Study to Evaluate the Safety and Pharmacokinetics of Single Doses of ASP2151 in Healthy Male Subjects and the Effects of Food
- Registration Number
- NCT02852876
- Lead Sponsor
- Astellas Pharma Europe Ltd.
- Brief Summary
The objective of this study is to evaluate the safety and tolerability of single rising doses of ASP2151 under fasted condition in healthy male subjects.
The study will also evaluate the pharmacokinetics (PK) of a single dose of ASP2151 under fasted versus fed conditions in healthy male subjects.
- Detailed Description
Study will be divided into two parts. Part 1 will evaluate the safety and tolerability of ASP2151 single rising doses in groups A-H in fasted condition and to determine the maximum tolerable dose (MTD) if possible.
Part 2 will evaluate the effect of fasted versus fed conditions on the safety, tolerability and PK of a single dose of ASP2151 in two treatment cycles. The wash-out period between the two treatment cycles will be at least 5 days and not shorter than five times the average elimination half-life of ASP2151, as determined in part 1 of the study.
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- Male
- Target Recruitment
- 72
- Body weight between 60 and 100 kg, and BMI between 18 and 30 kg/m2 inclusive
- Known or suspected hypersensitivity to ASP2151 or any components of the formulation used
- Any clinically significant history of asthma, eczema, any other allergic condition or previous severe hypersensitivity to any drug
- Any clinically significant history of genital herpes symptoms and/or herpes zoster symptoms in the 3 months prior to admission to the Clinical Unit
- Any clinically significant history of any other disease or disorder - gastrointestinal, cardiovascular, respiratory, renal, hepatic, neurological, dermatological, psychiatric or metabolic
- Abnormal pulse rate and/or blood pressure measurements at the pre-study visit as follows: Pulse rate <40 or >90 bpm (beats per minute); mean systolic blood pressure <90 or >140 mmHg (millimeter of mercury); mean diastolic blood pressure <40 or >95 mmHg
- Regular use of any prescribed or OTC (over the counter) drugs in the 4 weeks prior to admission to the Clinical Unit OR any use of such drugs in the 2 weeks prior to admission to the Clinical Unit
- Any use of drugs of abuse within 3 months prior to admission to the Clinical Unit
- History of smoking more than 10 cigarettes per day within 3 months prior to admission to the Clinical Unit
- History of drinking more than 21 units of alcohol per week within 3 months prior to admission to the Clinical Unit
- Donation of blood or blood products within 3 months, prior to admission to the Clinical Unit
- Positive serology test for HBsAg (Hepatitis B surface antigen), HAV IgM (Hepatitis A Virus), anti-HCV (Hepatitis C Virus) or anti-HIV (Human Immunodeficiency Virus) 1 and 2
- Not willing or able to swallow size 00 capsules
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- CROSSOVER
- Arm && Interventions
Group Intervention Description Part 1: ASP2151 Single Ascending Dose Group B (Fasting) ASP2151 Participants will receive single dose of ASP2151 assigned to Group B on day 1 Part 1: ASP2151 Single Ascending Dose Group H (Fasting) ASP2151 Participants will receive single dose of ASP2151 assigned to Group H on day 1 Part 1: Placebo Single Ascending Dose (Fasting) Placebo Participants will receive single dose of matching placebo on day 1 Part 1: ASP2151 Single Ascending Dose Group F (Fasting) ASP2151 Participants will receive single dose of ASP2151 assigned to Group F on day 1 Part 1: ASP2151 Single Ascending Dose Group C (Fasting) ASP2151 Participants will receive single dose of ASP2151 assigned to Group C on day 1 Part 1: ASP2151 Single Ascending Dose Group D (Fasting) ASP2151 Participants will receive single dose of ASP2151 assigned to Group D on day 1 Part 1: ASP2151 Single Ascending Dose Group A (Fasting) ASP2151 Participants will receive single dose of ASP2151 assigned to Group A on day 1 Part 1: ASP2151 Single Ascending Dose Group E (Fasting) ASP2151 Participants will receive