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| ID | Type | Description | Link |
|---|---|---|---|
| 1UH2NS094258-01 | U.S. NIH Grant/Contract | View source |
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| Name | Class |
|---|---|
| National Institute of Neurological Disorders and Stroke (NINDS) | NIH |
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This is a first-in-human study with EC5026, a new drug candidate intended to treat neuropathic pain. The purpose of the study is to provide initial safety, tolerability, and pharmacokinetics data of single ascending oral doses of EC5026 in healthy subjects.
This is a single-center, double-blind, placebo-controlled, Phase 1a single ascending dose study evaluating the safety, tolerability and pharmacokinetics of sequential doses of oral EC5026 in healthy male and female subjects. EC5026 is an inhibitor of the soluble Epoxide Hydrolase (sEH) enzyme developed as a first-in-class analgesic for the treatment of pain. This study will help refine the dosing strategy for subsequent multiple-dose studies in healthy subjects and for future clinical trials in patients with neuropathic pain.
sEH is an enzyme that is downstream in the cytochrome P450 (CYP) pathway of the arachidonic acid (AA) cascade. The sEH enzyme is responsible of metabolizing a class of epoxy-fatty acids known as epoxyeicosatrienoic acids (EETs), which are potent, naturally occurring analgesics. EETs are produced at high concentrations in areas of tissue damage and inflammation, but are rapidly metabolized by the sEH enzyme into inactive compounds. Effective inhibition of sEH activity prolongs the ability of EETs to exert their analgesic activity.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| EC5026 | Experimental | Single Ascending Doses of oral EC5026 |
|
| Placebo | Placebo Comparator | Single doses of matching oral placebo |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| EC5026 oral capsule | Drug | 5 sequential cohorts of 8 subjects randomly assigned to receive single ascending oral doses of EC5026 (n=6 per cohort) or matching placebo (n=2 per cohort). Oral doses of EC5026 tested in each cohort: 0.5 mg (Cohort 1), 2 mg (Cohort 2), 8 mg (Cohort 3), 16 mg (Cohort 4), and 24 mg (Cohort 5). A blinded sentinel group of 2 subjects (1 active and 1 placebo) will be dosed at least 2 days before the remaining 6 subjects (5 active and 1 placebo) will receive blinded doses of active study drug or placebo. |
| Measure | Description | Time Frame |
|---|---|---|
| Incidence of Adverse Events (AEs) [Safety and Tolerability] | 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. | 14 days |
| 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]. | 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. | 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 |
| Maximum Observed Plasma Concentration (Cmax) in Response to Escalating Dose Regimens of Oral EC5026 [Plasma Pharmacokinetics]. | 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. |
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Inclusion Criteria:
Each subject must meet all of the following criteria to be enrolled in this study:
Exclusion Criteria:
Subjects meeting any of the following criteria will be excluded from the study:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| PPD Phase I Clinic | Austin | Texas | 78744 | United States |
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| ID | Title | Description |
|---|---|---|
| FG000 | EC5026 0.5 mg | Single 0.5 mg dose of oral EC5026 |
| FG001 | EC5026 2 mg | Single 2 mg dose of oral EC5026 |
| FG002 | EC5026 8 mg | Single 8 mg dose of oral EC5026 |
| FG003 | EC5026 16 mg | Single 16 mg dose of oral EC5026 |
| FG004 | EC5026 24 mg | Single 24 mg dose of oral EC5026 |
| FG005 | Placebo | Single dose of matching oral placebo |
| Title | Milestones | Reasons Not Completed | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study |
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| ID | Title | Description |
|---|---|---|
| BG000 | EC5026 0.5 mg | Single 0.5 mg dose of oral EC5026 |
| BG001 | EC5026 2 mg | Single 2 mg dose of oral EC5026 |
| Units | Counts |
|---|---|
| Participants |
|
| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes |
|---|---|---|---|---|---|---|---|---|---|
| Age, Continuous | Median |
| Type | Title | Description | Population Description | Reporting Status | Anticipated Posting Date | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Time Frame | Units Analyzed | Denominator Units Selected | Arm/Group Information | Denominators | Classes | Analyses | ||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Primary | Incidence of Adverse Events (AEs) [Safety and Tolerability] | 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. | Posted | Count of Participants | Participants | 14 days |
|
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.
