Trial Review

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Trial details imported from ClinicalTrials.gov

For full trial details, please see the original record at https://clinicaltrials.gov/study/NCT03491748




Registration number
NCT03491748
Ethics application status
Date submitted
23/03/2018
Date registered
9/04/2018
Date last updated
14/01/2020

Titles & IDs
Public title
A Study to Evaluate the Safety, Tolerability, and Pharmacokinetics (PK, the Measure of How the Human Body Processes a Substance) of ETX0282 When Administered Orally to Healthy Participants
Scientific title
A Phase 1, Double-Blind, Randomized, Placebo-Controlled Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Oral ETX0282 Administered in Healthy Subjects
Secondary ID [1] 0 0
1010452
Secondary ID [2] 0 0
CS0282-2017-0001
Universal Trial Number (UTN)
Trial acronym
Linked study record

Health condition
Health condition(s) or problem(s) studied:
Healthy Volunteers 0 0
Condition category
Condition code

Intervention/exposure
Study type
Interventional
Description of intervention(s) / exposure
Treatment: Drugs - ETX0282
Treatment: Drugs - Cefpodoxime proxetil
Treatment: Drugs - Placebo

Experimental: Part A (SAD): Cohort 1, 100 mg ETX0282/Placebo - Part A of the study will explore the safety, tolerability, and pharmacokinetics (PK) of a single ascending dose (SAD) of oral ETX0282. Participants will be treated with a single oral dose of 100 milligrams (mg) ETX0282 or placebo in a fasted state. They will be confined to the Study Unit from Day -1 and discharged following collection of the 72-hour postdose assessments (Day 4).

Experimental: Part A (SAD): Cohort 2, 200 mg ETX0282/Placebo - Part A of the study will explore the safety, tolerability, and PK of a SAD of oral ETX0282. Participants will be treated with a single oral dose of 200 mg ETX0282 or placebo in a fasted state. They will be confined to the Study Unit from Day -1 and discharged following collection of the 72-hour postdose assessments (Day 4).

Experimental: Part A (SAD): Cohort 3, 400 mg ETX0282/Placebo - Part A of the study will explore the safety, tolerability, and PK of a SAD of oral ETX0282. Participants will be treated with a single oral dose of 400 mg ETX0282 or placebo in a fasted state. They will be confined to the Study Unit from Day -1 and discharged following collection of the 72-hour postdose assessments (Day 4).

Experimental: Part A (SAD): Cohort 4, 800 mg ETX0282/Placebo - Part A of the study will explore the safety, tolerability, and PK of a SAD of oral ETX0282. Participants will be treated with a single oral dose of 800 mg ETX0282 or placebo in a fasted state. They will be confined to the Study Unit from Day -1 and discharged following collection of the 72-hour postdose assessments (Day 4).

Experimental: Part A (SAD): Cohort 5, 600 mg ETX0282/Placebo - Part A of the study will explore the safety, tolerability, and PK of a SAD of oral ETX0282. Participants will be treated with a single oral dose of 600 mg ETX0282 or placebo in a fasted state. They will be confined to the Study Unit from Day -1 and discharged following collection of the 72-hour postdose assessments (Day 4).

Experimental: Part A (SAD): Cohort 6 (Elderly), 300 mg ETX0282/Placebo - Part A of the study will explore the safety, tolerability, and PK of a SAD of oral ETX0282. Elderly participants (aged 65 years or older) will be treated with a single oral dose of 300 mg ETX0282 or placebo in a fasted state. They will be confined to the Study Unit from Day -1 and discharged following collection of the 72-hour postdose assessments (Day 4).

Experimental: Part B (Food Effect): Cohort 7, 100 mg ETX0282/Placebo - Part B of the study will explore the effect of food on oral ETX0282. Participants will be treated with a single oral dose of 100 mg ETX0282 or placebo (Day 1) while fasted and with a single oral dose of 100 mg ETX0282 or placebo (Day 4) with a high-fat meal. They will be confined to the Study Unit from Day -1 and discharged following collection of the 72-hour post fed state dose assessments (Day 7).

Experimental: Part C (MAD): Cohort 9, 200 mg ETX0282/Placebo - Part C of the study will explore the safety, tolerability, and PK of MAD of oral ETX0282. Part C will be administered in a fed state. Participants will be treated with a single oral dose of 200 mg ETX0282 or placebo on the morning of Day 1, and will then be dosed three times a day (TID) beginning on the morning of Day 2 (i.e., 24 hours after the Day 1 dose) through Day 7. Participants will be treated with a single oral dose of 200 mg ETX0282 or placebo on the morning of Day 8. They will be confined to the Study Unit from Day -1 and discharged following collection of the 72-hour post Day 8 dose assessments (Day 11).

Experimental: Part C (MAD): Cohort 10, 200 mg ETX0282/Placebo - Part C of the study will explore the safety, tolerability, and PK of MAD of oral ETX0282. Part C will be administered in a fed state. Participants will be treated with a single oral dose of 200 mg ETX0282 or placebo on the morning of Day 1, and will then be dosed TID beginning on the morning of Day 2 (i.e., 24 hours after the Day 1 dose) through Day 7. Participants will be treated with a single oral dose of 200 mg ETX0282 or placebo on the morning of Day 8. They will be confined to the Study Unit from Day -1 and discharged following collection of the 72-hour post Day 8 dose assessments (Day 11).

Experimental: Part D: Cohort 12, ETX0282/Placebo plus Cefpodoxime Proxetil - Part D of the study will explore the safety, tolerability, and PK of oral ETX0282 when administered as a single oral dose in combination with cefpodoxime proxetil tablets to healthy participants in a fed state. Participants will be treated with a single oral dose of 600 mg ETX0282 or placebo in a fed state on Day 1, with a single oral dose of 400 mg cefpodoxime proxetil in a fed state on Day 4, and with a single oral dose of 600 mg ETX0282 or placebo plus a single oral dose of 400 mg cefpodoxime proxetil dosed at the same time in a fed state on Day 7. They will be confined to the Study Unit from Day -1 and discharged following collection of the 72-hour post Day 7 dose assessments (Day 10).

