Trial Outcomes & Findings for Relative Bioavailability and Food Effect Study of IX-01 Capsules in Healthy Men (NCT NCT02139826)

Results Overview

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

12 participants

Primary outcome timeframe

Pre-dose up to 96 hours post dose

Results posted on

2020-08-20

Participant Flow

One participant withdrew between arms following a non-serious adverse event - unlikely to be treatment-related

Participant milestones

Participant milestones
Measure	Overall Study Single oral dose of 800 milligrams IX-01 as an aqueous dispersion while fasting, or as a capsule while fasting, or as capsule while fed, in each of 3 treatment periods IX-01
Overall Study STARTED	12
Overall Study COMPLETED	11
Overall Study NOT COMPLETED	1

Reasons for withdrawal

Reasons for withdrawal
Measure	Overall Study Single oral dose of 800 milligrams IX-01 as an aqueous dispersion while fasting, or as a capsule while fasting, or as capsule while fed, in each of 3 treatment periods IX-01
Overall Study Adverse Event	1

Baseline Characteristics

Relative Bioavailability and Food Effect Study of IX-01 Capsules in Healthy Men

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure	Overall Study n=12 Participants All 12 randomized participants
Age, Continuous	32.5 years STANDARD_DEVIATION 9.22 • n=5 Participants
Sex: Female, Male Female	0 Participants n=5 Participants
Sex: Female, Male Male	12 Participants n=5 Participants
Ethnicity (NIH/OMB) Hispanic or Latino	0 Participants n=5 Participants
Ethnicity (NIH/OMB) Not Hispanic or Latino	12 Participants n=5 Participants
Ethnicity (NIH/OMB) Unknown or Not Reported	0 Participants n=5 Participants
Race (NIH/OMB) American Indian or Alaska Native	0 Participants n=5 Participants
Race (NIH/OMB) Asian	1 Participants n=5 Participants
Race (NIH/OMB) Native Hawaiian or Other Pacific Islander	0 Participants n=5 Participants
Race (NIH/OMB) Black or African American	0 Participants n=5 Participants
Race (NIH/OMB) White	10 Participants n=5 Participants
Race (NIH/OMB) More than one race	1 Participants n=5 Participants
Race (NIH/OMB) Unknown or Not Reported	0 Participants n=5 Participants
Region of Enrollment United Kingdom	12 participants n=5 Participants

PRIMARY outcome

Timeframe: Pre-dose up to 96 hours post dose

Outcome measures

Outcome measures
Measure	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule While Fasting Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule After Food Single oral dose of 800 milligrams IX-01 as a capsule, after food, in 1 of 3 treatment periods IX-01
Relative Bioavailability (Frel) of a Capsule Compared to a Liquid Formulation of IX-01 While Fasting, as Calculated by a Ratio of Area Under the Plasma Concentration Time Curve From Time 0 to Infinity	99.93 Ratio: capsule fasted/acqueous fasted Interval 90.8 to 109.98	—	—

PRIMARY outcome

Timeframe: Pre-dose up to 96 hours post dose

Outcome measures

Outcome measures
Measure	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule While Fasting Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule After Food Single oral dose of 800 milligrams IX-01 as a capsule, after food, in 1 of 3 treatment periods IX-01
Relative Bioavailability (Frel) of a Capsule Formulation of IX-01 in the Fed State Compared to the Fasted State, as Calculated by a Ratio of Area Under the Plasma Concentration Time Curve From Time 0 to Infinity	148.85 Ratio: capsule fed/fasted Interval 135.25 to 163.82	—	—

PRIMARY outcome

Timeframe: Pre-dose up to 96 hours post dose

Outcome measures

Outcome measures
Measure	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule While Fasting Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule After Food Single oral dose of 800 milligrams IX-01 as a capsule, after food, in 1 of 3 treatment periods IX-01
Relative Bioavailability (Frel) of a Capsule Compared With a Liquid Formulation of IX-01 While Fasting, as Calculated by a Ratio of Peak Plasma Concentrations	123.78 Ratio: capsule/aqueous Interval 96.76 to 158.36	—	—

