Trial Outcomes & Findings for Effect of Activated Charcoal and Time of Dose on the Pharmacokinetics of LY2624803 in Healthy Subject (NCT NCT01236105)
NCT ID: NCT01236105
Last Updated: 2011-12-22
Results Overview
AUC from time 0, extrapolated to infinity, estimated for both LY2624803 and the metabolite LSN2797276.
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
21 participants
Primary outcome timeframe
Predose and up to Day 4
Results posted on
2011-12-22
Participant Flow
Participant milestones
| Measure |
LY2624803
Participants received each of the following 3 study treatments:
LY2624803 Alone Morning Dosing: Participants received 6 milligrams (mg) LY2624803 alone, orally (po) once at approximately 0800 hours following an overnight fast.
LY2624803 Morning Dosing Plus Activated Charcoal: Participants received 6 mg LY2624803 po once at approximately 0800 hours following an overnight fast, followed 1 hour later by a single po dose of 1 gram per kilogram (g/kg) body weight of activated charcoal, mixed with caffeine-free diet cola.
LY2624803 Alone Evening Dosing: Participants received 6 mg LY2624803 alone po once at approximately 2200 hours following a 4-hour fast.
|
|---|---|
|
Overall Study
STARTED
|
21
|
|
Overall Study
COMPLETED
|
21
|
|
Overall Study
NOT COMPLETED
|
0
|
Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
Effect of Activated Charcoal and Time of Dose on the Pharmacokinetics of LY2624803 in Healthy Subject
Baseline characteristics by cohort
| Measure |
LY2624803
n=21 Participants
Participants received each of the following 3 study treatments:
LY2624803 Alone Morning Dosing: Participants received 6 milligrams (mg) LY2624803 alone, orally (po) once at approximately 0800 hours following an overnight fast.
LY2624803 Morning Dosing Plus Activated Charcoal: Participants received 6 mg LY2624803 po once at approximately 0800 hours following an overnight fast, followed 1 hour later by a single po dose of 1 gram per kilogram (g/kg) body weight of activated charcoal, mixed with caffeine-free diet cola.
LY2624803 Alone Evening Dosing: Participants received 6 mg LY2624803 alone po once at approximately 2200 hours following a 4-hour fast.
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|---|---|
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Age Continuous
|
32.3 years
STANDARD_DEVIATION 11.7 • n=93 Participants
|
|
Sex: Female, Male
Female
|
4 Participants
n=93 Participants
|
|
Sex: Female, Male
Male
|
17 Participants
n=93 Participants
|
|
Race/Ethnicity, Customized
White
|
20 participants
n=93 Participants
|
|
Race/Ethnicity, Customized
Black
|
1 participants
n=93 Participants
|
|
Region of Enrollment
United Kingdom
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21 participants
n=93 Participants
|
PRIMARY outcome
Timeframe: Predose and up to Day 4Population: All participants who received at least 1 dose of LY2624803 and have evaluable pharmacokinetic (PK) data.
AUC from time 0, extrapolated to infinity, estimated for both LY2624803 and the metabolite LSN2797276.
Outcome measures
| Measure |
LY2624803 Alone Morning Dosing
n=21 Participants
Participants received 6 milligrams (mg) LY2624803 alone, orally (po) once (QD) at approximately 0800 hours following an overnight fast.
|
LY2624803 Morning Dosing Plus Activated Charcoal
n=20 Participants
Participants received 6 mg LY2624803 po QD at approximately 0800 hours following an overnight fast, followed 1 hour later by a single po dose of 1 gram per kilogram (g/kg) body weight of activated charcoal, mixed with caffeine-free diet cola.
|
LY2624803 Alone Evening Dosing
n=21 Participants
Participants received 6 mg LY2624803 alone po QD at approximately 2200 hours following a 4-hour fast.
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|---|---|---|---|
|
Area Under the Concentration-Time Curve (AUC) for LY2624803 and the Metabolite LSN2797276
LY2624803
|
5240 nanogram*hour per milliliter (ng*h/mL)
Geometric Coefficient of Variation 30
|
3340 nanogram*hour per milliliter (ng*h/mL)
Geometric Coefficient of Variation 30
|
4620 nanogram*hour per milliliter (ng*h/mL)
Geometric Coefficient of Variation 30
|
|
Area Under the Concentration-Time Curve (AUC) for LY2624803 and the Metabolite LSN2797276
LSN2797276 (N=18, 12, 15)
|
192 nanogram*hour per milliliter (ng*h/mL)
Geometric Coefficient of Variation 23
|
112 nanogram*hour per milliliter (ng*h/mL)
Geometric Coefficient of Variation 19
|
188 nanogram*hour per milliliter (ng*h/mL)
Geometric Coefficient of Variation 26
|
PRIMARY outcome
Timeframe: Predose and up to Day 4Population: All participants who received at least 1 dose of LY2624803 and have evaluable pharmacokinetic (PK) data.
