Trial Outcomes & Findings for A Study of LY2140023 in Healthy Males and Females (NCT NCT01591330)
NCT ID: NCT01591330
Last Updated: 2021-09-21
Results Overview
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
35 participants
Primary outcome timeframe
Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose
Results posted on
2021-09-21
Participant Flow
Participant milestones
| Measure |
Sequence 1
LY2140023 80 milligrams (mg) reference form (RF) in Period 1, LY2140023 80 mg Test-low in Period 2, LY2140023 80 mg Test-medium in Period 3, LY2140023 80 mg Test-high in Period 4.
Each LY2140023 dose was administered once, orally. There was a minimum 3-day washout period between dosing in one period and dosing in the next dosing period.
|
Sequence 2
LY2140023 80 mg Test-low in Period 1, LY2140023 80 mg Test-high in Period 2, LY2140023 80 mg RF Period 3, LY2140023 80 mg Test-medium in Period 4.
Each LY2140023 dose was administered once, orally. There was a minimum 3-day washout period between dosing in one period and dosing in the next dosing period.
|
Sequence 3
LY2140023 80 mg Test-high in Period 1, LY2140023 80 mg Test-medium in Period 2, LY2140023 80 mg Test-low in Period 3, LY2140023 80 mg RF in Period 4.
Each LY2140023 dose was administered once, orally. There was a minimum 3-day washout period between dosing in one period and dosing in the next dosing period.
|
Sequence 4
LY2140023 80 mg Test-medium in Period 1, LY2140023 80 mg RF in Period 2, LY2140023 80 mg Test-high in Period 3, LY2140023 80 mg Test-low in Period 4.
Each LY2140023 dose was administered once, orally. There was a minimum 3-day washout period between dosing in one period and dosing in the next dosing period.
|
|---|---|---|---|---|
|
Period 1
STARTED
|
8
|
9
|
9
|
9
|
|
Period 1
Received at Least 1 Dose of Study Drug
|
8
|
9
|
9
|
9
|
|
Period 1
COMPLETED
|
7
|
9
|
9
|
9
|
|
Period 1
NOT COMPLETED
|
1
|
0
|
0
|
0
|
|
Washout of at Least 3 Days
STARTED
|
5
|
9
|
9
|
9
|
|
Washout of at Least 3 Days
COMPLETED
|
5
|
9
|
9
|
9
|
|
Washout of at Least 3 Days
NOT COMPLETED
|
0
|
0
|
0
|
0
|
|
Period 2
STARTED
|
6
|
9
|
9
|
9
|
|
Period 2
COMPLETED
|
5
|
9
|
9
|
9
|
|
Period 2
NOT COMPLETED
|
1
|
0
|
0
|
0
|
|
Period 3
STARTED
|
5
|
9
|
9
|
9
|
|
Period 3
COMPLETED
|
5
|
9
|
9
|
9
|
|
Period 3
NOT COMPLETED
|
0
|
0
|
0
|
0
|
|
Period 4
STARTED
|
5
|
9
|
9
|
9
|
|
Period 4
COMPLETED
|
5
|
9
|
9
|
9
|
|
Period 4
NOT COMPLETED
|
0
|
0
|
0
|
0
|
Reasons for withdrawal
| Measure |
Sequence 1
LY2140023 80 milligrams (mg) reference form (RF) in Period 1, LY2140023 80 mg Test-low in Period 2, LY2140023 80 mg Test-medium in Period 3, LY2140023 80 mg Test-high in Period 4.
Each LY2140023 dose was administered once, orally. There was a minimum 3-day washout period between dosing in one period and dosing in the next dosing period.
|
Sequence 2
LY2140023 80 mg Test-low in Period 1, LY2140023 80 mg Test-high in Period 2, LY2140023 80 mg RF Period 3, LY2140023 80 mg Test-medium in Period 4.
Each LY2140023 dose was administered once, orally. There was a minimum 3-day washout period between dosing in one period and dosing in the next dosing period.
|
Sequence 3
LY2140023 80 mg Test-high in Period 1, LY2140023 80 mg Test-medium in Period 2, LY2140023 80 mg Test-low in Period 3, LY2140023 80 mg RF in Period 4.
