Trial Outcomes & Findings for Phase I Study of the Safety, Tolerability, PK & PD of Lomitapide in Japanese and Caucasian Subjects With Elevated LDL-C (NCT NCT01760187)
NCT ID: NCT01760187
Last Updated: 2018-11-20
Results Overview
Maximum observed plasma concentration for lomitapide
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
72 participants
Primary outcome timeframe
1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 7
Results posted on
2018-11-20
Participant Flow
Participant milestones
| Measure |
Cohort 1
10 Japanese and 10 Caucasian subjects will receive 10 mg lomitapide.
|
Cohort 2
6 Japanese and 6 Caucasian subjects will receive 20 mg lomitapide.
|
Cohort 3
6 Japanese and 6 Caucasian subjects will receive 40 mg lomitapide.
|
Cohort 4
6 Japanese and 6 Caucasian subjects will receive 60 mg lomitapide.
|
Placebo
8 Japanese and 8 Caucasian subjects will receive placebo.
|
|---|---|---|---|---|---|
|
Overall Study
STARTED
|
20
|
12
|
12
|
12
|
16
|
|
Overall Study
COMPLETED
|
19
|
12
|
12
|
10
|
16
|
|
Overall Study
NOT COMPLETED
|
1
|
0
|
0
|
2
|
0
|
Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
Phase I Study of the Safety, Tolerability, PK & PD of Lomitapide in Japanese and Caucasian Subjects With Elevated LDL-C
Baseline characteristics by cohort
| Measure |
Placebo - Japanese Patients
n=8 Participants
8 Japanese patients will receive placebo, across the cohorts.
(2 at each cohort)
|
Placebo - Caucasian Patients
n=8 Participants
8 Caucasian patients will receive placebo, across the cohorts.
(2 at each cohort)
|
Cohort 1- Japanese Patients
n=10 Participants
10 Japanese subjects will receive 10 mg of lomitapide.
|
Cohort 1 - Caucasian Patients
n=10 Participants
10 Caucasian subjects will receive 10 mg of lomitapide.
|
Cohort 2 - Japanese Patients
n=6 Participants
6 Japanese subjects will receive 20 mg of lomitapide.
|
Cohort 2 - Caucasian Patients
n=6 Participants
6 Caucasian subjects will receive 20 mg of lomitapide.
|
Cohort 3 - Japanese Patients
n=6 Participants
6 Japanese subjects will receive 40 mg of lomitapide.
|
Cohort 3 - Caucasian Patients
n=6 Participants
6 Caucasian subjects will receive 40 mg of lomitapide.
|
Cohort 4 - Japanese Patients
n=6 Participants
6 Japanese subjects will receive 60 mg of lomitapide.
|
Cohort 4 - Caucasian Patients
n=6 Participants
6 Caucasian subjects will receive 60 mg of lomitapide.
|
Total
n=72 Participants
Total of all reporting groups
|
|---|---|---|---|---|---|---|---|---|---|---|---|
|
Age, Categorical
>=65 years
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
0 Participants
n=21 Participants
|
0 Participants
n=10 Participants
|
0 Participants
n=115 Participants
|
0 Participants
n=6 Participants
|
0 Participants
n=6 Participants
|
0 Participants
n=64 Participants
|
0 Participants
n=17 Participants
|
|
Age, Categorical
<=18 years
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
0 Participants
n=21 Participants
|
0 Participants
n=10 Participants
|
0 Participants
n=115 Participants
|
0 Participants
n=6 Participants
|
0 Participants
n=6 Participants
|
0 Participants
n=64 Participants
|
0 Participants
n=17 Participants
|
|
Age, Categorical
Between 18 and 65 years
|
8 Participants
n=5 Participants
|
8 Participants
n=7 Participants
|
10 Participants
n=5 Participants
|
10 Participants
n=4 Participants
|
6 Participants
n=21 Participants
|
6 Participants
n=10 Participants
|
6 Participants
n=115 Participants
|
6 Participants
n=6 Participants
|
6 Participants
n=6 Participants
|
6 Participants
n=64 Participants
|
72 Participants
n=17 Participants
|
|
Age, Continuous
|