Cmax estimated for both LY2624803 and the metabolite LSN2797276.
Outcome measures
| Measure |
LY2624803 Alone Morning Dosing
n=21 Participants
Participants received 6 milligrams (mg) LY2624803 alone, orally (po) once (QD) at approximately 0800 hours following an overnight fast.
|
LY2624803 Morning Dosing Plus Activated Charcoal
n=20 Participants
Participants received 6 mg LY2624803 po QD at approximately 0800 hours following an overnight fast, followed 1 hour later by a single po dose of 1 gram per kilogram (g/kg) body weight of activated charcoal, mixed with caffeine-free diet cola.
|
LY2624803 Alone Evening Dosing
n=21 Participants
Participants received 6 mg LY2624803 alone po QD at approximately 2200 hours following a 4-hour fast.
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|---|---|---|---|
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Maximum Concentration (Cmax) for LY2624803 and the Metabolite, LSN2797276,
LY2624803
|
368 nanogram per milliliter (ng/mL)
Geometric Coefficient of Variation 26
|
335 nanogram per milliliter (ng/mL)
Geometric Coefficient of Variation 35
|
273 nanogram per milliliter (ng/mL)
Geometric Coefficient of Variation 17
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|
Maximum Concentration (Cmax) for LY2624803 and the Metabolite, LSN2797276,
LSN2797276
|
6.22 nanogram per milliliter (ng/mL)
Geometric Coefficient of Variation 27
|
5.11 nanogram per milliliter (ng/mL)
Geometric Coefficient of Variation 41
|
5.94 nanogram per milliliter (ng/mL)
Geometric Coefficient of Variation 28
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SECONDARY outcome
Timeframe: Predose and up to day 4Population: All participants who received at least 1 dose of LY2624803 and have evaluable pharmacokinetic (PK) data.
Tmax, estimated for both LY2624803 and the metabolite LSN2797276.
Outcome measures
| Measure |
LY2624803 Alone Morning Dosing
n=21 Participants
Participants received 6 milligrams (mg) LY2624803 alone, orally (po) once (QD) at approximately 0800 hours following an overnight fast.
|
LY2624803 Morning Dosing Plus Activated Charcoal
n=20 Participants
Participants received 6 mg LY2624803 po QD at approximately 0800 hours following an overnight fast, followed 1 hour later by a single po dose of 1 gram per kilogram (g/kg) body weight of activated charcoal, mixed with caffeine-free diet cola.
|
LY2624803 Alone Evening Dosing
n=21 Participants
Participants received 6 mg LY2624803 alone po QD at approximately 2200 hours following a 4-hour fast.
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|---|---|---|---|
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Time to Maximum Plasma Concentration (Tmax) for LY2624803 and the Metabolite, LSN2797276
LY2624803
|
1.50 hours (h)
Interval 0.5 to 2.5
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0.75 hours (h)
Interval 0.5 to 1.5
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2.00 hours (h)
Interval 1.5 to 6.0
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Time to Maximum Plasma Concentration (Tmax) for LY2624803 and the Metabolite, LSN2797276
LSN2797276
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4.00 hours (h)
Interval 2.0 to 8.0
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4.00 hours (h)
Interval 0.75 to 6.03
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8.00 hours (h)
Interval 2.0 to 12.0
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Adverse Events
LY2624803 Morning Dosing
Serious events: 0 serious events
Other events: 13 other events
Deaths: 0 deaths
LY2624803 Morning Dosing + Activated Charcoal
Serious events: 0 serious events
Other events: 8 other events
Deaths: 0 deaths
LY2624803 Evening Dosing
Serious events: 0 serious events
Other events: 10 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
LY2624803 Morning Dosing
n=21 participants at risk
LY2624803 Alone Morning Dosing: Participants received 6 milligrams (mg) LY2624803 alone, orally (po) once at approximately 0800 hours following an overnight fast.
|
LY2624803 Morning Dosing + Activated Charcoal
n=21 participants at risk
LY2624803 Morning Dosing Plus Activated Charcoal: Participants received 6 mg LY2624803 po once at approximately 0800 hours following an overnight fast, followed 1 hour later by a single po dose of 1 gram per kilogram (g/kg) body weight of activated charcoal, mixed with caffeine-free diet cola.
|
LY2624803 Evening Dosing
n=21 participants at risk
LY2624803 Alone Evening Dosing: Participants received 6 mg LY2624803 alone po once at approximately 2200 hours following a 4-hour fast.
