Trial Outcomes & Findings for Safety, Tolerability, and Pharmacokinetics of Oral EC5026 in Healthy Subjects (NCT NCT04228302)

Results Overview

All AEs reported or observed during the study will be recorded on the electronic case report forms (eCRF). Information to be collected includes drug treatment, type of event, time of onset, dosage, investigator-specified assessment of severity and relationship to study drug, time of resolution of the event, seriousness, any required treatment or evaluations, and outcome. Any AEs resulting from concurrent illnesses, reactions to concurrent illnesses, reactions to concurrent medications, or progression of disease states must also be reported. All AEs will be followed until they are resolved, stable, or judged by the investigator to be not clinically significant. The Medical Dictionary for Regulatory Activities will be used to code all AEs. A TEAE is defined as any event not present before exposure to study drug or any event already present that worsens in intensity or frequency after exposure.

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

40 participants

Primary outcome timeframe

14 days

Results posted on

2021-07-01

Participant Flow

Participant milestones

Participant milestones
Measure	EC5026 0.5 mg Single 0.5 mg dose of oral EC5026	EC5026 2 mg Single 2 mg dose of oral EC5026	EC5026 8 mg Single 8 mg dose of oral EC5026	EC5026 16 mg Single 16 mg dose of oral EC5026	EC5026 24 mg Single 24 mg dose of oral EC5026	Placebo Single dose of matching oral placebo
Overall Study STARTED	6	6	6	6	6	10
Overall Study COMPLETED	6	6	6	6	5	10
Overall Study NOT COMPLETED	0	0	0	0	1	0

Reasons for withdrawal

Reasons for withdrawal
Measure	EC5026 0.5 mg Single 0.5 mg dose of oral EC5026	EC5026 2 mg Single 2 mg dose of oral EC5026	EC5026 8 mg Single 8 mg dose of oral EC5026	EC5026 16 mg Single 16 mg dose of oral EC5026	EC5026 24 mg Single 24 mg dose of oral EC5026	Placebo Single dose of matching oral placebo
Overall Study Adverse Event	0	0	0	0	1	0