34.1 years
STANDARD_DEVIATION 6.0 • n=5 Participants
|
33.6 years
STANDARD_DEVIATION 7.3 • n=7 Participants
|
33.8 years
STANDARD_DEVIATION 6.0 • n=5 Participants
|
31.2 years
STANDARD_DEVIATION 6.6 • n=4 Participants
|
32.2 years
STANDARD_DEVIATION 5.4 • n=21 Participants
|
36.0 years
STANDARD_DEVIATION 7.5 • n=10 Participants
|
32.5 years
STANDARD_DEVIATION 4.6 • n=115 Participants
|
31.2 years
STANDARD_DEVIATION 9.7 • n=6 Participants
|
30.2 years
STANDARD_DEVIATION 5.4 • n=6 Participants
|
37.7 years
STANDARD_DEVIATION 3.4 • n=64 Participants
|
33.3 years
STANDARD_DEVIATION 6.2 • n=17 Participants
|
|
Sex: Female, Male
Female
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
0 Participants
n=21 Participants
|
0 Participants
n=10 Participants
|
0 Participants
n=115 Participants
|
0 Participants
n=6 Participants
|
0 Participants
n=6 Participants
|
0 Participants
n=64 Participants
|
0 Participants
n=17 Participants
|
|
Sex: Female, Male
Male
|
8 Participants
n=5 Participants
|
8 Participants
n=7 Participants
|
10 Participants
n=5 Participants
|
10 Participants
n=4 Participants
|
6 Participants
n=21 Participants
|
6 Participants
n=10 Participants
|
6 Participants
n=115 Participants
|
6 Participants
n=6 Participants
|
6 Participants
n=6 Participants
|
6 Participants
n=64 Participants
|
72 Participants
n=17 Participants
|
|
Region of Enrollment
United Kingdom
|
8 participants
n=5 Participants
|
8 participants
n=7 Participants
|
10 participants
n=5 Participants
|
10 participants
n=4 Participants
|
6 participants
n=21 Participants
|
6 participants
n=10 Participants
|
6 participants
n=115 Participants
|
6 participants
n=6 Participants
|
6 participants
n=6 Participants
|
6 participants
n=64 Participants
|
72 participants
n=17 Participants
|
PRIMARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 7Population: All subjects with evaluable concentrations
Maximum observed plasma concentration for lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
Cmax for Lomitapide
|
0.570 ng/mL
Standard Deviation 0.285
|
0.436 ng/mL
Standard Deviation 0.166
|
1.70 ng/mL
Standard Deviation 0.49
|
1.01 ng/mL
Standard Deviation 0.17
|
3.93 ng/mL
Standard Deviation 0.75
|
3.00 ng/mL
Standard Deviation 1.52
|
8.29 ng/mL
Standard Deviation 3.44
|
5.75 ng/mL
Standard Deviation 1.78
|
PRIMARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 7Population: All subjects with evaluable concentrations
Time to maximum observed concentration for lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
Tmax for Lomitapide
|
4 hr
Interval 2.0 to 6.0
|
5 hr
Interval 2.0 to 12.0
|
9 hr
Interval 4.0 to 12.0
|
6 hr
Interval 2.0 to 12.0
|
4 hr
Interval 2.0 to 6.0
|
5 hr
Interval 4.0 to 8.0
|
6 hr
Interval 4.0 to 6.0
|
5 hr
Interval 2.0 to 6.0
|
PRIMARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 7Population: All subjects with evaluable concentrations
Area under the plasma concentration versus time curve from hour 0 to the last measurable concentration for lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
AUC0-t for Lomitapide
|
29.1 ng*hr/mL
Standard Deviation 13.0
|
27.5 ng*hr/mL
Standard Deviation 11.0
|
63.0 ng*hr/mL
Standard Deviation 16.0
|
54.2 ng*hr/mL
Standard Deviation 9.6
|
152 ng*hr/mL
Standard Deviation 48
|
123 ng*hr/mL
Standard Deviation 53
|
238 ng*hr/mL
Standard Deviation 84
|
241 ng*hr/mL
Standard Deviation 72
|
PRIMARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 7Population: AUC0-∞ and t1/2 were not calculated for 3 subjects in the Japanese 10mg arm because the estimated t1/2 was being much longer than half of the total sampling time.
