Trial Outcomes & Findings for A Study to Evaluate the Effect of Activated Charcoal on the Absorption of LY2216684 in Healthy Subjects (NCT NCT01389752)
NCT ID: NCT01389752
Last Updated: 2019-01-04
Results Overview
The AUC0-∞ of LY2216684 was measured. The AUC was calculated for LY2216684 administered alone (reference) and LY2216684 co-administered with charcoal (test). Geometric Least Squares (LS) means were calculated according to the following model: Log(PK) = sequence + period + treatment + subject + random error for AUC.
COMPLETED
PHASE1
22 participants
Predose, up to 72 hours after administration of study drug
2019-01-04
Participant Flow
Participant milestones
| Measure |
LY2216684 Without Charcoal, Then With Charcoal
Period 1: Single 18-mg (milligram) (two 9-mg tablets) oral dose of LY2216684 administered without Activated Charcoal. Period 2: Single 18-mg (two 9-mg tablets) oral dose of LY2216684 administered with single oral dose of 1 g/kg (gram/kilogram) of Activated Charcoal. Periods will be separated by a minimum of 7 days.
|
LY2216684 With Charcoal, Then Without Charcoal
Period 1: Single 18-mg (two 9-mg tablets) oral dose of LY2216684 administered with single oral dose of 1 g/kg of Activated Charcoal. Period 2: Single 18-mg (two 9-mg tablets) oral dose of LY2216684 administered without Activated Charcoal. Periods will be separated by a minimum of 7 days.
|
|---|---|---|
|
Study Period 1
STARTED
|
11
|
11
|
|
Study Period 1
COMPLETED
|
11
|
9
|
|
Study Period 1
NOT COMPLETED
|
0
|
2
|
|
Study Period 2
STARTED
|
11
|
9
|
|
Study Period 2
COMPLETED
|
10
|
9
|
|
Study Period 2
NOT COMPLETED
|
1
|
0
|
Reasons for withdrawal
| Measure |
LY2216684 Without Charcoal, Then With Charcoal
Period 1: Single 18-mg (milligram) (two 9-mg tablets) oral dose of LY2216684 administered without Activated Charcoal. Period 2: Single 18-mg (two 9-mg tablets) oral dose of LY2216684 administered with single oral dose of 1 g/kg (gram/kilogram) of Activated Charcoal. Periods will be separated by a minimum of 7 days.
|
LY2216684 With Charcoal, Then Without Charcoal
Period 1: Single 18-mg (two 9-mg tablets) oral dose of LY2216684 administered with single oral dose of 1 g/kg of Activated Charcoal. Period 2: Single 18-mg (two 9-mg tablets) oral dose of LY2216684 administered without Activated Charcoal. Periods will be separated by a minimum of 7 days.
|
|---|---|---|
|
Study Period 1
Sponsor decision
|
0
|
2
|
|
Study Period 2
Sponsor decision
|
1
|
0
|
Baseline Characteristics
A Study to Evaluate the Effect of Activated Charcoal on the Absorption of LY2216684 in Healthy Subjects
Baseline characteristics by cohort
| Measure |
Overall
n=22 Participants
During Study Period 1, participants received a single oral dose of 18 mg LY2216684 alone or in combination with 1 g/kg Activated Charcoal 1 hour after LY2216684 administration. After at least 7 days, participants who initially received 18 mg LY2216684 alone received another single oral dose of 18 mg LY2216684 in combination with 1 g/kg Activated Charcoal 1 hour after LY2216684 administration during Study Period 2; participants who initially received 18 mg LY2216684 in combination with 1 g/kg Activated Charcoal received another single oral dose of 18 mg LY2216684 alone during Study Period 2.
|
|---|---|
|
Age, Continuous
|
35.2 years
STANDARD_DEVIATION 9.3 • n=93 Participants
|
|
Sex: Female, Male
Female
|
11 Participants
n=93 Participants
|
|
Sex: Female, Male
Male
|
11 Participants
n=93 Participants
|
|
Ethnicity (NIH/OMB)
Hispanic or Latino
|
13 Participants
n=93 Participants
|
|
Ethnicity (NIH/OMB)
Not Hispanic or Latino
|
8 Participants
n=93 Participants
|
|
Ethnicity (NIH/OMB)
Unknown or Not Reported
|
1 Participants
n=93 Participants
|
|
Race (NIH/OMB)
American Indian or Alaska Native
|
0 Participants
n=93 Participants
|
|
Race (NIH/OMB)
Asian
|
0 Participants
n=93 Participants
|
|
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
|
0 Participants
n=93 Participants
|
|
Race (NIH/OMB)
Black or African American
|
6 Participants
n=93 Participants
|
|
Race (NIH/OMB)
White
|
15 Participants
n=93 Participants
|
|
Race (NIH/OMB)
More than one race
|
1 Participants
n=93 Participants
|
|
Race (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=93 Participants
|
|
Region of Enrollment
United States
|
22 Participants
n=93 Participants
|
PRIMARY outcome
Timeframe: Predose, up to 72 hours after administration of study drugPopulation: All participants who were randomized, for whom AUC0-∞ data were available, and who were not excluded due to vomiting within twice the median time to maximum plasma concentration (tmax) of LY2216684.
