Study to Evaluate the Pharmacokinetics (PK), Safety, Tolerability of Single-Dose Transdermal Rotigotine in Japanese and Caucasian Healthy Male / Female Subjects
- Registration Number
- NCT01761526
- Lead Sponsor
- UCB BIOSCIENCES GmbH
- Brief Summary
To investigate the Pharmacokinetics (PK) of transdermally delivered Rotigotine in Japanese and Caucasian Female and Male Healthy Subjects.
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- All
- Target Recruitment
- 50
- Subject is healthy according to assessments done at eligibility assessment (medical history, physical examination, blood pressure, heart rate, Electrocardiogram (ECG), hematology, clinical chemistry, urinalysis)
- Subject is of normal body-weight as determined by a body mass index ranging between 18 to 28 kg / m²
- Subject is Japanese or Caucasian. Japanese subjects are born in Japan and left Japan not more than 10 years ago. Both parents of the Japanese subjects are 100 % Japanese
- Subjects (females) without medically adequate contraception (e.g. mechanical contraception (Intrauterine-Device IUD), sterilization, hysterectomy) or on lactation or pregnant women. Subjects with oral contraception or hormone replacement within 4 weeks prior to eligibility assessment
- Subject has a history of chronic alcohol or drug abuse
- Subject has a consumption of more than 20 g of alcohol / day (amount corresponds to 0.5 l of beer / day or 0.25 l of wine / day or 3 glasses (à 2 cl) of liquor / day
- Subject has a clinically relevant allergy
- Subject has a known or suspected drug hypersensitivity in particular, to any component of the trial medication
- Subject has any clinically significant abnormality in physical examination
- Subject has a heart rate at rest less than 50 beats per minute (bpm) or more than 100 bpm
- Subject has systolic blood pressure lower than 100 mmHg or higher than 145 mmHg or diastolic blood pressure higher than 95 mmHg or lower than 60 mmHg
- Subject has an atopic or eczematous dermatitis and / or an active skin disease or skin tumors
- Subject has a history of significant skin hypersensitivity to adhesives or other transdermal products or recent unresolved contact dermatitis
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- SINGLE_GROUP
- Arm && Interventions
Group Intervention Description Rotigotine in Healthy Japanese Rotigotine transdermal patch * Rotigotine transdermal patch * Single dose application of 2 mg / 24 hours Rotigotine in Healthy Japanese subjects * Transdermal patch over 24 hours Rotigotine in Caucasian Rotigotine transdermal patch * Rotigotine transdermal patch * Single-Dose application of 2 mg / 24 hours Rotigotine in healthy Caucasian subjects * Transdermal patch over 24 hours
- Primary Outcome Measures
Name Time Method Area under the concentration-time curve (AUC) from zero up to the last measured concentration greater than the Lower Limit of Quantitation (LOQ) [AUC (0-t)] of unconjugated Rotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Area under the concentration-time curve from zero up to the last measured concentration greater than the Lower Limit of Quantitation (LOQ) normalized [AUC (0-t)norm] of unconjugated Rotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Maximum concentration in plasma [Cmax] of unconjugated Rotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Maximum concentration in plasma normalized by body weight [Cmax,norm] of unconjugated Rotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Maximum concentration in plasma normalized by body weight [Cmax,norm] of total Rotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Area under the concentration-time curve from zero up to the last measured concentration greater than the Lower Limit of Quantitation (LOQ) [AUC (0-t)] of total Rotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Maximum concentration in plasma [Cmax] of total Rotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Area under the concentration-time curve from zero up to the last measured concentration greater than the Lower Limit of Quantitation (LOQ) [AUC (0-t)] of total Despropylrotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Maximum concentration in plasma normalized by body weight [Cmax, norm] of total Desthienylethylrotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Area under the concentration-time curve from zero up to the last measured concentration greater than the Lower Limit of Quantitation (LOQ) normalized by body weight [AUC (0-t)] of total Despropylrotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Maximum concentration in plasma [Cmax] of total Despropylrotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Maximum concentration in plasma normalized by body weight [Cmax,norm] of total Despropylrotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Area under the concentration-time curve from zero up to the last measured concentration greater than the Lower Limit of Quantitation (LOQ) [AUC (0-t)] of total Desthienylethylrotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Area under the concentration-time curve from zero up to the last measured concentration greater than the Lower Limit of Quantitation (LOQ) normalized by body weight [AUC (0-t)] of total Desthienylethylrotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Maximum concentration in plasma [Cmax] of total Desthienylethylrotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
- Secondary Outcome Measures
Name Time Method Terminal half-life [t1/2] of unconjugated Rotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Time of maximum concentration [tmax] of unconjugated Rotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Area under the concentration-time curve from zero to infinity [AUC (0-inf)] of unconjugated Rotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Total body clearance (CL) of unconjugated Rotigotine normalized by body weight (BW) [CL/f/BW] From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Apparent volume of distribution of unconjugated Rotigotine normalized by body weight [Vz/f/BW] From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Renal Clearance [CLR] of unconjugated Rotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Amounts of unconjugated Rotigotine excreted in urine [Ae] From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Fraction of unconjugated Rotigotine excreted into urine [fe (% of dose)] From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Terminal half-life [t1/2] of total Rotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Time of maximum concentration [tmax] of total Rotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Area under the concentration-time curve from zero to infinity [AUC (0-inf)] of total Rotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Amount of total Rotigotine excreted into urine [Ae] From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Renal clearance [CLR] of total Rotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Time of maximum concentration [tmax] of total Despropylrotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Area under the concentration-time curve from zero to infinity [AUC (0-inf)] of total Despropylrotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Time of maximum concentration [tmax] of total Desthienylethylrotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Area under the concentration-time curve from zero to infinity [AUC (0-inf)] of total Desthienylethylrotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Apparent volume of distribution of total Desthienylethylrotigotine normalized by body weight [Vz/f/BW] From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Total body clearance of total Rotigotine normalized by body weight [CL/f/BW] From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Fraction of total Despropylrotigotine excreted into urine [fe (% of dose)] From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Total body clearance of total Desthienylethylrotigotine normalized by body weight [CL/f/BW] From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Amount of total Desthienylethylrotigotine excreted into urine [Ae] From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Fraction of total Desthienylethylrotigotine excreted into urine [fe (%of dose)] From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Renal clearance [CLR] of total Desthienylethylrotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Apparent volume of distribution normalized of total Rotigotine by body weight [Vz/f/BW] From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Terminal half-life [t1/2] of total Despropylrotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Total body clearance of total Despropylrotigotine normalized by body weight [CL/f/BW] From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Fraction of total Rotigotine excreted into urine [fe (% of dose)] From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Apparent volume of distribution of total Despropylrotigotine normalized by body weight [Vz/f/BW] From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Amount of total Despropylrotigotine excreted into urine [Ae] From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Renal Clearance [CLR] of total Despropylrotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Terminal half-life [t1/2] of total Desthienylethylrotigotine From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose Blood sampling at 0 hours (Pre-Dose), 1 hour, 2 hours, 4 hours, 8 hours, 12 hours, 16 hours, 24 hours, 25 hours, 26 hours, 28 hours, 30 hours, 33 hours, 36 hours, 48 hours, and 60 hours Post-Dose
Trial Locations
- Locations (1)
01
🇩🇪Neuss, Germany