Each LY2140023 dose was administered once, orally. There was a minimum 3-day washout period between dosing in one period and dosing in the next dosing period.
|
Sequence 4
LY2140023 80 mg Test-medium in Period 1, LY2140023 80 mg RF in Period 2, LY2140023 80 mg Test-high in Period 3, LY2140023 80 mg Test-low in Period 4.
Each LY2140023 dose was administered once, orally. There was a minimum 3-day washout period between dosing in one period and dosing in the next dosing period.
|
|---|---|---|---|---|
|
Period 1
Adverse Event
|
1
|
0
|
0
|
0
|
|
Washout of at Least 3 Days
Withdrawal by Subject
|
1
|
0
|
0
|
0
|
|
Period 2
Adverse Event
|
1
|
0
|
0
|
0
|
Baseline Characteristics
A Study of LY2140023 in Healthy Males and Females
Baseline characteristics by cohort
| Measure |
Overall Study
n=35 Participants
All participants
|
|---|---|
|
Age, Continuous
|
34.1 years
STANDARD_DEVIATION 13.2 • n=93 Participants
|
|
Sex: Female, Male
Female
|
17 Participants
n=93 Participants
|
|
Sex: Female, Male
Male
|
18 Participants
n=93 Participants
|
|
Race/Ethnicity, Customized
White
|
33 participants
n=93 Participants
|
|
Race/Ethnicity, Customized
Black or African American
|
2 participants
n=93 Participants
|
|
Region of Enrollment
United Kingdom
|
35 participants
n=93 Participants
|
|
Weight
|
71.71 kilograms (kg)
STANDARD_DEVIATION 13.34 • n=93 Participants
|
|
Body Mass Index (BMI)
|
24.73 kilograms per meter squared (kg/m^2)
STANDARD_DEVIATION 3.70 • n=93 Participants
|
PRIMARY outcome
Timeframe: Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdosePopulation: All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY2140023 plasma concentration data.
Outcome measures
| Measure |
LY2140023 Reference Form
n=30 Participants
LY2140023: 80 milligrams (mg), administered once, orally.
|
LY2140023 Test-Low
n=28 Participants
LY2140023: 80 mg, low particle size, administered once, orally.
|
LY2140023 Test-Medium
n=28 Participants
LY2140023: 80 mg, medium particle size, administered once, orally.
|
LY2140023 Test-High
n=27 Participants
LY2140023: 80 mg, high particle size, administered once, orally.
|
|---|---|---|---|---|
|
Pharmacokinetics: Maximum Concentration (Cmax) of LY2140023
|
277 nanograms per milliliter (ng/mL)
Geometric Coefficient of Variation 25
|
290 nanograms per milliliter (ng/mL)
Geometric Coefficient of Variation 23
|
304 nanograms per milliliter (ng/mL)
Geometric Coefficient of Variation 37
|
284 nanograms per milliliter (ng/mL)
Geometric Coefficient of Variation 29
|
PRIMARY outcome
Timeframe: Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdosePopulation: All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY2140023 plasma concentration data.
Outcome measures
| Measure |
LY2140023 Reference Form
n=30 Participants
LY2140023: 80 milligrams (mg), administered once, orally.
|
LY2140023 Test-Low
n=28 Participants
LY2140023: 80 mg, low particle size, administered once, orally.
|
LY2140023 Test-Medium
n=28 Participants
LY2140023: 80 mg, medium particle size, administered once, orally.
|
LY2140023 Test-High
n=27 Participants
LY2140023: 80 mg, high particle size, administered once, orally.
|
|---|---|---|---|---|
|
Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Last Time Point of Measurable Concentration (AUC[0-tlast]) of LY2140023
|
1200 nanograms*hours per milliliter (ng*h/mL)
Geometric Coefficient of Variation 28
|
1190 nanograms*hours per milliliter (ng*h/mL)
Geometric Coefficient of Variation 30
|
1210 nanograms*hours per milliliter (ng*h/mL)
Geometric Coefficient of Variation 32
|
1210 nanograms*hours per milliliter (ng*h/mL)
Geometric Coefficient of Variation 32
|
PRIMARY outcome
Timeframe: Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdosePopulation: All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY404039 (active moiety) plasma concentration data following administration of LY2140023.
