Healthy
Conditions
Keywords
Fasting, Fed condition, Pharmacokinetics
Brief summary
This is a single centre, open label, randomized, two-treatment, two-period, two-sequence, single dose crossover food effect study in 18 subjects. The subjects will receive the study medication under either fed or fast during each treatment period.
Detailed description
The present study will be conducted in healthy male volunteers. A single oral dose will be administered to the subject in each treatment period (under either fasting or fed state). Each treatment period will be separated by at least 7 calendar days. Post dose PK blood samples will be collected in each treatment period to evaluate the food effect on bioavailability of RP6530. The safety and tolerability of single dose will also be evaluated.
Interventions
DRUGRP6530
Single oral dose
Sponsors
Rhizen Pharmaceuticals SA
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 45 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy male volunteers; aged 18 to 45 years; * Body mass index (BMI) between 18.0 and 30.0 kg/m2 inclusive, weight ≥ 50 kg; * Non- smokers or ex-smokers; * Able to give informed consent.
Exclusion criteria
* Subjects with evidence or history of clinically significant disease; * Positive results to HIV Ag/Ab Combo, Hepatitis B surface Antigen (HBsAG (B) (hepatitis B)) or Hepatitis C Virus (HCV (C)) tests; * Subjects who have received any investigational drug in the previous 28 days; * Subjects participated in a study with PI3k inhibitors at least once in past year; * Subjects who have received drugs metabolised by CYP3A4 enzyme in the previous 28 days.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Pharmacokinetic Parameters (Area Under the Plasma Concentration Versus Time Curve (AUC)) | up to 24 hours post-dose. | Pharmacokinetic parameters (Area under the plasma concentration versus time curve (AUC)) AUC0-T of RP6530 in fed and fast state. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Number of Participants Who Were Evaluated for Adverse Events | 7 days | Number of Participants Who Were Evaluated for Adverse Events as Assessed by CTCAE v4.0 |
| Pharmacokinetic Parameters | up to 24 hours post-dose. | Peak Plasma Concentration (Cmax) |
Countries
Canada
Participant flow
Participants by arm
| Arm | Count |
|---|---|
| All Participants A single dose of RP6530 following fasting and Fed condition
RP6530: Single oral dose | 18 |
| Total | 18 |
Withdrawals & dropouts
| Period | Reason | FG000 | FG001 |
|---|---|---|---|
| Overall Study | Adverse Event | 2 | 2 |
Baseline characteristics
| Characteristic | All Participants |
|---|---|
| Age, Continuous | 29 Years STANDARD_DEVIATION 6 |
| Body Mass Index | 24.50 kg/m^2 STANDARD_DEVIATION 2.46 |
| Ethnicity (NIH/OMB) Hispanic or Latino | 3 Participants |
| Ethnicity (NIH/OMB) Not Hispanic or Latino | 15 Participants |
| Ethnicity (NIH/OMB) Unknown or Not Reported | 0 Participants |
| Height | 173.7 cm STANDARD_DEVIATION 7.2 |
| Race (NIH/OMB) American Indian or Alaska Native | 0 Participants |
| Race (NIH/OMB) Asian | 01 Participants |
| Race (NIH/OMB) Black or African American | 0 Participants |
| Race (NIH/OMB) More than one race | 0 Participants |
| Race (NIH/OMB) Native Hawaiian or Other Pacific Islander | 0 Participants |
| Race (NIH/OMB) Unknown or Not Reported | 1 Participants |
| Race (NIH/OMB) White | 16 Participants |
| Region of Enrollment Canada | 18 participants |
| Sex: Female, Male Female | 0 Participants |
| Sex: Female, Male Male | 18 Participants |
| Weight | 73.9 Kg STANDARD_DEVIATION 8.1 |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk |
|---|---|---|
| deaths Total, all-cause mortality | 0 / 16 | 0 / 16 |
| other Total, other adverse events | 5 / 16 | 5 / 16 |
| serious Total, serious adverse events | 0 / 16 | 0 / 16 |
Outcome results
Primary
Pharmacokinetic Parameters (Area Under the Plasma Concentration Versus Time Curve (AUC))
Pharmacokinetic parameters (Area under the plasma concentration versus time curve (AUC)) AUC0-T of RP6530 in fed and fast state.
Time frame: up to 24 hours post-dose.
Population: subjects who provided evaluable data for both treatments (Fasting and fed conditions)
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| RP6530 in Fast Condition | Pharmacokinetic Parameters (Area Under the Plasma Concentration Versus Time Curve (AUC)) | 5277.01 nanogram*hour per millilitre (ng*h/mL) | Geometric Coefficient of Variation 33.4 |
| RP6530 in Fed Condition | Pharmacokinetic Parameters (Area Under the Plasma Concentration Versus Time Curve (AUC)) | 6726.99 nanogram*hour per millilitre (ng*h/mL) | Geometric Coefficient of Variation 29.4 |
p-value: 0.000290% CI: [119.13, 138.59]ANOVA
Secondary
Number of Participants Who Were Evaluated for Adverse Events
Number of Participants Who Were Evaluated for Adverse Events as Assessed by CTCAE v4.0
Time frame: 7 days
Population: Healthy volunteers
| Arm | Measure | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|
| RP6530 in Fast Condition | Number of Participants Who Were Evaluated for Adverse Events | 16 Participants |
| RP6530 in Fed Condition | Number of Participants Who Were Evaluated for Adverse Events | 16 Participants |
Secondary
Pharmacokinetic Parameters
Peak Plasma Concentration (Cmax)
Time frame: up to 24 hours post-dose.
Population: Subjects who provided evaluable data for both treatments
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| RP6530 in Fast Condition | Pharmacokinetic Parameters | 1311.77 nanogram per millilitre (ng/mL) | Geometric Coefficient of Variation 42 |
| RP6530 in Fed Condition | Pharmacokinetic Parameters | 1753.78 nanogram per millilitre (ng/mL) | Geometric Coefficient of Variation 32.6 |
p-value: 0.027890% CI: [111.01, 174.73]ANOVA