PRIMARY outcome

Timeframe: Pre-dose up to 96 hours post dose

Outcome measures

Outcome measures
Measure	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule While Fasting Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule After Food Single oral dose of 800 milligrams IX-01 as a capsule, after food, in 1 of 3 treatment periods IX-01
Relative Bioavailability (Frel) of a Capsule Formulation of IX-01 in a Fed State Compared to a Fasted State, as Calculated by a Ratio of Peak Plasma Concentrations	175.46 Ratio: capsule fed/fasting Interval 137.15 to 224.47	—	—

PRIMARY outcome

Timeframe: Pre-dose and up to 96 hours post dose

Outcome measures

Outcome measures
Measure	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule After Food n=12 Participants Single oral dose of 800 milligrams IX-01 as a capsule, after food, in 1 of 3 treatment periods IX-01
Area Under the Plasma Concentration Time Curve From Time 0 to Infinity, Following a Single Dose of IX-01	20465 h*ng/mL Geometric Coefficient of Variation 38.9	20522 h*ng/mL Geometric Coefficient of Variation 31.7	31613 h*ng/mL Geometric Coefficient of Variation 27.3

PRIMARY outcome

Timeframe: Pre-dose and up to 96 hours post dose

Outcome measures

Outcome measures
Measure	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule After Food n=12 Participants Single oral dose of 800 milligrams IX-01 as a capsule, after food, in 1 of 3 treatment periods IX-01
Peak Plasma Concentration (Cmax) of IX-01	1147 ng/mL Geometric Coefficient of Variation 39.9	1428 ng/mL Geometric Coefficient of Variation 47.9	2518.5 ng/mL Geometric Coefficient of Variation 22.7

PRIMARY outcome

Timeframe: Pre-dose up to 96 hours post dose

Outcome measures

Outcome measures
Measure	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule After Food n=12 Participants Single oral dose of 800 milligrams IX-01 as a capsule, after food, in 1 of 3 treatment periods IX-01
Time to Peak Plasma Concentration (Tmax) of IX-01	1 hours Interval 0.5 to 8.0	1.5 hours Interval 0.75 to 4.0	4 hours Interval 2.0 to 8.0

PRIMARY outcome

Timeframe: Pre-dose up to 96 hours post dose

Outcome measures

Outcome measures
Measure	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule After Food n=12 Participants Single oral dose of 800 milligrams IX-01 as a capsule, after food, in 1 of 3 treatment periods IX-01
Elimination Half Life (t1/2) of IX-01	15 hours Geometric Coefficient of Variation 60.7	12.6 hours Geometric Coefficient of Variation 32	12.2 hours Geometric Coefficient of Variation 40.2

PRIMARY outcome

Timeframe: Pre-dose up to 96 hours post last dose

Outcome measures

Outcome measures
Measure	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule After Food n=12 Participants Single oral dose of 800 milligrams IX-01 as a capsule, after food, in 1 of 3 treatment periods IX-01
Elimination Rate Constant (Kel) of IX-01	0.046 1/h Geometric Coefficient of Variation 60.7	0.055 1/h Geometric Coefficient of Variation 32	0.057 1/h Geometric Coefficient of Variation 40.2

PRIMARY outcome

Timeframe: Pre-dose to the time of the last measurable sample

Outcome measures

Outcome measures
Measure	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule After Food n=12 Participants Single oral dose of 800 milligrams IX-01 as a capsule, after food, in 1 of 3 treatment periods IX-01
Area Under the Plasma Concentration Time Curve From Time 0 to the Time of the Last Measurable Sample of IX-01	19529 h*ng/mL Geometric Coefficient of Variation 34.5	20218 h*ng/mL Geometric Coefficient of Variation 31.1	31270 h*ng/mL Geometric Coefficient of Variation 26.7

