Study to Evaluate the Pharmacokinetics (PK), Safety, Tolerability of Single-Dose Transdermal Rotigotine in Japanese and Caucasian Healthy Male / Female Subjects

Phase 1CompletedNCT01761526

UCB BIOSCIENCES GmbH50 enrolled

Overview

To investigate the Pharmacokinetics (PK) of transdermally delivered Rotigotine in Japanese and Caucasian Female and Male Healthy Subjects.

Study Type

INTERVENTIONAL

Allocation

NON_RANDOMIZED

Masking

NONE

Enrollment

50

Conditions

Interventions

Rotigotine transdermal patchDRUG

Rotigotine transdermal patch, single-dose application over 24 hours 2 mg /24 hours (10 cm2)

Eligibility

Sex: ALLMin age: 20 YearsMax age: 45 YearsHealthy volunteers:

Medical Language ↔ Plain English

Inclusion Criteria: * 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 Exclusion Criteria: * 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

Locations (1)

01

Neuss, Germany

Outcomes

Primary Outcomes

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

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 frame: From Baseline (0 hours Pre-Dose) up to 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

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Maximum concentration in plasma [Cmax] of unconjugated Rotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Maximum concentration in plasma normalized by body weight [Cmax,norm] of unconjugated Rotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 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

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

Data from ClinicalTrials.gov

This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.

Secondary Outcomes

Terminal half-life [t1/2] of unconjugated Rotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Time of maximum concentration [tmax] of unconjugated Rotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Area under the concentration-time curve from zero to infinity [AUC (0-inf)] of unconjugated Rotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Total body clearance (CL) of unconjugated Rotigotine normalized by body weight (BW) [CL/f/BW]

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Apparent volume of distribution of unconjugated Rotigotine normalized by body weight [Vz/f/BW]

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Amounts of unconjugated Rotigotine excreted in urine [Ae]

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Fraction of unconjugated Rotigotine excreted into urine [fe (% of 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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Renal Clearance [CLR] of unconjugated Rotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Terminal half-life [t1/2] of total Rotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Time of maximum concentration [tmax] of total Rotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Area under the concentration-time curve from zero to infinity [AUC (0-inf)] of total Rotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Total body clearance of total Rotigotine normalized by body weight [CL/f/BW]

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Apparent volume of distribution normalized of total Rotigotine by body weight [Vz/f/BW]

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Amount of total Rotigotine excreted into urine [Ae]

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Fraction of total Rotigotine excreted into urine [fe (% of 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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Renal clearance [CLR] of total Rotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Terminal half-life [t1/2] of total Despropylrotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Time of maximum concentration [tmax] of total Despropylrotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Area under the concentration-time curve from zero to infinity [AUC (0-inf)] of total Despropylrotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Total body clearance of total Despropylrotigotine normalized by body weight [CL/f/BW]

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Apparent volume of distribution of total Despropylrotigotine normalized by body weight [Vz/f/BW]

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Amount of total Despropylrotigotine excreted into urine [Ae]

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Fraction of total Despropylrotigotine excreted into urine [fe (% of 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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Renal Clearance [CLR] of total Despropylrotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Terminal half-life [t1/2] of total Desthienylethylrotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Time of maximum concentration [tmax] of total Desthienylethylrotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Area under the concentration-time curve from zero to infinity [AUC (0-inf)] of total Desthienylethylrotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Total body clearance of total Desthienylethylrotigotine normalized by body weight [CL/f/BW]

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Apparent volume of distribution of total Desthienylethylrotigotine normalized by body weight [Vz/f/BW]

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Amount of total Desthienylethylrotigotine excreted into urine [Ae]

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Fraction of total Desthienylethylrotigotine excreted into urine [fe (%of 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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

Renal clearance [CLR] of total Desthienylethylrotigotine

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 frame: From Baseline (0 hours Pre-Dose) up to 60 hours Post-Dose

NCT01761526 - Study to Evaluate the Pharmacokinetics (PK), Safety, Tolerability of Single-Dose Transdermal Rotigotine in Japanese and Caucasian Healthy Male / Female Subjects | Crick | Crick