Outcome measures
| Measure |
LY2140023 Reference Form
n=30 Participants
LY2140023: 80 milligrams (mg), administered once, orally.
|
LY2140023 Test-Low
n=28 Participants
LY2140023: 80 mg, low particle size, administered once, orally.
|
LY2140023 Test-Medium
n=28 Participants
LY2140023: 80 mg, medium particle size, administered once, orally.
|
LY2140023 Test-High
n=27 Participants
LY2140023: 80 mg, high particle size, administered once, orally.
|
|---|---|---|---|---|
|
Pharmacokinetics: Maximum Concentration (Cmax) of LY404039 (Active Moiety)
|
476 ng/mL
Geometric Coefficient of Variation 14
|
485 ng/mL
Geometric Coefficient of Variation 17
|
494 ng/mL
Geometric Coefficient of Variation 17
|
490 ng/mL
Geometric Coefficient of Variation 16
|
PRIMARY outcome
Timeframe: Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdosePopulation: All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY404039 (active moiety) plasma concentration data following administration of LY2140023.
Outcome measures
| Measure |
LY2140023 Reference Form
n=30 Participants
LY2140023: 80 milligrams (mg), administered once, orally.
|
LY2140023 Test-Low
n=28 Participants
LY2140023: 80 mg, low particle size, administered once, orally.
|
LY2140023 Test-Medium
n=28 Participants
LY2140023: 80 mg, medium particle size, administered once, orally.
|
LY2140023 Test-High
n=27 Participants
LY2140023: 80 mg, high particle size, administered once, orally.
|
|---|---|---|---|---|
|
Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Last Time Point of Measurable Concentration (AUC[0-tlast]) of LY404039 (Active Moiety)
|
2640 ng*h/mL
Geometric Coefficient of Variation 17
|
2640 ng*h/mL
Geometric Coefficient of Variation 19
|
2710 ng*h/mL
Geometric Coefficient of Variation 17
|
2700 ng*h/mL
Geometric Coefficient of Variation 16
|
SECONDARY outcome
Timeframe: Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdosePopulation: All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY2140023 plasma concentration data.
Outcome measures
| Measure |
LY2140023 Reference Form
n=30 Participants
LY2140023: 80 milligrams (mg), administered once, orally.
|
LY2140023 Test-Low
n=28 Participants
LY2140023: 80 mg, low particle size, administered once, orally.
|
LY2140023 Test-Medium
n=28 Participants
LY2140023: 80 mg, medium particle size, administered once, orally.
|
LY2140023 Test-High
n=27 Participants
LY2140023: 80 mg, high particle size, administered once, orally.
|
|---|---|---|---|---|
|
Pharmacokinetics: Time of Maximum Observed Drug Concentration (Tmax) of LY2140023
|
3.00 hours (h)
Interval 2.0 to 5.0
|
3.00 hours (h)
Interval 2.0 to 5.02
|
3.00 hours (h)
Interval 1.0 to 7.0
|
3.00 hours (h)
Interval 2.0 to 5.0
|
SECONDARY outcome
Timeframe: Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdosePopulation: All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY2140023 plasma concentration data.
Outcome measures
| Measure |
LY2140023 Reference Form
n=30 Participants
LY2140023: 80 milligrams (mg), administered once, orally.
|
LY2140023 Test-Low
n=28 Participants
LY2140023: 80 mg, low particle size, administered once, orally.
|
LY2140023 Test-Medium
n=28 Participants
LY2140023: 80 mg, medium particle size, administered once, orally.
|
LY2140023 Test-High
n=27 Participants
LY2140023: 80 mg, high particle size, administered once, orally.
|
|---|---|---|---|---|
|
Pharmacokinetics: Terminal Half Life (t1/2) of LY2140023
|
2.13 h
Interval 1.61 to 3.27
|
1.93 h
Interval 1.55 to 2.95
|
2.02 h
Interval 1.47 to 3.06
|
2.13 h
Interval 1.43 to 3.38
|
SECONDARY outcome
Timeframe: Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdosePopulation: All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY2140023 plasma concentration data.