Baseline Characteristics

Safety, Tolerability, and Pharmacokinetics of Oral EC5026 in Healthy Subjects

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure	EC5026 0.5 mg n=6 Participants Single 0.5 mg dose of oral EC5026	EC5026 2 mg n=6 Participants Single 2 mg dose of oral EC5026	EC5026 8 mg n=6 Participants Single 8 mg dose of oral EC5026	EC5026 16 mg n=6 Participants Single 16 mg dose of oral EC5026	EC5026 24 mg n=6 Participants Single 24 mg dose of oral EC5026	Placebo n=10 Participants Single dose of matching oral placebo	Total n=40 Participants Total of all reporting groups
Age, Continuous	40.5 years n=5 Participants	33.5 years n=7 Participants	28.0 years n=5 Participants	42.0 years n=4 Participants	37.5 years n=21 Participants	45.0 years n=10 Participants	36.0 years n=115 Participants
Sex: Female, Male Female	2 Participants n=5 Participants	3 Participants n=7 Participants	4 Participants n=5 Participants	4 Participants n=4 Participants	4 Participants n=21 Participants	5 Participants n=10 Participants	22 Participants n=115 Participants
Sex: Female, Male Male	4 Participants n=5 Participants	3 Participants n=7 Participants	2 Participants n=5 Participants	2 Participants n=4 Participants	2 Participants n=21 Participants	5 Participants n=10 Participants	18 Participants n=115 Participants
Ethnicity (NIH/OMB) Hispanic or Latino	2 Participants n=5 Participants	1 Participants n=7 Participants	2 Participants n=5 Participants	3 Participants n=4 Participants	5 Participants n=21 Participants	4 Participants n=10 Participants	17 Participants n=115 Participants
Ethnicity (NIH/OMB) Not Hispanic or Latino	4 Participants n=5 Participants	5 Participants n=7 Participants	4 Participants n=5 Participants	3 Participants n=4 Participants	1 Participants n=21 Participants	6 Participants n=10 Participants	23 Participants n=115 Participants
Ethnicity (NIH/OMB) Unknown or Not Reported	0 Participants n=5 Participants	0 Participants n=7 Participants	0 Participants n=5 Participants	0 Participants n=4 Participants	0 Participants n=21 Participants	0 Participants n=10 Participants	0 Participants n=115 Participants
Race (NIH/OMB) American Indian or Alaska Native	0 Participants n=5 Participants	0 Participants n=7 Participants	0 Participants n=5 Participants	0 Participants n=4 Participants	0 Participants n=21 Participants	0 Participants n=10 Participants	0 Participants n=115 Participants
Race (NIH/OMB) Asian	0 Participants n=5 Participants	0 Participants n=7 Participants	0 Participants n=5 Participants	0 Participants n=4 Participants	0 Participants n=21 Participants	0 Participants n=10 Participants	0 Participants n=115 Participants
Race (NIH/OMB) Native Hawaiian or Other Pacific Islander	0 Participants n=5 Participants	0 Participants n=7 Participants	0 Participants n=5 Participants	0 Participants n=4 Participants	0 Participants n=21 Participants	0 Participants n=10 Participants	0 Participants n=115 Participants
Race (NIH/OMB) Black or African American	3 Participants n=5 Participants	3 Participants n=7 Participants	3 Participants n=5 Participants	1 Participants n=4 Participants	0 Participants n=21 Participants	4 Participants n=10 Participants	14 Participants n=115 Participants
Race (NIH/OMB) White	3 Participants n=5 Participants	3 Participants n=7 Participants	3 Participants n=5 Participants	5 Participants n=4 Participants	6 Participants n=21 Participants	6 Participants n=10 Participants	26 Participants n=115 Participants
Race (NIH/OMB) More than one race	0 Participants n=5 Participants	0 Participants n=7 Participants	0 Participants n=5 Participants	0 Participants n=4 Participants	0 Participants n=21 Participants	0 Participants n=10 Participants	0 Participants n=115 Participants
Race (NIH/OMB) Unknown or Not Reported	0 Participants n=5 Participants	0 Participants n=7 Participants	0 Participants n=5 Participants	0 Participants n=4 Participants	0 Participants n=21 Participants	0 Participants n=10 Participants	0 Participants n=115 Participants
Region of Enrollment United States	6 participants n=5 Participants	6 participants n=7 Participants	6 participants n=5 Participants	6 participants n=4 Participants	6 participants n=21 Participants	10 participants n=10 Participants	40 participants n=115 Participants

PRIMARY outcome

Timeframe: 14 days

All AEs reported or observed during the study will be recorded on the electronic case report forms (eCRF). Information to be collected includes drug treatment, type of event, time of onset, dosage, investigator-specified assessment of severity and relationship to study drug, time of resolution of the event, seriousness, any required treatment or evaluations, and outcome. Any AEs resulting from concurrent illnesses, reactions to concurrent illnesses, reactions to concurrent medications, or progression of disease states must also be reported. All AEs will be followed until they are resolved, stable, or judged by the investigator to be not clinically significant. The Medical Dictionary for Regulatory Activities will be used to code all AEs. A TEAE is defined as any event not present before exposure to study drug or any event already present that worsens in intensity or frequency after exposure.

Outcome measures

Outcome measures
Measure	EC5026 0.5 mg n=6 Participants Single 0.5 mg dose of oral EC5026	EC5026 2 mg n=6 Participants Single 2 mg dose of oral EC5026	EC5026 8 mg n=6 Participants Single 8 mg dose of oral EC5026	EC5026 16 mg n=6 Participants Single 16 mg dose of oral EC5026	EC5026 24 mg n=6 Participants Single 24 mg dose of oral EC5026	Placebo n=10 Participants Single dose of matching oral placebo
Incidence of Adverse Events (AEs) [Safety and Tolerability] Any Treatment Emergent Adverse Event (TEAE)	2 Participants	4 Participants	2 Participants	4 Participants	4 Participants	3 Participants
Incidence of Adverse Events (AEs) [Safety and Tolerability] Any Treatment-Related TEAE	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants
Incidence of Adverse Events (AEs) [Safety and Tolerability] Any Adverse Events	2 Participants	4 Participants	3 Participants	6 Participants	4 Participants	5 Participants

PRIMARY outcome

Timeframe: Predose (0 hour), and at 1.25, 2.25, 4.25, 6.25, 8.25, 12.25, 24, 36, 48, 72, 84, 96, and 108 hours after dosing

Population: Plasma concentrations following EC5026 0.5 mg were below the limit of quantification for all subjects at all timepoints. For 2 subjects in the EC5026 2 mg dose group, plasma concentrations were quantifiable in fewer than 3 samples. These subjects were excluded from the PK population.