single dose of ASP2151 assigned to Group E on day 1 Part 2: ASP2151 (Fasting) ASP2151 Participants will receive a single dose of ASP2151 under fasted conditions on day 1 in the first treatment period (period 1). Following a wash-out period of at least five days, the treatment will be repeated in the reverse orientation (period 2) Part 1: ASP2151 Single Ascending Dose Group G (Fasting) ASP2151 Participants will receive single dose of ASP2151 assigned to Group G on day 1 Part 2: ASP2151 (Fed) ASP2151 Participants will receive a single dose of ASP2151 under fed conditions on day 1 in the first treatment period (period 1). Following a wash-out period of at least five days, the treatment will be repeated in the reverse orientation (period 2)
- Primary Outcome Measures
Name Time Method Safety assessed by vital sign measurement: pulse rate Up to Day 15 of each treatment period For Part 1 and Part 2
Safety assessed by physical exam: body weight Up to Day 15 of each treatment period For Part 1 and Part 2
Safety assessed by vital sign measurement: blood pressure Up to Day 15 of each treatment period For Part 1 and Part 2 includes systolic and blood diastolic pressure
Safety assessed by physical exam: body mass index (BMI) Up to Day 15 of each treatment period For Part 1 and Part 2
Safety assessed by laboratory test: biochemical Up to Day 15 of each treatment period For Part 1 and Part 2
Safety assessed by laboratory test: urinalysis Up to Day 15 of each treatment period For Part 1 and Part 2
Safety and tolerability assessed by nature, frequency, and severity of Adverse Events (AEs) Up to Day 15 of each treatment period For Part 1 and Part 2
Safety assessed by 12- lead electrocardiogram (ECG) Up to Day 15 of each treatment period For Part 1 and Part 2
Safety assessed by laboratory test: hematological Up to Day 15 of each treatment period For Part 1 and Part 2
Safety assessed by laboratory test: serology Up to Day 15 of each treatment period For Part 1 and Part 2
Safety assessed by physical exam: height Up to Day 15 of each treatment period For Part 1 and Part 2
- Secondary Outcome Measures
Name Time Method Pharmacokinetics of ASP2151 in plasma: Cmax Up to 48 hours in each treatment period For Part 1 and 2. Cmax: Maximum concentration
Pharmacokinetics of ASP2151 in plasma: Vz/F Up to 48 hours in each treatment period For Part 1 and 2. Vz/F: Apparent volume of distribution
Pharmacokinetics of ASP2151 in plasma: AUC0-inf Up to 48 hours in each treatment period For Part 1 and 2. AUC0-inf: Area under the concentration time curve from the time of dosing extrapolated to time infinity
Pharmacokinetics of ASP2151 in plasma: t1/2 Up to 48 hours in each treatment period For Part 1 and 2. t1/2: Apparent terminal elimination half-life
Pharmacokinetics of ASP2151 in plasma: tmax Up to 48 hours in each treatment period For Part 1 and 2. tmax: The time after dosing when Cmax occurs
Pharmacokinetics of ASP2151 in urine: Ae0-inf Up to 48 hours in each treatment period For Part 1 and 2. Ae0-inf: Amount excreted unchanged in urine from time of dosing extrapolated to infinity
Pharmacokinetics of ASP2151 in urine: CLr Up to 48 hours in each treatment period For Part 1 and 2. CLr: Renal clearance
Pharmacokinetics of ASP2151 in plasma: CL/F Up to 48 hours in each treatment period For Part 1 and 2. CL/F: Oral clearance
Pharmacokinetics of ASP2151 in urine: Aelast Up to 48 hours in each treatment period For Part 1 and 2. Aelast: Amount excreted unchanged in urine from time of dosing up to the last quantifiable sample
Pharmacokinetics of ASP2151 in plasma: AUClast Up to 48 hours in each treatment period For Part 1 and 2. AUClast: Area under the plasma concentration time curve from time of dosing up to the last quantifiable sample
Pharmacokinetics of ASP2151 in plasma: tlag Up to 48 hours in each treatment period For Part 1 and 2. tlag: Absorption lag time
Pharmacokinetics of ASP2151 in urine: Ae% Up to 48 hours in each treatment period For Part 1 and 2. Ae%: Percent of ASP2151 amount excreted in urine
Trial Locations
- Locations (1)
Site FR1717
🇫🇷Paris, France