Experimental: Part B (Food Effect): Cohort 14, 300 mg ETX0282/Placebo - Part B of the study will explore the effect of food on oral ETX0282. Participants will be treated with a single oral dose of 300 mg ETX0282 or placebo (Day 1) while fasted and with a single oral dose of 300 mg ETX0282 or placebo (Day 4) with a high-fat meal. They will be confined to the Study Unit from Day -1 and discharged following collection of the 72-hour post fed state dose assessments (Day 7).

Experimental: Part G: Cohort 17, 300 mg ETX0282/Placebo - Part G of the study will explore the tolerability and PK profile of oral ETX0282 when administered either as a single dose (i.e., 300 mg as a single dose) or in 4 equal, divided doses over a 6 hour period (i.e., 75 mg every 2 hours for 4 doses \[a 300 mg total dose\]) when administered in a fasted state. Participants will receive the 2 treatments in a cross-over design according to one of 2 randomized sequences: AB or BA. Treatment A: 0 hours, 4 × 75 mg ETX0282/placebo; 2, 4, and 6 hours, 1 × 75 mg placebo. Treatment B: 0 hours, 1 × 75 mg ETX0282/placebo and 3 × 75 mg placebo; 2, 4, and 6 hours, 1 × 75 mg ETX0282/placebo. Participants will be confined to the Study Unit from Day -1 and discharged following collection of the 24 hours post Day 4 dose assessments (Day 5).


Treatment: Drugs: ETX0282
Oral Gelatin capsules

Treatment: Drugs: Cefpodoxime proxetil
Oral tablets

Treatment: Drugs: Placebo
Oral Gelatin capsules
Intervention code [1] 0 0
Treatment: Drugs
Comparator / control treatment
Control group