PRIMARY outcome

Timeframe: 1, 2, 4 and 6 hours after dosing

Listed by time point of 1, 2, 4, 6 hours post dose

Outcome measures

Outcome measures
Measure	IX-01 Capsule While Fasting n=10 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule While Fasting Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule After Food Single oral dose of 800 milligrams IX-01 as a capsule, after food, in 1 of 3 treatment periods IX-01
Concentration of IX-01 in Cerebrospinal Fluid (CSF) After a Single Dose of the Liquid Formulation of IX-01 At 1 hour, 1 participant analyzed	27.8 ng/mL Standard Deviation 0	—	—
Concentration of IX-01 in Cerebrospinal Fluid (CSF) After a Single Dose of the Liquid Formulation of IX-01 At 2 hours, 2 participants analyzed	24.4 ng/mL Standard Deviation 2.97	—	—
Concentration of IX-01 in Cerebrospinal Fluid (CSF) After a Single Dose of the Liquid Formulation of IX-01 At 4 hours, 3 participants analyzed	54 ng/mL Standard Deviation 17.67	—	—
Concentration of IX-01 in Cerebrospinal Fluid (CSF) After a Single Dose of the Liquid Formulation of IX-01 At 6 hours, 4 participants analyzed	40 ng/mL Standard Deviation 21.04	—	—

SECONDARY outcome

Timeframe: Baseline to study completion (approximately 6 weeks)

Outcome measures

Outcome measures
Measure	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule While Fasting n=11 Participants Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule After Food n=12 Participants Single oral dose of 800 milligrams IX-01 as a capsule, after food, in 1 of 3 treatment periods IX-01
Number of Participants With One or More Drug-Related Adverse Events (AEs) or Any Serious AEs	1 participants	1 participants	2 participants

Adverse Events

IX-01 Aqueous Dispersion While Fasting

Serious events: 0 serious events

Other events: 8 other events

Deaths: 0 deaths

IX-01 Capsule While Fasting

Serious events: 0 serious events

Other events: 3 other events

Deaths: 0 deaths

IX-01 Capsule After Food

Serious events: 0 serious events

Other events: 4 other events

Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Other adverse events
Measure	IX-01 Aqueous Dispersion While Fasting n=11 participants at risk Single oral dose of 800 milligrams IX-01 as an aqueous dispersion, while fasting in 1 of 3 treatment periods IX-01	IX-01 Capsule While Fasting n=11 participants at risk Singe oral dose of 800 milligrams of IX-01 as a capsule, while fasting, in 1 of 3 treatment periods IX-01	IX-01 Capsule After Food n=12 participants at risk Single oral dose of 800 milligrams IX-01 as a capsule, after food, in 1 of 3 treatment periods IX-01
Injury, poisoning and procedural complications Procedural Headache	9.1% 1/11 • Number of events 1 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/12 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated
Cardiac disorders Atrioventricular block second degree	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	8.3% 1/12 • Number of events 1 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated
Respiratory, thoracic and mediastinal disorders Oropharyngeal pain	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	8.3% 1/12 • Number of events 1 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated
Nervous system disorders Headache	18.2% 2/11 • Number of events 2 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	18.2% 2/11 • Number of events 3 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	8.3% 1/12 • Number of events 1 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated
Nervous system disorders Presyncope	18.2% 2/11 • Number of events 2 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/12 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated
Nervous system disorders Dizziness	9.1% 1/11 • Number of events 1 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/12 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated
Nervous system disorders Somnolence	9.1% 1/11 • Number of events 1 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/12 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated
Nervous system disorders Head discomfort	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	8.3% 1/12 • Number of events 1 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated
Gastrointestinal disorders Nausea	9.1% 1/11 • Number of events 1 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/12 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated
Gastrointestinal disorders Toothache	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	9.1% 1/11 • Number of events 1 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/12 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated
Musculoskeletal and connective tissue disorders Back pain	36.4% 4/11 • Number of events 4 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	8.3% 1/12 • Number of events 1 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated
Musculoskeletal and connective tissue disorders Myalgia	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	8.3% 1/12 • Number of events 1 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated
Infections and infestations Nasopharyngitis	9.1% 1/11 • Number of events 1 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	8.3% 1/12 • Number of events 1 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated
Infections and infestations Rhinitis	0.00% 0/11 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	9.1% 1/11 • Number of events 1 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated	0.00% 0/12 • Up to 6 weeks The onset date/time of one non-serious event (toothache) was not recorded, so the treatment arm was unknown and not shown below, otherwise all events that occurred during the study period are shown including those that were unrelated

Additional Information

Chief Medical Officer

Ixchelsis Limited

Phone: 44(0)1227-832760

Email: [email protected]

Results disclosure agreements

Principal investigator is a sponsor employee Sponsor may choose to collaborate on authorship, and sponsor's agent has 60-day review
Publication restrictions are in place

Restriction type: OTHER