Trial Outcomes & Findings for A Study of LY2140023 in Healthy Participants (NCT NCT01609218)

NCT ID: NCT01609218

Last Updated: 2021-09-21

Results Overview

Venous blood samples were collected for pharmacokinetic parameter estimates for LY2140023 alone and in the presence of aqueous activated charcoal.

• Recruitment status: COMPLETED
• Study phase: PHASE1
• Target enrollment: 27 participants
• Primary outcome timeframe: Predose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose
• Results posted on: 2021-09-21

Participant Flow

This was a 2-period crossover study. Participants received single doses of LY2140023 on 2 different occasions: 1) LY2140023 administered alone (Treatment A) and 2) LY2140023 administered and followed 1 hour later by a single dose of aqueous activated charcoal (Treatment B). Participants were randomized to Treatment Sequence AB or BA.

Participant milestones

Measure	First LY2140023 Alone, Then LY2140023 + Activated Charcoal Period 1: Single oral dose of 80 milligrams (mg) LY2140023 administered alone Period 2: Single oral dose of 80 mg LY2140023 followed 1 hour later by single oral dose of 75 grams (g) aqueous activated charcoal There was a washout period of at least 3 days between dosing occasions.	First LY2140023 + Activated Charcoal, Then LY2140023 Alone Period 1: Single oral dose of 80 mg LY2140023 followed 1 hour later by single oral dose of 75 g aqueous activated charcoal Period 2: Single oral dose of 80 mg LY2140023 administered alone There was a washout period of at least 3 days between dosing occasions.
Period 1 STARTED	13	14
Period 1 Received LY2140023	13	14
Period 1 Received Activated Charcoal	0	12
Period 1 COMPLETED	10	8
Period 1 NOT COMPLETED	3	6
Period 2 STARTED	10	9
Period 2 Received LY2140023	10	9
Period 2 Received Activated Charcoal	9	0
Period 2 COMPLETED	9	9
Period 2 NOT COMPLETED	1	0

Reasons for withdrawal

Measure	First LY2140023 Alone, Then LY2140023 + Activated Charcoal Period 1: Single oral dose of 80 milligrams (mg) LY2140023 administered alone Period 2: Single oral dose of 80 mg LY2140023 followed 1 hour later by single oral dose of 75 grams (g) aqueous activated charcoal There was a washout period of at least 3 days between dosing occasions.	First LY2140023 + Activated Charcoal, Then LY2140023 Alone Period 1: Single oral dose of 80 mg LY2140023 followed 1 hour later by single oral dose of 75 g aqueous activated charcoal Period 2: Single oral dose of 80 mg LY2140023 administered alone There was a washout period of at least 3 days between dosing occasions.
Period 1 Adverse Event	3	5
Period 1 Sponsor Decision	0	1
Period 2 Adverse Event	1	0

Baseline Characteristics

A Study of LY2140023 in Healthy Participants

Baseline characteristics by cohort

Measure	All Participants n=27 Participants This was 2-period crossover study. Participants received single oral doses of LY2140023 on 2 different occasions: 1) 80 mg LY2140023 administered alone (Treatment A) and 2) 80 mg LY2140023 administered and followed 1 hour later by a single oral dose of 75 g aqueous activated charcoal (Treatment B). Participants were randomly assigned to treatment sequence AB or BA.
Age, Continuous	29.1 years STANDARD_DEVIATION 14.0 • n=5 Participants
Sex: Female, Male Female	8 Participants n=5 Participants
Sex: Female, Male Male	19 Participants n=5 Participants
Race/Ethnicity, Customized White	24 participants n=5 Participants
Race/Ethnicity, Customized Black or African American	1 participants n=5 Participants
Race/Ethnicity, Customized Asian	2 participants n=5 Participants
Region of Enrollment United Kingdom	27 participants n=5 Participants

PRIMARY outcome

Timeframe: Predose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose

Population: Participants who received study drug(s), did not have an incidence of vomiting following administration of LY2140023, and had evaluable Cmax data.

Venous blood samples were collected for pharmacokinetic parameter estimates for LY2140023 alone and in the presence of aqueous activated charcoal.

