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| ID | Type | Description | Link |
|---|---|---|---|
| 2013-005018-36 | EudraCT Number |
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The purpose of this study is to evaluate the safety, tolerability and pharmacokinetics (PK) of single ascending oral doses of ASP3700 in healthy male subjects. This study will also explore the effect of itraconazole (another drug) on the PK of ASP3700, as well as to evaluate the safety and tolerability of ASP3700 alone and in combination with itraconazole in healthy male subjects.
This study consists of 2 parts: Part 1 is a single ascending dose study where subjects will receive either ASP3700 or matching placebo; Part 2 is a drug-drug interaction (DDI) open-label, crossover study comprised of 1 sequence with 2 investigational periods where subjects will receive ASP3700 alone and in combination with itraconazole.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| ASP3700 single ascending dose cohort | Experimental | Part 1 |
|
| Placebo single ascending dose cohort | Placebo Comparator | Part 1 |
|
| ASP3700 alone | Experimental | Part 2 |
|
| ASP3700 and itraconazole | Active Comparator | Part 2 |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| ASP3700 | Drug | oral |
|
| Measure | Description | Time Frame |
|---|---|---|
| Safety as assessed by adverse events (Part 1) | up to end of study visit (up to 16 days) | |
| Safety as assessed by vital signs (Part 1) | up to end of study visit (up to 16 days) | |
| Safety as assessed by laboratory tests (Part 1) | Laboratory tests includes the measurement of sex-hormone related biomarkers and exploratory renal biomarkers. | up to end of study visit (up to 16 days) |
| Safety as assessed by electrocardiogram (ECG) measurements (Part 1) | ECG measurements include routine 12-lead ECG, continuous cardiac monitoring (Holter ECG) and real-time cardiac monitoring (ECG telemetry) | up to end of study visit (up to 16 days) |
| Safety as assessed by Bond and Lader VAS (Part 1) | visual analogue scale (VAS) | Up to Day 2 |
| Safety as assessed by C-SSRS (Part 1) | Columbia - Suicide Severity Rating Scale (C-SSRS) | Up to end of study visit (up to 16 days) |
| Safety as assessed by ARCI-49 (Part 1) | Addiction Research Center Inventory (ARCI)-49 (49-item) | Up to Day 2 |
| Pharmacokinetic parameter of itraconazole (plasma): Ctrough (Part 2) | Concentration immediately prior to dosing at multiple dosing |
| Measure | Description | Time Frame |
|---|---|---|
| Composite of pharmacokinetics of ASP3700: AUCinf, AUCinf(%extrap), AUClast, Cmax, CL/F, λz, MRT, tlag, tmax, t½, Vz/F (plasma) (Part 1) | up to Day 7 | |
| Title: Composite of pharmacokinetics of ASP3700: Aelast, Aeinf, Aelast%, Aeinf%, CLR (urine) (Part 1) |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Medical Director | Astellas Pharma Europe B.V. | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Parexel Early Phase Clinical Unit | Harrow | HA1 3UJ | United Kingdom |
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| ID | Term |
|---|---|
| D017964 | Itraconazole |
| ID | Term |
|---|---|
| D014230 | Triazoles |
| D001393 | Azoles |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
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| itraconazole | Drug | oral |
|
| Placebo | Drug | oral |
|
| Days 3-13 |
| Pharmacokinetic parameter of ASP3700 with and without itraconazole (plasma): AUCinf (Part 2) | Area under the concentration-time curve from time of dosing extrapolated to time infinity (AUCinf) | Days 1-7 (period 1) and Days 1-13 (period 2) |
| Pharmacokinetic parameter of ASP3700 with and without itraconazole (plasma): AUCinf (%extrap) (Part 2) | Percentage of AUCinf due to extrapolation from tlast to time infinity (AUCinf [%extrap]) | Days 1-7 (period 1) and Days 1-13 (period 2) |
| Pharmacokinetic parameter of ASP3700 with and without itraconazole (plasma): AUClast (Part 2) | Area under the concentration-time curve from the time of dosing to the last measurable concentration (AUClast) | Days 1-7 (period 1) and Days 1-13 (period 2) |
| Pharmacokinetic parameter of ASP3700 with and without itraconazole (plasma): Cmax (Part 2) | Maximum concentration (Cmax) | Days 1-7 (period 1) and Days 1-13 (period 2) |
| Pharmacokinetic parameter of ASP3700 with and without itraconazole (plasma):λz (Part 2) | Terminal elimination rate constant (λz) | Days 1-7 (period 1) and Days 1-13 (period 2) |
| Pharmacokinetic parameter of ASP3700 with and without itraconazole (plasma): MRT (Part 2) | Mean residence time (MRT) | Days 1-7 (period 1) and Days 1-13 (period 2) |
| Pharmacokinetic parameter of ASP3700 with and without itraconazole (plasma): tlag (Part 2) | Time prior to the time corresponding to the first measurable (nonzero) concentration (tlag) | Day 1 (period 1 and 2) |
| Pharmacokinetic parameter of ASP3700 with and without itraconazole (plasma): tmax (Part 2) | Time of maximum concentration (tmax) | Days 1-7 (period 1) and Days 1-13 (period 2) |
| Pharmacokinetic parameter of ASP3700 with and without itraconazole (plasma): t1/2 (Part 2) | Terminal elimination half-life (t1/2) | Days 1-7 (period 1) and Days 1-13 (period 2) |
| Pharmacokinetic parameter of ASP3700 with and without itraconazole (plasma): Vz/F (Part 2) | Apparent volume of distribution during the terminal elimination phase after extravascular dosing (Vz/F) | Days 1-7 (period 1) and Days 1-13 (period 2) |
| Pharmacokinetic parameter of ASP3700 with and without itraconazole (urine): Aelast (Part 2) | Cumulative amount of study drug excreted into urine from time of dosing up to the collection time of the last measurable concentration (Aelast) | Days 1-7 (period 1) and Days 1-13 (period 2) |
| Pharmacokinetic parameter of ASP3700 with and without itraconazole (urine): Aeinf (Part 2) | Cumulative amount of study drug excreted into urine from time of dosing extrapolated to time infinity (Aeinf) | Days 1-7 (period 1) and Days 1-13 (period 2) |
| Pharmacokinetic parameter of ASP3700 with and without itraconazole (urine): Aelast% (Part 2) | Percentage of study drug excreted into urine from the time of dosing up to the collection time of the last measurable concentration (Aelast%) | Days 1-7 (period 1) and Days 1-13 (period 2) |
| Pharmacokinetic parameter of ASP3700 with and without itraconazole (urine): Aeinf% (Part 2) | Percentage of study drug excreted into urine from time of dosing extrapolated to time infinity (Aeinf%) | Days 1-7 (period 1) and Days 1-13 (period 2) |
| Pharmacokinetic parameter of ASP3700 with and without itraconazole (urine): CLR (Part 2) | Renal clearance (CLR) | Days 1-7 (period 1) and Days 1-13 (period 2) |
| Safety as assessed by orthostatic evaluation (or blood pressure change in orthostatic challenge test) (Part 1) | Up to Day 7 |
| up to Day 7 |
| Safety as assessed by adverse events, vital signs, orthostatic evaluation, laboratory tests, ECG measurements, C-SSRS, Bond & Lader VAS, ARCI-49 (Part 2) | Days 1-7 (period 1) and Days 1-13 (period 2) and at end of study visit (up to 22 days) |
| D010879 |
| Piperazines |