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| ID | Type | Description | Link |
|---|---|---|---|
| U1111-1165-3362 | Registry Identifier | WHO | |
| 2012-004576-18 | EudraCT Number |
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The purpose of this study is to estimate phosphodiesterase 10A (PDE10A) occupancy in brain following a single dose of TAK-063.
The drug being tested in this study is called TAK-063. TAK-063 is was tested to estimate phosphodiesterase10A (PDE10A) occupancy in the brain following a single dose of TAK-063. This study used positron emission tomography (PET) scans to look at changes in the volume of tissue distribution before and after TAK-063 administration to calculate PDE10A occupancy in the brain.
The study enrolled 13 participants. Participants were assigned to a treatment group based on an enrollment schedule. The first 4 participants were assigned to the Pilot Cohort and received one dose of TAK-063 30 mg or 1000 mg tablets. The remaining participants were enrolled into the Main Cohort and received one dose of TAK-063 at 3, 10, 30 or 100 mg. Participants in both cohorts also received 3 separate intravenous infusions of [^11C]T-773 <8 μg; 400MBq ± 10% followed by a PET scan.
This single-centre trial was conducted in Sweden. The overall time to participate in this study was 46 days. Participants made 3 visits to the clinic, including one 3-day period of confinement to the clinic. Participants were contacted by phone on Day 16 for follow-up safety assessments.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Pilot Cohort: [^11C]T-773 + TAK-063 | Experimental | [^11C]T-773 <8 μg; 400MBq ± 10%, intravenous (IV), once on Days 1 and 2 prior to PET scans and TAK-063 30 mg or 1000 mg, tablets, orally, once on Day 2 and after PET scan #2 and prior to PET scan #3 and [^11C]T-773 IV after TAK-063 and prior to PET scan #3 on Day 2. |
|
| Main Cohort: TAK-063 + [^11C]T-773 | Experimental | TAK-063 3 to 100 mg, tablets, orally, once, on Day 1, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2 . |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| TAK-063 | Drug | TAK-063 tablets |
|
| Measure | Description | Time Frame |
|---|---|---|
| Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 3 Hours Following a Single Dose of TAK-063 | Volume of tissue distribution (Vt) values will be estimated by several quantitative methods for each positron emission tomography (PET) scan. Based on the change in Vt before and after TAK-063 administration, PDE10A occupancy will be calculated. PET scan #2 in the Pilot Cohort and PET scan #1 in the Main Cohort will be used as a baseline for the occupancy calculation. Occupancy is reported for putamen only. | 3 hours post-dose |
| Measure | Description | Time Frame |
|---|---|---|
| Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 23 Hours Following a Single Dose of TAK-063 | Volume of tissue distribution (Vt) values will be estimated by several quantitative methods for each positron emission tomography (PET) scan. Based on the change in Vt before and after TAK-063 administration, PDE10A occupancy will be calculated. PET scan #2 in the Pilot Cohort and PET scan #1 in the Main Cohort will be used as a baseline for the occupancy calculation. Data was not available for participants in the pilot cohort. Occupancy is reported for putamen only. |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Medical Director Clinical Science | Takeda (Note: This product was divested to Axsome in 2026) | Study Director |
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Healthy Volunteers received 1 of 5 treatments: 11C T-773,Tak-063 3 mg, Tak-063 10 mg, Tak-063 30 mg, Tak-063 100 mg or Tak-063 1000 mg.
Participants took part in the study at 1 investigative site in Sweden from 13 August 2013 to 12 March 2014.