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| ID | Title | Description | Deaths (Affected) | Deaths (At Risk) | Serious Events (Affected) | Serious Events (At Risk) | Other Events (Affected) | Other Events (At Risk) |
|---|---|---|---|---|---|---|---|---|
| EG000 | EC5026 0.5 mg | Single 0.5 mg dose of oral EC5026 | 0 |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Medical device site dermatitis | General disorders | MedDRA 22.1 | Systematic Assessment | Dermatitis related to electrocardiogram electrodes placement |
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| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Dr. William Schmidt | EicOsis | 650-438-3018 | wkschmidt@eicosis.com |
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| Type | Includes Protocol | Includes SAP | Includes ICF | Document Label | Document Date | Document Uploaded Date | Document File Name |
|---|---|---|---|---|---|---|---|
| Prot | Yes | No | No | Study Protocol | Oct 15, 2019 | Jun 9, 2021 | Prot_000.pdf |
| SAP | No | Yes | No | Statistical Analysis Plan | Jan 21, 2020 | Jun 9, 2021 | SAP_001.pdf |
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| ID | Term |
|---|---|
| C000717068 | EC5026 |
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|
| Placebo oral capsule | Other | 5 sequential cohorts of 8 subjects randomly assigned to receive single ascending oral doses of EC5026 (n=6 per cohort) or matching placebo (n=2 per cohort) |
|
| 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 |
| Time to Maximum Observed Plasma Concentration (Tmax) in Response to Escalating Dose Regimens of Oral EC5026 [Plasma Pharmacokinetics]. | 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. | 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 |
| Terminal Phase Half-life in Plasma (t1/2) in Response to Escalating Dose Regimens of Oral EC5026 [Plasma Pharmacokinetics]. | 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. | 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 |
| Apparent Total Body Clearance (CL/F) in Response to Escalating Dose Regimens of Oral EC5026 [Plasma Pharmacokinetics]. | 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. | 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 |
| 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]. | 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. | 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 |
| Renal Clearance (CLR) in Response to Escalating Dose Regimens of Oral EC5026 [Urine Pharmacokinetics]. | 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. | 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 |
| 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]. | 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. | 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 |
| 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]. | 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. | 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 |
| 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]. | 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. | 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 |
| 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]. | 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. | Predose (0 hour), and at 1.25, 2.25, 4.25, 6.25, 8.25, 12.25, 24, 36, 48 after dosing |
| BG002 |
| EC5026 8 mg |
Single 8 mg dose of oral EC5026 |
| BG003 | EC5026 16 mg | Single 16 mg dose of oral EC5026 |
| BG004 | EC5026 24 mg | Single 24 mg dose of oral EC5026 |
| BG005 | Placebo | Single dose of matching oral placebo |
| BG006 | Total | Total of all reporting groups |
| years |
|
| Sex: Female, Male | Count of Participants | Participants |
|
| Ethnicity (NIH/OMB) | Count of Participants | Participants |
|
| Race (NIH/OMB) | Count of Participants | Participants |
|
| Region of Enrollment | Number | participants |
|
Single 0.5 mg dose of oral EC5026 |
| OG001 | EC5026 2 mg | Single 2 mg dose of oral EC5026 |
| OG002 | EC5026 8 mg | Single 8 mg dose of oral EC5026 |
| OG003 | EC5026 16 mg | Single 16 mg dose of oral EC5026 |
| OG004 | EC5026 24 mg | Single 24 mg dose of oral EC5026 |
| OG005 | Placebo | Single dose of matching oral placebo |
|
|
| Primary | 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]. | 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. | 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. | Posted | Geometric Mean | Geometric Coefficient of Variation | ng*h/mL | 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 |
|
|
|
| Primary | Maximum Observed Plasma Concentration (Cmax) in Response to Escalating Dose Regimens of Oral EC5026 [Plasma Pharmacokinetics]. | 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. | 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. | Posted | Geometric Mean | Geometric Coefficient of Variation | ng/mL | 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 |
|
|
|
