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| Name | Class |
|---|---|
| OCT LLC | INDUSTRY |
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Open-label prospective non-comparative safety, tolerability and pharmacokinetics ascending dose randomized cohort study of PBTZ169 (capsules 40 mg) in fasted healthy volunteers after single and multiple oral administration
Open-label prospective non-comparative safety, tolerability and pharmacokinetics ascending dose randomized cohort study of PBTZ169 (capsules 40 mg) in adult man healthy volunteers after single and multiple oral fasting administration. Study was conducted in one study center in Russian Federation. The study included two stages:
Screening procedures for each cohort performed within 7 days before the drug prescription and after the end of administration period in previous cohort. Screening in cohorts 2 and 6 was started only after safety tolerability and PK data analysis of previous cohorts.
All volunteers met the study inclusion/exclusion criteria was included successively into the following cohorts on Stage 1 (actual data):
On Stage 2 (actual data):
Safety was assessed throughout the study. For every volunteer series of urine and venous blood samples was collected for the safety, tolerability and PK assessment of PBTZ169.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Cohort 1 | Experimental | 6 male healthy volunteers each of whom received once single oral dose of PBTZ169 - 40 mg (1 capsule) |
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| Cohort 2 | Experimental | 6 male healthy volunteers each of whom received once single oral dose of PBTZ169 - 80 mg (2 capsules) |
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| Cohort 3 | Experimental | 6 male healthy volunteers each of whom received once single oral dose of PBTZ169 - 160 mg (4 capsules) |
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| Cohort 4 | Experimental | 6 male healthy volunteers each of whom received once single oral dose of PBTZ169 - 320 mg (8 capsules) |
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| Cohort 5 | Experimental | 6 male healthy volunteers each of whom received once single oral dose of PBTZ169 - 640 mg (16 capsules) |
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| Cohort 6 | Experimental |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| PBTZ169 - 40 mg | Drug | 40 mg of PBTZ169 (1 capsule) orally once in fasting state |
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| Measure | Description | Time Frame |
|---|---|---|
| Incidence of Drug-related Adverse Events [Safety and Tolerability] | The frequency of adverse events for which a relationship to the test drug PBTZ169 was noted | 14±1 days after the drug administration (up to last visit time point) |
| Measure | Description | Time Frame |
|---|---|---|
| Peak Plasma Concentration (Сmax) of PBTZ169 | Up to 72 hours after the last drug administration: Single dosing (Cohorts 1-5): up to Day 4 (72 h after the dosing (Day 1)) Multiple dosing (Cohorts 6. 7): up to Day 17 (72 h after the last (14th) dosing) | Up to 72 hours after the last drug administration |
| Time to Reach Maximum Concentration (Tmax) of PBTZ169 |
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Inclusion Criteria:
Written informed consent received from a volunteer.
Man aged 18 to 45 years old, inclusive.
Body mass index of 18.5-25 kg/m2.
Verified diagnosis: "healthy" according to data of standard clinical, laboratory and instrumental examination methods performed at screening:
Ability, according to investigators opinion, to comply with all requirements of the protocol.