Outcomes
Primary outcome [1] 0 0
Number of participants with any non-serious adverse event
Timepoint [1] 0 0
Up to 14 days after the last dose of study drug (Study Day [SD] 210)
Primary outcome [2] 0 0
Number of participants with any serious adverse event
Timepoint [2] 0 0
Up to 14 days after the last dose of study drug (SD 210)
Primary outcome [3] 0 0
Number of participants with an adverse event of the indicated causality and severity
Timepoint [3] 0 0
Up to 14 days after the last dose of study drug (SD 210)
Primary outcome [4] 0 0
Part A: Number of participants with abnormal, clinically significant hematology, clinical chemistry, and urinalysis laboratory values at the indicated time points
Timepoint [4] 0 0
Screening (Day -1) up to Day 15±2 (Follow-up)
Primary outcome [5] 0 0
Part B: Number of participants with abnormal, clinically significant hematology, clinical chemistry, and urinalysis laboratory values at the indicated time points
Timepoint [5] 0 0
Screening (Day -1; SD 44) up to Day 18±2 (SD 62±2; Follow-up)
Primary outcome [6] 0 0
Part C: Number of participants with abnormal, clinically significant hematology, clinical chemistry, and urinalysis laboratory values at the indicated time points
Timepoint [6] 0 0
Screening (Day -1; SD 91) up to Day 22±2 (SD 113±2; Follow-up)
Primary outcome [7] 0 0
Part D: Number of participants with abnormal, clinically significant hematology, clinical chemistry, and urinalysis laboratory values at the indicated time points
Timepoint [7] 0 0
Screening (Day -1; SD 142) up to Day 21±2 (SD 163±2; Follow-up)
Primary outcome [8] 0 0
Part G: Number of participants with abnormal, clinically significant hematology, clinical chemistry, and urinalysis laboratory values at the indicated time points
Timepoint [8] 0 0
Screening (Day -1; SD 192) up to Day 18±2 (SD 210±2; Follow-up)
Primary outcome [9] 0 0
Part A: Number of participants with abnormal, clinically significant vital sign values at the indicated time points
Timepoint [9] 0 0
Screening (Day -1) up to Day 15±2 (Follow-up)
Primary outcome [10] 0 0
Part B: Number of participants with abnormal, clinically significant vital sign values at the indicated time points
Timepoint [10] 0 0
Screening (Day -1; SD 44) up to Day 18±2 (SD 62±2; Follow-up)
Primary outcome [11] 0 0
Part C: Number of participants with abnormal, clinically significant vital sign values at the indicated time points
Timepoint [11] 0 0
Screening (Day -1; SD 91) up to Day 22±2 (SD 113±2; Follow-up)
Primary outcome [12] 0 0
Part D: Number of participants with abnormal, clinically significant vital sign values at the indicated time points
Timepoint [12] 0 0
Screening (Day -1; SD 142) up to Day 21±2 (SD 163±2; Follow-up)
Primary outcome [13] 0 0
Part G: Number of participants with abnormal, clinically significant vital sign values at the indicated time points
Timepoint [13] 0 0
Screening (Day -1; SD 192) up to Day 18±2 (SD 210±2; Follow-up)
Primary outcome [14] 0 0
Part A: Number of participants with abnormal, clinically significant electrocardiogram values at the indicated time points
Timepoint [14] 0 0
Screening (Day -1) up to Day 15±2 (Follow-up)
Primary outcome [15] 0 0
Part B: Number of participants with abnormal, clinically significant electrocardiogram values at the indicated time points
Timepoint [15] 0 0
Screening (Day -1; SD 44) up to Day 18±2 (SD 62±2; Follow-up)
Primary outcome [16] 0 0
Part C: Number of participants with abnormal, clinically significant electrocardiogram values at the indicated time points
Timepoint [16] 0 0
Screening (Day -1; SD 91) up to Day 22±2 (SD 113±2; Follow-up)
Primary outcome [17] 0 0
Part D: Number of participants with abnormal, clinically significant electrocardiogram values at the indicated time points
Timepoint [17] 0 0
Screening (Day -1; SD 142) up to Day 21±2 (SD 163±2; Follow-up)
Primary outcome [18] 0 0
Part G: Number of participants with abnormal, clinically significant electrocardiogram values at the indicated time points
Timepoint [18] 0 0
Screening (Day -1; SD 192) up to Day 18±2 (SD 210±2; Follow-up)
Primary outcome [19] 0 0
Part A: Mean peak plasma concentration (Cmax) of ETX0282 and ETX1317 in blood in Cohorts 1 to 5
Timepoint [19] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Primary outcome [20] 0 0
Part A: Mean plasma concentration at time t (Ct) of ETX0282 and ETX1317 in blood in Cohorts 1 to 5
Timepoint [20] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Primary outcome [21] 0 0
Part A: Mean time to peak plasma concentration (Tmax) of ETX0282 and ETX1317 in blood in Cohorts 1 to 5
Timepoint [21] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Primary outcome [22] 0 0
Part A: Mean area under the concentration-time curve from time 0 to 24 hours (AUC0-24) of ETX0282 and ETX1317 in blood in Cohorts 1 to 5
Timepoint [22] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), and 24 (Day 2) hours postdose
Primary outcome [23] 0 0
Part A: Mean area under the concentration-time curve from time 0 to the last time point evaluated (AUC0-t) of ETX0282 and ETX1317 in blood in Cohorts 1 to 5
Timepoint [23] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Primary outcome [24] 0 0
Part A: Mean area under the concentration-time curve from time 0 and extrapolated to infinity (AUC0-8) of ETX0282 and ETX1317 in blood in Cohorts 1 to 5
Timepoint [24] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Primary outcome [25] 0 0
Part A: Mean elimination rate constant (Kel) of ETX0282 and ETX1317 in blood in Cohorts 1 to 5
Timepoint [25] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Primary outcome [26] 0 0
Part A: Mean elimination half-life (t½) of ETX0282 and ETX1317 in blood in Cohorts 1 to 5
Timepoint [26] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Primary outcome [27] 0 0
Part A: Mean clearance (CL) of ETX0282 and ETX1317 in blood in Cohorts 1 to 5
Timepoint [27] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Primary outcome [28] 0 0
Part A: Mean volume of distribution (Vdss) of ETX0282 and ETX1317 in blood in Cohorts 1 to 5
Timepoint [28] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Primary outcome [29] 0 0
Part A: Mean cumulative excretion of unchanged ETX0282 and ETX1317 in urine (Ae) in Cohorts 1 to 5
Timepoint [29] 0 0
Prior to dosing (-6 to 0 hours; Day 1); 0 to 8 (Day 1), 8 to 24 (Day 2), 24 to 48 (Day 3), and 48 to 72 (Day 4) hours postdose
Primary outcome [30] 0 0
Part A: Mean urinary clearance (CLR) of ETX0282 and ETX1317 in Cohorts 1 to 5
Timepoint [30] 0 0
Prior to dosing (-6 to 0 hours; Day 1); 0 to 8 (Day 1), 8 to 24 (Day 2), 24 to 48 (Day 3), and 48 to 72 (Day 4) hours postdose
Primary outcome [31] 0 0
Part A: Mean fraction of the administered dose of ETX0282 and ETX1317 that is excreted unchanged in the urine (fe) in Cohorts 1 to 5
Timepoint [31] 0 0
Prior to dosing (-6 to 0 hours; Day 1); 0 to 8 (Day 1), 8 to 24 (Day 2), 24 to 48 (Day 3), and 48 to 72 (Day 4) hours postdose
Primary outcome [32] 0 0
Part A: Mean dose proportionality of ETX0282 and ETX1317 in Cohorts 1 to 5
Timepoint [32] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Primary outcome [33] 0 0
Part C: Mean Cmax of ETX0282 and ETX1317 in blood
Timepoint [33] 0 0
Days 1-3, 5, and 8 (SDs 92-94, 96, and 99): predose (30 min); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, and 24 hours post first dose; at troughs of Days 3, 5, and 8 (SDs 94, 96, and 99); at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post last dose
Primary outcome [34] 0 0
Part C: Mean Ct of ETX0282 and ETX1317 in blood
Timepoint [34] 0 0
Days 1-3, 5, and 8 (SDs 92-94, 96, and 99): predose (30 min); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, and 24 hours post first dose; at troughs of Days 3, 5, and 8 (SDs 94, 96, and 99); at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post last dose
