Cancer, Pharmacokinetics, Safety, Tolerability
Conditions
Keywords
Dexanabinol, Oral, Safety, Tolerability, Pharmacokinetics
Brief summary
The purpose of this study is to test the safety and observe the pharmacokinetics (distribution and elimination of the drug) of the compound dexanabinol (ETS2101) in healthy male subjects following a single oral dose.
Interventions
DRUGDexanabinol Dose Level 1
Oral formulation of dexanabinol
DRUGDexanabinol Dose Level 2
Oral formulation of dexanabinol
DRUGDexanabinol Dose Level 3
Oral formulation of dexanabinol
DRUGDexanabinol Dose Level 4
Oral formulation of dexanabinol
DRUGDexanabinol Dose Level 5
Oral formulation of dexanabinol
DRUGPlacebo
Sponsors
e-Therapeutics PLC
Study design
Allocation
RANDOMIZED
Intervention model
PARALLEL
Primary purpose
BASIC_SCIENCE
Masking
DOUBLE (Subject, Investigator)
Eligibility
Sex/Gender
MALE
Age
18 Years to 45 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy males aged 18 to 45 years * Body mass index 18.0 to 32.0 kg/m2, or if outside the range, considered not clinically significant by the investigator
Exclusion criteria
* Participation in a clinical research study within the previous 3 months * Current smokers and those who have smoked within the last 12 months * History of any drug or alcohol abuse in the past 2 years
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Safety and Tolerability Based on the Number of Participants With Adverse Events and Comparison of Baseline and Post Dose Parameters | Participants will be followed until follow up visit, 6-11 days after dosing | Safety and tolerability based on the number of participants with adverse events. Assessment and comparison to baseline of the following: * Physical exam * Safety bloods and urinalysis * 12-lead ECG * Vital signs |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Area Under the Curve of the Compound Dexanabinol (ETS2101) From Pre-dose up to 48 Hours Post Dose | Pre-dose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16,24,36,48 hours post dose | Pharmacokinetic parameters will be assessed in a blinded fashion at the end of each cohort, prior to dose escalation. |
Other
| Measure | Time frame | Description |
|---|---|---|
| Pharmacodynamic Biomarker Assessment | Pre-dose, 1, 6 and 24 hours post dose | Blood samples taken and analysed for the purposes of the identification and quantification of pharmacodynamic biomarkers pre-dose and at several points after dosing. |
Countries
United Kingdom
Participant flow
Participants by arm
| Arm | Count |
|---|---|
| Dexanabinol Single oral dose of dexanabinol
Dexanabinol: Oral formulation of dexanabinol | 30 |
| Placebo Single oral dose of matching placebo
Placebo | 10 |
| Total | 40 |
Baseline characteristics
| Characteristic | Dexanabinol | Placebo | Total |
|---|---|---|---|
| Age, Continuous | 32.8 years STANDARD_DEVIATION 8.5 | 28.1 years STANDARD_DEVIATION 8.3 | 31.1 years STANDARD_DEVIATION 8.5 |
| Sex: Female, Male Female | 0 Participants | 0 Participants | 0 Participants |
| Sex: Female, Male Male | 30 Participants | 10 Participants | 40 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk | EG002 affected / at risk | EG003 affected / at risk | EG004 affected / at risk | EG005 affected / at risk |
|---|---|---|---|---|---|---|
| deaths Total, all-cause mortality | — / — | — / — | — / — | — / — | — / — | — / — |
| other Total, other adverse events | 3 / 6 | 1 / 6 | 1 / 6 | 3 / 6 | 1 / 6 | 1 / 10 |
| serious Total, serious adverse events | 0 / 6 | 0 / 6 | 0 / 6 | 0 / 6 | 0 / 6 | 0 / 10 |
Outcome results
Primary
Safety and Tolerability Based on the Number of Participants With Adverse Events and Comparison of Baseline and Post Dose Parameters
Safety and tolerability based on the number of participants with adverse events. Assessment and comparison to baseline of the following: * Physical exam * Safety bloods and urinalysis * 12-lead ECG * Vital signs
Time frame: Participants will be followed until follow up visit, 6-11 days after dosing
| Arm | Measure | Value (NUMBER) |
|---|---|---|
| Dexanabinol | Safety and Tolerability Based on the Number of Participants With Adverse Events and Comparison of Baseline and Post Dose Parameters | 9 participants |
| Placebo | Safety and Tolerability Based on the Number of Participants With Adverse Events and Comparison of Baseline and Post Dose Parameters | 1 participants |
Secondary
Area Under the Curve of the Compound Dexanabinol (ETS2101) From Pre-dose up to 48 Hours Post Dose
Pharmacokinetic parameters will be assessed in a blinded fashion at the end of each cohort, prior to dose escalation.
Time frame: Pre-dose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16,24,36,48 hours post dose
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| Dexanabinol | Area Under the Curve of the Compound Dexanabinol (ETS2101) From Pre-dose up to 48 Hours Post Dose | 37.5 ng.h/mL | Standard Deviation 0 |
| Placebo | Area Under the Curve of the Compound Dexanabinol (ETS2101) From Pre-dose up to 48 Hours Post Dose | 61.3 ng.h/mL | Standard Deviation 75.7 |
| Dose Level 3 | Area Under the Curve of the Compound Dexanabinol (ETS2101) From Pre-dose up to 48 Hours Post Dose | 109 ng.h/mL | Standard Deviation 102.7 |
| Dose Level 4 | Area Under the Curve of the Compound Dexanabinol (ETS2101) From Pre-dose up to 48 Hours Post Dose | 226 ng.h/mL | Standard Deviation 50.7 |
| Dose Level 5 | Area Under the Curve of the Compound Dexanabinol (ETS2101) From Pre-dose up to 48 Hours Post Dose | 192 ng.h/mL | Standard Deviation 68.6 |
Other Pre-specified
Pharmacodynamic Biomarker Assessment
Blood samples taken and analysed for the purposes of the identification and quantification of pharmacodynamic biomarkers pre-dose and at several points after dosing.
Time frame: Pre-dose, 1, 6 and 24 hours post dose