To Evaluate the Food Effect on Relative Bioavailability of RP6530 in Healthy Volunteers

• Sponsor: Rhizen Pharmaceuticals SA (Industry)
• Overall Status: Completed
• CT.gov ID: NCT02690727
• Collaborator: (none)
• Enrollment: 18
• Location: 1
• Arms: 2
• Duration (Days): 29
• Patients Per Site Per Month: 18.9

Study Details

Study Description

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.

Condition or Disease	Intervention/Treatment	Phase
Healthy	Drug: RP6530	Phase 1

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.

Study Design

• Study Type: Interventional
• Actual Enrollment: 18 participants
• Allocation: Randomized
• Intervention Model: Crossover Assignment
• Masking: None (Open Label)
• Primary Purpose: Treatment
• Official Title: An Open Label, Randomized, Single Dose, Cross Over Study to Evaluate Food Effects on Relative Bioavailability of RP6530 Administered in Fasting and Fed Conditions in Healthy Volunteers
• Study Start Date: Feb 1, 2016
• Actual Primary Completion Date: Mar 1, 2016
• Actual Study Completion Date: Mar 1, 2016

Arms and Interventions

Arm	Intervention/Treatment
Experimental: RP6530 in fast condition A single dose of RP6530 following fast condition	Drug: RP6530; Single oral dose; Other Names: A dual PI3K delta/gamma inhibitor
Experimental: RP6530 in fed condition A single dose of RP6530 following fed condition	Drug: RP6530; Single oral dose; Other Names: A dual PI3K delta/gamma inhibitor

Outcome Measures

Primary Outcome Measures

1. 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 Outcome Measures

1. 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

2. Pharmacokinetic Parameters [up to 24 hours post-dose.]

   Peak Plasma Concentration (Cmax)

Eligibility Criteria

Criteria

• Ages Eligible for Study: 18 Years to 45 Years
• Sexes Eligible for Study: Male
• Accepts 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.

Contacts and Locations

Locations

	Site	City	State	Country	Postal Code
1	Algorithme Pharma Inc	Quebec		Canada	H3P 3P1

Sponsors and Collaborators

• Rhizen Pharmaceuticals SA

Investigators

• Principal Investigator: Eric Sicard, M.D, Algorithme Pharma Inc

Study Documents (Full-Text)

None provided.

More Information

Publications

None provided.

• Responsible Party: Rhizen Pharmaceuticals SA
• ClinicalTrials.gov Identifier: NCT02690727
• Other Study ID Numbers: RP6530-1501; ISI-P5-416
• First Posted: Feb 24, 2016
• Last Update Posted: Nov 28, 2017
• Last Verified: Feb 1, 2016

• Individual Participant Data (IPD) Sharing Statement: No
• Plan to Share IPD: No
• Keywords provided by Rhizen Pharmaceuticals SA: Fasting; Fed condition; Pharmacokinetics
• Additional relevant MeSH terms: Tenalisib

Study Results

Participant Flow

Arm/Group Title	RP6530: Fast Condition First, Then Fed Condition	RP6530: Fed Condition First, Then Fast Condition
Arm/Group Description	Fast Condition first, then Fed Condition RP6530: Single oral dose	Fed Condition first, then Fast Condition RP6530: Single oral dose
Period Title: Overall Study
STARTED	9	9
COMPLETED	7	7
NOT COMPLETED	2	2

Baseline Characteristics

Arm/Group Title	All Participants
Arm/Group Description	A single dose of RP6530 following fasting and Fed condition RP6530: Single oral dose
Overall Participants	18
Age (Years) [Mean (Standard Deviation) ]
Mean (Standard Deviation) [Years]	29 (6)
Sex: Female, Male (Count of Participants)
Female	0 0%
Male	18 100%
Ethnicity (NIH/OMB) (Count of Participants)
Hispanic or Latino	3 16.7%
Not Hispanic or Latino	15 83.3%
Unknown or Not Reported	0 0%
Race (NIH/OMB) (Count of Participants)
American Indian or Alaska Native	0 0%
Asian	01 5.6%
Native Hawaiian or Other Pacific Islander	0 0%
Black or African American	0 0%
White	16 88.9%
More than one race	0 0%
Unknown or Not Reported	1 5.6%
Region of Enrollment (participants) [Number]
Canada	18 100%
Weight (Kg) [Mean (Standard Deviation) ]
Mean (Standard Deviation) [Kg]	73.9 (8.1)
Height (cm) [Mean (Standard Deviation) ]
Mean (Standard Deviation) [cm]	173.7 (7.2)
Body Mass Index (kg/m^2) [Mean (Standard Deviation) ]
Mean (Standard Deviation) [kg/m^2]	24.50 (2.46)

Outcome Measures

1. Primary Outcome

Title	Pharmacokinetic Parameters (Area Under the Plasma Concentration Versus Time Curve (AUC))
Description	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.