Area under the plasma concentration versus time curve from zero to infinity for lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=7 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
AUC0-∞ for Lomitapide
|
37.3 ng*hr/mL
Standard Deviation 16.7
|
35.9 ng*hr/mL
Standard Deviation 15.3
|
68.6 ng*hr/mL
Standard Deviation 17.4
|
64.7 ng*hr/mL
Standard Deviation 14.7
|
168 ng*hr/mL
Standard Deviation 59
|
133 ng*hr/mL
Standard Deviation 58
|
251 ng*hr/mL
Standard Deviation 89
|
260 ng*hr/mL
Standard Deviation 74
|
PRIMARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 7Population: AUC0-∞ and t1/2 were not calculated for 3 subjects in the Japanese 10mg arm because the estimated t1/2 was being much longer than half of the total sampling time.
Apparent terminal elimination half-life for lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=7 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
t1/2 for Lomitapide
|
79.5 hr
Standard Deviation 5.6
|
82.8 hr
Standard Deviation 5.9
|
50.5 hr
Standard Deviation 2.6
|
64.3 hr
Standard Deviation 20.6
|
58.8 hr
Standard Deviation 13.3
|
56.2 hr
Standard Deviation 7.1
|
44.9 hr
Standard Deviation 5.7
|
51.5 hr
Standard Deviation 10.9
|
PRIMARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 27Population: All subjects with evaluable concentrations
Maximum observed plasma concentration for lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
Cmax for Lomitapide
|
2.46 ng/mL
Standard Deviation 0.88
|
3.31 ng/mL
Standard Deviation 2.91
|
5.96 ng/mL
Standard Deviation 2.79
|
4.35 ng/mL
Standard Deviation 1.07
|
19.7 ng/mL
Standard Deviation 6.2
|
13.8 ng/mL
Standard Deviation 5.1
|
29.6 ng/mL
Standard Deviation 11.1
|
24.6 ng/mL
Standard Deviation 9.0
|
PRIMARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 27Population: All subjects with evaluable concentrations
Time to maximum observed concentration for lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
Tmax for Lomitapide
|
4 hr
Interval 1.0 to 4.0
|
4 hr
Interval 2.0 to 6.0
|
4 hr
Interval 1.0 to 8.0
|
4 hr
Interval 4.0 to 4.0
|
4 hr
Interval 4.0 to 4.0
|
4 hr
Interval 4.0 to 6.0
|
4 hr
Interval 2.0 to 6.0
|
4 hr
Interval 2.0 to 4.0
|
PRIMARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 27Population: All subjects with evaluable concentrations
Area under the plasma concentration versus time curve from hour 0 to the last measurable concentration for lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
AUC0-t for Lomitapide
|
38.1 ng*hr/mL
Standard Deviation 14.1
|
44.5 ng*hr/mL
Standard Deviation 29.0
|
91.3 ng*hr/mL
Standard Deviation 29.5
|
74.4 ng*hr/mL
Standard Deviation 18.8
|
263 ng*hr/mL
Standard Deviation 64
|
204 ng*hr/mL
Standard Deviation 79
|
388 ng*hr/mL
Standard Deviation 86
|
403 ng*hr/mL
Standard Deviation 130
|
PRIMARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 27Population: All subjects with evaluable concentrations
Apparent terminal elimination half-life for lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
t1/2 for Lomitapide
|
62.6 hr
Standard Deviation 10.1
|
57.6 hr
Standard Deviation 8.9
|
56.1 hr
Standard Deviation 9.9
|
53.3 hr
Standard Deviation 8.5
|
49.7 hr
Standard Deviation 11.3
|
44.8 hr
Standard Deviation 6.4
|
48.9 hr
Standard Deviation 9.9
|
46.5 hr
Standard Deviation 6.3
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 7Population: All subjects with evaluable concentrations
Maximum observed plasma concentration for M1 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
Cmax for M1
|
1.23 ng/mL
Standard Deviation 0.23
|
1.02 ng/mL
Standard Deviation 0.23
|
2.27 ng/mL
