Trial Outcomes & Findings for A Study of LY2140023 in Healthy Participants (NCT NCT01637142)
NCT ID: NCT01637142
Last Updated: 2021-09-21
Results Overview
Exposure of LY2140023 (parent compound), LY404039 (active metabolite), 14C-radiolabeled LY2140023, and 14C-radiolabeled LY404039 in terms of Area Under the Concentration Versus Time Curve from time 0 extrapolated to infinity (AUC\[0-inf\]) is summarized for participants in Treatment Period 1.
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
18 participants
Primary outcome timeframe
Predose and 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 |
Oral 80 mg LY2140023 on Two Separate Occasions
Participants received a single oral dose of 80 milligrams (mg) LY2140023 (parent compound) on 2 separate occasions.
In Treatment Period 1, a single oral dose of 80 mg LY2140023 followed by a single 2-hour intravenous (IV) infusion of approximately 100 micrograms (µg) LY2140023 containing approximately 100 nanocuries (nCi) \[14C\]-LY2140023.
In Treatment Period 2, a single oral dose of 80 mg LY2140023 followed by a single 2-hour IV infusion of approximately 100 µg LY404039 (active metabolite) containing approximately 100 nCi \[14C\]-LY404039.
There was a washout period of at least 3 days between Treatment Period 1 and Treatment Period 2.
|
|---|---|
|
Treatment Period 1
STARTED
|
18
|
|
Treatment Period 1
Received at Least 1 Dose of Study Drug
|
18
|
|
Treatment Period 1
COMPLETED
|
18
|
|
Treatment Period 1
NOT COMPLETED
|
0
|
|
Washout Period (at Least 3 Days)
STARTED
|
18
|
|
Washout Period (at Least 3 Days)
COMPLETED
|
17
|
|
Washout Period (at Least 3 Days)
NOT COMPLETED
|
1
|
|
Treatment Period 2
STARTED
|
17
|
|
Treatment Period 2
Received at Least 1 Dose of Study Drug
|
17
|
|
Treatment Period 2
COMPLETED
|
17
|
|
Treatment Period 2
NOT COMPLETED
|
0
|
Reasons for withdrawal
| Measure |
Oral 80 mg LY2140023 on Two Separate Occasions
Participants received a single oral dose of 80 milligrams (mg) LY2140023 (parent compound) on 2 separate occasions.
In Treatment Period 1, a single oral dose of 80 mg LY2140023 followed by a single 2-hour intravenous (IV) infusion of approximately 100 micrograms (µg) LY2140023 containing approximately 100 nanocuries (nCi) \[14C\]-LY2140023.
In Treatment Period 2, a single oral dose of 80 mg LY2140023 followed by a single 2-hour IV infusion of approximately 100 µg LY404039 (active metabolite) containing approximately 100 nCi \[14C\]-LY404039.
There was a washout period of at least 3 days between Treatment Period 1 and Treatment Period 2.
|
|---|---|
|
Washout Period (at Least 3 Days)
Physician Decision
|
1
|
Baseline Characteristics
A Study of LY2140023 in Healthy Participants
Baseline characteristics by cohort
| Measure |
Oral 80 mg LY2140023 on Two Separate Occasions
n=18 Participants
Participants received a single oral dose of 80 mg LY2140023 (parent compound) on 2 separate occasions.
In Treatment Period 1, a single oral dose of 80 mg LY2140023 followed by a single 2-hour IV infusion of approximately 100 µg LY2140023 containing approximately 100 nCi \[14C\]-LY2140023.
In Treatment Period 2, a single oral dose of 80 mg LY2140023 followed by a single 2-hour IV infusion of approximately 100 µg LY404039 (active metabolite) containing approximately 100 nCi \[14C\]-LY404039.
There was a washout period of at least 3 days between Treatment Period 1 and Treatment Period 2.
|
|---|---|
|
Age, Continuous
|
34.2 years
STANDARD_DEVIATION 11.5 • n=93 Participants
|
|
Sex: Female, Male
Female
|
0 Participants
n=93 Participants
|
|
Sex: Female, Male
Male
|
18 Participants
n=93 Participants
|
|
Ethnicity (NIH/OMB)
Hispanic or Latino
|
0 Participants
n=93 Participants
|
|
Ethnicity (NIH/OMB)
Not Hispanic or Latino
|
18 Participants
n=93 Participants
|
|
Ethnicity (NIH/OMB)
Unknown or Not Reported
|
0 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
|
0 Participants
n=93 Participants
|
|
Race (NIH/OMB)
White
|
18 Participants
n=93 Participants
|
|
Race (NIH/OMB)
More than one race
|
0 Participants
n=93 Participants
|
|
Race (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=93 Participants
|
|
Region of Enrollment
United Kingdom
|
18 participants
n=93 Participants
|
PRIMARY outcome
Timeframe: Predose and 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16 and 24 hours postdosePopulation: Participants who received oral LY2140023 with IV \[14C\]-LY2140023 and had evaluable pharmacokinetic (PK) concentration data.