Standard noncompartmental methods will be used to determine the AUC in response to single oral doses of 0.5, 2, 8,16, and 24 mg of EC5026. The PK population will include subjects who received a single dose of EC5026 and have sufficient concentration data to support accurate estimation of at least 1 PK parameter. Subjects were excluded from the PK population when there were fewer than 3 quantifiable plasma samples.

Outcome measures

Outcome measures
Measure	EC5026 0.5 mg Single 0.5 mg dose of oral EC5026	EC5026 2 mg n=4 Participants Single 2 mg dose of oral EC5026	EC5026 8 mg n=6 Participants Single 8 mg dose of oral EC5026	EC5026 16 mg n=6 Participants Single 16 mg dose of oral EC5026	EC5026 24 mg n=6 Participants Single 24 mg dose of oral EC5026	Placebo Single dose of matching oral placebo
Area Under the Plasma Concentration Versus Time Curve From Time 0 to the Last Quantifiable Concentration (AUC 0-t) in Response to Escalating Dose Regimens of Oral EC5026 [Plasma Pharmacokinetics].	—	258 ng*h/mL Geometric Coefficient of Variation 145.4	3450 ng*h/mL Geometric Coefficient of Variation 28.4	6780 ng*h/mL Geometric Coefficient of Variation 23.1	9030 ng*h/mL Geometric Coefficient of Variation 22.1	—

PRIMARY outcome

Timeframe: Predose (0 hour), and at 1.25, 2.25, 4.25, 6.25, 8.25, 12.25, 24, 36, 48, 72, 84, 96, and 108 hours after dosing

Population: Plasma concentrations following EC5026 0.5 mg were below the limit of quantification for all subjects at all time points. For 2 subjects in the EC5026 2 mg dose group, plasma concentrations were quantifiable in fewer than 3 samples.

Standard noncompartmental methods will be used to determine the Cmax in response to single oral doses of 0.5, 2, 8,16, and 24 mg of EC5026. The PK population will include subjects who received a single dose of EC5026 and have sufficient concentration data to support accurate estimation of at least 1 PK parameter. Subjects were excluded from the PK population when there were fewer than 3 quantifiable plasma samples.

Outcome measures

Outcome measures
Measure	EC5026 0.5 mg Single 0.5 mg dose of oral EC5026	EC5026 2 mg n=4 Participants Single 2 mg dose of oral EC5026	EC5026 8 mg n=6 Participants Single 8 mg dose of oral EC5026	EC5026 16 mg n=6 Participants Single 16 mg dose of oral EC5026	EC5026 24 mg n=6 Participants Single 24 mg dose of oral EC5026	Placebo Single dose of matching oral placebo
Maximum Observed Plasma Concentration (Cmax) in Response to Escalating Dose Regimens of Oral EC5026 [Plasma Pharmacokinetics].	—	4.69 ng/mL Geometric Coefficient of Variation 45.8	82.7 ng/mL Geometric Coefficient of Variation 11.1	220 ng/mL Geometric Coefficient of Variation 16.2	301 ng/mL Geometric Coefficient of Variation 14.6	—

PRIMARY outcome

Timeframe: Predose (0 hour), and at 1.25, 2.25, 4.25, 6.25, 8.25, 12.25, 24, 36, 48, 72, 84, 96, and 108 hours after dosing

Population: Plasma concentrations following EC5026 0.5 mg were below the limit of quantification for all subjects at all time points. For 2 subjects in the EC5026 2 mg dose group, plasma concentrations were quantifiable in fewer than 3 samples.

Standard noncompartmental methods will be used to determine the Tmax in response to single oral doses of 0.5, 2, 8,16, and 24 mg of EC5026. The PK population will include subjects who received a single dose of EC5026 and have sufficient concentration data to support accurate estimation of at least 1 PK parameter. Subjects were excluded from the PK population when there were fewer than 3 quantifiable plasma samples.