Agreement to use double contraception method during the study participation and for 3 months after the test drug administration - combination of male condom with not less than one of the following methods:
Exclusion Criteria:
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| ID | Title | Description |
|---|---|---|
| FG000 | Cohort 1 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 40 mg (1 capsule) PBTZ169 - 40 mg: 40 mg of PBTZ169 (1 capsule) orally once in fasting state |
| FG001 | Cohort 2 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 80 mg (2 capsules) PBTZ169 - 80 mg: 80 mg of PBTZ169 (2 capsules 40 mg) orally once in fasting state |
| FG002 | Cohort 3 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 160 mg (4 capsules) PBTZ169 - 160 mg: 160 mg of PBTZ169 (4 capsules 40 mg) orally once in fasting state |
| FG003 | Cohort 4 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 320 mg (8 capsules) PBTZ169 - 320 mg: 320 mg of PBTZ169 (8 capsules 40 mg) orally once in fasting state |
| FG004 | Cohort 5 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 640 mg (16 capsules) PBTZ169 - 640 mg: 640 mg of PBTZ169 (16 capsules 40 mg) orally once in fasting state |
| FG005 | Cohort 6 | 5 healthy volunteers each of whom received а daily dose of 320 mg of PBTZ169 (8 capsules 40 mg) for 14 days PBTZ169 - 320 mg (multiple administration): 320 mg of PBTZ169 (8 capsules 40 mg) orally once per day in fasting state for 14 days |
| FG006 | Cohort 7 | 5 healthy volunteers each of whom received a daily dose of 640 mg of PBTZ169 (16 capsules 40 mg) for 14 days PBTZ169 - 640 mg (multiple administration): 640 mg of PBTZ169 (16 capsules 40 mg) orally once per day in fasting state for 14 days |
| Title | Milestones | Reasons Not Completed | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study |
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Safety population
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| ID | Title | Description |
|---|---|---|
| BG000 | Cohort 1 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 40 mg (1 capsule) PBTZ169 - 40 mg: 40 mg of PBTZ169 (1 capsule) orally once in fasting state |
| BG001 | Cohort 2 |
| Units | Counts |
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| Participants |
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| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes |
|---|---|---|---|---|---|---|---|---|---|
| Age, Continuous | Mean |
| 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 Drug-related Adverse Events [Safety and Tolerability] | The frequency of adverse events for which a relationship to the test drug PBTZ169 was noted | Safety population: subjects who received at least one dose of PBTZ169. The population was used for the analysis and evaluation of the demographic and other baseline data and all safety parameters including AEs, physical examination, evaluation of the vital signs, previous and current therapy, ECG, all laboratory tests | Posted | Number | participants | 14±1 days after the drug administration (up to last visit time point) |
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SAD: 14±1 days after PBTZ169 administration (Day 14±1); MAD: 21±1 days after the last (14th) PBTZ169 administration (Day 35±1).
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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 | Cohort 1 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 40 mg (1 capsule) PBTZ169 - 40 mg: 40 mg of PBTZ169 (1 capsule) orally once in fasting state |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Blood glucose increased | Investigations | Systematic Assessment |
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| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Viсtoria Shcherbakova | Nearmedic Plus | +7 (495) 741 49 89 | 3869 | Viktoriya.Shcherbakova@nearmedic.ru |
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| Type | Includes Protocol | Includes SAP | Includes ICF | Document Label | Document Date | Document Uploaded Date | Document File Name |
|---|---|---|---|---|---|---|---|
| Prot_SAP | Yes | Yes | No | Study Protocol and Statistical Analysis Plan | Mar 17, 2016 | Mar 26, 2020 | Prot_SAP_000.pdf |
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| ID | Term |
|---|---|
| D014376 | Tuberculosis |
| ID | Term |
|---|---|
| D009164 | Mycobacterium Infections |
| D000193 | Actinomycetales Infections |
| D016908 | Gram-Positive Bacterial Infections |
| D001424 | Bacterial Infections |
