Trial Outcomes & Findings for Comparative Bioavailability of BAFIERTAM™ (Monomethyl Fumarate) and Tecfidera® (Dimethyl Fumarate) in Healthy Subjects (NCT NCT04570670)
NCT ID: NCT04570670
Last Updated: 2022-12-30
Results Overview
Pharmacokinetics: Plasma concentrations of MMF will be determined and used to calculate AUC0-inf MMF for each treatment. Venous blood samples were collected immediately prior to dosing (time 0), and then 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 6.5, 7, 7.5, 8, 9, 10, 11, 12, and 24 hours postdose.
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
50 participants
Primary outcome timeframe
24 hours
Results posted on
2022-12-30
Participant Flow
Participant milestones
| Measure |
Randomization Sequence AB
Treatment A: A single oral dose of BLS-11 190 mg (2 x 95 mg)
Treatment B: A single oral dose of Tecfidera® 240 mg (1 × 240 mg)
|
Randomization Sequence BA
Treatment B: A single oral dose of Tecfidera® 240 mg (1 × 240 mg)
Treatment A: A single oral dose of BLS-11 190 mg (2 x 95 mg)
|
|---|---|---|
|
Overall Study
STARTED
|
25
|
25
|
|
Overall Study
COMPLETED
|
24
|
25
|
|
Overall Study
NOT COMPLETED
|
1
|
0
|
Reasons for withdrawal
| Measure |
Randomization Sequence AB
Treatment A: A single oral dose of BLS-11 190 mg (2 x 95 mg)
Treatment B: A single oral dose of Tecfidera® 240 mg (1 × 240 mg)
|
Randomization Sequence BA
Treatment B: A single oral dose of Tecfidera® 240 mg (1 × 240 mg)
Treatment A: A single oral dose of BLS-11 190 mg (2 x 95 mg)
|
|---|---|---|
|
Overall Study
Withdrawal by Subject
|
1
|
0
|
Baseline Characteristics
Comparative Bioavailability of BAFIERTAM™ (Monomethyl Fumarate) and Tecfidera® (Dimethyl Fumarate) in Healthy Subjects
Baseline characteristics by cohort
| Measure |
Randomization Sequence AB
n=25 Participants
Treatment A: A single oral dose of BLS-11 190 mg (2 x 95 mg) MMF
Treatment B: A single oral dose of Tecfidera® 240 mg (1 × 240 mg) DMF
|
Randomization Sequence BA
n=25 Participants
Treatment B: A single oral dose of Tecfidera® 240 mg (1 × 240 mg) DMF
Treatment A: A single oral dose of BLS-11 190 mg (2 x 95 mg) MMF
|
Total
n=50 Participants
Total of all reporting groups
|
|---|---|---|---|
|
Age, Continuous
|
34.4 years
STANDARD_DEVIATION 9.85 • n=5 Participants
|
38.0 years
STANDARD_DEVIATION 8.22 • n=7 Participants
|
36.2 years
STANDARD_DEVIATION 9.17 • n=5 Participants
|
|
Sex: Female, Male
Female
|
6 Participants
n=5 Participants
|
8 Participants
n=7 Participants
|
14 Participants
n=5 Participants
|
|
Sex: Female, Male
Male
|
19 Participants
n=5 Participants
|
17 Participants
n=7 Participants
|
36 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Hispanic or Latino
|
15 Participants
n=5 Participants
|
12 Participants
n=7 Participants
|
27 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Not Hispanic or Latino
|
10 Participants
n=5 Participants
|
13 Participants
n=7 Participants
|
23 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
American Indian or Alaska Native
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Asian
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Black or African American
|
6 Participants
n=5 Participants
|
4 Participants
n=7 Participants
|
10 Participants
n=5 Participants
|
|
Race (NIH/OMB)
White
|
19 Participants
n=5 Participants
|
19 Participants
n=7 Participants
|
38 Participants
n=5 Participants
|
|
Race (NIH/OMB)
More than one race
|
0 Participants
n=5 Participants
|
2 Participants
n=7 Participants
|
2 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
|
Region of Enrollment
United States
|
25 participants
n=5 Participants
|
25 participants
n=7 Participants
|
50 participants
n=5 Participants
|
|
Weight
|
72.98 kg
STANDARD_DEVIATION 9.450 • n=5 Participants
|
74.78 kg
STANDARD_DEVIATION 12.512 • n=7 Participants
|
74.78 kg
STANDARD_DEVIATION 11.011 • n=5 Participants
|
|
Height
|
168.6 cm
STANDARD_DEVIATION 7.55 • n=5 Participants
|
170.3 cm
STANDARD_DEVIATION 10.58 • n=7 Participants
|
169.5 cm
STANDARD_DEVIATION 9.14 • n=5 Participants
|
|
Body Mass Index (kg/m^2)
|
25.625 kg/m^2
STANDARD_DEVIATION 2.4142 • n=5 Participants
|
25.678 kg/m^2
STANDARD_DEVIATION 2.9237 • n=7 Participants
|
25.651 kg/m^2
STANDARD_DEVIATION 2.6537 • n=5 Participants
|
PRIMARY outcome
Timeframe: 24 hoursPopulation: One subject in the Reference (Tecfidera) group was excluded from AUC0-inf calculations because of missing or unreportable values and was excluded from the statistical analyses.
Pharmacokinetics: Plasma concentrations of MMF will be determined and used to calculate AUC0-inf MMF for each treatment. Venous blood samples were collected immediately prior to dosing (time 0), and then 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 6.5, 7, 7.5, 8, 9, 10, 11, 12, and 24 hours postdose.