Outcome measures
| Measure |
LY2140023 Reference Form
n=30 Participants
LY2140023: 80 milligrams (mg), administered once, orally.
|
LY2140023 Test-Low
n=28 Participants
LY2140023: 80 mg, low particle size, administered once, orally.
|
LY2140023 Test-Medium
n=28 Participants
LY2140023: 80 mg, medium particle size, administered once, orally.
|
LY2140023 Test-High
n=27 Participants
LY2140023: 80 mg, high particle size, administered once, orally.
|
|---|---|---|---|---|
|
Pharmacokinetics: Apparent Total Body Clearance (CL/F) of LY2140023
|
66.8 liters per hour (L/h)
Geometric Coefficient of Variation 28
|
67.0 liters per hour (L/h)
Geometric Coefficient of Variation 30
|
65.9 liters per hour (L/h)
Geometric Coefficient of Variation 32
|
66.2 liters per hour (L/h)
Geometric Coefficient of Variation 32
|
SECONDARY outcome
Timeframe: Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdosePopulation: All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY2140023 plasma concentration data.
Outcome measures
| Measure |
LY2140023 Reference Form
n=30 Participants
LY2140023: 80 milligrams (mg), administered once, orally.
|
LY2140023 Test-Low
n=28 Participants
LY2140023: 80 mg, low particle size, administered once, orally.
|
LY2140023 Test-Medium
n=28 Participants
LY2140023: 80 mg, medium particle size, administered once, orally.
|
LY2140023 Test-High
n=27 Participants
LY2140023: 80 mg, high particle size, administered once, orally.
|
|---|---|---|---|---|
|
Pharmacokinetics: Volume of Distribution During the Terminal Phase (Vz/F) of LY2140023
|
205 Liters (L)
Geometric Coefficient of Variation 25
|
187 Liters (L)
Geometric Coefficient of Variation 23
|
192 Liters (L)
Geometric Coefficient of Variation 26
|
204 Liters (L)
Geometric Coefficient of Variation 27
|
SECONDARY outcome
Timeframe: Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdosePopulation: All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY404039 (active moiety) plasma concentration data following administration of LY2140023.
Outcome measures
| Measure |
LY2140023 Reference Form
n=30 Participants
LY2140023: 80 milligrams (mg), administered once, orally.
|
LY2140023 Test-Low
n=28 Participants
LY2140023: 80 mg, low particle size, administered once, orally.
|
LY2140023 Test-Medium
n=28 Participants
LY2140023: 80 mg, medium particle size, administered once, orally.
|
LY2140023 Test-High
n=27 Participants
LY2140023: 80 mg, high particle size, administered once, orally.
|
|---|---|---|---|---|
|
Pharmacokinetics: Time of Maximum Observed Drug Concentrations (Tmax) of LY404039 (Active Moiety)
|
4.00 h
Interval 3.0 to 6.0
|
4.00 h
Interval 2.0 to 6.0
|
4.00 h
Interval 1.0 to 6.0
|
4.00 h
Interval 3.0 to 5.0
|
SECONDARY outcome
Timeframe: Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdosePopulation: All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY404039 (active moiety) plasma concentration data following administration of LY2140023.
Outcome measures
| Measure |
LY2140023 Reference Form
n=30 Participants
LY2140023: 80 milligrams (mg), administered once, orally.
|
LY2140023 Test-Low
n=28 Participants
LY2140023: 80 mg, low particle size, administered once, orally.
|
LY2140023 Test-Medium
n=28 Participants
LY2140023: 80 mg, medium particle size, administered once, orally.
|
LY2140023 Test-High
n=27 Participants
LY2140023: 80 mg, high particle size, administered once, orally.
|
|---|---|---|---|---|
|
Pharmacokinetics: Terminal Half Life (t1/2) of LY404039 (Active Moiety)
|
3.10 h
Interval 2.46 to 4.24
|
3.05 h
Interval 2.35 to 4.79
|
2.95 h
Interval 2.39 to 4.11
|
3.07 h
Interval 2.71 to 3.85
|
SECONDARY outcome
Timeframe: Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdosePopulation: All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY404039 (active moiety) plasma concentration data following administration of LY2140023.
Outcome measures
| Measure |
LY2140023 Reference Form
n=30 Participants
LY2140023: 80 milligrams (mg), administered once, orally.
|
LY2140023 Test-Low
n=28 Participants
LY2140023: 80 mg, low particle size, administered once, orally.
|
LY2140023 Test-Medium
n=28 Participants
LY2140023: 80 mg, medium particle size, administered once, orally.
|
LY2140023 Test-High
n=27 Participants
LY2140023: 80 mg, high particle size, administered once, orally.
|
|---|---|---|---|---|
|
Pharmacokinetics: Apparent Total Body Clearance (CL/F) of LY404039 (Active Moiety)
|
19.3 L/h
Geometric Coefficient of Variation 17
|
19.3 L/h
Geometric Coefficient of Variation 19
|
18.9 L/h
Geometric Coefficient of Variation 17
|
18.9 L/h
Geometric Coefficient of Variation 16
|
SECONDARY outcome
Timeframe: Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdosePopulation: All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY404039 (active moiety) plasma concentration data following administration of LY2140023.