The AUC0-∞ of LY2216684 was measured. The AUC was calculated for LY2216684 administered alone (reference) and LY2216684 co-administered with charcoal (test). Geometric Least Squares (LS) means were calculated according to the following model: Log(PK) = sequence + period + treatment + subject + random error for AUC.
Outcome measures
| Measure |
LY2216684 in Combination With Activated Charcoal
n=17 Participants
Participants received a single oral dose of 18 mg (milligram) LY2216684 and a single oral dose of 1 g/kg (gram/kilogram) of Activated Charcoal 1 hour after administration of LY2216684.
|
LY2216684 Alone
n=19 Participants
Participants received a single oral dose of 18 mg LY2216684.
|
|---|---|---|
|
Pharmacokinetics: Area Under the Plasma Concentration-Time Curve From Time 0 to Infinity (AUC0-∞) of LY2216684
|
509 nanogram*hour/milliliter (ng*h/mL)
Interval 454.0 to 571.0
|
786 nanogram*hour/milliliter (ng*h/mL)
Interval 701.0 to 881.0
|
PRIMARY outcome
Timeframe: Predose, up to 72 hours after administration of study drugPopulation: All participants who were randomized, for whom Cmax data were available, and who were not excluded due to vomiting within twice the median time to maximum plasma concentration (tmax) of LY2216684.
The Cmax of LY2216684 was assessed. The Cmax was calculated for LY2216684 administered alone (reference) and LY2216684 co-administered with charcoal (test). Geometric LSMeans were calculated according to the following model: Log(PK) = sequence + period + treatment + subject + random error for Cmax.
Outcome measures
| Measure |
LY2216684 in Combination With Activated Charcoal
n=17 Participants
Participants received a single oral dose of 18 mg (milligram) LY2216684 and a single oral dose of 1 g/kg (gram/kilogram) of Activated Charcoal 1 hour after administration of LY2216684.
|
LY2216684 Alone
n=19 Participants
Participants received a single oral dose of 18 mg LY2216684.
|
|---|---|---|
|
Pharmacokinetics: Maximum Observed Plasma Concentration (Cmax) of LY2216684
|
54.06 nanogram/milliliter (ng/mL)
Interval 49.16 to 59.44
|
59.84 nanogram/milliliter (ng/mL)
Interval 54.55 to 65.63
|
PRIMARY outcome
Timeframe: Predose, up to 72 hours after administration of study drugPopulation: All participants who were randomized, for whom tmax data were available, and who were not excluded due to vomiting within twice the median tmax of LY2216684.
The tmax for LY2216684 was assessed.
Outcome measures
| Measure |
LY2216684 in Combination With Activated Charcoal
n=17 Participants
Participants received a single oral dose of 18 mg (milligram) LY2216684 and a single oral dose of 1 g/kg (gram/kilogram) of Activated Charcoal 1 hour after administration of LY2216684.
|
LY2216684 Alone
n=17 Participants
Participants received a single oral dose of 18 mg LY2216684.
|
|---|---|---|
|
Pharmacokinetics: Time to Maximum Plasma Concentration (Tmax) of LY2216684
|
2.00 hours
Interval 0.92 to 3.0
|
2.03 hours
Interval 2.0 to 5.0
|
Adverse Events
LY2216684 in Combination With Activated Charcoal
LY2216684 Alone
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
LY2216684 in Combination With Activated Charcoal
n=22 participants at risk
Participants received a single oral dose of 18 mg (milligram) LY2216684 and a single oral dose of 1 g/kg (gram/kilogram) of Activated Charcoal 1 hour after administration of LY2216684.
|
LY2216684 Alone
n=20 participants at risk
Participants received a single oral dose of 18 mg LY2216684.
|
|---|---|---|
|
Gastrointestinal disorders
Nausea
|
9.1%
2/22 • Number of events 3
|
5.0%
1/20 • Number of events 1
|
|
Gastrointestinal disorders
Vomiting
|
22.7%
5/22 • Number of events 5
|
5.0%
1/20 • Number of events 1
|
|
General disorders
Vessel puncture site pain
|
0.00%
0/22
|
5.0%
1/20 • Number of events 1
|
|
Musculoskeletal and connective tissue disorders
Muscle spasms
|
0.00%
0/22
|
5.0%
1/20 • Number of events 1
|
|
Nervous system disorders
Dizziness
|
9.1%
2/22 • Number of events 2
|
0.00%
0/20
|
|
Nervous system disorders
Headache
|
13.6%
3/22 • Number of events 3
|
0.00%
0/20
|
|
Psychiatric disorders
Insomnia
|
0.00%
0/22
|
5.0%
1/20 • Number of events 1
|
|
Renal and urinary disorders
Urinary hesitation
|
0.00%
0/22
|
5.0%
1/20 • Number of events 1
|
|
Reproductive system and breast disorders
Dysmenorrhoea
|
9.1%
1/11 • Number of events 1
|
10.0%
1/10 • Number of events 1
|
Additional Information
Chief Medical Officer
Eli Lilly and Company
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place
Restriction type: GT60