Healthy Volunteers
Conditions
Brief summary
The purpose of this study is to evaluate the amount of drug available in the body when given to healthy participants as two different formulations with or without a meal. In addition, this study will evaluate how much of the drug gets into the blood stream and how long the body takes to get rid of it. Information about any side effects that may occur will also be collected. Each participant will receive a total of five different treatments. Each treatment is given by mouth, once a day. The treatment period lasts for five consecutive days.
Detailed description
The reference formulation is an orally disintegrating tablet without Magnasweet® (ODT1) and the test formulation is an orally disintegrating tablet containing Magnasweet® (ODT2).
Interventions
DRUGPrasugrel ODT1 - Tablet
Administered orally as tablet.
DRUGPrasugrel ODT2 - Tablet
Administered orally as tablet.
DRUGPrasugrel ODT2 - Suspension
Administered orally as suspension.
Sponsors
Daiichi Sankyo
Eli Lilly and Company
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to No maximum
Healthy volunteers
Yes
Inclusion criteria
* Body mass index (BMI) of 18.5 to 32.0 kilograms per square meter (kg/m\^2)
Exclusion criteria
* No known allergies to Prasugrel or related compound * No regular alcohol intake greater than 21 units per week for males or 14 units per week for females
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Pharmacokinetics: Maximum Concentration (Cmax) of Prasugrel Test and Reference Formulation | Predose through 8 Hours Post Dose | Cmax= maximum concentration measured from predose through 8 hours postdose. Test formulation is defined as the orally disintegrating tablet containing Magnasweet® (ODT2) and the reference formulation is defined as the orally disintegrating tablet without Magnasweet® (ODT1) specific to the 5 milligrams (mg) prasugrel dosing. Pharmacokinetics will measure prasugrel's (LY640315) active metabolite. |
| Pharmacokinetics: Area Under the Concentration Curve (AUC) of Prasugrel Reference and Test Formulation | Predose through 8 Hours Post Dose | AUC(0-tlast) = area under the concentration versus time curve from time zero to time t, where t is the last time point with a measurable concentration. Test formulation is defined as the orally disintegrating tablet containing Magnasweet® (ODT2) and the reference formulation is defined as the orally disintegrating tablet without Magnasweet® (ODT1) specific to the 5 mg prasugrel dosing. Pharmacokinetics will measure prasugrel's active metabolite. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Pharmacokinetics: Maximum Concentration (Cmax) of Prasugrel Test Formulation in Fasted and Fed State | Predose through 8 Hours Post Dose | Cmax= maximum concentration measured from predose through 8 hours postdose. Test formulation is defined as the orally disintegrating tablet containing Magnasweet® (ODT2) specific to the 5 mg prasugrel dosing in the fasted and fed state. Pharmacokinetics will measure prasugrel's active metabolite. |
| Pharmacokinetics: Area Under the Concentration Curve (AUC) of Prasugrel Test Formulation in Fasted and Fed State | Predose through 8 Hours Post Dose | AUC(0-tlast) = area under the concentration versus time curve from time zero to time t, where t is the last time point with a measurable concentration. Test formulation is defined as the orally disintegrating tablet containing Magnasweet® (ODT2) specific to the 5 mg prasugrel dosing in the fasted and fed state. Pharmacokinetics will measure prasugrel's active metabolite. |
Countries
United States
Participant flow
Pre-assignment details
Participants were to be given 5 single doses of prasugrel in 5 different sequences on each of 5 consecutive mornings of treatment.