Outcome measures

Outcome measures
Measure	EC5026 0.5 mg Single 0.5 mg dose of oral EC5026	EC5026 2 mg n=4 Participants Single 2 mg dose of oral EC5026	EC5026 8 mg n=6 Participants Single 8 mg dose of oral EC5026	EC5026 16 mg n=6 Participants Single 16 mg dose of oral EC5026	EC5026 24 mg n=6 Participants Single 24 mg dose of oral EC5026	Placebo Single dose of matching oral placebo
Time to Maximum Observed Plasma Concentration (Tmax) in Response to Escalating Dose Regimens of Oral EC5026 [Plasma Pharmacokinetics].	—	1.25 hours Interval 1.25 to 1.3	1.25 hours Interval 1.25 to 1.3	1.25 hours Interval 1.25 to 1.25	1.25 hours Interval 1.25 to 1.25	—

PRIMARY outcome

Timeframe: Predose (0 hour), and at 1.25, 2.25, 4.25, 6.25, 8.25, 12.25, 24, 36, 48, 72, 84, 96, and 108 hours after dosing

Population: Plasma concentrations following EC5026 0.5 mg were below the limit of quantification for all subjects at all time points. For 2 subjects in the EC5026 2 mg dose group, plasma concentrations were quantifiable in fewer than 3 samples. Given that plasma concentrations for the 2 mg dose group were near the limit of quantification, the estimates for t½ should be viewed with caution.

Standard noncompartmental methods will be used to determine the t1/2 in response to single oral doses of 0.5, 2, 8,16, and 24 mg of EC5026. The PK population will include subjects who received a single dose of EC5026 and have sufficient concentration data to support accurate estimation of at least 1 PK parameter. Subjects were excluded from the PK population when there were fewer than 3 quantifiable plasma samples.

Outcome measures

Outcome measures
Measure	EC5026 0.5 mg Single 0.5 mg dose of oral EC5026	EC5026 2 mg n=4 Participants Single 2 mg dose of oral EC5026	EC5026 8 mg n=6 Participants Single 8 mg dose of oral EC5026	EC5026 16 mg n=6 Participants Single 16 mg dose of oral EC5026	EC5026 24 mg n=6 Participants Single 24 mg dose of oral EC5026	Placebo Single dose of matching oral placebo
Terminal Phase Half-life in Plasma (t1/2) in Response to Escalating Dose Regimens of Oral EC5026 [Plasma Pharmacokinetics].	—	143 hours Standard Deviation 63.3	59.1 hours Standard Deviation 19.0	44.8 hours Standard Deviation 14.0	41.8 hours Standard Deviation 14.6	—

PRIMARY outcome

Timeframe: Predose (0 hour), and at 1.25, 2.25, 4.25, 6.25, 8.25, 12.25, 24, 36, 48, 72, 84, 96, and 108 hours after dosing

Population: Values for CL/F were excluded from summary statistics when %AUCextrap was \>20%. Plasma concentrations following EC5026 0.5 mg were below the limit of quantification for all subjects at all time points. For 2 subjects in the EC5026 2 mg dose group, plasma concentrations were quantifiable in fewer than 3 samples.

Standard noncompartmental methods will be used to determine the CL/F in response to single oral doses of 0.5, 2, 8,16, and 24 mg of EC5026. The PK population will include subjects who received a single dose of EC5026 and have sufficient concentration data to support accurate estimation of at least 1 PK parameter. Subjects were excluded from the PK population when there were fewer than 3 quantifiable plasma samples.

Outcome measures

Outcome measures
Measure	EC5026 0.5 mg Single 0.5 mg dose of oral EC5026	EC5026 2 mg Single 2 mg dose of oral EC5026	EC5026 8 mg n=6 Participants Single 8 mg dose of oral EC5026	EC5026 16 mg n=6 Participants Single 16 mg dose of oral EC5026	EC5026 24 mg n=6 Participants Single 24 mg dose of oral EC5026	Placebo Single dose of matching oral placebo
Apparent Total Body Clearance (CL/F) in Response to Escalating Dose Regimens of Oral EC5026 [Plasma Pharmacokinetics].	—	—	2.23 L/h Standard Deviation 0.56	2.35 L/h Standard Deviation 0.52	2.62 L/h Standard Deviation 0.54	—

PRIMARY outcome

Timeframe: Predose (0 hour), and at 1.25, 2.25, 4.25, 6.25, 8.25, 12.25, 24, 36, 48, 72, 84, 96, and 108 hours after dosing

Population: Plasma concentrations following EC5026 0.5 mg were below the limit of quantification for all subjects at all time points. For 2 subjects in the EC5026 2 mg dose group, plasma concentrations were quantifiable in fewer than 3 samples. Values for Vz/F were excluded from summary statistics when %AUCextrap was \>20.

