Pharmacokinetics of ASP3662Phase 1NCT02194491
A Positron Emission Tomography Occupancy Study Using Ligand [11C]AS2471907 and Following Oral Dosing of ASP3662
A Phase 1 study testing [11C]AS2471907, Positron Emission Tomography (PET) and ASP3662 in people with Pharmacokinetics of ASP3662 and Displacement of Radiotracer, run by Astellas Pharma Global Development, Inc. at 1 site in United States.
Trial summary
The purpose of this study is to evaluate a novel PET tracer ([11C]AS2471907), and to use [11C]AS2471907 to assess the level and time-course of enzyme occupancy in the human brain prior to and following single oral dose administration of ASP3662. Read more about this study
- Who is it for?
- Ages 18 to 55 years, men onlyHealthy volunteers can take part
- Conditions the study is for
- Pharmacokinetics of ASP3662, Displacement of Radiotracer, Healthy Volunteers
- What is being tested?
- [11C]AS2471907, Positron Emission Tomography (PET) and ASP3662
- Type of treatment
- Pill or oral medicine, Injection or infusion, Surgery or procedure
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 18 participants
- Where
- 1 siteUnited States
- Study dates
- Apr 2014to May 2016
- Phase
- Phase 1
- Are there results?
- None posted in the registry
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 55 years
- Men only
- Healthy volunteers accepted
- Adult
Who may be able to join
- Subject is of non-Asian descent.
- Subject has a body mass index (BMI) range of 18.5 to 32 kg/m2, inclusive and weighs at least 50 kg at screening.
- Subject and his female spouse/partner who is of childbearing potential must be using highly effective contraception1 consisting of 2 forms of birth control (at least one of which must be a barrier method) starting at screening and continuing throughout the study period and for 90 days after final study drug administration.
- Subject must not donate sperm starting at screening, throughout the study period and for at least 90 days after final study drug administration.
- Subject agrees not to participate in another investigational study while on study treatment.
Who cannot join
- Subject has a known or suspected hypersensitivity to ASP3662, [11C]AS2471907 or intolerance of drugs with the same mechanism of action as ASP3662.
- Subject has an allergy to topical anesthetics, such as, lidocaine (if used for catheter placement).
- Subject has previously participated in a clinical study with ASP3662 or part 1 of the current study.
- Subject has any of the liver enzymes (aspartate aminotransferase [AST], alanine transaminase [ALT], alkaline phosphatase [ALP], gamma-glutamyl transferase [GGT]) or total bilirubin (TBIL) above the upper limit of normal (ULN). If any liver enzyme is > 1 x ULN but ≤ 1.5 x ULN, the assessment may be repeated once during the screening period or on check-in. If the repeated assessment is above the ULN, it is exclusionary. If the initial value is > 1.5 x ULN, it cannot be repeated and is exclusionary.
- Subject has any clinically significant history of allergic conditions.
- Subject with a history of a suicide attempt or suicidal behavior.
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- Subject has a history of smoking within the past 6 months.
- Subject has any history or evidence of any clinically significant cardiovascular, gastrointestinal (GI), endocrinologic, hematologic, hepatic, immunologic, metabolic, urologic, pulmonary, neurologic, dermatologic, psychiatric, renal and/or other major disease or malignancy, as judged by the investigator or designee.
- Subject has/had febrile illness or symptomatic viral, bacterial (including upper respiratory infection) or fungal (non-cutaneous) infection within 1 week before clinic check-in.
- Subject has any clinically significant abnormality following the investigator's review of the physical examination, electrocardiogram (ECG) and protocol-defined clinical laboratory tests at screening or clinic check-in.
- Subject has a mean pulse < 40 or > 90 beats per minute; mean systolic blood pressure > 140 mmHg or mean diastolic blood pressure > 90 mmHg (measurements taken in triplicate after subject has been resting in supine position for 10 minutes) at screening. If the mean pulse or mean systolic blood pressure (SBP) or mean diastolic blood pressure (DBP) is out of the range specified above, 1 additional triplicate measurement may be taken at screening.
- Subject has a mean QTcF interval of > 430 msec at screening or check-in. If the mean QTcF exceeds the limits above, 1 additional triplicate ECG can be taken at screening. If this triplicate also gives an abnormal result, the subject should be excluded.
- Subject has a history of unexplained syncope, cardiac arrest, unexplained cardiac arrhythmias or torsade de pointes, structural heart disease or a family history of Long QT Syndrome.