Primary outcome [35] 0 0
Part C: Mean Tmax of ETX0282 and ETX1317 in blood
Timepoint [35] 0 0
Days 1-3, 5, and 8 (SDs 92-94, 96, and 99): predose (30 min); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, and 24 hours post first dose; at troughs of Days 3, 5, and 8 (SDs 94, 96, and 99); at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post last dose
Primary outcome [36] 0 0
Part C: Mean AUC0-24 of ETX0282 and ETX1317 in blood
Timepoint [36] 0 0
Days 1-3, 5, and 8 (SDs 92-94, 96, and 99): predose (30 min); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, and 24 hours post first dose; at troughs of Days 3, 5, and 8 (SDs 94, 96, and 99); at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post last dose
Primary outcome [37] 0 0
Part C: Mean AUC0-t of ETX0282 and ETX1317 in blood
Timepoint [37] 0 0
Days 1-3, 5, and 8 (SDs 92-94, 96, and 99): predose (30 min); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, and 24 hours post first dose; at troughs of Days 3, 5, and 8 (SDs 94, 96, and 99); at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post last dose
Primary outcome [38] 0 0
Part C: Mean AUC0-8 of ETX0282 and ETX1317 in blood
Timepoint [38] 0 0
Days 1-3, 5, and 8 (SDs 92-94, 96, and 99): predose (30 min); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, and 24 hours post first dose; at troughs of Days 3, 5, and 8 (SDs 94, 96, and 99); at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post last dose
Primary outcome [39] 0 0
Part C: Mean AUC from time 0 to the end of the dosing period (AUC0-tau) of ETX0282 and ETX1317 in blood
Timepoint [39] 0 0
Days 1-3, 5, and 8 (SDs 92-94, 96, and 99): predose (30 min); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, and 24 hours post first dose; at troughs of Days 3, 5, and 8 (SDs 94, 96, and 99); at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post last dose
Primary outcome [40] 0 0
Part C: Mean accumulation ratio (R0) of ETX0282 and ETX1317 in blood
Timepoint [40] 0 0
Days 1-3, 5, and 8 (SDs 92-94, 96, and 99): predose (30 min); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, and 24 hours post first dose; at troughs of Days 3, 5, and 8 (SDs 94, 96, and 99); at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post last dose
Primary outcome [41] 0 0
Part C: Mean Kel of ETX0282 and ETX1317 in blood
Timepoint [41] 0 0
Days 1-3, 5, and 8 (SDs 92-94, 96, and 99): predose (30 min); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, and 24 hours post first dose; at troughs of Days 3, 5, and 8 (SDs 94, 96, and 99); at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post last dose
Primary outcome [42] 0 0
Part C: Mean t½ of ETX0282 and ETX1317 in blood
Timepoint [42] 0 0
Days 1-3, 5, and 8 (SDs 92-94, 96, and 99): predose (30 min); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, and 24 hours post first dose; at troughs of Days 3, 5, and 8 (SDs 94, 96, and 99); at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post last dose
Primary outcome [43] 0 0
Part C: Mean CL of ETX0282 and ETX1317 in blood
Timepoint [43] 0 0
Days 1-3, 5, and 8 (SDs 92-94, 96, and 99): predose (30 min); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, and 24 hours post first dose; at troughs of Days 3, 5, and 8 (SDs 94, 96, and 99); at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post last dose
Primary outcome [44] 0 0
Part C: Mean Vdss of ETX0282 and ETX1317 in blood
Timepoint [44] 0 0
Days 1-3, 5, and 8 (SDs 92-94, 96, and 99): predose (30 min); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, and 24 hours post first dose; at troughs of Days 3, 5, and 8 (SDs 94, 96, and 99); at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post last dose
Primary outcome [45] 0 0
Part C: Mean Ae of ETX0282 and ETX1317
Timepoint [45] 0 0
Days 1-4 and 8-11 (SDs 92-95 and 99-102): prior to dosing (-6 to 0 hours; first and last doses) and at 0-8, 8-24, 24-48, and 48-72 hours post first and last dose
Primary outcome [46] 0 0
Part C: Mean CLR of ETX0282 and ETX1317
Timepoint [46] 0 0
Days 1-4 and 8-11 (SDs 92-95 and 99-102): prior to dosing (-6 to 0 hours; first and last doses) and at 0-8, 8-24, 24-48, and 48-72 hours post first and last dose
Primary outcome [47] 0 0
Part C: Mean fe of ETX0282 and ETX1317
Timepoint [47] 0 0
Days 1-4 and 8-11 (SDs 92-95 and 99-102): prior to dosing (-6 to 0 hours; first and last doses) and at 0-8, 8-24, 24-48, and 48-72 hours post first and last dose
Primary outcome [48] 0 0
Part C: Mean dose proportionality of ETX0282 and ETX1317
Timepoint [48] 0 0
Days 1-3, 5, and 8 (SDs 92-94, 96, and 99): predose (30 min); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, and 24 hours post first dose; at troughs of Days 3, 5, and 8 (SDs 94, 96, and 99); at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post last dose
Primary outcome [49] 0 0
Part D: Mean Cmax of ETX0282 and ETX1317 in blood
Timepoint [49] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [50] 0 0
Part D: Mean Ct of ETX0282 and ETX1317 in blood
Timepoint [50] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [51] 0 0
Part D: Mean Tmax of ETX0282 and ETX1317 in blood
Timepoint [51] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [52] 0 0
Part D: Mean AUC0-24 of ETX0282 and ETX1317 in blood
Timepoint [52] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, and 24 hours postdose
Primary outcome [53] 0 0
Part D: Mean AUC0-t of ETX0282 and ETX1317 in blood
Timepoint [53] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [54] 0 0
Part D: Mean AUC0-8 of ETX0282 and ETX1317 in blood
Timepoint [54] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [55] 0 0
Part D: Mean Kel of ETX0282 and ETX1317 in blood
Timepoint [55] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [56] 0 0
Part D: Mean t½ of ETX0282 and ETX1317 in blood
Timepoint [56] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [57] 0 0
Part D: Mean CL of ETX0282 and ETX1317 in blood
Timepoint [57] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [58] 0 0
Part D: Mean Vdss of ETX0282 and ETX1317 in blood
Timepoint [58] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [59] 0 0
Part D: Mean Ae of ETX0282 and ETX1317
Timepoint [59] 0 0
Days 1-10 (SDs 143-152): prior to dosing (-6 to 0 hours) and at 0-8, 8-24, 24-48, and 48-72 hours postdose
Primary outcome [60] 0 0
Part D: Mean CLR of ETX0282 and ETX1317
Timepoint [60] 0 0
Days 1-10 (SDs 143-152): prior to dosing (-6 to 0 hours) and at 0-8, 8-24, 24-48, and 48-72 hours postdose
Primary outcome [61] 0 0
Part D: Mean fe of ETX0282 and ETX1317
Timepoint [61] 0 0
Days 1-10 (SDs 143-152): prior to dosing (-6 to 0 hours) and at 0-8, 8-24, 24-48, and 48-72 hours postdose
Primary outcome [62] 0 0
Part D: Mean dose proportionality of ETX0282 and ETX1317
Timepoint [62] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [63] 0 0
Part D: Mean Cmax of cefpodoxime proxetil and cefpodoxime following administration of cefpodoxime proxetil as a single oral dose either alone or in combination with ETX0282
Timepoint [63] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [64] 0 0
Part D: Mean Ct of cefpodoxime proxetil and cefpodoxime following administration of cefpodoxime proxetil as a single oral dose either alone or in combination with ETX0282
Timepoint [64] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [65] 0 0
Part D: Mean Tmax of cefpodoxime proxetil and cefpodoxime following administration of cefpodoxime proxetil as a single oral dose either alone or in combination with ETX0282
Timepoint [65] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [66] 0 0
Part D: Mean AUC0-24 of cefpodoxime proxetil and cefpodoxime following administration of cefpodoxime proxetil as a single oral dose either alone or in combination with ETX0282