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| ID | Term |
|---|---|
| C000592783 | macozinone |
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5 male healthy volunteers each of whom received once daily for 14 days 320 mg of PBTZ169 (8 capsules 40 mg) |
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| Cohort 7 | Experimental | 5 male healthy volunteers each of whom received once daily for 14 days 640 mg of PBTZ169 (16 capsules 40 mg) |
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| PBTZ169 - 80 mg | Drug | 80 mg of PBTZ169 (2 capsules 40 mg) orally once in fasting state |
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| PBTZ169 - 160 mg | Drug | 160 mg of PBTZ169 (4 capsules 40 mg) orally once in fasting state |
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| PBTZ169 - 320 mg | Drug | 320 mg of PBTZ169 (8 capsules 40 mg) orally once in fasting state |
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| PBTZ169 - 640 mg | Drug | 640 mg of PBTZ169 (16 capsules 40 mg) orally once in fasting state |
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| PBTZ169 - 320 mg (multiple administration) | Drug | 320 mg of PBTZ169 (8 capsules 40 mg) orally once per day in fasting state for 14 days |
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| PBTZ169 - 640 mg (multiple administration) | Drug | 640 mg of PBTZ169 (16 capsules 40 mg) orally once per day in fasting state for 14 days |
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Single dosing (Cohorts 1-5): data for the dosing day (Day 1). Multiple dosing (Cohorts 6, 7): data for days 1 (1st dose), 7 and 14 (last dose) |
| Up to 72 hours after the last drug administration |
| Area Under the Concentration-time Curve (AUC0-∞) | In the time interval from 0 to infinity | Up to 72 hours after the last drug administration |
| Plasma Half-life Time (T1/2) of PBTZ169 | Single dosing (Cohorts 1-5): data for the dosing day (Day 1). Multiple dosing (Cohorts 6, 7): data for days 1 (1st dose), 7 and 14 (last dose) | Up to 72 hours after the last drug administration |
| Mean Plasma Retention Time (MRT) of PBTZ169 | Up to 72 hours after the last drug administration |
| Total (Plasma) Clearance (Cl) of PBTZ169 | The Cl parameter was calculated using the following formulas: for Day 1: Cl=D/AUCinf; for Days 7 and 14: Clss=D/AUCτ | Up to 72 hours after the last drug administration |
| Volume of Distribution (Vd) of PBTZ169 | Up to 72 hours after the last drug administration |
| Elimination Constant (Kel) of PBTZ169 | Data for doses 320 mg (Cohorts 4 and 6, total 11 volunters) & 640 mg (Cohorts 5 and 7, total 11 volunters) were combined | Up to 72 hours after the last drug administration |
| Renal Clearance (Clren) of PBTZ169 | The renal clearance was calculated using values of the cumulative excretion in urine (from zero to 24 hours) and the area under the pharmacokinetic curve (from zero to 24 hours) (the ratio of the cumulative excretion to AUC0-24) | Up to 24 hours after the drug administration |
| Peak Steady State Plasma Concentration (Cmax,ss) of PBTZ169 | For cohorts 6 and 7 (multiple administration) only | Up to 72 hours after the last drug administration |
| Time to Reach Maximum Steady State Concentration (Tmax,ss) of PBTZ169 | For cohorts 6 and 7 (multiple administration) only | Up to 72 hours after the last drug administration |
| Area Under the Plasma Concentration Versus Time Curve in Steady State (AUCss) of PBTZ169 | For cohorts 6 and 7 (multiple administration) only | Up to 72 hours after the last drug administration |
| Volume of Steady State Distribution (Vd,ss) of PBTZ169 | For cohorts 6 and 7 (multiple administration) only | Up to 72 hours after the last drug administration |
| Area Under the Concentration-time Curve (AUC0-t) | The area under the concentration-time curve from 0 to last blood sampling | Up to 72 hours after the last drug administration |
| AUC0-t/AUC0-∞ | AUC0-t/AUC0-∞ ratio | Up to 72 hours after the last drug administration |
6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 80 mg (2 capsules)
PBTZ169 - 80 mg: 80 mg of PBTZ169 (2 capsules 40 mg) orally once in fasting state
| BG002 | Cohort 3 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 160 mg (4 capsules) PBTZ169 - 160 mg: 160 mg of PBTZ169 (4 capsules 40 mg) orally once in fasting state |
| BG003 | Cohort 4 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 320 mg (8 capsules) PBTZ169 - 320 mg: 320 mg of PBTZ169 (8 capsules 40 mg) orally once in fasting state |