Outcome Measure Data

Analysis Population Description

subjects who provided evaluable data for both treatments (Fasting and fed conditions)

Arm/Group Title	RP6530 in Fast Condition	RP6530 in Fed Condition
Arm/Group Description	A single dose of RP6530 following fast condition RP6530: Single oral dose	A single dose of RP6530 following fed condition RP6530: Single oral dose
Measure Participants	14	14
Geometric Mean (Geometric Coefficient of Variation) [nanogram*hour per millilitre (ng*h/mL)]	5277.01 (33.4)	6726.99 (29.4)

Statistical Analysis 1

Statistical Analysis Overview	Comparison Group Selection	RP6530 in Fast Condition, RP6530 in Fed Condition
	Comments
	Type of Statistical Test	Superiority or Other
	Comments
Statistical Test of Hypothesis	p-Value	0.0002
	Comments
	Method	ANOVA
	Comments
Method of Estimation	Estimation Parameter	Ratio (%)
	Estimated Value	128.49
	Confidence Interval	(2-Sided) 90%; 119.13 to 138.59
	Parameter Dispersion	Type: Value:
	Estimation Comments

2. Secondary Outcome

Title	Number of Participants Who Were Evaluated for Adverse Events
Description	Number of Participants Who Were Evaluated for Adverse Events as Assessed by CTCAE v4.0
Time Frame	7 days

Outcome Measure Data

Analysis Population Description

Healthy volunteers

Arm/Group Title	RP6530 in Fast Condition	RP6530 in Fed Condition
Arm/Group Description	A single dose of RP6530 following fast Condition RP6530: Single oral dose	A single dose of RP6530 following fed Condition RP6530: Single oral dose
Measure Participants	16	16
Count of Participants [Participants]	16 88.9%	16 NaN

3. Secondary Outcome

Title	Pharmacokinetic Parameters
Description	Peak Plasma Concentration (Cmax)
Time Frame	up to 24 hours post-dose.

Outcome Measure Data

Analysis Population Description

Subjects who provided evaluable data for both treatments

Arm/Group Title	RP6530 in Fast Condition	RP6530 in Fed Condition
Arm/Group Description	A single dose of RP6530 following fast condition RP6530: Single oral dose	A single dose of RP6530 following fed condition RP6530: Single oral dose
Measure Participants	14	14
Geometric Mean (Geometric Coefficient of Variation) [nanogram per millilitre (ng/mL)]	1311.77 (42.0)	1753.78 (32.6)

Statistical Analysis 1

Statistical Analysis Overview	Comparison Group Selection	RP6530 in Fast Condition, RP6530 in Fed Condition
	Comments
	Type of Statistical Test	Superiority or Other
	Comments
Statistical Test of Hypothesis	p-Value	0.0278
	Comments
	Method	ANOVA
	Comments
Method of Estimation	Estimation Parameter	Ratio (%)
	Estimated Value	139.27
	Confidence Interval	(2-Sided) 90%; 111.01 to 174.73
	Parameter Dispersion	Type: Value:
	Estimation Comments

Adverse Events

Time Frame	Day 1 to Day 7
Adverse Event Reporting Description	Subjects who entered the study and received at lease one of the treatments under study. 2 HV dropped in 2nd period in "Fast Condition first, then Fed Condition sequence" similarly, two HV dropped in second period in "Fed Condition first sequence", therefore each treatment had 16 HV for AE evaluation; Fasting 16 and fed 16
Arm/Group Title	RP6530 in Fast Condition		RP6530 in Fed Condition
Arm/Group Description	A single dose of RP6530 following fast condition RP6530: Single oral dose		A single dose of RP6530 following fed condition RP6530: Single oral dose
All Cause Mortality
	RP6530 in Fast Condition		RP6530 in Fed Condition
	Affected / at Risk (%)	# Events	Affected / at Risk (%)	# Events
Total	0/16 (0%)		0/16 (0%)
Serious Adverse Events
	RP6530 in Fast Condition		RP6530 in Fed Condition
	Affected / at Risk (%)	# Events	Affected / at Risk (%)	# Events
Total	0/16 (0%)		0/16 (0%)
Other (Not Including Serious) Adverse Events
	RP6530 in Fast Condition		RP6530 in Fed Condition
	Affected / at Risk (%)	# Events	Affected / at Risk (%)	# Events
Total	5/16 (31.3%)		5/16 (31.3%)
Gastrointestinal disorders
Abdominal distension	1/16 (6.3%)	1	1/16 (6.3%)	1
General disorders
Fatigue	1/16 (6.3%)	1	0/16 (0%)	0
Injury, poisoning and procedural complications
Vessel puncture site bleeding	2/16 (12.5%)	2	1/16 (6.3%)	1
vessel puncture site swelling	1/16 (6.3%)	1	0/16 (0%)	0
Investigations
Hepatic enzyme increased	1/16 (6.3%)	1	2/16 (12.5%)	2
Blood glucose increased	0/16 (0%)	0	1/16 (6.3%)	1
Protein urine present	1/16 (6.3%)	1	0/16 (0%)	0
Nervous system disorders
Dizziness	0/16 (0%)	0	1/16 (6.3%)	1
Headache	1/16 (6.3%)	1	0/16 (0%)	0

Limitations/Caveats

[Not Specified]

More Information

Certain Agreements

Principal Investigators are NOT employed by the organization sponsoring the study.