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|---|---|---|---|
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Ear and labyrinth disorders
Ear pain
|
0.00%
0/21
|
4.8%
1/21 • Number of events 1
|
0.00%
0/21
|
|
Eye disorders
Vision blurred
|
0.00%
0/21
|
0.00%
0/21
|
4.8%
1/21 • Number of events 1
|
|
Gastrointestinal disorders
Abdominal pain upper
|
0.00%
0/21
|
4.8%
1/21 • Number of events 1
|
4.8%
1/21 • Number of events 1
|
|
Gastrointestinal disorders
Nausea
|
9.5%
2/21 • Number of events 2
|
4.8%
1/21 • Number of events 1
|
4.8%
1/21 • Number of events 1
|
|
Gastrointestinal disorders
Vomiting
|
0.00%
0/21
|
9.5%
2/21 • Number of events 2
|
0.00%
0/21
|
|
General disorders
Fatigue
|
14.3%
3/21 • Number of events 3
|
0.00%
0/21
|
9.5%
2/21 • Number of events 2
|
|
General disorders
Pain
|
0.00%
0/21
|
4.8%
1/21 • Number of events 1
|
0.00%
0/21
|
|
Infections and infestations
Nasopharyngitis
|
4.8%
1/21 • Number of events 1
|
4.8%
1/21 • Number of events 1
|
4.8%
1/21 • Number of events 1
|
|
Infections and infestations
Sinusitis
|
0.00%
0/21
|
0.00%
0/21
|
4.8%
1/21 • Number of events 1
|
|
Injury, poisoning and procedural complications
Contusion
|
4.8%
1/21 • Number of events 1
|
0.00%
0/21
|
0.00%
0/21
|
|
Metabolism and nutrition disorders
Decreased appetite
|
0.00%
0/21
|
4.8%
1/21 • Number of events 1
|
0.00%
0/21
|
|
Musculoskeletal and connective tissue disorders
Back pain
|
9.5%
2/21 • Number of events 2
|
0.00%
0/21
|
4.8%
1/21 • Number of events 1
|
|
Musculoskeletal and connective tissue disorders
Limb discomfort
|
0.00%
0/21
|
0.00%
0/21
|
4.8%
1/21 • Number of events 1
|
|
Musculoskeletal and connective tissue disorders
Neck pain
|
0.00%
0/21
|
4.8%
1/21 • Number of events 1
|
0.00%
0/21
|
|
Nervous system disorders
Dizziness
|
0.00%
0/21
|
4.8%
1/21 • Number of events 1
|
4.8%
1/21 • Number of events 1
|
|
Nervous system disorders
Headache
|
14.3%
3/21 • Number of events 3
|
0.00%
0/21
|
9.5%
2/21 • Number of events 2
|
|
Nervous system disorders
Hypoaesthesia
|
0.00%
0/21
|
0.00%
0/21
|
4.8%
1/21 • Number of events 1
|
|
Nervous system disorders
Presyncope
|
4.8%
1/21 • Number of events 2
|
0.00%
0/21
|
0.00%
0/21
|
|
Nervous system disorders
Somnolence
|
4.8%
1/21 • Number of events 1
|
4.8%
1/21 • Number of events 1
|
0.00%
0/21
|
|
Nervous system disorders
Tremor
|
0.00%
0/21
|
0.00%
0/21
|
4.8%
1/21 • Number of events 1
|
|
Psychiatric disorders
Insomnia
|
4.8%
1/21 • Number of events 1
|
0.00%
0/21
|
4.8%
1/21 • Number of events 1
|
|
Respiratory, thoracic and mediastinal disorders
Cough
|
0.00%
0/21
|
0.00%
0/21
|
4.8%
1/21 • Number of events 1
|
|
Respiratory, thoracic and mediastinal disorders
Nasal congestion
|
0.00%
0/21
|
0.00%
0/21
|
4.8%
1/21 • Number of events 1
|
|
Respiratory, thoracic and mediastinal disorders
Oropharyngeal pain
|
0.00%
0/21
|
4.8%
1/21 • Number of events 1
|
4.8%
1/21 • Number of events 1
|
Additional Information
Chief Medical Officer
Eli Lilly and Company
Phone: 800-545-5979
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place
Restriction type: GT60