Participants by arm
| Arm | Count |
|---|---|
| All Participants 5 mg Prasugrel as orally disintegrating tablet without Magnasweet® formulation (ODT1) or orally disintegrating tablet containing Magnasweet® formulation (ODT2) given either on top of tongue or dispersed in water administered in either the fasted or fed state. 2 mg prasugrel ODT2 given on top of tongue in the fasted state. | 20 |
| Total | 20 |
Withdrawals & dropouts
| Period | Reason | FG000 | FG001 | FG002 | FG003 | FG004 |
|---|---|---|---|---|---|---|
| Treatment 3 | Withdrawal by Subject | 0 | 0 | 0 | 1 | 0 |
Baseline characteristics
| Characteristic | All Participants |
|---|---|
| Age Continuous | 39.3 years STANDARD_DEVIATION 10.5 |
| Ethnicity (NIH/OMB) Hispanic or Latino | 5 Participants |
| Ethnicity (NIH/OMB) Not Hispanic or Latino | 15 Participants |
| Ethnicity (NIH/OMB) Unknown or Not Reported | 0 Participants |
| Race (NIH/OMB) American Indian or Alaska Native | 1 Participants |
| Race (NIH/OMB) Asian | 0 Participants |
| Race (NIH/OMB) Black or African American | 11 Participants |
| Race (NIH/OMB) More than one race | 0 Participants |
| Race (NIH/OMB) Native Hawaiian or Other Pacific Islander | 0 Participants |
| Race (NIH/OMB) Unknown or Not Reported | 0 Participants |
| Race (NIH/OMB) White | 8 Participants |
| Region of Enrollment United States | 20 participants |
| Sex: Female, Male Female | 2 Participants |
| Sex: Female, Male Male | 18 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk | EG002 affected / at risk | EG003 affected / at risk | EG004 affected / at risk |
|---|---|---|---|---|---|
| deaths Total, all-cause mortality | — / — | — / — | — / — | — / — | — / — |
| other Total, other adverse events | 1 / 19 | 0 / 19 | 0 / 20 | 2 / 20 | 1 / 19 |
| serious Total, serious adverse events | 0 / 19 | 0 / 19 | 0 / 20 | 0 / 20 | 0 / 19 |
Outcome results
Primary
Pharmacokinetics: Area Under the Concentration Curve (AUC) of Prasugrel Reference and Test Formulation
AUC(0-tlast) = area under the concentration versus time curve from time zero to time t, where t is the last time point with a measurable concentration. Test formulation is defined as the orally disintegrating tablet containing Magnasweet® (ODT2) and the reference formulation is defined as the orally disintegrating tablet without Magnasweet® (ODT1) specific to the 5 mg prasugrel dosing. Pharmacokinetics will measure prasugrel's active metabolite.
Time frame: Predose through 8 Hours Post Dose
Population: Pharmacokinetic population consists of all participants who received at least one dose of study drug and have evaluable pharmacokinetic data.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 5 mg Prasugrel (ODT1) | Pharmacokinetics: Area Under the Concentration Curve (AUC) of Prasugrel Reference and Test Formulation | 27.1 nanograms*hour per milliliter (ng*h/mL) | Geometric Coefficient of Variation 31 |
| 5 mg Prasugrel (ODT2) | Pharmacokinetics: Area Under the Concentration Curve (AUC) of Prasugrel Reference and Test Formulation | 26.8 nanograms*hour per milliliter (ng*h/mL) | Geometric Coefficient of Variation 38 |
90% CI: [0.918, 1.06]
Primary
Pharmacokinetics: Maximum Concentration (Cmax) of Prasugrel Test and Reference Formulation
Cmax= maximum concentration measured from predose through 8 hours postdose. Test formulation is defined as the orally disintegrating tablet containing Magnasweet® (ODT2) and the reference formulation is defined as the orally disintegrating tablet without Magnasweet® (ODT1) specific to the 5 milligrams (mg) prasugrel dosing. Pharmacokinetics will measure prasugrel's (LY640315) active metabolite.
Time frame: Predose through 8 Hours Post Dose
Population: Pharmacokinetic population consists of all participants who received at least one dose of study drug and have evaluable pharmacokinetic data.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 5 mg Prasugrel (ODT1) | Pharmacokinetics: Maximum Concentration (Cmax) of Prasugrel Test and Reference Formulation | 28.6 nanograms per milliliter (ng/mL) | Geometric Coefficient of Variation 41 |
| 5 mg Prasugrel (ODT2) | Pharmacokinetics: Maximum Concentration (Cmax) of Prasugrel Test and Reference Formulation | 28.1 nanograms per milliliter (ng/mL) | Geometric Coefficient of Variation 51 |
90% CI: [0.819, 1.18]
Secondary
Pharmacokinetics: Area Under the Concentration Curve (AUC) of Prasugrel Test Formulation in Fasted and Fed State
AUC(0-tlast) = area under the concentration versus time curve from time zero to time t, where t is the last time point with a measurable concentration. Test formulation is defined as the orally disintegrating tablet containing Magnasweet® (ODT2) specific to the 5 mg prasugrel dosing in the fasted and fed state. Pharmacokinetics will measure prasugrel's active metabolite.
