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A single and multiple ascending dose study of ANA001 in healthy adults to assess the safety and pharmacokinetics
This is a Phase 1, single center, randomized, double blind, single ascending dose (SAD) and multiple ascending dose (MAD) study to assess the safety and pharmacokinetics of ANA001 in healthy adult subjects. In the single ascending dose portion of the study, subjects in 3 cohorts of 10 subjects each will be randomized to receive a single daily oral dose of ANA001 or matching placebo. In the multiple ascending dose portion of the study, subjects in 3 cohorts of 12 subjects each will be randomized to receive twice or thrice daily oral dose of ANA001 or matching placebo.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| SAD Cohort 1: ANA001 1000 mg po | Experimental | Subjects will receive a 1000 mg single oral dose of ANA001 with a standardized light meal presented at 4 x 250 mg capsules. Each capsule is 250 mg. |
|
| SAD Cohort 2: ANA001 2000 mg po | Experimental | Subjects will a 2000 mg single oral dose of ANA001 with a standardized light meal presented at 8 x 250 mg capsules. Each capsule is 250 mg. |
|
| SAD Cohort 3: ANA001 3000 mg po | Experimental | Subjects will a 3000 mg single oral dose of ANA001 with a standardized light meal presented at 12 x 250 mg capsules. Each capsule is 250 mg. |
|
| SAD Cohorts 1, 2 & 3: Pooled Matching Placebo | Placebo Comparator | Subjects will receive matching placebo hydroxypropylmethylcellulose (HPMC) as a single oral dose (4, 8, or 12 capsules) with a standardized light meal. |
|
| MAD Cohort 1: ANA001 1000 mg po BID | Experimental | Subjects will receive an oral dose of 1000mg ANA001 twice daily (BID) with a standardized light meal for 7 consecutive days. Each dose will be presented as 4 250mg capsules. |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Niclosamide | Drug | Niclosamide is an antihelmintic with in-vitro antiviral activity |
|
| Measure | Description | Time Frame |
|---|---|---|
| SAD: Number of Subjects Reporting TEAEs and STEAEs | Number of Subjects Reporting treatment-emergent AEs (TEAEs) and Serious treatment-emergent AEs (STEAEs) in the SAD | Baseline to Day 7. |
| MAD: Number of Subjects Reporting TEAEs and STEAEs | Number of Subjects Reporting treatment-emergent AEs (TEAEs) and Serious treatment-emergent AEs (STEAEs) in the MAD | Baseline to Day 14. |
| SAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in ECG Parameters | Number of Subjects with Clinically Significant changes in ECG parameters from Baseline (PR, QRS, QT, and QTc intervals) | Baseline to Day 7 |
| MAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in ECG Parameters | Number of Subjects with Clinically Significant changes in ECG parameters from Baseline (PR, QRS, QT, and QTc intervals) | Baseline to Day 14 |
| SAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in Haematology | Number of Subjects with Clinically Significant changes in Haematology (Basophils (%),Eosinophils (%, Ery. Mean Corpuscular Hemoglobin, Ery. Mean Corpuscular Volume, Erythrocytes (10^12/L), Hematocrit (%), Hemoglobin (g/dL). Hemoglobin (g/dL), Lymphocytes (%), Monocytes (%), Neutrophils (%)' Platelets (10^9/L), Reticulocytes (%)) | Baseline to Day 7 |
| MAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in Haematology | Number of Subjects with Clinically Significant changes in Haematology (Basophils (%),Eosinophils (%, Ery. Mean Corpuscular Hemoglobin, Ery. Mean Corpuscular Volume, Erythrocytes (10^12/L), Hematocrit (%), Hemoglobin (g/dL). Hemoglobin (g/dL), Lymphocytes (%), Monocytes (%), Neutrophils (%)' Platelets (10^9/L), Reticulocytes (%)) |
| Measure | Description | Time Frame |
|---|---|---|
| SAD: Tmax | Time to reach the maximum plasma concentration (SAD) | PK samples were collected before dosing and at 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 hours. A Follow-up sample was taken Day 7 (±2) after dosing. |
| SAD: Cmax |
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Inclusion Criteria:
Sign the study informed consent form
Man or woman, 18 to 65 years of age inclusive at the time of signing the informed consent form
Overtly healthy as determined by medical evaluation
Body mass index (BMI) within 18 to 30.0 kg/m2 (inclusive) and body weight not less than 50 kg
Blood pressure at Screening and Day -1 between 90 and 140 mmHg systolic, inclusive, and no higher than 90 mmHg diastolic.
