured matrix after single dose administration (Cmax) of BAY1002670

Description

In subjects with normal and moderately reduced renal function.

Time Frame

-1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d

Secondary Outcome Measure Information:

Title

Number of participants with adverse events

Description

In subjects with normal, moderately, and severely reduced renal function.

Time Frame

Up to 6 weeks

Title

AUC

Description

In subjects with normal, moderately, and severely reduced renal function.

Time Frame

-1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d

Title

unbound AUC (AUCu)

Description

In subjects with normal, moderately, and severely reduced renal function.

Time Frame

-1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d

Title

Cmax

Description

In subjects with normal, moderately, and severely reduced renal function.

Time Frame

-1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d

Title

Unbound Cmax (Cmax,u)

Description

In subjects with normal, moderately, and severely reduced renal function.

Time Frame

-1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d

Title

Apparent oral clearance (CL/F)

Description

In subjects with normal, moderately, and severely reduced renal function.

Time Frame

-1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d

Title

Unbound CL/F (CLu/F)

Description

In subjects with normal, moderately, and severely reduced renal function.

Time Frame

-1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d

Title

Half-life associated with the terminal slope (t1/2)

Description

In subjects with normal, moderately, and severely reduced renal function.

Time Frame

-1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d

Title

Renal clearance (CLR)

Description

In subjects with normal, moderately, and severely reduced renal function.

Time Frame

-1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d

Title

Fraction of free (unbound) drug in plasma (fu)

Description

In subjects with normal, moderately, and severely reduced renal function.

Time Frame

-1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d

10. Eligibility

Sex

All

Minimum Age & Unit of Time

18 Years

Maximum Age & Unit of Time

79 Years

Accepts Healthy Volunteers

Eligibility Criteria

Inclusion Criteria: BMI: 18 to 40 kg/m*2 (inclusive) Decreased renal function, as assessed at screening, based on serum creatinine and calculated according to the Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI) formula, either: Moderately impaired renal function: eGFR: 30 to 59 mL/min/1.73 m*2; or Severely impaired renal function: eGFR <30 mL/min/1.73 m*2 but not on dialysis - Normal renal function, as assessed at screening and based on serum creatinine according to the CKD-EPI formula: eGFR ≥90 mL/min/1.73 m*2 Exclusion Criteria: Any relevant disease within 4 weeks prior to study drug administration including infections and acute gastrointestinal diseases (vomiting, diarrhea, constipation) requiring medical treatment. Severe cerebrovascular or cardiac disorders less than 6 months prior to study drug administration, e.g. stroke, myocardial infarction, unstable angina pectoris, percutaneous transluminal coronary angioplasty or coronary artery bypass graft, congestive heart failure of Grade III or IV according to New York Heart Association, or arrhythmia requiring antiarrhythmic treatment. Malignancy diagnosed or treated within the past 5 years. This does not include adequately treated basal cell carcinoma or localized squamous cell carcinoma of the skin. Acute renal failure or acute nephritis within the past 2 years. Pregnancy or lactation. Use of CYP3A4 inducers from 2 weeks before study drug administration until last day of blood sampling for PK after study drug administration, including grapefruits. Insufficiently controlled diabetes mellitus with fasting blood glucose >220 mg/dL or HbA1c >10%.

Facility Information:

Facility Name

Clinical Pharmacology of Miami, Inc.

City

Miami

State/Province

Florida

ZIP/Postal Code

33014

Country

United States

Facility Name

Orlando Clinical Research Center

City

Orlando

State/Province

Florida

ZIP/Postal Code

32809

Country

United States

12. IPD Sharing Statement

Links:

URL

http://clinicaltrials.bayer.com/

Description

Click here to find results for studies related to Bayer products

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Pharmacokinetics and Safety of Vilaprisan in Renal Impairment

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