| BG004 | Cohort 5 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 640 mg (16 capsules) PBTZ169 - 640 mg: 640 mg of PBTZ169 (16 capsules 40 mg) orally once in fasting state |
| BG005 | Cohort 6 | 5 healthy volunteers each of whom received а daily dose of 320 mg of PBTZ169 (8 capsules 40 mg) for 14 days PBTZ169 - 320 mg (multiple administration): 320 mg of PBTZ169 (8 capsules 40 mg) orally once per day in fasting state for 14 days |
| BG006 | Cohort 7 | 5 healthy volunteers each of whom received a daily dose of 640 mg of PBTZ169 (16 capsules 40 mg) for 14 days PBTZ169 - 640 mg (multiple administration): 640 mg of PBTZ169 (16 capsules 40 mg) orally once per day in fasting state for 14 days |
| BG007 | Total | Total of all reporting groups |
| years |
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| Sex: Female, Male | Count of Participants | Participants |
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| Race (NIH/OMB) | Count of Participants | Participants |
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| Region of Enrollment | Number | participants |
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| Cohort 2 |
6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 80 mg (2 capsules) PBTZ169 - 80 mg: 80 mg of PBTZ169 (2 capsules 40 mg) orally once in fasting state |
| OG002 | Cohort 3 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 160 mg (4 capsules) PBTZ169 - 160 mg: 160 mg of PBTZ169 (4 capsules 40 mg) orally once in fasting state |
| OG003 | Cohort 4 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 320 mg (8 capsules) PBTZ169 - 320 mg: 320 mg of PBTZ169 (8 capsules 40 mg) orally once in fasting state |
| OG004 | Cohort 5 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 640 mg (16 capsules) PBTZ169 - 640 mg: 640 mg of PBTZ169 (16 capsules 40 mg) orally once in fasting state |
| OG005 | Cohort 6 | 5 healthy volunteers each of whom received а daily dose of 320 mg of PBTZ169 (8 capsules 40 mg) for 14 days PBTZ169 - 320 mg (multiple administration): 320 mg of PBTZ169 (8 capsules 40 mg) orally once per day in fasting state for 14 days |
| OG006 | Cohort 7 | 5 healthy volunteers each of whom received a daily dose of 640 mg of PBTZ169 (16 capsules 40 mg) for 14 days PBTZ169 - 640 mg (multiple administration): 640 mg of PBTZ169 (16 capsules 40 mg) orally once per day in fasting state for 14 days |
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| Secondary | Peak Plasma Concentration (Сmax) of PBTZ169 | Up to 72 hours after the last drug administration: Single dosing (Cohorts 1-5): up to Day 4 (72 h after the dosing (Day 1)) Multiple dosing (Cohorts 6. 7): up to Day 17 (72 h after the last (14th) dosing) | Pharmacokinetics analysis population (PKA): C1-5: sbjs who received PBTZ169 and had at least one measurement of PBTZ169 concentration; C6-7: sbjs who received PBTZ169 at least 7 times and had measurements of PBTZ169 concentration after the first and seventh administration. | Posted | Mean | Standard Deviation | ng/ml | Up to 72 hours after the last drug administration |
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| Secondary | Time to Reach Maximum Concentration (Tmax) of PBTZ169 | Single dosing (Cohorts 1-5): data for the dosing day (Day 1). Multiple dosing (Cohorts 6, 7): data for days 1 (1st dose), 7 and 14 (last dose) | PKA | Posted | Median | Full Range | h | Up to 72 hours after the last drug administration |
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| Secondary | Area Under the Concentration-time Curve (AUC0-∞) | In the time interval from 0 to infinity | PKA: C1-5 - SAD, C6-7 - MAD for 14 days | Posted | Mean | Standard Deviation | ng*h/ml | Up to 72 hours after the last drug administration |
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| Secondary | Plasma Half-life Time (T1/2) of PBTZ169 | Single dosing (Cohorts 1-5): data for the dosing day (Day 1). Multiple dosing (Cohorts 6, 7): data for days 1 (1st dose), 7 and 14 (last dose) | PKA | Posted | Mean | Standard Deviation | h | Up to 72 hours after the last drug administration |
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| Secondary | Mean Plasma Retention Time (MRT) of PBTZ169 | PKA | Posted | Mean | Standard Deviation | h | Up to 72 hours after the last drug administration |
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| Secondary | Total (Plasma) Clearance (Cl) of PBTZ169 | The Cl parameter was calculated using the following formulas: for Day 1: Cl=D/AUCinf; for Days 7 and 14: Clss=D/AUCτ | PKA | Posted | Mean | Standard Deviation | L/h | Up to 72 hours after the last drug administration |