| Primary | Time to Maximum Observed Plasma Concentration (Tmax) in Response to Escalating Dose Regimens of Oral EC5026 [Plasma Pharmacokinetics]. | 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. | 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. | Posted | Median | Full Range | hours | 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 |
|
|
|
| Primary | Terminal Phase Half-life in Plasma (t1/2) in Response to Escalating Dose Regimens of Oral EC5026 [Plasma Pharmacokinetics]. | 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. | 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. | Posted | Mean | Standard Deviation | hours | 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 |
|
|
|
| Primary | Apparent Total Body Clearance (CL/F) in Response to Escalating Dose Regimens of Oral EC5026 [Plasma Pharmacokinetics]. | 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. | 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. | Posted | Mean | Standard Deviation | L/h | 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 |
|
|
|
| Primary | 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]. | 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. | 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. | Posted | Mean | Standard Deviation | liters | 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 |
|
|
|
| Primary | Renal Clearance (CLR) in Response to Escalating Dose Regimens of Oral EC5026 [Urine Pharmacokinetics]. | 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. | All urine concentrations were below the limit of quantification for the EC5026 0.5 and 2 mg dose groups. | Posted | Geometric Mean | Geometric Coefficient of Variation | L/h | 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 |
|
|
|
| Primary | 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]. | 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. | All urine concentrations were below the limit of quantification for the EC5026 0.5 and 2 mg dose groups. | Posted | Geometric Mean | Geometric Coefficient of Variation | mg | 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 |
|
|
|
| Primary | 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]. | 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. | All urine concentrations were below the limit of quantification for the EC5026 0.5 and 2 mg groups. | Posted | Geometric Mean | Geometric Coefficient of Variation | percentage of eliminated dose | 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 |
|
|
|
| Primary | 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]. | 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. | 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%. | Posted | Geometric Mean | Geometric Coefficient of Variation | ng*h/mL | 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 |
|
|
|
| Primary | 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]. | 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. | 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. | Posted | Geometric Mean | Geometric Coefficient of Variation | ng*h/mL | Predose (0 hour), and at 1.25, 2.25, 4.25, 6.25, 8.25, 12.25, 24, 36, 48 after dosing |
|
|
|
| 6 |
| 0 |
| 6 |
| 2 |
| 6 |
| EG001 | EC5026 2 mg | Single 2 mg dose of oral EC5026 | 0 | 6 | 0 | 6 | 4 | 6 |
| EG002 | EC5026 8 mg | Single 8 mg dose of oral EC5026 | 0 | 6 | 0 | 6 | 2 | 6 |
| EG003 | EC5026 16 mg | Single 16 mg dose of oral EC5026 | 0 | 6 | 0 | 6 | 4 | 6 |
| EG004 | EC5026 24 mg | Single 24 mg dose of oral EC5026 | 0 | 6 | 0 | 6 | 4 | 6 |
| EG005 | Placebo | Single dose of matching oral placebo | 0 | 10 | 0 | 10 | 3 | 10 |
|
| Feeling Hot | General disorders | MedDRA 22.1 | Systematic Assessment |
|
| Coronavirus infection | Infections and infestations | MedDRA 22.1 | Systematic Assessment | Mild COVID-19 |
|
| Laryngitis | Infections and infestations | MedDRA 22.1 | Systematic Assessment |
|
| Trichomoniasis | Infections and infestations | MedDRA 22.1 | Systematic Assessment |
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| Urinary tract infection | Infections and infestations | MedDRA 22.1 | Systematic Assessment |
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| Headache | Nervous system disorders | MedDRA 22.1 | Systematic Assessment | Mild headache |
|
| Palpitations | Cardiac disorders | MedDRA 22.1 | Systematic Assessment |
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| Ventricular extrasystoles | Cardiac disorders | MedDRA 22.1 | Systematic Assessment |
|
| Limb injury | Injury, poisoning and procedural complications | MedDRA 22.1 | Systematic Assessment |
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| Insomnia | Psychiatric disorders | MedDRA 22.1 | Systematic Assessment |
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| Dysuria | Renal and urinary disorders | MedDRA 22.1 | Systematic Assessment |
|
| Dyspnoea | Respiratory, thoracic and mediastinal disorders | MedDRA 22.1 | Systematic Assessment |
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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.