Standard noncompartmental methods will be used to determine the Vz/F in response to single oral doses of 0.5, 2, 8,16, and 24 mg of EC5026. The PK population will include subjects who received a single dose of EC5026 and have sufficient concentration data to support accurate estimation of at least 1 PK parameter. Subjects were excluded from the PK population when there were fewer than 3 quantifiable plasma samples.

Outcome measures

Outcome measures
Measure	EC5026 0.5 mg Single 0.5 mg dose of oral EC5026	EC5026 2 mg Single 2 mg dose of oral EC5026	EC5026 8 mg n=6 Participants Single 8 mg dose of oral EC5026	EC5026 16 mg n=6 Participants Single 16 mg dose of oral EC5026	EC5026 24 mg n=6 Participants Single 24 mg dose of oral EC5026	Placebo Single dose of matching oral placebo
Apparent Volume of Distribution Based on the Terminal Elimination Rate Constant in Plasma (Vz/F) in Response to Escalating Dose Regimens of Oral EC5026 [Plasma Pharmacokinetics].	—	—	178 liters Standard Deviation 21.0	146 liters Standard Deviation 34.5	153 liters Standard Deviation 40.2	—

PRIMARY outcome

Timeframe: Urine is collected for analysis of EC5026 during the following time intervals: before dosing and 0 to 8 hours, 8 to 16 hours, 16 to 24 hours, 24 to 32 hours, 32 to 40 hours, and 40 to 48 hours after dosing

Population: All urine concentrations were below the limit of quantification for the EC5026 0.5 and 2 mg dose groups.

Standard noncompartmental methods will be used to determine CLR in response to single oral doses of 0.5, 2, 8,16, and 24 mg of EC5026. Subjects will be excluded from the PK population when there were fewer than 3 quantifiable plasma samples.

Outcome measures

Outcome measures
Measure	EC5026 0.5 mg Single 0.5 mg dose of oral EC5026	EC5026 2 mg Single 2 mg dose of oral EC5026	EC5026 8 mg n=6 Participants Single 8 mg dose of oral EC5026	EC5026 16 mg n=6 Participants Single 16 mg dose of oral EC5026	EC5026 24 mg n=6 Participants Single 24 mg dose of oral EC5026	Placebo Single dose of matching oral placebo
Renal Clearance (CLR) in Response to Escalating Dose Regimens of Oral EC5026 [Urine Pharmacokinetics].	—	—	0.00679 L/h Geometric Coefficient of Variation 64.8	0.00473 L/h Geometric Coefficient of Variation 76.7	0.00794 L/h Geometric Coefficient of Variation 58.7	—

PRIMARY outcome

Timeframe: Urine is collected for analysis of EC5026 during the following time intervals: before dosing and 0 to 8 hours, 8 to 16 hours, 16 to 24 hours, 24 to 32 hours, 32 to 40 hours, and 40 to 48 hours after dosing

Population: All urine concentrations were below the limit of quantification for the EC5026 0.5 and 2 mg dose groups.

Standard noncompartmental methods will be used to determine the Ae in response to single oral doses of 0.5, 2, 8,16, and 24 mg of EC5026. Subjects will be excluded from the PK population when there were fewer than 3 quantifiable plasma samples.

Outcome measures

Outcome measures
Measure	EC5026 0.5 mg Single 0.5 mg dose of oral EC5026	EC5026 2 mg Single 2 mg dose of oral EC5026	EC5026 8 mg n=6 Participants Single 8 mg dose of oral EC5026	EC5026 16 mg n=6 Participants Single 16 mg dose of oral EC5026	EC5026 24 mg n=6 Participants Single 24 mg dose of oral EC5026	Placebo Single dose of matching oral placebo
Amount of Drug Excreted Unchanged in Urine Within the Time Interval 0 to 48 (Ae 0-48) in Response to Escalating Dose Regimens of Oral EC5026 [Urine Pharmacokinetics].	—	—	0.0127 mg Geometric Coefficient of Variation 65.9	0.0210 mg Geometric Coefficient of Variation 86.2	0.0487 mg Geometric Coefficient of Variation 70.9	—

PRIMARY outcome

Timeframe: Urine is collected for analysis of EC5026 during the following time intervals: before dosing and 0 to 8 hours, 8 to 16 hours, 16 to 24 hours, 24 to 32 hours, 32 to 40 hours, and 40 to 48 hours after dosing

Population: All urine concentrations were below the limit of quantification for the EC5026 0.5 and 2 mg groups.