A 12-lead electrocardiogram (ECG) at Screening consistent with normal cardiac conduction and function, including:
Non-smoker or ex-smoker for >12 months
If male, must agree to use contraception methods outlined for the study during the treatment period and for at least 30 days (a spermatogenesis cycle) after the last dose of study treatment and refrain from donating sperm during this period
If female, is not pregnant, not breastfeeding, and meets at least one of the following conditions:
Not a woman of childbearing potential (WOCBP)
OR
A WOCBP who agrees to follow the contraceptive guidance during the treatment period and for at least 30 days (one menstrual cycle) after the last dose of study treatment.
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Doug Rank, MD | NeuroBo Pharmaceuticals Inc. | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| WCCT Global Inc. | Cypress | California | 90630 | United States |
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| ID | Title | Description |
|---|---|---|
| FG000 | SAD Cohort 1: ANA001 1000 mg po | Subjects will receive a 1000 mg single oral dose of ANA001 with a standardized light meal presented at 4 x 250 mg capsules. Each capsule is 250 mg. Niclosamide: Niclosamide is an antihelmintic with in-vitro antiviral activity |
| FG001 | SAD Cohort 2: ANA001 2000 mg po | Subjects will a 2000 mg single oral dose of ANA001 with a standardized light meal presented at 8 x 250 mg capsules. Each capsule is 250 mg. Niclosamide: Niclosamide is an antihelmintic with in-vitro antiviral activity |
| FG002 | SAD Cohort 3: ANA001 3000 mg po | Subjects will a 3000 mg single oral dose of ANA001 with a standardized light meal presented at 12 x 250 mg capsules. Each capsule is 250 mg. Niclosamide: Niclosamide is an antihelmintic with in-vitro antiviral activity |
| FG003 | SAD Cohorts 1, 2 & 3: Pooled Matching Placebo | For the single ascending dose (SAD) portion of the study, subjects will receive matching placebo hydroxypropylmethylcellulose (HPMC) as a single oral dose (4, 8, or 12 capsules) with a standardized light meal. Placebo: Matching hydroxypropylmethylcellulose HPMC capsules with no active ingredients |
| FG004 | MAD Cohort 1: ANA001 1000 mg po BID | Subjects will receive an oral dose of 1000mg ANA001 twice daily (BID) with a standardized light meal for 7 consecutive days. Each dose will be presented as 4 250mg capsules. Niclosamide: Niclosamide is an antihelmintic with in-vitro antiviral activity |
| FG005 | MAD Cohort 2: ANA001 1000 mg po TID | Subjects will receive an oral dose of 1000mg ANA001 three times daily (TID) with a standardized light meal for 7 consecutive days. Each dose will be presented as 4 250mg capsules. Niclosamide: Niclosamide is an antihelmintic with in-vitro antiviral activity |
| FG006 | MAD Cohorts 1 & 2: Pooled Matching Placebo | Subjects will receive an oral dose of matching Placebo to ANA001 two (BID) three times daily (TID) with a standardized light meal for 7 consecutive days. Each dose will be presented as 4 250mg capsules of hydroxypropylmethylcellulose (HPMC) Placebo: Matching hydroxypropylmethylcellulose HPMC capsules with no active ingredients |
| Title | Milestones | Reasons Not Completed | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study |
|
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| ID | Title | Description |
|---|---|---|
| BG000 | SAD Cohort 1: ANA001 1000 mg po | Subjects will receive a 1000 mg single oral dose of ANA001 with a standardized light meal presented at 4 x 250 mg capsules. Each capsule is 250 mg |
| BG001 | SAD Cohort 2: ANA001 2000 mg po |
| 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 | SAD: Number of Subjects Reporting TEAEs and STEAEs | Number of Subjects Reporting treatment-emergent AEs (TEAEs) and Serious treatment-emergent AEs (STEAEs) in the SAD | Posted | Number | participants | Baseline to Day 7. |
|
SAD: Adverse Event Collected from Dosing to 7 days after dosing (8 days). MAD: Adverse Event Collected from Dosing on Day 1 to 7 days after final dosing day (15 days).
