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Effect of Renal Impairment on Evobrutinib Pharmacokinetics (PK)

Phase 1
Completed
Conditions
Renal Impairment
Interventions
Registration Number
NCT03436394
Lead Sponsor
Merck KGaA, Darmstadt, Germany
Brief Summary

The study will investigate the PK and safety of evobrutinib in subjects with different degree of renal impairment as compared to subjects with normal renal function.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
31
Inclusion Criteria
  • Male and Female subjects with total body weight between 50.0 and 100.0 kilograms(kg) (inclusive) and body mass index (BMI) between 19.0 and 36.0 kg per meter square (inclusive) at the time of the screening examination
  • For subjects with impaired renal function: Subjects must have an eGFR according to the Modification of diet in renal disease (MDRD) equation of less than 90 mL per minute at screening and the possibility of stratification to one of the groups and a stable renal function as defined by either: if the time interval between screening and dosing is greater than 10 days, two eGFR with the second estimate within 20% of prior value or historical records of stable function over the past 3 months if within 20 percentage of screening value and within 10 days of dosing
  • Other protocol defined inclusion criteria could apply
Exclusion Criteria
  • History or presence of respiratory, gastrointestinal (including bariatric or other gastric surgeries, or other conditions that may affect drug absorption) hepatic (including hepatorenal syndrome), hematological, lymphatic, neurological (including seizures), cardiovascular (including ventricular dysfunction and congestive heart failure), psychiatric, musculoskeletal, genitourinary, immunological, dermatological, connective tissue diseases or disorders that may affect the safety of the subject.
  • Clinical history of any autoimmune disorder
  • Prior history of cholecystectomy or splenectomy, and any clinically relevant surgery within 6 months prior to Screening, which might interfere with the objectives of the study or the study procedures
  • History of any malignancy except superficial basal cell carcinoma treated for curative intent may be allowed
  • Other protocol defined exclusion criteria could apply

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Evobrutinib: Severe Renal ImpairmentEvobrutinibSubjects with eGFR less than (\<) 30 mL/min/1.73 m\^2 will receive a single oral dose of evobrutinib under fasting conditions.
Evobrutinib: Normal Renal FunctionEvobrutinibSubjects with estimated glomerular filtration rate (eGFR) greater than or equal to (\>=) 90 milliliter per minute per 1.73 meter square (mL/min/1.73 m\^2) will receive a single oral dose of evobrutinib under fasting conditions.
Evobrutinib: Mild Renal ImpairmentEvobrutinibSubjects with eGFR \>= to 60 mL/min/1.73 m\^2 and \< 90 mL/min/1.73 m\^2 will receive a single oral dose of evobrutinib under fasting conditions.
Evobrutinib: Moderate Renal ImpairmentEvobrutinibSubjects with eGFR \>= to 30 mL/min/1.73 m\^2 and \< 60 mL/min/1.73 m\^2 will receive a single oral dose of evobrutinib under fasting conditions.
Primary Outcome Measures
NameTimeMethod
Area Under the Plasma Concentration-Time Curve From Time Zero to the Last Quantifiable Concentration (AUC 0-t) of EvobrutinibPre-dose up to 30 hours post-dose
Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinity (AUC 0-inf) of EvobrutinibPre-dose up to 30 hours post-dose
Maximum Observed Plasma Concentration (Cmax) of EvobrutinibPre-dose up to 30 hours post-dose
Secondary Outcome Measures
NameTimeMethod
Number of Subjects With Clinically Significant Abnormalities in Vital Signs, Laboratory Parameters and 12-lead Electrocardiogram (ECG) FindingsDay 1 up to Day 6

Number of subjects with clinically significant abnormalities will be reported.

Time to Reach the Maximum Plasma Concentration (tmax) of EvobrutinibPre-dose up to 30 hours post-dose
Time Prior to the First Measurable (Non-Zero) Concentration (t lag) of EvobrutinibPre-dose up to 30 hours post-dose
Amount of Unchanged Drug (Evobrutinib) Excreted in Urine During Collection Interval (0-8 hours) (Ae0-8h)Pre-dose up to 8 hours post-dose
Renal Clearance of Evobrutinib (CLR)Pre-dose up to 30 hours post-dose
Non-Renal Clearance of Evobrutinib (CLNonR/f)Pre-dose up to 30 hours post-dose
Terminal Rate Constant (λz) of EvobrutinibPre-dose up to 30 hours post-dose
Terminal Half-Life (t1/2) of EvobrutinibPre-dose up to 30 hours post-dose
Area Under the Plasma Concentration-Time Curve From Time Zero to 8 Hours After Dosing (AUC 0-8h) of EvobrutinibPre-dose up to 8 hours post-dose
Occurrences of Treatment-emergent Adverse Events (TEAEs)Day 1 up to Day 6
Number of Subjects With TEAEs According to SeverityDay 1 up to Day 6
Area Under the Plasma Concentration-Time Curve From Time Zero to 24 Hours After Dosing (AUC 0-24h) of EvobrutinibPre-dose up to 24 hours post-dose
Apparent Volume of Distribution During Terminal Phase (Vz/f) of EvobrutinibPre-dose up to 30 hours post-dose
Fraction of Administered Drug (Evobrutinib) Excreted in Urine (fe)Pre-dose up to 30 hours post-dose
Fraction of Unbound Drug (Evobrutinib) in the Plasma (fu)Pre-dose up to 30 hours post-dose
Apparent Clearance (CL/f) of EvobrutinibPre-dose up to 30 hours post-dose

Trial Locations

Locations (1)

Please Contact the Merck KGaA Communication Center

🇩🇪

Darmstadt, Germany

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