Timepoint [66] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, and 24 hours postdose
Primary outcome [67] 0 0
Part D: Mean AUC0-t of cefpodoxime proxetil and cefpodoxime following administration of cefpodoxime proxetil as a single oral dose either alone or in combination with ETX0282
Timepoint [67] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [68] 0 0
Part D: Mean AUC0-8 of cefpodoxime proxetil and cefpodoxime following administration of cefpodoxime proxetil as a single oral dose either alone or in combination with ETX0282
Timepoint [68] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [69] 0 0
Part D: Mean Kel of cefpodoxime proxetil and cefpodoxime following administration of cefpodoxime proxetil as a single oral dose either alone or in combination with ETX0282
Timepoint [69] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [70] 0 0
Part D: Mean t½ of cefpodoxime proxetil and cefpodoxime following administration of cefpodoxime proxetil as a single oral dose either alone or in combination with ETX0282
Timepoint [70] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [71] 0 0
Part D: Mean CL of cefpodoxime proxetil and cefpodoxime following administration of cefpodoxime proxetil as a single oral dose either alone or in combination with ETX0282
Timepoint [71] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [72] 0 0
Part D: Mean Vdss of cefpodoxime proxetil and cefpodoxime following administration of cefpodoxime proxetil as a single oral dose either alone or in combination with ETX0282
Timepoint [72] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [73] 0 0
Part D: Mean Ae of cefpodoxime proxetil and cefpodoxime following administration of cefpodoxime proxetil as a single oral dose either alone or in combination with ETX0282
Timepoint [73] 0 0
Days 1-10 (SDs 143-152): prior to dosing (-6 to 0 hours) and at 0-8, 8-24, 24-48, and 48-72 hours postdose
Primary outcome [74] 0 0
Part D: Mean CLR of cefpodoxime proxetil and cefpodoxime following administration of cefpodoxime proxetil as a single oral dose either alone or in combination with ETX0282
Timepoint [74] 0 0
Days 1-10 (SDs 143-152): prior to dosing (-6 to 0 hours) and at 0-8, 8-24, 24-48, and 48-72 hours postdose
Primary outcome [75] 0 0
Part D: Mean fe of cefpodoxime proxetil and cefpodoxime following administration of cefpodoxime proxetil as a single oral dose either alone or in combination with ETX0282
Timepoint [75] 0 0
Days 1-10 (SDs 143-152): prior to dosing (-6 to 0 hours) and at 0-8, 8-24, 24-48, and 48-72 hours postdose
Primary outcome [76] 0 0
Part D: Mean dose proportionality of cefpodoxime proxetil and cefpodoxime following administration of cefpodoxime proxetil as a single oral dose either alone or in combination with ETX0282
Timepoint [76] 0 0
Days 1-10 (SDs 143-152): predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16, 24, 48, and 72 hours postdose
Primary outcome [77] 0 0
Part G: Mean Cmax of ETX0282 and ETX1317 in blood
Timepoint [77] 0 0
Days 1 and 4 (SDs 193 and 196): 30 minutes predose; 0.25, 0.5, 0.75, 1, 1.5, 2 (predose prior to subsequent dose), 2.5, 3, 4 (predose prior to subsequent dose), 7, 8, 12, and 16 hours postdose. Days 2 and 5 (SDs 194 and 197): 24 hours postdose
Primary outcome [78] 0 0
Part G: Mean Ct of ETX0282 and ETX1317 in blood
Timepoint [78] 0 0
Days 1 and 4 (SDs 193 and 196): 30 minutes predose; 0.25, 0.5, 0.75, 1, 1.5, 2 (predose prior to subsequent dose), 2.5, 3, 4 (predose prior to subsequent dose), 7, 8, 12, and 16 hours postdose. Days 2 and 5 (SDs 194 and 197): 24 hours postdose
Primary outcome [79] 0 0
Part G: Mean Tmax of ETX0282 and ETX1317 in blood
Timepoint [79] 0 0
Days 1 and 4 (SDs 193 and 196): 30 minutes predose; 0.25, 0.5, 0.75, 1, 1.5, 2 (predose prior to subsequent dose), 2.5, 3, 4 (predose prior to subsequent dose), 7, 8, 12, and 16 hours postdose. Days 2 and 5 (SDs 194 and 197): 24 hours postdose
Primary outcome [80] 0 0
Part G: Mean AUC0-24 of ETX0282 and ETX1317 in blood
Timepoint [80] 0 0
Days 1 and 4 (SDs 193 and 196): 30 minutes predose; 0.25, 0.5, 0.75, 1, 1.5, 2 (predose prior to subsequent dose), 2.5, 3, 4 (predose prior to subsequent dose), 7, 8, 12, and 16 hours postdose. Days 2 and 5 (SDs 194 and 197): 24 hours postdose
Primary outcome [81] 0 0
Part G: Mean AUC0-t of ETX0282 and ETX1317 in blood
Timepoint [81] 0 0
Days 1 and 4 (SDs 193 and 196): 30 minutes predose; 0.25, 0.5, 0.75, 1, 1.5, 2 (predose prior to subsequent dose), 2.5, 3, 4 (predose prior to subsequent dose), 7, 8, 12, and 16 hours postdose. Days 2 and 5 (SDs 194 and 197): 24 hours postdose
Primary outcome [82] 0 0
Part G: Mean AUC0-8 of ETX0282 and ETX1317 in blood
Timepoint [82] 0 0
Days 1 and 4 (SDs 193 and 196): 30 minutes predose; 0.25, 0.5, 0.75, 1, 1.5, 2 (predose prior to subsequent dose), 2.5, 3, 4 (predose prior to subsequent dose), 7, 8, 12, and 16 hours postdose. Days 2 and 5 (SDs 194 and 197): 24 hours postdose
Primary outcome [83] 0 0
Part G: Mean AUC0-tau of ETX0282 and ETX1317 in blood
Timepoint [83] 0 0
Days 1 and 4 (SDs 193 and 196): 30 minutes predose; 0.25, 0.5, 0.75, 1, 1.5, 2 (predose prior to subsequent dose), 2.5, 3, 4 (predose prior to subsequent dose), 7, 8, 12, and 16 hours postdose. Days 2 and 5 (SDs 194 and 197): 24 hours postdose
Primary outcome [84] 0 0
Part G: Mean R0 of ETX0282 and ETX1317 in blood
Timepoint [84] 0 0
Days 1 and 4 (SDs 193 and 196): 30 minutes predose; 0.25, 0.5, 0.75, 1, 1.5, 2 (predose prior to subsequent dose), 2.5, 3, 4 (predose prior to subsequent dose), 7, 8, 12, and 16 hours postdose. Days 2 and 5 (SDs 194 and 197): 24 hours postdose
Primary outcome [85] 0 0
Part G: Mean Kel of ETX0282 and ETX1317 in blood
Timepoint [85] 0 0
Days 1 and 4 (SDs 193 and 196): 30 minutes predose; 0.25, 0.5, 0.75, 1, 1.5, 2 (predose prior to subsequent dose), 2.5, 3, 4 (predose prior to subsequent dose), 7, 8, 12, and 16 hours postdose. Days 2 and 5 (SDs 194 and 197): 24 hours postdose
Primary outcome [86] 0 0
Part G: Mean t½ of ETX0282 and ETX1317 in blood
Timepoint [86] 0 0
Days 1 and 4 (SDs 193 and 196): 30 minutes predose; 0.25, 0.5, 0.75, 1, 1.5, 2 (predose prior to subsequent dose), 2.5, 3, 4 (predose prior to subsequent dose), 7, 8, 12, and 16 hours postdose. Days 2 and 5 (SDs 194 and 197): 24 hours postdose
Primary outcome [87] 0 0
Part G: Mean CL of ETX0282 and ETX1317 in blood
Timepoint [87] 0 0
Days 1 and 4 (SDs 193 and 196): 30 minutes predose; 0.25, 0.5, 0.75, 1, 1.5, 2 (predose prior to subsequent dose), 2.5, 3, 4 (predose prior to subsequent dose), 7, 8, 12, and 16 hours postdose. Days 2 and 5 (SDs 194 and 197): 24 hours postdose
Primary outcome [88] 0 0
Part G: Mean Vdss of ETX0282 and ETX1317 in blood
Timepoint [88] 0 0
Days 1 and 4 (SDs 193 and 196): 30 minutes predose; 0.25, 0.5, 0.75, 1, 1.5, 2 (predose prior to subsequent dose), 2.5, 3, 4 (predose prior to subsequent dose), 7, 8, 12, and 16 hours postdose. Days 2 and 5 (SDs 194 and 197): 24 hours postdose
Primary outcome [89] 0 0
Part G: Mean Ae of ETX0282 and ETX1317
Timepoint [89] 0 0
Days 1 and 4 (SDs 193 and 196): 30 minutes predose; 0.25, 0.5, 0.75, 1, 1.5, 2 (predose prior to subsequent dose), 2.5, 3, 4 (predose prior to subsequent dose), 7, 8, 12, and 16 hours postdose. Days 2 and 5 (SDs 194 and 197): 24 hours postdose
Primary outcome [90] 0 0
Part G: Mean CLR of ETX0282 and ETX1317
Timepoint [90] 0 0
Days 1 and 4 (SDs 193 and 196): 30 minutes predose; 0.25, 0.5, 0.75, 1, 1.5, 2 (predose prior to subsequent dose), 2.5, 3, 4 (predose prior to subsequent dose), 7, 8, 12, and 16 hours postdose. Days 2 and 5 (SDs 194 and 197): 24 hours postdose
Primary outcome [91] 0 0
Part G: Mean fe of ETX0282 and ETX1317
Timepoint [91] 0 0