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| ID | Title | Description |
|---|---|---|
| FG000 | [^11C]T-773 Only | [^11C]T-773 <8 μg; 400MBq ± 10%, intravenous (IV), once on Days 1 and 2 only. |
| FG001 | TAK-063 3 mg + [^11C]T-773 | TAK-063 3 mg, tablets, orally, once, on Day 1, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2. |
| FG002 | TAK-063 10 mg + [^11C]T-773 | TAK-063 10 mg, tablets, orally, once, on Day 1, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2. |
| FG003 | TAK-063 30 mg + [^11C]T-773 | For main cohort, TAK-063 30 mg, tablets, orally, once, on Day 1, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2. For pilot cohort, TAK-063 30 mg, tablets, orally, once on Day 2, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, once on Day 1 (before and after administration of TAK-063) and twice on Day 2. |
| FG004 | TAK-063 100 mg + [^11C]T-773 | TAK-063 100 mg, tablets, orally, once, on Day 1, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2. |
| FG005 | TAK-063 1000 mg + [^11C]T-773 | TAK-063 1000 mg, tablets, orally, once, on Day 2, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, once on Day 1 and twice on Day 2 (before and after administration of TAK-063). |
| Title | Milestones | Reasons Not Completed | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study |
|
|
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| ID | Title | Description |
|---|---|---|
| BG000 | [^11C]T-773 | [^11C]T-773 <8 μg; 400MBq ± 10%, intravenous (IV), once on Days 1 and 2 only. |
| BG001 | TAK-063 3 mg + [^11C]T-773 | TAK-063 3 mg, tablets, orally, once, on Day 1, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2. |
| Units | Counts |
|---|---|
| Participants |
|
| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes |
|---|---|---|---|---|---|---|---|---|---|
| Age, Continuous | Mean |
| Type | Title | Description | Population Description | Reporting Status | Anticipated Posting Date | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Time Frame | Units Analyzed | Denominator Units Selected | Arm/Group Information | Denominators | Classes | Analyses | |||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Primary | Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 3 Hours Following a Single Dose of TAK-063 | Volume of tissue distribution (Vt) values will be estimated by several quantitative methods for each positron emission tomography (PET) scan. Based on the change in Vt before and after TAK-063 administration, PDE10A occupancy will be calculated. PET scan #2 in the Pilot Cohort and PET scan #1 in the Main Cohort will be used as a baseline for the occupancy calculation. Occupancy is reported for putamen only. | Pharmacodynamic Analysis Set includes all participants with data available for pharmacodynamic analysis.. | Posted | Mean | Standard Deviation | Percent | 3 hours post-dose |
|
First dose of study drug to 30 days after last dose of study drug (up to 46 days)
At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
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| ID | Title | Description | Deaths (Affected) | Deaths (At Risk) | Serious Events (Affected) | Serious Events (At Risk) | Other Events (Affected) | Other Events (At Risk) |
|---|---|---|---|---|---|---|---|---|
| EG000 | [^11C]T-773 | [^11C]T-773 <8 μg; 400MBq ± 10%, intravenous (IV), once on Days 1 and 2 only. |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Haematoma | Vascular disorders | MedDRA 16.0 |
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| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Medical Director, Clinical Science | Takeda (Note: This product was divested to Axsome in 2026) | +1-877-825-3327 | clinicaltrialregistry@tpna.com |
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| ID | Term |
|---|---|
| C000594749 | 1-(2-fluoro-4-(1H-pyrazol-1-yl)phenyl)-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one |
| C000601031 | T-773 compound |
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| [^11C]T-773 | Drug | [^11C]T-773 IV solution |
|
| 23 hours post-dose |
| Percentage of Participants Who Experienced at Least 1 Treatment-Emergent Adverse Event | An adverse event (AE) is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (eg, a clinically significant abnormal laboratory finding), symptom, or disease temporally associated with the use of a drug, whether or not it is considered related to the drug. A treatment-emergent adverse event is defined as an adverse event with an onset that occurs after receiving study drug. | First dose of study drug to 30 days after last dose of study drug (up to 46 days) |
| Percentage of Participants With Markedly Abnormal Safety Laboratory Findings | The percentage of participants with any markedly abnormal standard safety laboratory values was collected throughout study. | From Day 1 to Day 16 |
| Percentage of Participants With Markedly Abnormal Vital Sign Measurements | The percentage of participants with any markedly abnormal standard vital sign measurements was collected throughout study. BL=baseline. bpm=beats per minute. | From Day 1 to Day 16 |
| Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | The percentage of participants with any markedly abnormal standard 12-lead ECG measurements. QTc - Bazett's Interval (msec) is ≥500 msec OR ≥30 msec change from Baseline and ≥450 msec | From Day 1 to Day 16 |
| Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-I | Maximum observed plasma concentration (Cmax) is the peak plasma concentration of a drug after administration, obtained directly from the plasma concentration-time curve. | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. |
| Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-I | Time to reach the maximum plasma concentration (Cmax), equal to time (hours) to Cmax. | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. |
| AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-063 and TAK-063 Metabolite M-I | (AUC(0-tlqc) is a measure of total plasma exposure to the drug from Time 0 to Time of the Last Quantifiable Concentration (AUC[0-tlqc]). | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. |
| AUC(0-24): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-I | AUC(0-24) is a measure of total plasma exposure to the drug from Time 0 to 24 hours post-dose. | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. |
| Average Plasma Concentration on Day 1 (Cavg) for TAK-063 and TAK-063 Metabolite M-I | Cavg is the average plasma concentration on Day 1, calculated as AUC(0-24)/24. | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. |
| CL/F: Oral Clearance of TAK-063 | CL/F is apparent clearance of the drug from the plasma, calculated as the drug dose divided by area under the curve from time 0 to 24 hours post-dose, after multiple dosing (at steady state). | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. |
| Ratio of TAK-063 Metabolite Cmax to TAK-063 Cmax | Cmax Ratio is the ratio of Cmax values of the metabolite compared to the parent calculated by dividing Cmax values of metabolite M-I with those of the parent drug TAK-063. | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. |
| Ratio of TAK-063 Metabolite M-I AUC( 0-24) to TAK-063 AUC (0-24) | AUC Ratio is the ratio of AUC values of the metabolite compared to the parent calculated by dividing AUC values of metabolite M-I with those of the parent drug TAK-063. | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. |
| AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | AUC values of TAK-063 and TAK-063 metabolite M-I during the PET scan at approximately 3 hours post TAK-063 administration. | 3 hours post-dose |
| Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | Cavg values of TAK-063 and TAK-063 metabolite M-I during the PET scan at approximately 3 hours post TAK-063 administration. | 3 hours post-dose |
| AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | AUC values of TAK-063 and TAK-063 metabolite M-I during the PET scan at approximately 23 hours post TAK-063 administration. Data was not available for participants in the pilot cohort. | 23 hours post-dose |
| Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | Cavg values of TAK-063 and TAK-063 metabolite M-I during the PET scan at approximately 23 hours post TAK-063 administration. Data is not available for the pilot cohort. | 23 hours post-dose |
| BG002 | TAK-063 10 mg + [^11C]T-773 | TAK-063 10 mg, tablets, orally, once, on Day 1, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2. |
| BG003 | TAK-063 30 mg + [^11C]T-773 | For main cohort, TAK-063 30 mg, tablets, orally, once, on Day 1, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2. For pilot cohort, TAK-063 30 mg, tablets, orally, once on Day 2, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, once on Day 1 (before and after administration of TAK-063) and twice on Day 2. |
| BG004 | TAK-063 100 mg + [^11C]T-773 | TAK-063 100 mg, tablets, orally, once, on Day 1, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2. |
| BG005 | TAK-063 1000 mg + [^11C]T-773 | TAK-063 1000 mg, tablets, orally, once, on Day 2, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, once on Day 1 and twice on Day 2 (before and after administration of TAK-063). |
| BG006 | Total | Total of all reporting groups |
| years |
|
| Sex: Female, Male | Count of Participants | Participants |
|
| Race/Ethnicity, Customized | Number | participants |
|
| Region of Enrollment | Number | participants |
|
| Height | Mean | Standard Deviation | cm |
|
| Weight | Mean | Standard Deviation | kg |
|
| Body Mass Index (BMI) | Mean | Standard Deviation | kg/m^2 |
|
| Smoking Classification | Number | participants |
|
| OG001 | TAK-063 10 mg | TAK-063 10 mg, tablets, orally, once, on Day 1, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2. |
| OG002 | TAK-063 30 mg + [^11C]T-773 | For main cohort, TAK-063 30 mg, tablets, orally, once, on Day 1, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2. For pilot cohort, TAK-063 30 mg, tablets, orally, once on Day 2, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, once on Day 1 (before and after administration of TAK-063) and twice on Day 2. |
| OG003 | TAK-063 100 mg + [^11C]T-773 | TAK-063 100 mg, tablets, orally, once, on Day 1, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2. |
| OG004 | TAK-063 1000 mg + [^11C]T-773 | TAK-063 1000 mg, tablets, orally, once, on Day 2, and [^11C]T-773 <8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, once on Day 1 and twice on Day 2 (before and after administration of TAK-063). |
|
|
