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Primary objective:
- to investigate the effect of food on the bioavailability of DF 2156Y after single dose administration of 400 mg of ladarixin to healthy male and female volunteers under fed and fasting conditions.
Secondary objectives:
This is a Single center, single dose, open label, randomized, two-way, crossover, food effect on bioavailability study.
More precisely, a single oral dose of 400 mg of ladarixin (two 200 mg capsules) was administered to healthy male and female volunteers under fed (Test treatment) and fasting (Reference treatment) conditions in two consecutive study periods, according to a two-way crossover design, with a wash-out interval of at least 14 days between the two administrations.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| T - R (fed then fasting condition) | Experimental | Subjects were assigned to the sequence of treatments TR to receive Ladarixin in fed conditions (T treatment) during period 1 and in fasting conditions (R treatment) in period 2. |
|
| R - T (fasting then fed condition) | Experimental | Subjects were assigned to the sequence of treatments RT to receive Ladarixin ini fasting conditions (R treatment) in period 1 and in fed conditions (T treatment) during period 2. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Ladarixin | Drug | A single oral dose of 400 mg of ladarixin (two 200 mg capsules) was administered to healthy male and female volunteers under fed (Test treatment) and fasting (Reference treatment) conditions in two consecutive study periods, according to a two-way crossover design, with a wash-out interval of at least 14 days between the two administrations. |
| Measure | Description | Time Frame |
|---|---|---|
| Cmax of Plasma DF 2156Y | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. Cmax = maximum plasma concentration | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| AUC0-t of Plasma DF 2156Y | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. AUC0-t = area under the concentration-time curve (AUC) from zero to the last quantifiable concentrations | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| Measure | Description | Time Frame |
|---|---|---|
| AUC0-∞ of Plasma DF 2156Y | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions: AUC0-∞ = area under the concentration-time curve (AUC) from zero to infinity | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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Inclusion Criteria:
Informed consent: signed written informed consent before inclusion in the study
Sex and Age: men/women, 18-55 years old inclusive
Body Mass Index: 18.5-30 kg/m2 inclusive
Vital signs: systolic blood pressure 100-139 mmHg, diastolic blood pressure 50-89 mmHg, pulse rate 50-90 bpm and body temperature 35.5-37.5° C, measured after 5 min at rest in the sitting position
Full comprehension: ability to comprehend the full nature and purpose of the study, including possible risks and side effects; ability to co-operate with the investigator and to comply with the requirements of the entire study
Contraception and fertility (women only): women of child-bearing potential must not wish to get pregnant within 30 days after the end of the study and must be using at least one of the following reliable methods of contraception:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Milko Radicioni, MD | CROSS Research S.A., I Unit, | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| CROSS Research S.A., I Unit | Arzo | Canton Ticino | 6864 | Switzerland |
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Thirty-six (36) subjects were enrolled in the study, as planned, and 32 of them completed the study as per protocol.
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| ID | Title | Description |
|---|---|---|
| FG000 | T - R (Fed Then Fasting Condition) | Subjects were assigned to the sequence of treatments TR to receive Ladarixin in fed conditions (T treatment) during period 1 and in fasting conditions (R treatment) in period 2. Ladarixin: A single oral dose of 400 mg of ladarixin (two 200 mg capsules) was administered to healthy male and female volunteers under fed (Test treatment) and fasting (Reference treatment) conditions in two consecutive study periods, according to a two-way crossover design, with a wash-out interval of at least 14 days between the two administrations. |
| FG001 | R - T (Fasting Then Fed Condition) | Subjects were assigned to the sequence of treatments RT to receive Ladarixin ini fasting conditions (R treatment) in period 1 and in fed conditions (T treatment) during period 2. Ladarixin: A single oral dose of 400 mg of ladarixin (two 200 mg capsules) was administered to healthy male and female volunteers under fed (Test treatment) and fasting (Reference treatment) conditions in two consecutive study periods, according to a two-way crossover design, with a wash-out interval of at least 14 days between the two administrations. |
| Title | Milestones | Reasons Not Completed | ||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study |
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Enrolled set: all enrolled subjects. This analysis set was used for demographic, baseline and background characteristics
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| ID | Title | Description |
|---|---|---|
| BG000 | Enrolled and Safety Set, PK Set 1 and PK Set 2 | Demographics are reported for the "enrolled set" (N=36), which has the same number of participants of the "safety set", the "PK set 1", and the "PK set 2". |
| Units | Counts |
|---|---|
| Participants |
|
| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes |
|---|---|---|---|---|---|---|---|---|---|
| Age, Categorical | Count of Participants |
| 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 | Cmax of Plasma DF 2156Y | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. Cmax = maximum plasma concentration | PK set 1: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2156Y with no major deviations that could affect the PK results. This analysis set was used for the statistical analysis of the PK results for DF 2156Y. | Posted | Mean | Standard Deviation | μg/mL | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
|
Throughout the study, from screening to final visit /ETV (at day 4 of period 2 or early termination up to 22 days)
The TEAE were calculated based on the safety set. The Safety set consists of all subjects who received at least one dose of study treatments. This analysis set was used for the safety and tolerability analyses.