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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 | SAD Cohort 1: ANA001 1000 mg po | Subjects will receive a 1000 mg single oral dose of ANA001 with a standardized light meal presented at 4 x 250 mg capsules. Each capsule is 250 mg |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Dizziness | Nervous system disorders | Non-systematic Assessment |
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| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Sr. Vice President Clinical Operations | NeurobBo | 8572991035 | crinfo@neurobopharma.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 | Jan 9, 2021 | May 21, 2024 | Prot_000.pdf |
| SAP | No | Yes | No | Statistical Analysis Plan | Oct 22, 2020 | May 21, 2024 | SAP_001.pdf |
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| ID | Term |
|---|---|
| D009534 | Niclosamide |
| ID | Term |
|---|---|
| D012458 | Salicylanilides |
| D000813 | Anilides |
| D000577 | Amides |
| D009930 | Organic Chemicals |
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Randomized, Double-Blind Study
|
| MAD Cohort 2: ANA001 1000 mg po TID | Experimental | Subjects will receive an oral dose of 1000mg ANA001 three times daily (TID) with a standardized light meal for 7 consecutive days. Each dose will be presented as 4 250mg capsules. |
|
| MAD Cohorts 1 & 2: Pooled Matching Placebo | Placebo Comparator | Subjects will receive an oral dose of matching Placebo to ANA001 two (BID) three times daily (TID) with a standardized light meal for 7 consecutive days. Each dose will be presented as 4 250mg capsules of hydroxypropylmethylcellulose (HPMC) |
|
|
| Placebo | Drug | Matching hydroxypropylmethylcellulose HPMC capsules with no active ingredients |
|
|
| Baseline to Day 14 |
| SAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in Serum Chemistry | Number of Subjects with Clinically Significant changes in Serum Chemistry (Alanine Aminotransferase (U/L), Alkaline Phosphatase (U/L), Aspartate Aminotransferase (U/L), Bilirubin (mg/dL), Calcium (mg/dL), Creatinine (mg/dL), Direct Bilirubin (mg/dL, Glucose (mg/dL), Potassium (mmol/L), Protein (g/dL), Sodium (mmol/L), Urea Nitrogen (mg/dL) | Baseline to Day 7 |
| MAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in Serum Chemistry | Number of Subjects with Clinically Significant changes in Serum Chemistry (Alanine Aminotransferase (U/L), Alkaline Phosphatase (U/L), Aspartate Aminotransferase (U/L), Bilirubin (mg/dL), Calcium (mg/dL), Creatinine (mg/dL), Direct Bilirubin (mg/dL, Glucose (mg/dL), Potassium (mmol/L), Protein (g/dL), Sodium (mmol/L), Urea Nitrogen (mg/dL) | Baseline to Day 14 |
| SAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in Urinalysis | Number of Subjects with Clinically Significant changes in Urinalysis (Specific Gravity, Urobilinogen (EU), pH) | Baseline to Day 7 |
| MAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in Urinalysis | Number of Subjects with Clinically Significant changes in Urinalysis (Specific Gravity, Urobilinogen (EU), pH) | Baseline to Day 14 |
| SAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in Vital Signs | Number of Subjects with Clinically Significant changes in Vital Signs from Baseline (Diastolic Blood Pressure, Systolic Blood Pressure (mmHg), Pulse Rate (beats/min), Respiratory Rate (breaths/min)) | Baseline to Day 7 |
| MAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in Vital Signs | Number of Subjects with Clinically Significant changes in Vital Signs from Baseline (Diastolic Blood Pressure, Systolic Blood Pressure (mmHg), Pulse Rate (beats/min), Respiratory Rate (breaths/min)) | Baseline to Day 14 |
Maximum plasma concentration during a dosing interval (SAD)
| PK samples were collected before dosing and at 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 hours. A Follow-up sample was taken Day 7 (±2) after dosing. |
| SAD: AUC0-t | Area under the plasma concentration-time curve from time 0 to time the last quantifiable concentration (SAD) | PK samples were collected before dosing and at 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 hours. A Follow-up sample was taken Day 7 (±2) after dosing. |
| SAD: AUC0-∞ | Area under the plasma concentration time curve from time 0 extrapolated to infinity, calculated as AUC0-last + Clast/λ, where Clast is the last quantifiable concentration at time t (SAD) | PK samples were collected before dosing and at 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 hours. A Follow-up sample was taken Day 7 (±2) after dosing. |