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| Secondary | Volume of Distribution (Vd) of PBTZ169 | PKA | Posted | Mean | Standard Deviation | L | Up to 72 hours after the last drug administration |
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| Secondary | Elimination Constant (Kel) of PBTZ169 | Data for doses 320 mg (Cohorts 4 and 6, total 11 volunters) & 640 mg (Cohorts 5 and 7, total 11 volunters) were combined | PKA | Posted | Mean | Standard Deviation | 1/h | Up to 72 hours after the last drug administration |
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| Secondary | Renal Clearance (Clren) of PBTZ169 | The renal clearance was calculated using values of the cumulative excretion in urine (from zero to 24 hours) and the area under the pharmacokinetic curve (from zero to 24 hours) (the ratio of the cumulative excretion to AUC0-24) | PKA | Posted | Mean | Standard Deviation | mL/h | Up to 24 hours after the drug administration |
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| Secondary | Peak Steady State Plasma Concentration (Cmax,ss) of PBTZ169 | For cohorts 6 and 7 (multiple administration) only | Not Posted | Up to 72 hours after the last drug administration | Participants |
| Secondary | Time to Reach Maximum Steady State Concentration (Tmax,ss) of PBTZ169 | For cohorts 6 and 7 (multiple administration) only | Not Posted | Up to 72 hours after the last drug administration | Participants |
| Secondary | Area Under the Plasma Concentration Versus Time Curve in Steady State (AUCss) of PBTZ169 | For cohorts 6 and 7 (multiple administration) only | Not Posted | Up to 72 hours after the last drug administration | Participants |
| Secondary | Volume of Steady State Distribution (Vd,ss) of PBTZ169 | For cohorts 6 and 7 (multiple administration) only | Not Posted | Up to 72 hours after the last drug administration | Participants |
| Secondary | Area Under the Concentration-time Curve (AUC0-t) | The area under the concentration-time curve from 0 to last blood sampling | PKA | Posted | Mean | Standard Deviation | ng*h/ml | Up to 72 hours after the last drug administration |
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| Secondary | AUC0-t/AUC0-∞ | AUC0-t/AUC0-∞ ratio | PKA | Posted | Number | ratio | Up to 72 hours after the last drug administration |
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| 0 |
| 6 |
| 0 |
| 6 |
| 2 |
| 6 |
| EG001 | Cohort 2 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 80 mg (2 capsules) PBTZ169 - 80 mg: 80 mg of PBTZ169 (2 capsules 40 mg) orally once in fasting state | 0 | 6 | 0 | 6 | 2 | 6 |
| EG002 | Cohort 3 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 160 mg (4 capsules) PBTZ169 - 160 mg: 160 mg of PBTZ169 (4 capsules 40 mg) orally once in fasting state | 0 | 6 | 0 | 6 | 1 | 6 |
| EG003 | Cohort 4 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 320 mg (8 capsules) PBTZ169 - 320 mg: 320 mg of PBTZ169 (8 capsules 40 mg) orally once in fasting state | 0 | 6 | 0 | 6 | 0 | 6 |
| EG004 | Cohort 5 | 6 healthy volunteers each of whom received one single oral dose of PBTZ169 - 640 mg (16 capsules) PBTZ169 - 640 mg: 640 mg of PBTZ169 (16 capsules 40 mg) orally once in fasting state | 0 | 6 | 0 | 6 | 0 | 6 |
| EG005 | Cohort 6 | 5 healthy volunteers each of whom received а daily dose of 320 mg of PBTZ169 (8 capsules 40 mg) for 14 days PBTZ169 - 320 mg (multiple administration): 320 mg of PBTZ169 (8 capsules 40 mg) orally once per day in fasting state for 14 days | 0 | 5 | 0 | 5 | 0 | 5 |
| EG006 | Cohort 7 | 5 healthy volunteers each of whom received a daily dose of 640 mg of PBTZ169 (16 capsules 40 mg) for 14 days PBTZ169 - 640 mg (multiple administration): 640 mg of PBTZ169 (16 capsules 40 mg) orally once per day in fasting state for 14 days | 0 | 5 | 0 | 5 | 1 | 5 |
| Headache | Nervous system disorders | Systematic Assessment |
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| Leukocytosis | Blood and lymphatic system disorders | Systematic Assessment |
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There IS an agreement between the Principal Investigator and the Sponsor (or its agents) that restricts the PI's rights to discuss or publish trial results after the trial is completed
| D001423 | Bacterial Infections and Mycoses |
| D007239 | Infections |
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