Days 1 and 4 (SDs 193 and 196): 30 minutes predose; 0.25, 0.5, 0.75, 1, 1.5, 2 (predose prior to subsequent dose), 2.5, 3, 4 (predose prior to subsequent dose), 7, 8, 12, and 16 hours postdose. Days 2 and 5 (SDs 194 and 197): 24 hours postdose
Primary outcome [92] 0 0
Part G: Mean dose proportionality of ETX0282 and ETX1317
Timepoint [92] 0 0
Days 1 and 4 (SDs 193 and 196): 30 minutes predose; 0.25, 0.5, 0.75, 1, 1.5, 2 (predose prior to subsequent dose), 2.5, 3, 4 (predose prior to subsequent dose), 7, 8, 12, and 16 hours postdose. Days 2 and 5 (SDs 194 and 197): 24 hours postdose
Secondary outcome [1] 0 0
Number of elderly participants with any non-serious adverse event
Timepoint [1] 0 0
Up to 14 days after the last dose of study drug (SD 210)
Secondary outcome [2] 0 0
Number of elderly participants with any serious adverse event
Timepoint [2] 0 0
Up to 14 days after the last dose of study drug (SD 210)
Secondary outcome [3] 0 0
Number of elderly participants with an adverse event of the indicated causality and severity
Timepoint [3] 0 0
Up to 14 days after the last dose of study drug (SD 210)
Secondary outcome [4] 0 0
Part A: Number of elderly participants with abnormal, clinically significant hematology, clinical chemistry, and urinalysis laboratory values at the indicated time points
Timepoint [4] 0 0
Screening (Day -1); Days 2, 3, 4, 7, and 15±2 (Follow-up)
Secondary outcome [5] 0 0
Part A: Number of elderly participants with abnormal, clinically significant vital sign values at the indicated time points
Timepoint [5] 0 0
Screening (Day -1); Days 2, 3, 4, 7, and 15±2 (Follow-up)
Secondary outcome [6] 0 0
Part A: Number of elderly participants with abnormal, clinically significant electrocardiogram values at the indicated time points
Timepoint [6] 0 0
Screening (Day -1); Days 1-7; Day 15±2 (Follow-up)
Secondary outcome [7] 0 0
Number of participants who received concomitant medications
Timepoint [7] 0 0
Up to 14 days after the last dose of study drug (SD 210)
Secondary outcome [8] 0 0
Part A: Mean Cmax of ETX0282 and ETX1317 in blood of elderly participants (Cohort 6)
Timepoint [8] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Secondary outcome [9] 0 0
Part A: Mean Ct of ETX0282 and ETX1317 in blood of elderly participants (Cohort 6)
Timepoint [9] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Secondary outcome [10] 0 0
Part A: Mean Tmax of ETX0282 and ETX1317 in blood of elderly participants (Cohort 6)
Timepoint [10] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Secondary outcome [11] 0 0
Part A: Mean AUC0-24 of ETX0282 and ETX1317 in blood of elderly participants (Cohort 6)
Timepoint [11] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), and 24 (Day 2) hours postdose
Secondary outcome [12] 0 0
Part A: Mean AUC0-t of ETX0282 and ETX1317 in blood of elderly participants (Cohort 6)
Timepoint [12] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Secondary outcome [13] 0 0
Part A: Mean AUC0-8 of ETX0282 and ETX1317 in blood of elderly participants (Cohort 6)
Timepoint [13] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Secondary outcome [14] 0 0
Part A: Mean Kel of ETX0282 and ETX1317 in blood of elderly participants (Cohort 6)
Timepoint [14] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Secondary outcome [15] 0 0
Part A: Mean t½ of ETX0282 and ETX1317 in blood of elderly participants (Cohort 6)
Timepoint [15] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Secondary outcome [16] 0 0
Part A: Mean CL of ETX0282 and ETX1317 in blood of elderly participants (Cohort 6)
Timepoint [16] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Secondary outcome [17] 0 0
Part A: Mean Vdss of ETX0282 and ETX1317 in blood of elderly participants (Cohort 6)
Timepoint [17] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Secondary outcome [18] 0 0
Part A: Mean Ae of ETX0282 and ETX1317 for elderly participants (Cohort 6)
Timepoint [18] 0 0
Prior to dosing (-6 to 0 hours; Day 1); 0 to 8 (Day 1), 8 to 24 (Day 2), 24 to 48 (Day 3), and 48 to 72 (Day 4) hours postdose
Secondary outcome [19] 0 0
Part A: Mean CLR of ETX0282 and ETX1317 in urine for elderly participants (Cohort 6)
Timepoint [19] 0 0
Prior to dosing (-6 to 0 hours; Day 1); 0 to 8 (Day 1), 8 to 24 (Day 2), 24 to 48 (Day 3), and 48 to 72 (Day 4) hours postdose
Secondary outcome [20] 0 0
Part A: Mean fe of ETX0282 and ETX1317 for elderly participants (Cohort 6)
Timepoint [20] 0 0
Prior to dosing (-6 to 0 hours; Day 1); 0 to 8 (Day 1), 8 to 24 (Day 2), 24 to 48 (Day 3), and 48 to 72 (Day 4) hours postdose
Secondary outcome [21] 0 0
Part A: Mean dose proportionality of ETX0282 and ETX1317 for elderly participants (Cohort 6)
Timepoint [21] 0 0
Predose (0); 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 16 (Day 1), 24 (Day 2), 48 (Day 3), and 72 (Day 4) hours postdose
Secondary outcome [22] 0 0
Part B: Mean Cmax of ETX0282 and ETX1317 in blood
Timepoint [22] 0 0
Days 1-7 (SDs 45-51): predose (0), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 8, 12, 16, 24, 48, and 72 hours postdose
Secondary outcome [23] 0 0
Part B: Mean Ct of ETX0282 and ETX1317 in blood
Timepoint [23] 0 0
Days 1-7 (SDs 45-51): predose (0), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 8, 12, 16, 24, 48, and 72 hours postdose
Secondary outcome [24] 0 0
Part B: Mean Tmax of ETX0282 and ETX1317 in blood
Timepoint [24] 0 0
Days 1-7 (SDs 45-51): predose (0), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 8, 12, 16, 24, 48, and 72 hours postdose
Secondary outcome [25] 0 0
Part B: Mean AUC0-24 of ETX0282 and ETX1317 in blood
Timepoint [25] 0 0
Days 1-7 (SDs 45-51): predose (0), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 8, 12, 16, and 24 hours postdose
Secondary outcome [26] 0 0
Part B: Mean AUC0-t of ETX0282 and ETX1317 in blood
Timepoint [26] 0 0
Days 1-7 (SDs 45-51): predose (0), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 8, 12, 16, 24, 48, and 72 hours postdose
Secondary outcome [27] 0 0
Part B: Mean AUC0-8 of ETX0282 and ETX1317 in blood
Timepoint [27] 0 0
Days 1-7 (SDs 45-51): predose (0), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 8, 12, 16, 24, 48, and 72 hours postdose
Secondary outcome [28] 0 0
Part B: Mean Kel of ETX0282 and ETX1317 in blood
Timepoint [28] 0 0
Days 1-7 (SDs 45-51): predose (0), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 8, 12, 16, 24, 48, and 72 hours postdose
Secondary outcome [29] 0 0
Part B: Mean t½ of ETX0282 and ETX1317 in blood
Timepoint [29] 0 0
Days 1-7 (SDs 45-51): predose (0), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 8, 12, 16, 24, 48, and 72 hours postdose
Secondary outcome [30] 0 0
Part B: Mean CL of ETX0282 and ETX1317 in blood
Timepoint [30] 0 0
Days 1-7 (SDs 45-51): predose (0), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 8, 12, 16, 24, 48, and 72 hours postdose
Secondary outcome [31] 0 0
Part B: Mean Vdss of ETX0282 and ETX1317 in blood
Timepoint [31] 0 0
Days 1-7 (SDs 45-51): predose (0), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 8, 12, 16, 24, 48, and 72 hours postdose
Secondary outcome [32] 0 0
Part B: Mean Ae of ETX0282 and ETX1317
Timepoint [32] 0 0
Days 1-7 (SDs 45-51): prior to dosing (-6 to 0 hours) and at 0-8, 8-24, 24-48, and 48-72 hours postdose
Secondary outcome [33] 0 0
Part B: Mean CLR of ETX0282 and ETX1317
Timepoint [33] 0 0
Days 1-7 (SDs 45-51): prior to dosing (-6 to 0 hours) and at 0-8, 8-24, 24-48, and 48-72 hours postdose
Secondary outcome [34] 0 0
Part B: Mean fe of ETX0282 and ETX1317
Timepoint [34] 0 0
Days 1-7 (SDs 45-51): prior to dosing (-6 to 0 hours) and at 0-8, 8-24, 24-48, and 48-72 hours postdose
Secondary outcome [35] 0 0
Part B: Mean dose proportionality of ETX0282 and ETX1317
Timepoint [35] 0 0
Days 1-7 (SDs 45-51): predose (0), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 8, 12, 16, 24, 48, and 72 hours postdose