Standard noncompartmental methods will be used to determine the Fe% in response to single oral doses of 0.5, 2, 8,16, and 24 mg of EC5026. Subjects were excluded from the PK population when there were fewer than 3 quantifiable plasma samples.

Outcome measures

Outcome measures
Measure	EC5026 0.5 mg Single 0.5 mg dose of oral EC5026	EC5026 2 mg Single 2 mg dose of oral EC5026	EC5026 8 mg n=6 Participants Single 8 mg dose of oral EC5026	EC5026 16 mg n=6 Participants Single 16 mg dose of oral EC5026	EC5026 24 mg n=6 Participants Single 24 mg dose of oral EC5026	Placebo Single dose of matching oral placebo
Fraction of Eliminated Dose in Urine From 0 to 48 Hours (Fe 0-48%) in Response to Escalating Dose Regimens of Oral EC5026 [Urine Pharmacokinetics].	—	—	0.159 percentage of eliminated dose Geometric Coefficient of Variation 65.9	0.132 percentage of eliminated dose Geometric Coefficient of Variation 86.2	0.203 percentage of eliminated dose Geometric Coefficient of Variation 70.9	—

PRIMARY outcome

Timeframe: Predose (0 hour), and at 1.25, 2.25, 4.25, 6.25, 8.25, 12.25, 24, 36, 48, 72, 84, 96, and 108 hours after dosing

Population: Plasma concentrations following EC5026 0.5 mg were below the limit of quantification for all subjects at all timepoints. For 2 subjects in the EC5026 2 mg dose group, plasma concentrations were quantifiable in fewer than 3 samples. These subjects were excluded from the PK population. Values for AUC0 inf were excluded from summary statistics when %AUCextrap was \>20%.

Standard noncompartmental methods will be used to determine the AUC in response to single oral doses of 0.5, 2, 8,16, and 24 mg of EC5026. The PK population will include subjects who received a single dose of EC5026 and have sufficient concentration data to support accurate estimation of at least 1 PK parameter. Subjects were excluded from the PK population when there were fewer than 3 quantifiable plasma samples.

Outcome measures

Outcome measures
Measure	EC5026 0.5 mg Single 0.5 mg dose of oral EC5026	EC5026 2 mg Single 2 mg dose of oral EC5026	EC5026 8 mg n=6 Participants Single 8 mg dose of oral EC5026	EC5026 16 mg n=6 Participants Single 16 mg dose of oral EC5026	EC5026 24 mg n=6 Participants Single 24 mg dose of oral EC5026	Placebo Single dose of matching oral placebo
Area Under the Plasma Concentration Versus Time Curve From Time 0 Extrapolated to Infinity (AUC 0-inf) in Response to Escalating Dose Regimens of Oral EC5026 [Plasma Pharmacokinetics].	—	—	3690 ng*h/mL Geometric Coefficient of Variation 26.3	6960 ng*h/mL Geometric Coefficient of Variation 22.1	9310 ng*h/mL Geometric Coefficient of Variation 21.1	—

PRIMARY outcome

Timeframe: Predose (0 hour), and at 1.25, 2.25, 4.25, 6.25, 8.25, 12.25, 24, 36, 48 after dosing

Population: Plasma concentrations following EC5026 0.5 mg were below the limit of quantification for all subjects at all timepoints. For 2 subjects in the EC5026 2 mg dose group, plasma concentrations were quantifiable in fewer than 3 samples. These subjects were excluded from the PK population.

Standard noncompartmental methods will be used to determine the AUC in response to single oral doses of 0.5, 2, 8,16, and 24 mg of EC5026. The PK population will include subjects who received a single dose of EC5026 and have sufficient concentration data to support accurate estimation of at least 1 PK parameter. Subjects were excluded from the PK population when there were fewer than 3 quantifiable plasma samples.

