Trial Outcomes & Findings for A Study of the Absorption, Distribution, Metabolism and Excretion of LY3039478 in Healthy Participants (NCT NCT02917733)

NCT ID: NCT02917733

Last Updated: 2025-07-28

Results Overview

To determine the disposition of radioactivity and LY3039478 in healthy participants following oral administration of a single dose 14C-labeled LY3039478.

• Recruitment status: COMPLETED
• Study phase: PHASE1
• Target enrollment: 6 participants
• Primary outcome timeframe: Predose, and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, and 312 hours postdose
• Results posted on: 2025-07-28

Participant Flow

Participant milestones

Measure	75 mg [14C2] LY3039478 Participants received approximately 75 mg \[14C2\] LY3039478 containing approximately 100 μCi \[14C2\] LY3039478.
Overall Study STARTED	6
Overall Study COMPLETED	6
Overall Study NOT COMPLETED	0

Reasons for withdrawal

Withdrawal data not reported

Baseline Characteristics

A Study of the Absorption, Distribution, Metabolism and Excretion of LY3039478 in Healthy Participants

Baseline characteristics by cohort

Measure	75 mg [14C2] LY3039478 n=6 Participants Participants received approximately 75 mg \[14C2\] LY3039478 containing approximately 100 μCi \[14C2\] LY3039478.
Age, Continuous	55.0 years STANDARD_DEVIATION 8.7 • n=5 Participants
Sex: Female, Male Female	3 Participants n=5 Participants
Sex: Female, Male Male	3 Participants n=5 Participants
Race (NIH/OMB) American Indian or Alaska Native	0 Participants n=5 Participants
Race (NIH/OMB) Asian	0 Participants n=5 Participants
Race (NIH/OMB) Native Hawaiian or Other Pacific Islander	0 Participants n=5 Participants
Race (NIH/OMB) Black or African American	2 Participants n=5 Participants
Race (NIH/OMB) White	4 Participants n=5 Participants
Race (NIH/OMB) More than one race	0 Participants n=5 Participants
Race (NIH/OMB) Unknown or Not Reported	0 Participants n=5 Participants
Region of Enrollment United States	6 Participants n=5 Participants

PRIMARY outcome

Timeframe: Predose, and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, and 312 hours postdose

Population: All participants who received the \[14C2\]-LY3039478 dose.

To determine the disposition of radioactivity and LY3039478 in healthy participants following oral administration of a single dose 14C-labeled LY3039478.

Outcome measures

Measure	75 mg [14C2] LY3039478 n=6 Participants Participants received approximately 75 mg \[14C2\] LY3039478 containing approximately 100 μCi \[14C2\] LY3039478.
Urinary and Fecal Excretion of Radioactivity Over Time Expressed as a Percentage of the Total Radioactive Dose Administered	90.2 percentage of administered radioactivity Standard Deviation 2.32

SECONDARY outcome

Timeframe: Predose, and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All the participants who received \[14C2\]-LY3039478 dose and had evaluable data for this outcome.

The AUC[0-inf]) for plasma LY3039478 was evaluated by using a combination of the linear and logarithmic trapezoidal methods (linear-log trapezoidal rule).

Outcome measures

Measure	75 mg [14C2] LY3039478 n=5 Participants Participants received approximately 75 mg \[14C2\] LY3039478 containing approximately 100 μCi \[14C2\] LY3039478.
Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-inf]) of LY3039478	2570 nanograms*hour/milliliter (ng*h/mL) Geometric Coefficient of Variation 11

SECONDARY outcome

Timeframe: Predose, and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All the participants who received \[14C2\]-LY3039478 dose and had evaluable data for this outcome.

The AUC[0-inf]) for total plasma radioactivity was evaluated by using a combination of the linear and logarithmic trapezoidal methods (linear-log trapezoidal rule).

Outcome measures

Measure	75 mg [14C2] LY3039478 n=4 Participants Participants received approximately 75 mg \[14C2\] LY3039478 containing approximately 100 μCi \[14C2\] LY3039478.
Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-inf]) of Total Plasma Radioactivity	26100 ng quivalents*hour/gram (ng equiv.h/g) Geometric Coefficient of Variation 21

SECONDARY outcome

Timeframe: Predose, and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All the participants who received \[14C2\]-LY3039478 dose and had evaluable data for this outcome.

The Cmax of LY3039478 was evaluated.

Outcome measures

Measure	75 mg [14C2] LY3039478 n=5 Participants Participants received approximately 75 mg \[14C2\] LY3039478 containing approximately 100 μCi \[14C2\] LY3039478.
Pharmacokinetics: Maximum Observed Concentration (Cmax) of LY3039478	517 Nanograms/milliliter (ng/ml) Geometric Coefficient of Variation 15

SECONDARY outcome

Timeframe: Predose, and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received \[14C2\]-LY3039478 dose and had evaluable data for this outcome.