Time frame: Predose through 8 Hours Post Dose
Population: Pharmacokinetic population consists of all participants who received at least one dose of study drug and have evaluable pharmacokinetic data.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 5 mg Prasugrel (ODT1) | Pharmacokinetics: Area Under the Concentration Curve (AUC) of Prasugrel Test Formulation in Fasted and Fed State | 27.1 nanograms*hour per milliliter (ng*h/mL) | Geometric Coefficient of Variation 31 |
| 5 mg Prasugrel (ODT2) | Pharmacokinetics: Area Under the Concentration Curve (AUC) of Prasugrel Test Formulation in Fasted and Fed State | 26.8 nanograms*hour per milliliter (ng*h/mL) | Geometric Coefficient of Variation 38 |
| 5 mg Prasugrel (ODT2)-Suspension | Pharmacokinetics: Area Under the Concentration Curve (AUC) of Prasugrel Test Formulation in Fasted and Fed State | 27 nanograms*hour per milliliter (ng*h/mL) | Geometric Coefficient of Variation 32 |
| 5 mg Prasugrel (ODT2)-Fed | Pharmacokinetics: Area Under the Concentration Curve (AUC) of Prasugrel Test Formulation in Fasted and Fed State | 20.8 nanograms*hour per milliliter (ng*h/mL) | Geometric Coefficient of Variation 39 |
| 2 mg Prasugrel (ODT2) | Pharmacokinetics: Area Under the Concentration Curve (AUC) of Prasugrel Test Formulation in Fasted and Fed State | 8.97 nanograms*hour per milliliter (ng*h/mL) | Geometric Coefficient of Variation 31 |
90% CI: [0.724, 0.837]
Secondary
Pharmacokinetics: Maximum Concentration (Cmax) of Prasugrel Test Formulation in Fasted and Fed State
Cmax= maximum concentration measured from predose through 8 hours postdose. Test formulation is defined as the orally disintegrating tablet containing Magnasweet® (ODT2) specific to the 5 mg prasugrel dosing in the fasted and fed state. Pharmacokinetics will measure prasugrel's active metabolite.
Time frame: Predose through 8 Hours Post Dose
Population: Pharmacokinetic population consists of all participants who received at least one dose of study drug and have evaluable pharmacokinetic data.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 5 mg Prasugrel (ODT1) | Pharmacokinetics: Maximum Concentration (Cmax) of Prasugrel Test Formulation in Fasted and Fed State | 28.6 nanograms per milliliter (ng/mL) | Geometric Coefficient of Variation 41 |
| 5 mg Prasugrel (ODT2) | Pharmacokinetics: Maximum Concentration (Cmax) of Prasugrel Test Formulation in Fasted and Fed State | 28.1 nanograms per milliliter (ng/mL) | Geometric Coefficient of Variation 51 |
| 5 mg Prasugrel (ODT2)-Suspension | Pharmacokinetics: Maximum Concentration (Cmax) of Prasugrel Test Formulation in Fasted and Fed State | 31.5 nanograms per milliliter (ng/mL) | Geometric Coefficient of Variation 45 |
| 5 mg Prasugrel (ODT2)-Fed | Pharmacokinetics: Maximum Concentration (Cmax) of Prasugrel Test Formulation in Fasted and Fed State | 7.79 nanograms per milliliter (ng/mL) | Geometric Coefficient of Variation 60 |
| 2 mg Prasugrel (ODT2) | Pharmacokinetics: Maximum Concentration (Cmax) of Prasugrel Test Formulation in Fasted and Fed State | 8.81 nanograms per milliliter (ng/mL) | Geometric Coefficient of Variation 47 |
90% CI: [0.233, 0.335]