- Subject has use of any prescribed or non-prescribed drugs (including vitamins, natural and herbal remedies, e.g., St. John's wort) in the 2 weeks before study drug administration, except for occasional use of acetaminophen (up to 2 g/day).
- Subject has history of consuming more than 14 units of alcoholic beverages per week within 6 months prior to screening or has a history of alcoholism or drug/chemical or substance abuse within the past 2 years prior to screening (Note: 1 unit = 12 ounces of beer, 4 ounces of wine or 1 ounce of spirits/hard liquor) or the subject tests positive at screening or clinic admission for alcohol or drugs of abuse (amphetamines, barbiturates, benzodiazepines, cannabinoids, cocaine and opiates).
- Subject has any use of drugs of abuse within 3 months before screening or check-in.
- Subject has use of any inducer of metabolism (e.g., barbiturates, rifampin) in the 3 months prior to check-in.
- Subject has consumed any caffeine-containing product within 24 hours prior to admission or grapefruit or star fruit within 7 days prior to admission.
- Subject has any significant blood loss, donated equal to 1 unit (450 mL) or more of blood or received a transfusion of any blood or blood products within 60 days or donated plasma within 7 days before check-in.
- Subject has a positive serology test for hepatitis B surface antigen, anti-hepatitis A virus (Immunoglobulin M), anti-hepatitis C virus or anti-human immunodeficiency virus (HIV) Type 1 or Type 2 at screening.
- Subject has participated in any interventional clinical study or has been treated with any investigational drugs within 30 days or 5 half-lives, whichever is longer, before the initiation of screening.
- Subject is an employee of the Astellas Group or vendors involved in the study.
- Additionally, a subject who meets the following imaging exclusion criteria will not be included in this study:
- Subject who suffers from claustrophobia.
- Subject who has received a diagnostic or therapeutic radiopharmaceutical within 7 days prior to participation in this study.
- Participation in other research studies involving ionizing radiation within 1 year of the PET scans that would cause the subject to exceed the US Nuclear Regulatory Commission yearly dose limits for healthy subjects, i.e., an effective dose of 5 Roentgen equivalent man (rem) received per year.
- Subject with history of IV drug use which would prevent venous access for PET tracer injection.
- Severe motor problems that prevent the subject from lying still for PET imaging.
- Subject who has chronic pain for any reason (e.g., as the result of rheumatoid arthritis).
- Subject who has an MRI scan deemed to be structurally abnormal by the investigator and thus precluding proper identification of the regions of interest (ROIs) (e.g., cortical atrophy). The MRI scan for an individual subject may be omitted if the required anatomical MRI scan for this subject is on file and was performed within approximately 6 months prior to dosing, as part of participation in an approved Yale Protocol.
- Subjects who has current, past or anticipated exposure to radiation in the work place.
Trial locations and contacts
1 site in 1 country.
About this study
Official title: A Phase 1 11β-Hydroxysteroid Dehydrogenase 1 Enzyme Occupancy Study Using a Positron Emission Tomography Ligand [11C]AS2471907- ([11C]MOZAT) and Following Single Oral Dose Administration of ASP3662 in Healthy Male Adult Subjects
The purpose of this study is to evaluate a novel PET tracer ([11C]AS2471907), and to use [11C]AS2471907 to assess the level and time-course of enzyme occupancy in the human brain prior to and following single oral dose administration of ASP3662.
Read the detailed description
This is a two-part study where Part 1 will assess the test/retest variability of the ligand ([11C]AS2471907). Part 2 will assess the level and time-course of enzyme occupancy following ASP3662 dosing. Subjects will be confined to the clinic for up to 2 days.
- Being tested
- [11C]AS2471907, Positron Emission Tomography (PET), ASP3662
- Keywords
- [11C]AS2471907, ASP3662, Positron Emission Tomography (PET), Brain enzyme occupancy
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
[11C]AS2471907Other
Also called Up to 4 single dose IV administrations (≤ 10 mL infused over approximately 1 minute) are planned, totaling less than 100 μg.
intravenous radiotracer
Positron Emission Tomography (PET)Radiation
Imaging scanning procedure
ASP3662Drug
oral
| Study group | Role | What they receive |
|---|---|---|
| [11C]AS2471907 administration (Part 1) | Experimental | Up to 4 single dose IV administrations (≤ 10 mL infused over approximately 1 minute) are planned, totaling less than 100 μg. Receives: Other: [11C]AS2471907; Radiation: Positron Emission Tomography (PET) |
| ASP3662 administration (Part 2) | Experimental | The dose levels used in part 2 will depend on the ongoing analysis of EO (enzyme occupancy) from previously dosed subjects. Receives: Radiation: Positron Emission Tomography (PET); Drug: ASP3662 |
What is being measured
The primary outcome is the main question the study is designed to answer.