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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 | Ladarixin Fed (T) | Ladarixin - Fed Conditions: A single oral dose of 400 mg of ladarixin (two 200 mg capsules) was administered to healthy male and female volunteers under fed (Test treatment) conditions. |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Headache | Nervous system disorders | MedDRA 23.0 revised | Systematic Assessment |
Limitations and Caveats not specified.
| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Clinical Development & Operations | Dompé farmaceutici SpA | +39 02 583831 | clinical.trials@dompe.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 | May 28, 2020 | Oct 22, 2021 | Prot_000.pdf |
| SAP | No | Yes | No | Statistical Analysis Plan | Feb 10, 2021 | Oct 22, 2021 | SAP_001.pdf |
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| ID | Term |
|---|---|
| C511776 | 2'-((4'-trifluoromethanesulfonyloxy)phenyl)-N-methanesulfonylpropionamide |
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This is an open-label trial. No masking procedure will be applied since an open-label design was considered adequate for evaluating objective measures such as pharmacokinetic parameters.
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|
|
| Tmax of Plasma DF 2156Y | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. tmax = time to maximum plasma concentration | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| t1/2 of Plasma DF 2156Y | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. t1/2 = half life, is the time required for a quantity to reduce to half of its initial value | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| Lambda-zeta of Plasma DF 2156Y | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. lambda-zeta is the Individual estimate of the terminal elimination rate constant, calculated using log-linear regression of the terminal portions of the plasma concentration-versus-time curves | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| Frel of Plasma DF 2156Y | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. Frel: Relative bioavailability, calculated as ratio AUC0-t (T)/ AUC0-t (R) (multiplicated by 100) | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| Cmax of Plasma DF 2108Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. Cmax = maximum plasma concentration | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| AUC0-t of Plasma DF 2108Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. AUC0-t = area under the concentration-time curve (AUC) from zero to the last quantifiable concentrations | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| AUC0-∞ of Plasma DF 2108Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. AUC0-∞ = area under the concentration-time curve (AUC) from zero to infinity | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| Tmax of Plasma DF 2108Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. tmax = time to maximum plasma concentration | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| t1/2 of Plasma DF 2108Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. t1/2 = half life, is the time required for a quantity to reduce to half of its initial value | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| Lambda-zeta of Plasma DF2108Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. Lambda-zeta is the individual estimate of the terminal elimination rate constant, calculated using log-linear regression of the terminal portions of the plasma concentration-versus-time curves. | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| Frel of Plasma DF2108Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. Frel: Relative bioavailability, calculated as ratio AUC0-t (T)/ AUC0-t (R) (multiplicated by 100) | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| Cmax of Plasma DF2227Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. Cmax = maximum plasma concentration | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| AUC0-t of Plasma DF2227Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. AUC0-t = area under the concentration-time curve (AUC) from zero to the last quantifiable concentrations | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| Tmax of Plasma DF2227Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. tmax = time to maximum plasma concentration | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| Frel of Plasma DF222Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. Frel: Relative bioavailability, calculated as ratio AUC0-t (T)/ AUC0-t (R) (multiplicated by 100) | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
| Participants |
|
| Age, Continuous | Mean | Standard Deviation | years |
|
| Sex: Female, Male | Count of Participants | Participants |
|
| Race (NIH/OMB) | Count of Participants | Participants |
|
| Region of Enrollment | Number | participants |
|
| OG001 | Ladarixin Fasting (R) | Ladarixin - Fasting condition: A single oral dose of 400 mg of ladarixin (two 200 mg capsules) was administered to healthy male and female volunteers under fasting (Reference treatment) condition. |