Exposure of LY2140023 (parent compound), LY404039 (active metabolite), 14C-radiolabeled LY2140023, and 14C-radiolabeled LY404039 in terms of Area Under the Concentration Versus Time Curve from time 0 extrapolated to infinity (AUC\[0-inf\]) is summarized for participants in Treatment Period 1.
Outcome measures
| Measure |
Oral 80 mg LY2140023 and IV LY2140023/[14C]-LY2140023
n=18 Participants
In Treatment Period 1, a single oral dose of 80 mg LY2140023 followed by a single 2-hour IV infusion of approximately 100 µg LY2140023 containing approximately 100 nCi \[14C\]-LY2140023.
|
|---|---|
|
Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-inf]) of LY2140023 and LY404039 in Treatment Period 1
LY2140023 (parent compound)
|
1160 nanograms times hours per milliliter
Geometric Coefficient of Variation 28
|
|
Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-inf]) of LY2140023 and LY404039 in Treatment Period 1
LY404039 (active metabolite)
|
2620 nanograms times hours per milliliter
Geometric Coefficient of Variation 23
|
|
Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-inf]) of LY2140023 and LY404039 in Treatment Period 1
[14C]-LY2140023 (parent)
|
2.01 nanograms times hours per milliliter
Geometric Coefficient of Variation 22
|
|
Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-inf]) of LY2140023 and LY404039 in Treatment Period 1
[14C]-LY404039 (active metabolite)
|
6.19 nanograms times hours per milliliter
Geometric Coefficient of Variation 20
|
PRIMARY outcome
Timeframe: Predose and 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 12, 16 and 24 hours postdosePopulation: Participants who received oral LY2140023 with IV \[14C\]-LY404039 and had evaluable PK concentration data.
Exposure of LY2140023 (parent compound), LY404039 (active metabolite), and 14C-radiolabeled LY404039 in terms of Area Under the Concentration Versus Time Curve from time 0 extrapolated to infinity (AUC\[0-inf\]) is summarized for participants in Treatment Period 2.
Outcome measures
| Measure |
Oral 80 mg LY2140023 and IV LY2140023/[14C]-LY2140023
n=17 Participants
In Treatment Period 1, a single oral dose of 80 mg LY2140023 followed by a single 2-hour IV infusion of approximately 100 µg LY2140023 containing approximately 100 nCi \[14C\]-LY2140023.
|
|---|---|
|
Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-inf]) of LY2140023 and LY404039 in Treatment Period 2
LY2140023 (parent compound)
|
1200 nanograms times hours per milliliter
Geometric Coefficient of Variation 27
|
|
Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-inf]) of LY2140023 and LY404039 in Treatment Period 2
LY404039 (active metabolite)
|
2690 nanograms times hours per milliliter
Geometric Coefficient of Variation 21
|
|
Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-inf]) of LY2140023 and LY404039 in Treatment Period 2
[14C]-LY404039 (active metabolite)
|
7.69 nanograms times hours per milliliter
Geometric Coefficient of Variation 20
|
Adverse Events
Oral 80 mg LY2140023 and IV LY2140023/[14C]-LY2140023
Serious events: 0 serious events
Other events: 8 other events
Deaths: 0 deaths
Oral 80 mg LY2140023 and IV LY404039/[14C]-LY404039
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 |
Oral 80 mg LY2140023 and IV LY2140023/[14C]-LY2140023
n=18 participants at risk
Treatment Period 1: On Day 1, a single oral dose of 80 mg LY2140023 (parent compound) followed by a single 2-hour IV infusion of approximately 100 µg LY2140023 containing approximately 100 nCi \[14C\]-LY2140023.
|
Oral 80 mg LY2140023 and IV LY404039/[14C]-LY404039
n=17 participants at risk
Treatment Period 2: On Day 1, a single oral dose of 80 mg LY2140023 (parent compound) followed by a single 2-hour IV infusion of approximately 100 µg LY404039 (active metabolite) containing approximately 100 nCi \[14C\]-LY404039.
|
|---|---|---|
|
Gastrointestinal disorders
Toothache
|
5.6%
1/18 • Number of events 1
|
0.00%
0/17
|
|
General disorders
Application site erythema
|
0.00%
0/18
|
5.9%
1/17 • Number of events 1
|
|
General disorders
Catheter site erythema
|
0.00%
0/18
|
11.8%
2/17 • Number of events 2
|
|
Infections and infestations
Herpes simplex
|
5.6%
1/18 • Number of events 1
|
0.00%
0/17
|
|
Injury, poisoning and procedural complications
Excoriation
|
5.6%
1/18 • Number of events 1
|
0.00%
0/17
|
|
Musculoskeletal and connective tissue disorders
Arthralgia
|
0.00%
0/18
|
5.9%
1/17 • Number of events 1
|
|
Nervous system disorders
Dizziness
|
11.1%
2/18 • Number of events 2
|
0.00%
0/17
|
|
Nervous system disorders
Headache
|
5.6%
1/18 • Number of events 1
|
0.00%
0/17
|
|
Nervous system disorders
Somnolence
|
27.8%
5/18 • Number of events 5
|
41.2%
7/17 • Number of events 7
|
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