Positron Emission Tomography measure: volume of distribution
Measured: Day 1 and 2 (Part 1 and Part 2)
Positron Emission Tomography measure: brain time-activity curves
Measured: Day 1 and 2 (Part 1 and Part 2)
Positron Emission Tomography measure: enzyme occupancy
Measured: Day 1 and 2 (Part 1 and Part 2)
Positron Emission Tomography measure: binding potentials
Measured: Day 1 and 2 (Part 1 and Part 2)
Pharmacokinetic parameter of ASP3662 and its metabolite (AS2570469): AUClast (Part 2 only)
Area under the plasma concentration - time curve from time zero to time of last measurable concentration (AUClast)
Measured: Day 1 and 2
Pharmacokinetic parameter of ASP3662 and its metabolite (AS2570469): Cmax (Part 2 only)
Maximum concentration (Cmax)
Measured: Day 1 and 2
Pharmacokinetic parameter of ASP3662 and its metabolite (AS2570469): tmax (Part 2 only)
Time to attain Cmax (tmax)
Measured: Day 1 and 2
Safety as assessed by laboratory tests, 12-lead electrocardiograms, vital signs, adverse events, physical exams, neurological exams and Columbia Suicide Severity Rating Scale
Measured: up to 9 days (Part 1 and Part 2)
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted18 Jul 2014 (estimated)
- Study startApr 2014
- Primary completionMay 2016
- Study completionMay 2016
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Other trials for Pharmacokinetics of ASP3662Studies of the same condition, open and under way.
- More trials run by Astellas Pharma Global Development, Inc.The sponsor's other registered studies.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Basic science
- Allocation
- Non-randomised
- Intervention model
- Single group
- Masking
- None (open label)
- Enrolment
- 18 participants (actual)
Sponsor and investigators
- Lead sponsor
- Astellas Pharma Global Development, Inc.
- Sponsor type
- Industry (pharma, biotech, devices)
- Collaborators
- Yale University
- Responsible party
- Sponsor
- Investigators
- Senior Medical Director, Study director, Astellas Pharma Global Development, Inc.
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT02194491
- Sponsor's protocol ID
- 3662-CL-0011
- Status last verified
- Jun 2016
- First submitted
- 16 Jul 2014
- Last updated
- 28 Jun 2016
- Results posted
- No
- Data monitoring committee
- No
- Individual data sharing
- Undecided
Study at a glance
From the registry record, last updated by the sponsor on 28 Jun 2016. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- A Phase 1 11β-Hydroxysteroid Dehydrogenase 1 Enzyme Occupancy Study Using a Positron Emission Tomography Ligand [11C]AS2471907- ([11C]MOZAT) and Following Single Oral Dose Administration of ASP3662 in Healthy Male Adult Subjects
- ClinicalTrials.gov ID
- NCT02194491
- Acronym / sponsor ID
- 3662-CL-0011
- Keywords
- [11C]AS2471907, ASP3662, Positron Emission Tomography (PET), Brain enzyme occupancy
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 18 participants (actual)
- Lead sponsor
- Astellas Pharma Global Development, Inc.Industry (pharma, biotech, devices)
- Collaborators
- Yale University
- Study start
- Apr 2014
- Primary completion
- May 2016 (actual)
- Study completion
- May 2016 (actual)
- First posted
- 18 Jul 2014 (estimated)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
The purpose of this study is to evaluate a novel PET tracer ([11C]AS2471907), and to use [11C]AS2471907 to assess the level and time-course of enzyme occupancy in the human brain prior to and following single oral dose administration of ASP3662.
Detailed description
This is a two-part study where Part 1 will assess the test/retest variability of the ligand ([11C]AS2471907). Part 2 will assess the level and time-course of enzyme occupancy following ASP3662 dosing. Subjects will be confined to the clinic for up to 2 days.