Outcome measures
| Measure |
Test (BLS-11)
n=49 Participants
A single oral dose administration of BLS-11 190 mg (2 × 95 mg monomethyl fumarate delayed-release capsules) at Hour 0 on Day 1
monomethyl fumarate 190 mg
|
Reference (Tecfidera)
n=48 Participants
A single oral dose administration of Tecfidera 240 mg (1 × 240 mg dimethyl fumarate delayed-release capsule) at Hour 0 on Day 1
dimethyl fumarate 240 mg
|
|---|---|---|
|
The Bioequivalent (BE) Comparison of AUC0-inf of Monomethyl Fumarate (MMF) Between Treatments
|
2984 ng*hr/mL
Geometric Coefficient of Variation 25.9
|
3116 ng*hr/mL
Geometric Coefficient of Variation 23.9
|
PRIMARY outcome
Timeframe: 24 hoursPharmacokinetics: Plasma concentrations of MMF will be determined and used to calculate the Cmax of MMF for each treatment.Venous blood samples were collected immediately prior to dosing, and then 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 6.5, 7, 7.5, 8, 9, 10, 11, 12, and 24 hours postdose.
Outcome measures
| Measure |
Test (BLS-11)
n=49 Participants
A single oral dose administration of BLS-11 190 mg (2 × 95 mg monomethyl fumarate delayed-release capsules) at Hour 0 on Day 1
monomethyl fumarate 190 mg
|
Reference (Tecfidera)
n=49 Participants
A single oral dose administration of Tecfidera 240 mg (1 × 240 mg dimethyl fumarate delayed-release capsule) at Hour 0 on Day 1
dimethyl fumarate 240 mg
|
|---|---|---|
|
The BE Comparison of Cmax of Monomethyl Fumarate (MMF) Between Treatments
|
1760 ng/mL
Geometric Coefficient of Variation 34.8
|
1680 ng/mL
Geometric Coefficient of Variation 33.8
|
Adverse Events
Test (BLS-11)
Serious events: 0 serious events
Other events: 31 other events
Deaths: 0 deaths
Reference (Tecfidera)
Serious events: 0 serious events
Other events: 29 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Test (BLS-11)
n=50 participants at risk
A single oral dose administration of BLS-11 190 mg (2 × 95 mg monomethyl fumarate delayed-release capsules) at Hour 0 on Day 1
monomethyl fumarate 190 mg
|
Reference (Tecfidera)
n=49 participants at risk
A single oral dose administration of Tecfidera 240 mg (1 × 240 mg dimethyl fumarate delayed-release capsule) at Hour 0 on Day 1
dimethyl fumarate 240 mg
|
|---|---|---|
|
Cardiac disorders
Palpitations
|
2.0%
1/50 • 7 days
|
0.00%
0/49 • 7 days
|
|
Gastrointestinal disorders
Abdominal distension
|
0.00%
0/50 • 7 days
|
2.0%
1/49 • 7 days
|
|
Gastrointestinal disorders
Abdominal pain
|
2.0%
1/50 • 7 days
|
0.00%
0/49 • 7 days
|
|
Gastrointestinal disorders
Abdominal pain upper
|
0.00%
0/50 • 7 days
|
2.0%
1/49 • 7 days
|
|
Gastrointestinal disorders
Diarrhea
|
0.00%
0/50 • 7 days
|
4.1%
2/49 • 7 days
|
|
Gastrointestinal disorders
Nausea
|
0.00%
0/50 • 7 days
|
2.0%
1/49 • 7 days
|
|
General disorders
Chills
|
2.0%
1/50 • 7 days
|
0.00%
0/49 • 7 days
|
|
General disorders
Feeling Hot
|
2.0%
1/50 • 7 days
|
0.00%
0/49 • 7 days
|
|
General disorders
Vessel puncture site erythema
|
0.00%
0/50 • 7 days
|
2.0%
1/49 • 7 days
|
|
General disorders
Vessel puncture site pain
|
0.00%
0/50 • 7 days
|
2.0%
1/49 • 7 days
|
|
General disorders
Vessel puncture site swelling
|
0.00%
0/50 • 7 days
|
2.0%
1/49 • 7 days
|
|
Nervous system disorders
Dizziness
|
2.0%
1/50 • 7 days
|
0.00%
0/49 • 7 days
|
|
Nervous system disorders
Hypoaesthesia
|
2.0%
1/50 • 7 days
|
0.00%
0/49 • 7 days
|
|
Psychiatric disorders
Anxiety
|
2.0%
1/50 • 7 days
|
0.00%
0/49 • 7 days
|
|
Psychiatric disorders
Euphoric mood
|
2.0%
1/50 • 7 days
|
0.00%
0/49 • 7 days
|
|
Reproductive system and breast disorders
Metrorrhagia
|
2.0%
1/50 • 7 days
|
0.00%
0/49 • 7 days
|
|
Respiratory, thoracic and mediastinal disorders
Nasal congestion
|
0.00%
0/50 • 7 days
|
4.1%
2/49 • 7 days
|
|
Respiratory, thoracic and mediastinal disorders
Rhinorrhoea
|
2.0%
1/50 • 7 days
|
0.00%
0/49 • 7 days
|
|
Skin and subcutaneous tissue disorders
Pruritus generalised
|
2.0%
1/50 • 7 days
|
0.00%
0/49 • 7 days
|
|
Skin and subcutaneous tissue disorders
Skin fissures
|
2.0%
1/50 • 7 days
|
2.0%
1/49 • 7 days
|
|
Vascular disorders
Flushing
|
60.0%
30/50 • 7 days
|
51.0%
25/49 • 7 days
|
Additional Information
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place
Restriction type: OTHER