| SAD: t1/2 | Elimination half-life associated with the terminal slope (λ) of the semilogarithmic drug concentration-time curve, calculated as 0.693/λ (SAD) | PK samples were collected before dosing and at 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 hours. A Follow-up sample was taken Day 7 (±2) after dosing. |
| SAD: CL/F | Systemic Clearance (SAD) | PK samples were collected before dosing and at 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 hours. A Follow-up sample was taken Day 7 (±2) after dosing. |
| SAD: Vz/F | Volume of distribution (SAD) | PK samples were collected before dosing and at 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 hours. A Follow-up sample was taken Day 7 (±2) after dosing. |
| MAD: Tmax Day 1 | Time to reach the maximum plasma concentration Day 1 | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
| MAD: Tmax Day 7 | Time to reach the maximum plasma concentration (Day 7) | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
| MAD: Cmax Day 1 | Maximum plasma concentration during a dosing interval (Day 1) | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: For BID but omitting samples at 10, and 12 hours after dosing. |
| MAD: Cmax Day 7 | Maximum plasma concentration during a dosing interval (Day 7) | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
| MAD: AUC0-t Day 1 | Area under the plasma concentration-time curve from time 0 to time the last quantifiable concentration (Day 1) | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
| MAD: AUC0-t Day 7 | Area under the plasma concentration-time curve from time 0 to time the last quantifiable concentration (Day 7) | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
| MAD: AUC0-tau Day 1 | Area under the plasma concentration-time curve over the dosing interval at steady-state, calculated from the dosing interval (Day 1) | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
| MAD: AUC0-tau Day 7 | Area under the plasma concentration-time curve over the dosing interval at steady-state, calculated from the dosing interval (Day 7) | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
| MAD: t1/2 Day 1 | Elimination half-life associated with the terminal slope (λ) of the semilogarithmic drug concentration-time curve, calculated as 0.693/λ (Day 1) | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
| MAD: t1/2 Day 7 | Elimination half-life associated with the terminal slope (λ) of the semilogarithmic drug concentration-time curve, calculated as 0.693/λ (Day 7) | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
| MAD: CLss Day 1 | Systemic Clearance at steady state (Day 1) | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
| MAD: CLss Day 7 | Systemic Clearance at steady state (Day 7) | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
| MAD: Vdss Day 1 | Volume of distribution at steady state (Day 1) | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
| MAD: Vdss Day 7 | Volume of distribution at steady state (Day 7) | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
Subjects will a 2000 mg single oral dose of ANA001 with a standardized light meal presented at 8 x 250 mg capsules. Each capsule is 250 mg.
| BG002 | SAD Cohort 3: ANA001 3000 mg po | Subjects will a 3000 mg single oral dose of ANA001 with a standardized light meal presented at 12 x 250 mg capsules. Each capsule is 250 mg. |
| BG003 | SAD Cohorts 1, 2 & 3: Pooled Matching Placebo | A matching placebo to a single oral 3000mg dose of 1000mg was administered with a standardized light meal (500 to 750 cal) after an overnight fast of at least 10 hours. |
| BG004 | MAD Cohort 1: ANA001 1000 mg po BID | Subjects will receive an oral dose of 1000mg ANA001 twice daily (BID) with a standardized light meal for 7 consecutive days. Each dose will be presented as 4 250mg capsules |
| BG005 | MAD Cohort 2: ANA001 1000 mg po TID | Subjects will receive an oral dose of 1000mg ANA001 three times daily (TID) with a standardized light meal for 7 consecutive days. Each dose will be presented as 4 250mg capsules. |
| BG006 | MAD Cohorts 1 & 2: Pooled Matching Placebo | Subjects will receive an oral dose of matching Placebo to ANA001 two (BID) three times daily (TID) with a standardized light meal for 7 consecutive days. Each dose will be presented as 4 250mg capsules of hydroxypropylmethylcellulose (HPMC) |
| BG007 | Total | Total of all reporting groups |
| Participants |
|
| Age, Continuous | Mean | Standard Deviation | Years |
|
| Sex: Female, Male | Count of Participants | Participants |
|
| Ethnicity (NIH/OMB) | Count of Participants | Participants |