Outcome measures
| Measure |
LY2140023 Reference Form
n=30 Participants
LY2140023: 80 milligrams (mg), administered once, orally.
|
LY2140023 Test-Low
n=28 Participants
LY2140023: 80 mg, low particle size, administered once, orally.
|
LY2140023 Test-Medium
n=28 Participants
LY2140023: 80 mg, medium particle size, administered once, orally.
|
LY2140023 Test-High
n=27 Participants
LY2140023: 80 mg, high particle size, administered once, orally.
|
|---|---|---|---|---|
|
Pharmacokinetics: Volume of Distribution During the Terminal Phase (Vz/F) of LY404039 (Active Moiety)
|
86.3 L
Geometric Coefficient of Variation 28
|
85.0 L
Geometric Coefficient of Variation 32
|
80.4 L
Geometric Coefficient of Variation 26
|
83.6 L
Geometric Coefficient of Variation 23
|
Adverse Events
LY2140023 Reference Form
Serious events: 0 serious events
Other events: 17 other events
Deaths: 0 deaths
LY2140023 Test-Low
Serious events: 0 serious events
Other events: 15 other events
Deaths: 0 deaths
LY2140023 Test-Medium
Serious events: 0 serious events
Other events: 12 other events
Deaths: 0 deaths
LY2140023 Test-High
Serious events: 0 serious events
Other events: 16 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
LY2140023 Reference Form
n=35 participants at risk
LY2140023: 80 mg, administered once, orally.
|
LY2140023 Test-Low
n=33 participants at risk
LY2140023: 80 mg, low particle size, administered once, orally.
|
LY2140023 Test-Medium
n=32 participants at risk
LY2140023: 80 mg, medium particle size, administered once, orally.
|
LY2140023 Test-High
n=32 participants at risk
LY2140023: 80 mg, high particle size, administered once, orally.
|
|---|---|---|---|---|
|
Gastrointestinal disorders
Abdominal pain upper
|
5.7%
2/35 • Number of events 2
|
0.00%
0/33
|
0.00%
0/32
|
0.00%
0/32
|
|
Gastrointestinal disorders
Diarrhoea
|
5.7%
2/35 • Number of events 2
|
0.00%
0/33
|
0.00%
0/32
|
3.1%
1/32 • Number of events 1
|
|
Gastrointestinal disorders
Nausea
|
31.4%
11/35 • Number of events 11
|
18.2%
6/33 • Number of events 6
|
21.9%
7/32 • Number of events 7
|
25.0%
8/32 • Number of events 8
|
|
Gastrointestinal disorders
Vomiting
|
14.3%
5/35 • Number of events 8
|
12.1%
4/33 • Number of events 6
|
12.5%
4/32 • Number of events 9
|
18.8%
6/32 • Number of events 10
|
|
General disorders
Feeling hot
|
2.9%
1/35 • Number of events 1
|
0.00%
0/33
|
0.00%
0/32
|
6.2%
2/32 • Number of events 2
|
|
Nervous system disorders
Dizziness
|
11.4%
4/35 • Number of events 4
|
6.1%
2/33 • Number of events 2
|
9.4%
3/32 • Number of events 3
|
12.5%
4/32 • Number of events 4
|
|
Nervous system disorders
Headache
|
14.3%
5/35 • Number of events 5
|
12.1%
4/33 • Number of events 5
|
12.5%
4/32 • Number of events 6
|
15.6%
5/32 • Number of events 8
|
|
Nervous system disorders
Presyncope
|
0.00%
0/35
|
6.1%
2/33 • Number of events 2
|
0.00%
0/32
|
3.1%
1/32 • Number of events 2
|
|
Nervous system disorders
Somnolence
|
0.00%
0/35
|
6.1%
2/33 • Number of events 2
|
3.1%
1/32 • Number of events 1
|
0.00%
0/32
|
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