Standard Deviation 0.54
|
1.86 ng/mL
Standard Deviation 0.54
|
4.18 ng/mL
Standard Deviation 1.22
|
4.20 ng/mL
Standard Deviation 1.72
|
7.43 ng/mL
Standard Deviation 1.88
|
5.53 ng/mL
Standard Deviation 0.83
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 7Population: All subjects with evaluable concentrations
Time to maximum observed concentration for M1 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
Tmax for M1
|
6 hr
Interval 4.0 to 8.0
|
6 hr
Interval 4.0 to 6.0
|
5 hr
Interval 4.0 to 6.0
|
6 hr
Interval 4.0 to 8.0
|
4 hr
Interval 1.0 to 8.0
|
6 hr
Interval 4.0 to 8.0
|
6 hr
Interval 4.0 to 6.0
|
6 hr
Interval 2.0 to 8.0
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 7Population: All subjects with evaluable concentrations
Area under the plasma concentration versus time curve from hour 0 to the last measurable concentration for M1 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
AUC0-t for M1
|
37.1 ng*hr/mL
Standard Deviation 9.7
|
32.1 ng*hr/mL
Standard Deviation 7.9
|
64.1 ng*hr/mL
Standard Deviation 15.6
|
56.7 ng*hr/mL
Standard Deviation 18.6
|
134 ng*hr/mL
Standard Deviation 37
|
129 ng*hr/mL
Standard Deviation 57
|
199 ng*hr/mL
Standard Deviation 64
|
177 ng*hr/mL
Standard Deviation 44
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 7Population: All subjects with evaluable concentrations
Area under the plasma concentration versus time curve from zero to infinity for M1 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
AUC0-∞ for M1
|
38.7 ng*hr/mL
Standard Deviation 10.1
|
34.0 ng*hr/mL
Standard Deviation 8.3
|
65.7 ng*hr/mL
Standard Deviation 15.9
|
59.1 ng*hr/mL
Standard Deviation 19.5
|
138 ng*hr/mL
Standard Deviation 39
|
132 ng*hr/mL
Standard Deviation 58
|
204 ng*hr/mL
Standard Deviation 67
|
183 ng*hr/mL
Standard Deviation 46
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 7Population: All subjects with evaluable concentrations
Apparent terminal elimination half-life for M1 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
t1/2 for M1
|
37.8 hr
Standard Deviation 11.3
|
44.0 hr
Standard Deviation 14.3
|
35.9 hr
Standard Deviation 8.7
|
35.9 hr
Standard Deviation 6.0
|
41.5 hr
Standard Deviation 4.3
|
36.3 hr
Standard Deviation 7.9
|
39.4 hr
Standard Deviation 3.4
|
43.6 hr
Standard Deviation 4.9
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 7Population: All subjects with evaluable concentrations
Maximum observed plasma concentration for M3 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
Cmax for M3
|
20.0 ng/mL
Standard Deviation 4.1
|
14.2 ng/mL
Standard Deviation 4.8
|
35.3 ng/mL
Standard Deviation 8.2
|
20.0 ng/mL
Standard Deviation 5.8
|
55.7 ng/mL
Standard Deviation 18.3
|
50.9 ng/mL
Standard Deviation 24.7
|
83.9 ng/mL
Standard Deviation 34.5
|
67.7 ng/mL
Standard Deviation 23.8
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 7Population: All subjects with evaluable concentrations
Time to maximum observed concentration for M3 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
Tmax for M3
|
4 hr
Interval 2.0 to 4.0
|
3 hr
Interval 2.0 to 4.0
|
4 hr
Interval 2.0 to 4.0
|
4 hr
Interval 2.0 to 4.0
|
3 hr
Interval 1.0 to 4.0
|
2 hr
Interval 2.0 to 4.0
|
4 hr
Interval 4.0 to 4.0
|
2 hr
Interval 1.0 to 4.0
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 7Population: All subjects with evaluable concentrations
Area under the plasma concentration versus time curve from hour 0 to the last measurable concentration for M3 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
AUC0-t for M3
|
265 ng*hr/mL
Standard Deviation 53
|
185 ng*hr/mL
Standard Deviation 86