Eligibility
Key inclusion criteria
* Aged 18 to 55 years (inclusive) for all participants except for those in Cohort 6 (in Part A); for Cohort 6, only participants aged = 65 years will be enrolled.
* Be in general good health without clinically significant medical history
* Provide voluntary written informed consent prior to any study procedures and are willing and able to comply with the prescribed treatment protocol and evaluations
* Body mass index (BMI) =18.0 kilograms per meters squared (kg/m^2) and =32.0 kg/m^2
* Clinical laboratory values within the normal limits as defined by the clinical laboratory, unless the Principal Investigator decides that out-of-range values are not clinically significant
* Negative screen for drugs of abuse, alcohol, hepatitis B surface antigen, hepatitis C virus antibody, and human immunodeficiency virus at Screening; and drugs of abuse, alcohol predose on Day -1
* Female participants must be of non-childbearing potential (postmenopausal or with evidence of tubal ligation) or using a medically acceptable (highly effective method) contraceptive regimen and must have a negative pregnancy test at Screening (serum) and on Day -1 (urine) prior to study drug dosing. Male participants must be surgically sterile or using a medically acceptable contraceptive regimen. Men should not donate sperm during the study or for 90 days after the final dose of study medication.
Minimum age
18 Years
Maximum age
No limit
Sex
Both males and females
Can healthy volunteers participate?
Yes
Key exclusion criteria
* History of any moderate or severe hypersensitivity or allergic reaction to any ß-lactam antimicrobial (e.g., penicillin or cephalosporin)
* History of hypersensitivity or severe allergic reaction of any type to medications, bee stings, food, or environmental factors. A severe allergic reaction is defined as any of the following: anaphylaxis, urticaria, or angioedema.
* Use of prescription or over-the-counter medications within 7 days of investigational product administration, with the exception of contraceptive medications, paracetamol, oral non-steroidal anti-inflammatory agents, topical over-the-counter preparations, and routine vitamins (if they do not exceed an intake of 20 to 600 times the recommended daily dose), unless agreed as non-clinically relevant by the Principal Investigator and Sponsor
* Participation in an investigational drug or device study within 30 days before study drug dosing, i.e., there were at least 30 days between the last dose in a prior study and dose administration in this study
* Current smoker or difficulty abstaining from smoking for the duration of study confinement
* History of major organ dysfunction
* Infection or any serious underlying medical condition that would impair the participant from receiving study drug
* History of excessive alcohol intake (more than 4 standard drinks daily, on average) or use of recreational drugs within the last 3 months
* Standard donation of blood within 30 days of the study
* Concomitant disease or condition, including laboratory abnormality, which could interfere with the conduct of the study or which would, in the opinion of the Investigator, pose an unacceptable risk to the participant in this study
* Anticipated need for surgery or hospitalization during the study
* Surgery within 30 days before study enrolment
* Unwillingness or inability to comply with the study protocol for any other reason