| Secondary | Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 23 Hours Following a Single Dose of TAK-063 | Volume of tissue distribution (Vt) values will be estimated by several quantitative methods for each positron emission tomography (PET) scan. Based on the change in Vt before and after TAK-063 administration, PDE10A occupancy will be calculated. PET scan #2 in the Pilot Cohort and PET scan #1 in the Main Cohort will be used as a baseline for the occupancy calculation. Data was not available for participants in the pilot cohort. Occupancy is reported for putamen only. | Pharmacodynamic Analysis Set includes all participants with data available for pharmacodynamic analysis. | Posted | Mean | Standard Deviation | Percent | 23 hours post-dose |
|
|
|
| Secondary | Percentage of Participants Who Experienced at Least 1 Treatment-Emergent Adverse Event | An adverse event (AE) is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (eg, a clinically significant abnormal laboratory finding), symptom, or disease temporally associated with the use of a drug, whether or not it is considered related to the drug. A treatment-emergent adverse event is defined as an adverse event with an onset that occurs after receiving study drug. | Safety analysis set included all participants who received at least one dose of study drug. | Posted | Number | percentage of participants | First dose of study drug to 30 days after last dose of study drug (up to 46 days) |
|
|
|
| Secondary | Percentage of Participants With Markedly Abnormal Safety Laboratory Findings | The percentage of participants with any markedly abnormal standard safety laboratory values was collected throughout study. | Safety analysis set included all participants who received at least one dose of study drug. | Posted | Number | percentage of participants | From Day 1 to Day 16 |
|
|
|
| Secondary | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | The percentage of participants with any markedly abnormal standard vital sign measurements was collected throughout study. BL=baseline. bpm=beats per minute. | Safety analysis set included all participants who received at least one dose of study drug. | Posted | Number | percentage of participants | From Day 1 to Day 16 |
|
|
|
| Secondary | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | The percentage of participants with any markedly abnormal standard 12-lead ECG measurements. QTc - Bazett's Interval (msec) is ≥500 msec OR ≥30 msec change from Baseline and ≥450 msec | Safety analysis set included all participants who received at least one dose of study drug. | Posted | Number | percentage of participants | From Day 1 to Day 16 |
|
|
|
| Secondary | Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-I | Maximum observed plasma concentration (Cmax) is the peak plasma concentration of a drug after administration, obtained directly from the plasma concentration-time curve. | Pharmacokinetic Analysis Set | Posted | Mean | Standard Deviation | ng/mL | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. |
|
|
|
| Secondary | Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-I | Time to reach the maximum plasma concentration (Cmax), equal to time (hours) to Cmax. | Pharmacokinetic Analysis Set | Posted | Mean | Standard Deviation | hour | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. |
|
|
|
| Secondary | AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-063 and TAK-063 Metabolite M-I | (AUC(0-tlqc) is a measure of total plasma exposure to the drug from Time 0 to Time of the Last Quantifiable Concentration (AUC[0-tlqc]). | Pharmacokinetic Analysis Set | Posted | Mean | Standard Deviation | ng*hr/mL | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. |
|
|
|
| Secondary | AUC(0-24): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-I | AUC(0-24) is a measure of total plasma exposure to the drug from Time 0 to 24 hours post-dose. | Pharmacokinetic Analysis Set | Posted | Mean | Standard Deviation | ng*hr/mL | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. |
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| Secondary | Average Plasma Concentration on Day 1 (Cavg) for TAK-063 and TAK-063 Metabolite M-I | Cavg is the average plasma concentration on Day 1, calculated as AUC(0-24)/24. | Pharmacokinetic Analysis Set | Posted | Mean | Standard Deviation | ng/mL | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. |
|
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| Secondary | CL/F: Oral Clearance of TAK-063 | CL/F is apparent clearance of the drug from the plasma, calculated as the drug dose divided by area under the curve from time 0 to 24 hours post-dose, after multiple dosing (at steady state). | Pharmacokinetic Analysis Set | Posted | Mean | Standard Deviation | liter/hour | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. |
|
|
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| Secondary | Ratio of TAK-063 Metabolite Cmax to TAK-063 Cmax | Cmax Ratio is the ratio of Cmax values of the metabolite compared to the parent calculated by dividing Cmax values of metabolite M-I with those of the parent drug TAK-063. | Pharmacokinetic Analysis Set | Posted | Mean | Standard Deviation | ratio | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. |
|
|
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| Secondary | Ratio of TAK-063 Metabolite M-I AUC( 0-24) to TAK-063 AUC (0-24) | AUC Ratio is the ratio of AUC values of the metabolite compared to the parent calculated by dividing AUC values of metabolite M-I with those of the parent drug TAK-063. | Pharmacokinetic Analysis Set | Posted | Mean | Standard Deviation | ratio | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. |
|
|