Cmax of total plasma radioactivity was evaluated.

Outcome measures

Measure	75 mg [14C2] LY3039478 n=5 Participants Participants received approximately 75 mg \[14C2\] LY3039478 containing approximately 100 μCi \[14C2\] LY3039478.
Pharmacokinetics: Maximum Observed Concentration (Cmax) of Total Plasma Radioactivity	1060 Nanograms equivalents/gram (ng equiv/g) Geometric Coefficient of Variation 10

SECONDARY outcome

Timeframe: Predose, and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose.

Population: All participants who received \[14C2\]-LY3039478 dose. For the feces profiling, only one participant had quantifiable radioactive dose recovered in feces adequate for metabolite profiling and was therefore eligible for analysis.

Following oral administration, radio high performance liquid chromatography (HPLC) and liquid chromatography-mass spectrometry (LC-MS) profiles were obtained from analysis of plasma, urine and feces.

Outcome measures

Measure	75 mg [14C2] LY3039478 n=6 Participants Participants received approximately 75 mg \[14C2\] LY3039478 containing approximately 100 μCi \[14C2\] LY3039478.
Total Number of Metabolites of LY3039478 in Plasma, Urine and Feces Number of Metabolites of LY3039478 in Plasma	8 Metabolites
Total Number of Metabolites of LY3039478 in Plasma, Urine and Feces Number of Metabolites of LY3039478 in Urine	10 Metabolites
Total Number of Metabolites of LY3039478 in Plasma, Urine and Feces Number of Metabolites of LY3039478 in Feces	3 Metabolites

Adverse Events

75 mg [14C2] LY3039478

Serious events: 0 serious events

Other events: 6 other events

Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Measure	75 mg [14C2] LY3039478 n=6 participants at risk All the participants received approximately 75 mg \[14C2\] LY3039478 containing approximately 100 μCi \[14C2\] LY3039478, with the exception of participant 01005 who received a lower than expected dose (84.5249 µCi, rather than the target dose of 100 µCi).
Gastrointestinal disorders Abdominal discomfort	16.7% 1/6 • Number of events 1 All the participants who received the \[14C2\]-LY3039478 dose.
Gastrointestinal disorders Constipation	33.3% 2/6 • Number of events 2 All the participants who received the \[14C2\]-LY3039478 dose.
Gastrointestinal disorders Haematochezia	16.7% 1/6 • Number of events 1 All the participants who received the \[14C2\]-LY3039478 dose.
Gastrointestinal disorders Nausea	16.7% 1/6 • Number of events 1 All the participants who received the \[14C2\]-LY3039478 dose.
General disorders Chills	16.7% 1/6 • Number of events 1 All the participants who received the \[14C2\]-LY3039478 dose.
General disorders Fatigue	33.3% 2/6 • Number of events 2 All the participants who received the \[14C2\]-LY3039478 dose.
General disorders Feeling hot	16.7% 1/6 • Number of events 1 All the participants who received the \[14C2\]-LY3039478 dose.
Injury, poisoning and procedural complications Scratch	16.7% 1/6 • Number of events 1 All the participants who received the \[14C2\]-LY3039478 dose.
Injury, poisoning and procedural complications Skin abrasion	16.7% 1/6 • Number of events 1 All the participants who received the \[14C2\]-LY3039478 dose.
Musculoskeletal and connective tissue disorders Back pain	16.7% 1/6 • Number of events 1 All the participants who received the \[14C2\]-LY3039478 dose.
Musculoskeletal and connective tissue disorders Myalgia	16.7% 1/6 • Number of events 1 All the participants who received the \[14C2\]-LY3039478 dose.
Nervous system disorders Dizziness	16.7% 1/6 • Number of events 1 All the participants who received the \[14C2\]-LY3039478 dose.
Nervous system disorders Headache	33.3% 2/6 • Number of events 2 All the participants who received the \[14C2\]-LY3039478 dose.
Nervous system disorders Presyncope	16.7% 1/6 • Number of events 1 All the participants who received the \[14C2\]-LY3039478 dose.
Respiratory, thoracic and mediastinal disorders Dry throat	16.7% 1/6 • Number of events 1 All the participants who received the \[14C2\]-LY3039478 dose.
Respiratory, thoracic and mediastinal disorders Epistaxis	16.7% 1/6 • Number of events 1 All the participants who received the \[14C2\]-LY3039478 dose.
Respiratory, thoracic and mediastinal disorders Oropharyngeal pain	16.7% 1/6 • Number of events 1 All the participants who received the \[14C2\]-LY3039478 dose.
Respiratory, thoracic and mediastinal disorders Sinus congestion	16.7% 1/6 • Number of events 1 All the participants who received the \[14C2\]-LY3039478 dose.
Skin and subcutaneous tissue disorders Erythema	16.7% 1/6 • Number of events 1 All the participants who received the \[14C2\]-LY3039478 dose.

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: LTE60