Study design
Purpose of the study
Treatment
Allocation to intervention
Randomised controlled trial
Procedure for enrolling a subject and allocating the treatment (allocation concealment procedures)
Methods used to generate the sequence in which subjects will be randomised (sequence generation)
Masking / blinding
Blinded (masking used)
Who is / are masked / blinded?
The people receiving the treatment/s

The people assessing the outcomes
The people analysing the results/data
Intervention assignment
Parallel
Other design features
Phase
Phase 1
Type of endpoint/s
Statistical methods / analysis

Recruitment
Recruitment status
Completed
Data analysis
Reason for early stopping/withdrawal
Other reasons
Date of first participant enrolment
Anticipated
Actual
16/03/2018
Date of last participant enrolment
Anticipated
Actual
Date of last data collection
Anticipated
Actual
11/09/2019
Sample size
Target
Accrual to date
Final
99
Recruitment in Australia
Recruitment state(s)
VIC
Recruitment hospital [1] 0 0
Nucleus Network - Melbourne
Recruitment postcode(s) [1] 0 0
3004 - Melbourne

Funding & Sponsors
Primary sponsor type
Commercial sector/industry
Name
Entasis Therapeutics
Address
Country

Ethics approval
Ethics application status

Summary
Brief summary
Trial website
Trial related presentations / publications
Public notes

Contacts
Principal investigator
Name 0 0
Address 0 0
Country 0 0
Phone 0 0
Fax 0 0
Email 0 0
Contact person for public queries
Name 0 0
Address 0 0
Country 0 0
Phone 0 0
Fax 0 0
Email 0 0
Contact person for scientific queries

No information has been provided regarding IPD availability


What supporting documents are/will be available?

No Supporting Document Provided



Results publications and other study-related documents

No documents have been uploaded by study researchers.

Results not provided in https://clinicaltrials.gov/study/NCT03491748