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| Primary | AUC0-t of Plasma DF 2156Y | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. AUC0-t = area under the concentration-time curve (AUC) from zero to the last quantifiable concentrations | PK set 1: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2156Y with no major deviations that could affect the PK results. This analysis set was used for the statistical analysis of the PK results for DF 2156Y. | Posted | Mean | Standard Deviation | h*μg/mL | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| Secondary | AUC0-∞ of Plasma DF 2156Y | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions: AUC0-∞ = area under the concentration-time curve (AUC) from zero to infinity | PK set 1: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2156Y with no major deviations that could affect the PK results. This analysis set was used for the statistical analysis of the PK results for DF 2156Y. | Posted | Mean | Standard Deviation | h*μg/mL | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| Secondary | Tmax of Plasma DF 2156Y | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. tmax = time to maximum plasma concentration | PK set 1: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2156Y with no major deviations that could affect the PK results. This analysis set was used for the statistical analysis of the PK results for DF 2156Y. | Posted | Mean | Standard Deviation | h | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| Secondary | t1/2 of Plasma DF 2156Y | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. t1/2 = half life, is the time required for a quantity to reduce to half of its initial value | PK set 1: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2156Y with no major deviations that could affect the PK results. This analysis set was used for the statistical analysis of the PK results for DF 2156Y. | Posted | Mean | Standard Deviation | h | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| Secondary | Lambda-zeta of Plasma DF 2156Y | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. lambda-zeta is the Individual estimate of the terminal elimination rate constant, calculated using log-linear regression of the terminal portions of the plasma concentration-versus-time curves | PK set 1: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2156Y with no major deviations that could affect the PK results. This analysis set was used for the statistical analysis of the PK results for DF 2156Y. | Posted | Mean | Standard Deviation | 1/h | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| Secondary | Frel of Plasma DF 2156Y | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. Frel: Relative bioavailability, calculated as ratio AUC0-t (T)/ AUC0-t (R) (multiplicated by 100) | PK sets 1 and 2 : PK set 1: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2156Y with no major deviations that could affect the PK results. PK set 2: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2108Y and DF 2227Y, with no major deviations that could affect the PK results. | Posted | Mean | Standard Deviation | percentage of bioavailability | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| Secondary | Cmax of Plasma DF 2108Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. Cmax = maximum plasma concentration | PK set 2: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2108Y and DF 2227Y, with no major deviations that could affect the PK results. This analysis set was used for the statistical analysis of the PK results for DF 2108Y and DF 2227Y. | Posted | Mean | Standard Deviation | μg/mL | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| Secondary | AUC0-t of Plasma DF 2108Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. AUC0-t = area under the concentration-time curve (AUC) from zero to the last quantifiable concentrations | PK set 2: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2108Y and DF 2227Y, with no major deviations that could affect the PK results. This analysis set was used for the statistical analysis of the PK results for DF 2108Y and DF 2227Y. | Posted | Mean | Standard Deviation | (h*μg/mL | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| Secondary | AUC0-∞ of Plasma DF 2108Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. AUC0-∞ = area under the concentration-time curve (AUC) from zero to infinity | PK set 2: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2108Y and DF 2227Y, with no major deviations that could affect the PK results. This analysis set was used for the statistical analysis of the PK results for DF 2108Y and DF 2227Y. | Posted | Mean | Standard Deviation | h*μg/mL | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| Secondary | Tmax of Plasma DF 2108Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. tmax = time to maximum plasma concentration | PK set 2: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2108Y and DF 2227Y, with no major deviations that could affect the PK results. This analysis set was used for the statistical analysis of the PK results for DF 2108Y and DF 2227Y. | Posted | Mean | Standard Deviation | h | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| Secondary | t1/2 of Plasma DF 2108Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. t1/2 = half life, is the time required for a quantity to reduce to half of its initial value | PK set 2: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2108Y and DF 2227Y, with no major deviations that could affect the PK results. This analysis set was used for the statistical analysis of the PK results for DF 2108Y and DF 2227Y. | Posted | Mean | Standard Deviation | h | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| Secondary | Lambda-zeta of Plasma DF2108Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. Lambda-zeta is the individual estimate of the terminal elimination rate constant, calculated using log-linear regression of the terminal portions of the plasma concentration-versus-time curves. | PK set 2: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2108Y and DF 2227Y, with no major deviations that could affect the PK results. This analysis set was used for the statistical analysis of the PK results for DF 2108Y and DF 2227Y. | Posted | Mean | Standard Deviation | 1/h | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| Secondary | Frel of Plasma DF2108Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. Frel: Relative bioavailability, calculated as ratio AUC0-t (T)/ AUC0-t (R) (multiplicated by 100) | PK sets 1 and 2 : PK set 1: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2156Y with no major deviations that could affect the PK results. PK set 2: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2108Y and DF 2227Y, with no major deviations that could affect the PK results. | Posted | Mean | Standard Deviation | percentage of bioavailability | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| Secondary | Cmax of Plasma DF2227Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. Cmax = maximum plasma concentration | PK set 2: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2108Y and DF 2227Y, with no major deviations that could affect the PK results. This analysis set was used for the statistical analysis of the PK results for DF 2108Y and DF 2227Y. | Posted | Mean | Standard Deviation | μg/mL | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| Secondary | AUC0-t of Plasma DF2227Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. AUC0-t = area under the concentration-time curve (AUC) from zero to the last quantifiable concentrations | PK set 2: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2108Y and DF 2227Y, with no major deviations that could affect the PK results. This analysis set was used for the statistical analysis of the PK results for DF 2108Y and DF 2227Y. | Posted | Mean | Standard Deviation | h*μg/mL | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| Secondary | Tmax of Plasma DF2227Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. tmax = time to maximum plasma concentration | PK set 2: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2108Y and DF 2227Y, with no major deviations that could affect the PK results. This analysis set was used for the statistical analysis of the PK results for DF 2108Y and DF 2227Y | Posted | Mean | Standard Deviation | hours | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| Secondary | Frel of Plasma DF222Y (DF 2156Y Metabolite) | PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. Frel: Relative bioavailability, calculated as ratio AUC0-t (T)/ AUC0-t (R) (multiplicated by 100) | PK sets 1 and 2 : PK set 1: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2156Y with no major deviations that could affect the PK results. PK set 2: all subjects randomised who fulfilled the study protocol requirements in terms of IMP intake and had evaluable PK data readouts for DF 2108Y and DF 2227Y, with no major deviations that could affect the PK results. | Posted | Mean | Standard Deviation | percentage of bioavailability | At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose) |
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| 0 |
| 33 |
| 0 |
| 33 |
| 4 |
| 33 |
| EG001 | Ladarixin Fasting (R) | Ladarixin - Fasting conditions: A single oral dose of 400 mg of ladarixin (two 200 mg capsules) was administered to healthy male and female volunteers under fasting (Reference treatment) conditions. | 0 | 35 | 0 | 35 | 4 | 35 |
| Presyncope | Nervous system disorders | MedDRA 23.0 revised | Systematic Assessment |
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| Nausea | Gastrointestinal disorders | MedDRA 23.0 revised | Systematic Assessment |
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| Toothache | Gastrointestinal disorders | MedDRA 23.0 revised | Systematic Assessment |
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| Vomiting | Gastrointestinal disorders | MedDRA 23.0 revised | Systematic Assessment |
|
| SARS-CoV-2 test positive | Investigations | MedDRA 23.0 revised | Systematic Assessment |
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| Neck pain | Musculoskeletal and connective tissue disorders | MedDRA 23.0 revised | Systematic Assessment |
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Not provided
Not provided