|
| Race (NIH/OMB) | Count of Participants | Participants |
|
| Region of Enrollment | Number | participants |
|
| OG002 |
| SAD Cohort 3: ANA001 3000 mg po |
Subjects will a 3000 mg single oral dose of ANA001 with a standardized light meal presented at 12 x 250 mg capsules. Each capsule is 250 mg. |
| OG003 | SAD Cohorts 1, 2 & 3: Pooled Matching Placebo | A matching placebo to a single oral 3000mg dose of 1000mg was administered with a standardized light meal (500 to 750 cal) after an overnight fast of at least 10 hours. |
|
|
| Primary | MAD: Number of Subjects Reporting TEAEs and STEAEs | Number of Subjects Reporting treatment-emergent AEs (TEAEs) and Serious treatment-emergent AEs (STEAEs) in the MAD | Posted | Number | participants | Baseline to Day 14. |
|
|
|
| Primary | SAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in ECG Parameters | Number of Subjects with Clinically Significant changes in ECG parameters from Baseline (PR, QRS, QT, and QTc intervals) | Posted | Number | participants | Baseline to Day 7 |
|
|
|
| Primary | MAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in ECG Parameters | Number of Subjects with Clinically Significant changes in ECG parameters from Baseline (PR, QRS, QT, and QTc intervals) | Posted | Number | participants | Baseline to Day 14 |
|
|
|
| Primary | SAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in Haematology | Number of Subjects with Clinically Significant changes in Haematology (Basophils (%),Eosinophils (%, Ery. Mean Corpuscular Hemoglobin, Ery. Mean Corpuscular Volume, Erythrocytes (10^12/L), Hematocrit (%), Hemoglobin (g/dL). Hemoglobin (g/dL), Lymphocytes (%), Monocytes (%), Neutrophils (%)' Platelets (10^9/L), Reticulocytes (%)) | Posted | Number | participants | Baseline to Day 7 |
|
|
|
| Primary | MAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in Haematology | Number of Subjects with Clinically Significant changes in Haematology (Basophils (%),Eosinophils (%, Ery. Mean Corpuscular Hemoglobin, Ery. Mean Corpuscular Volume, Erythrocytes (10^12/L), Hematocrit (%), Hemoglobin (g/dL). Hemoglobin (g/dL), Lymphocytes (%), Monocytes (%), Neutrophils (%)' Platelets (10^9/L), Reticulocytes (%)) | Posted | Number | participants | Baseline to Day 14 |
|
|
|
| Primary | SAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in Serum Chemistry | Number of Subjects with Clinically Significant changes in Serum Chemistry (Alanine Aminotransferase (U/L), Alkaline Phosphatase (U/L), Aspartate Aminotransferase (U/L), Bilirubin (mg/dL), Calcium (mg/dL), Creatinine (mg/dL), Direct Bilirubin (mg/dL, Glucose (mg/dL), Potassium (mmol/L), Protein (g/dL), Sodium (mmol/L), Urea Nitrogen (mg/dL) | Posted | Number | participants | Baseline to Day 7 |
|
|
|
| Primary | MAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in Serum Chemistry | Number of Subjects with Clinically Significant changes in Serum Chemistry (Alanine Aminotransferase (U/L), Alkaline Phosphatase (U/L), Aspartate Aminotransferase (U/L), Bilirubin (mg/dL), Calcium (mg/dL), Creatinine (mg/dL), Direct Bilirubin (mg/dL, Glucose (mg/dL), Potassium (mmol/L), Protein (g/dL), Sodium (mmol/L), Urea Nitrogen (mg/dL) | Posted | Number | participants | Baseline to Day 14 |
|
|
|
| Primary | SAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in Urinalysis | Number of Subjects with Clinically Significant changes in Urinalysis (Specific Gravity, Urobilinogen (EU), pH) | Posted | Number | participants | Baseline to Day 7 |
|
|
|
| Primary | MAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in Urinalysis | Number of Subjects with Clinically Significant changes in Urinalysis (Specific Gravity, Urobilinogen (EU), pH) | Posted | Number | participants | Baseline to Day 14 |
|
|
|
| Primary | SAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in Vital Signs | Number of Subjects with Clinically Significant changes in Vital Signs from Baseline (Diastolic Blood Pressure, Systolic Blood Pressure (mmHg), Pulse Rate (beats/min), Respiratory Rate (breaths/min)) | Posted | Number | participants | Baseline to Day 7 |
|
|
|
| Primary | MAD: Safety and Tolerability of ANA001 as Measured by Clinically Significant Changes in Vital Signs | Number of Subjects with Clinically Significant changes in Vital Signs from Baseline (Diastolic Blood Pressure, Systolic Blood Pressure (mmHg), Pulse Rate (beats/min), Respiratory Rate (breaths/min)) | Posted | Number | participants | Baseline to Day 14 |
|
|
|