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| Secondary | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | AUC values of TAK-063 and TAK-063 metabolite M-I during the PET scan at approximately 3 hours post TAK-063 administration. | Pharmacokinetic Analysis Set | Posted | Mean | Standard Deviation | ng*hr/mL | 3 hours post-dose |
|
|
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| Secondary | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | Cavg values of TAK-063 and TAK-063 metabolite M-I during the PET scan at approximately 3 hours post TAK-063 administration. | Pharmacokinetic Analysis Set | Posted | Mean | Standard Deviation | ng/mL | 3 hours post-dose |
|
|
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| Secondary | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | AUC values of TAK-063 and TAK-063 metabolite M-I during the PET scan at approximately 23 hours post TAK-063 administration. Data was not available for participants in the pilot cohort. | Pharmacokinetic Analysis Set | Posted | Mean | Standard Deviation | ng*hr/mL | 23 hours post-dose |
|
|
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| Secondary | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | Cavg values of TAK-063 and TAK-063 metabolite M-I during the PET scan at approximately 23 hours post TAK-063 administration. Data is not available for the pilot cohort. | Pharmacokinetic Analysis Set | Posted | Mean | Standard Deviation | ng/mL | 23 hours post-dose |
|
|
|
| 0 |
| 13 |
| 5 |
| 13 |
| EG001 | TAK-063 | TAK-063 3 to 1000 mg, tablets, orally, once, on Day 1. | 0 | 12 | 9 | 12 |
| Anxiety | Psychiatric disorders | MedDRA 16.0 |
|
| Headache | Nervous system disorders | MedDRA 16.0 |
|
| Infusion site pain | General disorders | MedDRA 16.0 |
|
| Nausea | Gastrointestinal disorders | MedDRA 16.0 |
|
| Tremor | Nervous system disorders | MedDRA 16.0 |
|
| Catheter site pain | General disorders | MedDRA 16.0 |
|
| Chest pain | General disorders | MedDRA 16.0 |
|
| Claustrophobia | Psychiatric disorders | MedDRA 16.0 |
|
| Dizziness | Nervous system disorders | MedDRA 16.0 |
|
| Fatigue | General disorders | MedDRA 16.0 |
|
| Infusion site erythema | General disorders | MedDRA 16.0 |
|
| Nasopharyngitis | Infections and infestations | MedDRA 16.0 |
|
Research Organization shall not publish any articles or papers nor make any presentations, nor assist any other person in publishing any articles or papers or in making any presentations relating or referring to the Study or any results, data or insights from or any data, information or materials obtained or generated in the performance of its obligations without the prior written consent of Takeda, which consent may be granted or withheld in Takeda's sole discretion.
| During tx - <Lower Cut-off |
|
| During tx - Change Relative to BL Upper Criteria |
|
| During tx - Change Relative to BL Lower Criteria |
|
| During tx - Overall |
|
| Pulse (bpm) - >120 bpm |
|
| Pulse (bpm) - <50 bpm |
|
| Pulse (bpm) - Increase of >30 bpm |
|
| Pulse (bpm) - Decrease of >30 bpm |
|
| Pulse (bpm) - Overall |
|
| Systolic Blood Pressure (mmHg) - >180 mmHg |
|
| Systolic Blood Pressure (mmHg) - <85 mmHg |
|
| Systolic Blood Pressure - Increase of >40 mmHg |
|
| Systolic Blood Pressure - Decrease of >40 mmHg |
|
| Systolic Blood Pressure (mmHg) - Overall |
|
| Diastolic Blood Pressure (mmHg) - >110 mmHg |
|
| Diastolic Blood Pressure (mmHg) - <50 mmHg |
|
| Diastolic BP (mmHg) - Increase of >20 mmHg |
|
| Diastolic BP (mmHg) - Decrease of >20 mmHg |
|
| Diastolic Blood Pressure (mmHg) - Overall |
|
| Temperature (Degree C) - >37.7 C |
|
| Temperature (Degree C) - <35.6 C |
|
| Temperature (Degree C) - Overall |
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| Heart Rate (bpm) - Overall |
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| RR Interval (msec) - ≥1440 msec |
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| RR Interval (msec) - ≤600 msec |
|
| RR Interval (msec) - Overall |
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| PR Interval (msec) - ≥200 msec |
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| PR Interval (msec) - ≤80 msec |
|
| PR Interval (msec) - Overall |
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| QRS Interval (msec) - ≥180 msec |
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| QRS Interval (msec) - ≤80 msec |
|
| QRS Interval (msec) - Overall |
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| QT Interval (msec) - ≥460 msec |
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| QT Interval (msec) - <280 msec |
|
| QT Interval (msec) - Overall |
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| QTc - Bazett's Interval (msec) - Overall |
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| QTc - Fredericia's Interval (msec) - Overall |
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| TAK-063 Metabolite M-I |
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| TAK-063 Metabolite M-I |
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| TAK-063 Metabolite M-I |
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| TAK-063 Metabolite M-I |
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| TAK-063 Metabolite M-I |
|
| TAK-063 Metabolite M-I |
|
| TAK-063 Metabolite M-I |
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| TAK-063 Metabolite M-I |
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| TAK-063 Metabolite M- |
|