This study will be conducted to evaluate the bioavailability of a single 12 milligram (mg) dose of perampanel intravenous infusions of different durations relative to a single 12 mg dose of perampanel oral tablet in healthy participants.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
48
IV infusion
Oral tablet
Anaheim Clinical Trials
Anaheim, California, United States
Mean maximum observed concentration (Cmax) postdose of perampanel
Cmax is the maximum plasma concentration of a drug after administration. Dosing will occur on Day 1 of Treatment Period 1 and Day 43 of Treatment Period 2.
Time frame: predose; 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, and 12 (Day [D]1 and D43); 24 and 36 (D2 and D44); 48 (D3 and D45); 72 (D4 and D46); 120 (D6 and D48); 168 (D8 and D50); 336 (D15 and D57); and 504 (D22 and D64) hours after dosing start
Mean value for area under the concentration versus time curve from time 0 to time of last measurable concentration (AUC[0-t]) postdose of perampanel
AUC is a measure of actual body exposure to drug after administration of the drug. Dosing will occur on Day 1 of Treatment Period 1 and Day 43 of Treatment Period 2.
Time frame: predose; 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, and 12 (D1 and D43); 24 and 36 (D2 and D44); 48 (D3 and D45); 72 (D4 and D46); 120 (D6 and D48); 168 (D8 and D50); 336 (D15 and D57); and 504 (D22 and D64) hours after dosing start
Mean value for AUC versus time curve from time 0 to infinity (AUC[0-inf]) postdose of perampanel
AUC is a measure of actual body exposure to drug after administration of the drug. Dosing will occur on Day 1 of Treatment Period 1 and Day 43 of Treatment Period 2.
Time frame: predose; 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, and 12 (D1 and D43); 24 and 36 (D2 and D44); 48 (D3 and D45); 72 (D4 and D46); 120 (D6 and D48); 168 (D8 and D50); 336 (D15 and D57); and 504 (D22 and D64) hours after dosing start
Mean value for AUC versus time curve from time 0 to 72 hours (AUC[0-72h]) postdose of perampanel
AUC is a measure of actual body exposure to drug after administration of the drug. Dosing will occur on Day 1 of Treatment Period 1 and Day 43 of Treatment Period 2.
Time frame: predose; 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, and 12 (D1 and D43); 24 and 36 (D2 and D44); 48 (D3 and D45); 72 (D4 and D46); 120 (D6 and D48); 168 (D8 and D50); 336 (D15 and D57); and 504 (D22 and D64) hours after dosing start
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Mean time to reach maximum concentration (tmax) postdose of perampanel
tmax is the time to reach maximum concentration following drug administration. Dosing will occur on Day 1 of Treatment Period 1 and Day 43 of Treatment Period 2.
Time frame: predose; 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, and 12 (D1 and D43); 24 and 36 (D2 and D44); 48 (D3 and D45); 72 (D4 and D46); 120 (D6 and D48); 168 (D8 and D50); 336 (D15 and D57); and 504 (D22 and D64) hours after dosing start
Mean terminal phase half-life (t1/2) postdose of perampanel
t1/2 is the time required for the concentration of the drug to reach half of its original value. Dosing will occur on Day 1 of Treatment Period 1 and Day 43 of Treatment Period 2.
Time frame: predose; 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, and 12 (D1 and D43); 24 and 36 (D2 and D44); 48 (D3 and D45); 72 (D4 and D46); 120 (D6 and D48); 168 (D8 and D50); 336 (D15 and D57); and 504 (D22 and D64) hours after dosing start
Mean total clearance (CL) post intravenous (IV) infusion of perampanel
CL is the volume of plasma cleared of drug per unit time. Dosing will occur on Day 1 of Treatment Period 1 and Day 43 of Treatment Period 2.
Time frame: predose; 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, and 12 (D1 and D43); 24 and 36 (D2 and D44); 48 (D3 and D45); 72 (D4 and D46); 120 (D6 and D48); 168 (D8 and D50); 336 (D15 and D57); and 504 (D22 and D64) hours after dosing start
Mean volume of distribution (Vd) post IV infusion of perampanel
Vd is the apparent volume in which a drug is distributed. Dosing will occur on Day 1 of Treatment Period 1 and Day 43 of Treatment Period 2.
Time frame: predose; 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, and 12 (D1 and D43); 24 and 36 (D2 and D44); 48 (D3 and D45); 72 (D4 and D46); 120 (D6 and D48); 168 (D8 and D50); 336 (D15 and D57); and 504 (D22 and D64) hours after dosing start
Number of participants with any treatment-emergent (TE) serious adverse event (SAE)
An SAE is any untoward medical occurrence that at any dose: results in death; is life threatening (an adverse event \[AE\] is considered life-threatening if, in the view of either the Investigator or Sponsor, its occurrence places the participant at immediate risk of death. It does not include an AE that, had it occurred in a more severe form, might have caused death.); requires inpatient hospitalization or prolongation of existing hospitalization; results in persistent or significant disability/incapacity; is a congenital anomaly/birth defect. A TEAE is defined as an AE that emerges during treatment, having been absent at pretreatment (baseline) or (1) reemerges during treatment, having been present at pretreatment (baseline) but stopped before treatment, or (2) worsens in severity during treatment relative to the pretreatment state, when the AE is continuous.
Time frame: Up to approximately 16 weeks
Number of participants with any non-serious TEAE
An AE is any untoward medical occurrence and does not necessarily have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of an investigational product (IP), whether or not related to the IP. AEs include pre-existing conditions that worsen. A TEAE is defined as an AE that emerges during treatment, having been absent at pretreatment (baseline) or (1) reemerges during treatment, having been present at pretreatment (baseline) but stopped before treatment, or (2) worsens in severity during treatment relative to the pretreatment state, when the AE is continuous.
Time frame: Up to approximately 16 weeks
Number of participants with an abnormal, clinically significant laboratory parameter value
Clinical significance will be determined by the Investigator.
Time frame: Up to approximately 16 weeks
Number of participants requiring concomitant medication
Concomitant medications are medications that started after the date of the first dose of perampanel until the end of the study.
Time frame: Up to approximately 16 weeks
Number of participants with an abnormal, clinically significant vital sign value
Clinical significance will be determined by the Investigator.
Time frame: Up to approximately 16 weeks
Number of participants with an abnormal, clinically significant physical examination finding
Clinical significance will be determined by the Investigator.
Time frame: Up to approximately 16 weeks