| Secondary | SAD: Tmax | Time to reach the maximum plasma concentration (SAD) | Posted | Median | Full Range | h | PK samples were collected before dosing and at 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 hours. A Follow-up sample was taken Day 7 (±2) after dosing. |
|
|
|
| Secondary | SAD: Cmax | Maximum plasma concentration during a dosing interval (SAD) | Posted | Mean | Standard Deviation | ng/mL | PK samples were collected before dosing and at 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 hours. A Follow-up sample was taken Day 7 (±2) after dosing. |
|
|
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| Secondary | SAD: AUC0-t | Area under the plasma concentration-time curve from time 0 to time the last quantifiable concentration (SAD) | Posted | Mean | Standard Deviation | h*ng/mL | PK samples were collected before dosing and at 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 hours. A Follow-up sample was taken Day 7 (±2) after dosing. |
|
|
|
| Secondary | SAD: AUC0-∞ | Area under the plasma concentration time curve from time 0 extrapolated to infinity, calculated as AUC0-last + Clast/λ, where Clast is the last quantifiable concentration at time t (SAD) | Posted | Mean | Standard Deviation | h*ng/mL | PK samples were collected before dosing and at 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 hours. A Follow-up sample was taken Day 7 (±2) after dosing. |
|
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|
| Secondary | SAD: t1/2 | Elimination half-life associated with the terminal slope (λ) of the semilogarithmic drug concentration-time curve, calculated as 0.693/λ (SAD) | Posted | Mean | Standard Deviation | h | PK samples were collected before dosing and at 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 hours. A Follow-up sample was taken Day 7 (±2) after dosing. |
|
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| Secondary | SAD: CL/F | Systemic Clearance (SAD) | Posted | Mean | Standard Deviation | L/h | PK samples were collected before dosing and at 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 hours. A Follow-up sample was taken Day 7 (±2) after dosing. |
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| Secondary | SAD: Vz/F | Volume of distribution (SAD) | Posted | Mean | Standard Deviation | L | PK samples were collected before dosing and at 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 hours. A Follow-up sample was taken Day 7 (±2) after dosing. |
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| Secondary | MAD: Tmax Day 1 | Time to reach the maximum plasma concentration Day 1 | Posted | Median | Full Range | h | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
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| Secondary | MAD: Tmax Day 7 | Time to reach the maximum plasma concentration (Day 7) | Posted | Median | Full Range | h | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
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| Secondary | MAD: Cmax Day 1 | Maximum plasma concentration during a dosing interval (Day 1) | Posted | Mean | Standard Deviation | ng/mL | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: For BID but omitting samples at 10, and 12 hours after dosing. |
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| Secondary | MAD: Cmax Day 7 | Maximum plasma concentration during a dosing interval (Day 7) | Posted | Mean | Standard Deviation | ng/mL | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
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| Secondary | MAD: AUC0-t Day 1 | Area under the plasma concentration-time curve from time 0 to time the last quantifiable concentration (Day 1) | Posted | Mean | Standard Deviation | h*ng/mL | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
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| Secondary | MAD: AUC0-t Day 7 | Area under the plasma concentration-time curve from time 0 to time the last quantifiable concentration (Day 7) | Posted | Mean | Standard Deviation | h*ng/mL | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
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| Secondary | MAD: AUC0-tau Day 1 | Area under the plasma concentration-time curve over the dosing interval at steady-state, calculated from the dosing interval (Day 1) | Posted | Mean | Standard Deviation | h*ng/mL | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
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| Secondary | MAD: AUC0-tau Day 7 | Area under the plasma concentration-time curve over the dosing interval at steady-state, calculated from the dosing interval (Day 7) | Posted | Mean | Standard Deviation | h*ng/mL | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