Outcome measures

Measure	80 mg LY2140023 n=18 Participants Single oral dose of 80 mg LY2140023 administered alone	80 mg LY2140023 + 75 g Aqueous Activated Charcoal n=14 Participants Single oral dose of 80 mg LY2140023 followed 1 hour later by single oral dose of 75 g aqueous activated charcoal
Pharmacokinetics: Maximum Observed Plasma Concentration (Cmax) of LY2140023	251 nanograms per milliliter (ng/mL) Geometric Coefficient of Variation 31	171 nanograms per milliliter (ng/mL) Geometric Coefficient of Variation 25

PRIMARY outcome

Timeframe: Predose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose

Population: Participants who received study drug(s), did not have an incidence of vomiting following administration of LY2140023, and had evaluable AUC(0-inf) data.

Venous blood samples were collected for pharmacokinetic parameter estimates for LY2140023 alone and in the presence of aqueous activated charcoal.

Outcome measures

Measure	80 mg LY2140023 n=18 Participants Single oral dose of 80 mg LY2140023 administered alone	80 mg LY2140023 + 75 g Aqueous Activated Charcoal n=14 Participants Single oral dose of 80 mg LY2140023 followed 1 hour later by single oral dose of 75 g aqueous activated charcoal
Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-inf]) of LY2140023	1120 nanogram hours per milliliter (ng*h/mL) Geometric Coefficient of Variation 24	876 nanogram hours per milliliter (ng*h/mL) Geometric Coefficient of Variation 26

PRIMARY outcome

Timeframe: Predose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose

Population: Participants who received study drug(s), did not have an incidence of vomiting following administration of LY2140023, and had evaluable Cmax data.

Venous blood samples were collected for pharmacokinetic parameter estimates for LY404039 alone and in the presence of aqueous activated charcoal.

Outcome measures

Measure	80 mg LY2140023 n=18 Participants Single oral dose of 80 mg LY2140023 administered alone	80 mg LY2140023 + 75 g Aqueous Activated Charcoal n=14 Participants Single oral dose of 80 mg LY2140023 followed 1 hour later by single oral dose of 75 g aqueous activated charcoal
Pharmacokinetics: Maximum Observed Plasma Concentration (Cmax) of LY404039 (Active Moiety)	474 ng/mL Geometric Coefficient of Variation 26	324 ng/mL Geometric Coefficient of Variation 20

PRIMARY outcome

Timeframe: Predose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose

Population: Participants who received study drug(s), did not have an incidence of vomiting following administration of LY2140023, and had evaluable AUC(0-inf) data.

Venous blood samples were collected for pharmacokinetic parameter estimates for LY404039 alone and in the presence of aqueous activated charcoal.

Outcome measures

Measure	80 mg LY2140023 n=18 Participants Single oral dose of 80 mg LY2140023 administered alone	80 mg LY2140023 + 75 g Aqueous Activated Charcoal n=14 Participants Single oral dose of 80 mg LY2140023 followed 1 hour later by single oral dose of 75 g aqueous activated charcoal
Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-inf]) of LY404039 (Active Moiety)	2780 ng*h/mL Geometric Coefficient of Variation 15	2190 ng*h/mL Geometric Coefficient of Variation 19

Adverse Events

80 mg LY2140023

Serious events: 0 serious events

Other events: 16 other events

Deaths: 0 deaths

80 mg LY2140023 + 75 g Aqueous Activated Charcoal

Serious events: 0 serious events

Other events: 13 other events

Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Measure	80 mg LY2140023 n=22 participants at risk Single oral dose of 80 mg LY2140023 administered alone	80 mg LY2140023 + 75 g Aqueous Activated Charcoal n=24 participants at risk Single oral dose of 80 mg LY2140023 followed 1 hour later by single oral dose of 75 g aqueous activated charcoal
Gastrointestinal disorders Nausea	40.9% 9/22 • Number of events 12	33.3% 8/24 • Number of events 8
Gastrointestinal disorders Vomiting	31.8% 7/22 • Number of events 11	29.2% 7/24 • Number of events 7
General disorders Feeling hot	18.2% 4/22 • Number of events 4	4.2% 1/24 • Number of events 1
Nervous system disorders Dizziness	22.7% 5/22 • Number of events 5	0.00% 0/24
Nervous system disorders Headache	27.3% 6/22 • Number of events 6	12.5% 3/24 • Number of events 3

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