Outcome measures

Outcome measures
Measure	EC5026 0.5 mg Single 0.5 mg dose of oral EC5026	EC5026 2 mg n=4 Participants Single 2 mg dose of oral EC5026	EC5026 8 mg n=6 Participants Single 8 mg dose of oral EC5026	EC5026 16 mg n=6 Participants Single 16 mg dose of oral EC5026	EC5026 24 mg n=6 Participants Single 24 mg dose of oral EC5026	Placebo Single dose of matching oral placebo
Area Under the Plasma Concentration Versus Time Curve From Time 0 to 48 Hours After Dosing (AUC 0-48) in Response to Escalating Dose Regimens of Oral EC5026 [Plasma Pharmacokinetics].	—	119 ng*h/mL Geometric Coefficient of Variation 59.7	1870 ng*h/mL Geometric Coefficient of Variation 7.9	4450 ng*h/mL Geometric Coefficient of Variation 14.7	6130 ng*h/mL Geometric Coefficient of Variation 13.4	—

Adverse Events

EC5026 0.5 mg

Serious events: 0 serious events

Other events: 2 other events

Deaths: 0 deaths

EC5026 2 mg

Serious events: 0 serious events

Other events: 4 other events

Deaths: 0 deaths

EC5026 8 mg

Serious events: 0 serious events

Other events: 2 other events

Deaths: 0 deaths

EC5026 16 mg

Serious events: 0 serious events

Other events: 4 other events

Deaths: 0 deaths

EC5026 24 mg

Serious events: 0 serious events

Other events: 4 other events

Deaths: 0 deaths

Placebo

Serious events: 0 serious events

Other events: 3 other events

Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Other adverse events
Measure	EC5026 0.5 mg n=6 participants at risk Single 0.5 mg dose of oral EC5026	EC5026 2 mg n=6 participants at risk Single 2 mg dose of oral EC5026	EC5026 8 mg n=6 participants at risk Single 8 mg dose of oral EC5026	EC5026 16 mg n=6 participants at risk Single 16 mg dose of oral EC5026	EC5026 24 mg n=6 participants at risk Single 24 mg dose of oral EC5026	Placebo n=10 participants at risk Single dose of matching oral placebo
General disorders Medical device site dermatitis	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	33.3% 2/6 • Number of events 2 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	66.7% 4/6 • Number of events 4 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	50.0% 3/6 • Number of events 3 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	30.0% 3/10 • Number of events 3 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.
General disorders Feeling Hot	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	16.7% 1/6 • Number of events 1 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/10 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.
Infections and infestations Coronavirus infection	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	16.7% 1/6 • Number of events 1 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/10 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.
Infections and infestations Laryngitis	16.7% 1/6 • Number of events 1 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/10 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.
Infections and infestations Trichomoniasis	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	16.7% 1/6 • Number of events 1 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/10 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.
Infections and infestations Urinary tract infection	16.7% 1/6 • Number of events 1 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/10 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.
Nervous system disorders Headache	16.7% 1/6 • Number of events 1 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	16.7% 1/6 • Number of events 1 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	16.7% 1/6 • Number of events 1 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/10 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.
Cardiac disorders Palpitations	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	16.7% 1/6 • Number of events 1 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/10 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.
Cardiac disorders Ventricular extrasystoles	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	16.7% 1/6 • Number of events 1 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/10 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.
Injury, poisoning and procedural complications Limb injury	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	16.7% 1/6 • Number of events 1 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/10 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.
Psychiatric disorders Insomnia	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	10.0% 1/10 • Number of events 1 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.
Renal and urinary disorders Dysuria	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	16.7% 1/6 • Number of events 1 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/10 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.
Respiratory, thoracic and mediastinal disorders Dyspnoea	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	16.7% 1/6 • Number of events 1 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/6 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.	0.00% 0/10 • 14 days A TEAE was defined as any event not present before exposure to study drug or any event already present that worsened in intensity or frequency after exposure. A treatment-related TEAE was defined as a TEAE considered related to the study drug.

Additional Information

Dr. William Schmidt

EicOsis

Phone: 650-438-3018

Email: [email protected]

Results disclosure agreements

Principal investigator is a sponsor employee PPD may not publish any articles or make any presentations relating to the Services provided to EicOsis hereunder with respect to a Project or referring to data, information or materials generated as part of the Services without the prior written consent of EicOsis.
Publication restrictions are in place

Restriction type: OTHER