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| Secondary | MAD: t1/2 Day 1 | Elimination half-life associated with the terminal slope (λ) of the semilogarithmic drug concentration-time curve, calculated as 0.693/λ (Day 1) | Posted | Mean | Standard Deviation | h | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
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| Secondary | MAD: t1/2 Day 7 | Elimination half-life associated with the terminal slope (λ) of the semilogarithmic drug concentration-time curve, calculated as 0.693/λ (Day 7) | Posted | Mean | Standard Deviation | h | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
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| Secondary | MAD: CLss Day 1 | Systemic Clearance at steady state (Day 1) | Posted | Mean | Standard Deviation | L/h | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
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| Secondary | MAD: CLss Day 7 | Systemic Clearance at steady state (Day 7) | Posted | Mean | Standard Deviation | L/h | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
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| Secondary | MAD: Vdss Day 1 | Volume of distribution at steady state (Day 1) | Posted | Mean | Standard Deviation | L | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
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| Secondary | MAD: Vdss Day 7 | Volume of distribution at steady state (Day 7) | Posted | Mean | Standard Deviation | L | BID: Samples on Days 1 and 7 before dosing and at 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after dosing; Days 2, 4, 6, and 8 before dosing and before the 12 h. dose on Days 2, 4, and 6.TID: As BID but omitting samples at 10, and 12 hours after dosing. |
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| 0 |
| 8 |
| 0 |
| 8 |
| 0 |
| 8 |
| EG001 | SAD Cohort 2: ANA001 2000 mg po | Subjects will a 2000 mg single oral dose of ANA001 with a standardized light meal presented at 8 x 250 mg capsules. Each capsule is 250 mg. | 0 | 8 | 0 | 8 | 0 | 8 |
| EG002 | SAD Cohort 3: ANA001 3000 mg po | Subjects will a 3000 mg single oral dose of ANA001 with a standardized light meal presented at 12 x 250 mg capsules. Each capsule is 250 mg. | 0 | 8 | 0 | 8 | 0 | 8 |
| EG003 | SAD Cohorts 1, 2 & 3: Pooled Matching Placebo | A matching placebo to a single oral 3000mg dose of 1000mg was administered with a standardized light meal (500 to 750 cal) after an overnight fast of at least 10 hours. | 0 | 6 | 0 | 6 | 1 | 6 |
| EG004 | MAD Cohort 1: ANA001 1000 mg po BID | Subjects will receive an oral dose of 1000mg ANA001 twice daily (BID) with a standardized light meal for 7 consecutive days. Each dose will be presented as 4 250mg capsules | 0 | 9 | 0 | 9 | 3 | 9 |
| EG005 | MAD Cohort 2: ANA001 1000 mg po TID | Subjects will receive an oral dose of 1000mg ANA001 three times daily (TID) with a standardized light meal for 7 consecutive days. Each dose will be presented as 4 250mg capsules. | 0 | 9 | 0 | 9 | 3 | 9 |
| EG006 | MAD Cohorts 1 & 2: Pooled Matching Placebo | Subjects will receive an oral dose of matching Placebo to ANA001 two (BID) three times daily (TID) with a standardized light meal for 7 consecutive days. Each dose will be presented as 4 250mg capsules of hydroxypropylmethylcellulose (HPMC) | 0 | 6 | 0 | 6 | 1 | 6 |
| Alopecia | Skin and subcutaneous tissue disorders | Non-systematic Assessment | Falling Hair |
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| Rash maculo-papular | Skin and subcutaneous tissue disorders | Non-systematic Assessment |
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| Headaches NEC | Nervous system disorders | Non-systematic Assessment | Headache |
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| Abdominal Pain | Gastrointestinal disorders | Non-systematic Assessment | Abdominal Cramps |
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| Haemorrhoids | Gastrointestinal disorders | Non-systematic Assessment |
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| Skin Laceration | Injury, poisoning and procedural complications | Non-systematic Assessment | Skin Tear |
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| Acne | Respiratory, thoracic and mediastinal disorders | Non-systematic Assessment | Pimples |
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Not provided
Not provided
| D012457 |
| Salicylamides |
| D000814 | Aniline Compounds |
| D000588 | Amines |
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