Study design
- Primary purpose
- Basic science
- Allocation
- Non-randomised
- Intervention model
- Single group
- Masking
- None (open label)
- Number of arms
- 2
| Arm | Type | Receives |
|---|---|---|
| [11C]AS2471907 administration (Part 1) | Experimental | Other: [11C]AS2471907, Radiation: Positron Emission Tomography (PET)Up to 4 single dose IV administrations (≤ 10 mL infused over approximately 1 minute) are planned, totaling less than 100 μg. |
| ASP3662 administration (Part 2) | Experimental | Radiation: Positron Emission Tomography (PET), Drug: ASP3662The dose levels used in part 2 will depend on the ongoing analysis of EO (enzyme occupancy) from previously dosed subjects. |
Who may qualify
- Ages
- 18 to 55 years
- Sex
- Male only
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (5 listed)
- Subject is of non-Asian descent.
- Subject has a body mass index (BMI) range of 18.5 to 32 kg/m2, inclusive and weighs at least 50 kg at screening.
- Subject and his female spouse/partner who is of childbearing potential must be using highly effective contraception1 consisting of 2 forms of birth control (at least one of which must be a barrier method) starting at screening and continuing throughout the study period and for 90 days after final study drug administration.
- Subject must not donate sperm starting at screening, throughout the study period and for at least 90 days after final study drug administration.
- Subject agrees not to participate in another investigational study while on study treatment.
Key exclusion criteria (31 listed)
- Subject has a known or suspected hypersensitivity to ASP3662, [11C]AS2471907 or intolerance of drugs with the same mechanism of action as ASP3662.
- Subject has an allergy to topical anesthetics, such as, lidocaine (if used for catheter placement).
- Subject has previously participated in a clinical study with ASP3662 or part 1 of the current study.
- Subject has any of the liver enzymes (aspartate aminotransferase [AST], alanine transaminase [ALT], alkaline phosphatase [ALP], gamma-glutamyl transferase [GGT]) or total bilirubin (TBIL) above the upper limit of normal (ULN). If any liver enzyme is > 1 x ULN but ≤ 1.5 x ULN, the assessment may be repeated once during the screening period or on check-in. If the repeated assessment is above the ULN, it is exclusionary. If the initial value is > 1.5 x ULN, it cannot be repeated and is exclusionary.
- Subject has any clinically significant history of allergic conditions.
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| [11C]AS2471907Also: Up to 4 single dose IV administrations (≤ 10 mL infused over approximately 1 minute) are planned, totaling less than 100 μg.intravenous radiotracer | Other | [11C]AS2471907 administration (Part 1) |
| Positron Emission Tomography (PET)Imaging scanning procedure | Radiation | ASP3662 administration (Part 2), [11C]AS2471907 administration (Part 1) |
| ASP3662oral | Drug | ASP3662 administration (Part 2) |
Primary outcome
Positron Emission Tomography measure: volume of distribution
Time frame: Day 1 and 2 (Part 1 and Part 2)
Positron Emission Tomography measure: brain time-activity curves
Time frame: Day 1 and 2 (Part 1 and Part 2)
Positron Emission Tomography measure: enzyme occupancy
Time frame: Day 1 and 2 (Part 1 and Part 2)
Positron Emission Tomography measure: binding potentials
Time frame: Day 1 and 2 (Part 1 and Part 2)
Pharmacokinetic parameter of ASP3662 and its metabolite (AS2570469): AUClast (Part 2 only)
Time frame: Day 1 and 2
Area under the plasma concentration - time curve from time zero to time of last measurable concentration (AUClast)
Pharmacokinetic parameter of ASP3662 and its metabolite (AS2570469): Cmax (Part 2 only)
Time frame: Day 1 and 2
Maximum concentration (Cmax)
Pharmacokinetic parameter of ASP3662 and its metabolite (AS2570469): tmax (Part 2 only)
Time frame: Day 1 and 2
Time to attain Cmax (tmax)
Safety as assessed by laboratory tests, 12-lead electrocardiograms, vital signs, adverse events, physical exams, neurological exams and Columbia Suicide Severity Rating Scale
Time frame: up to 9 days (Part 1 and Part 2)
Results and safety
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 28 Jun 2016.
- Individual participant dataSharing planned: Undecided
Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
Senior Medical Director study director
Astellas Pharma Global Development, Inc.
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing [11C]AS2471907, Positron Emission Tomography (PET) and ASP3662 in people with Pharmacokinetics of ASP3662 and Displacement of Radiotracer, run by Astellas Pharma Global Development, Inc. at 1 site in United States.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 5 inclusion and 31 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 28 Jun 2016. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 1 site in United States. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Positron Emission Tomography measure: volume of distribution (time frame: Day 1 and 2 (Part 1 and Part 2)). The study lists 8 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 28 Jun 2016.