|
486 ng*hr/mL
Standard Deviation 145
|
263 ng*hr/mL
Standard Deviation 115
|
760 ng*hr/mL
Standard Deviation 169
|
824 ng*hr/mL
Standard Deviation 355
|
1410 ng*hr/mL
Standard Deviation 675
|
1170 ng*hr/mL
Standard Deviation 541
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 7Population: All subjects with evaluable concentrations
Area under the plasma concentration versus time curve from zero to infinity for M3 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
AUC0-∞ for M3
|
276 ng*hr/mL
Standard Deviation 55
|
196 ng*hr/mL
Standard Deviation 91.2
|
501 ng*hr/mL
Standard Deviation 147
|
274 ng*hr/mL
Standard Deviation 119
|
780 ng*hr/mL
Standard Deviation 171
|
839 ng*hr/mL
Standard Deviation 361
|
1430 ng*hr/mL
Standard Deviation 693
|
1200 ng*hr/mL
Standard Deviation 551
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 7Population: All subjects with evaluable concentrations
Apparent terminal elimination half-life for M3 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
t1/2 for M3
|
56.3 hr
Standard Deviation 11.6
|
56.9 hr
Standard Deviation 10.2
|
53.1 hr
Standard Deviation 12.9
|
51.3 hr
Standard Deviation 6.4
|
50.5 hr
Standard Deviation 14.9
|
39.4 hr
Standard Deviation 6.1
|
47.0 hr
Standard Deviation 7.4
|
43.8 hr
Standard Deviation 5.3
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 27Population: All subjects with evaluable concentrations
Maximum observed plasma concentration for M1 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
Cmax for M1
|
2.56 ng/mL
Standard Deviation 0.44
|
2.15 ng/mL
Standard Deviation 0.53
|
4.36 ng/mL
Standard Deviation 0.88
|
4.24 ng/mL
Standard Deviation 1.30
|
9.98 ng/mL
Standard Deviation 4.13
|
10.7 ng/mL
Standard Deviation 3.6
|
13.5 ng/mL
Standard Deviation 3.4
|
12.6 ng/mL
Standard Deviation 3.2
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 27Population: All subjects with evaluable concentrations
Time to maximum observed concentration for M1 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
Tmax for M1
|
6 hr
Interval 2.0 to 8.0
|
6 hr
Interval 2.0 to 6.0
|
6 hr
Interval 4.0 to 6.0
|
6 hr
Interval 4.0 to 8.0
|
4 hr
Interval 4.0 to 8.0
|
6 hr
Interval 4.0 to 6.0
|
6 hr
Interval 4.0 to 8.0
|
4 hr
Interval 4.0 to 8.0
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 27Population: All subjects with evaluable concentrations
Area under the plasma concentration versus time curve from hour 0 to the last measurable concentration for M1 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
AUC0-t for M1
|
44.3 ng*hr/mL
Standard Deviation 8.5
|
36.1 ng*hr/mL
Standard Deviation 8.5
|
73.7 ng*hr/mL
Standard Deviation 14.4
|
75.3 ng*hr/mL
Standard Deviation 25.9
|
180 ng*hr/mL
Standard Deviation 78
|
176 ng*hr/mL
Standard Deviation 58
|
230 ng*hr/mL
Standard Deviation 71
|
223 ng*hr/mL
Standard Deviation 66
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 27Population: All subjects with evaluable concentrations
Apparent terminal elimination half-life for M1 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
t1/2 for M1
|
42.4 hr
Standard Deviation 9.0
|
41.9 hr
Standard Deviation 7.5
|
41.6 hr
Standard Deviation 8.5
|
39.7 hr
Standard Deviation 4.5
|
41.0 hr
Standard Deviation 6.6
|
36.0 hr
Standard Deviation 1.7
|
43.5 hr
Standard Deviation 7.8
|
41.2 hr
Standard Deviation 6.2
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 27Population: All subjects with evaluable concentrations
Maximum observed plasma concentration for M3 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
Cmax for M3
|
33.9 ng/mL
Standard Deviation 9.3
|
24.1 ng/mL
Standard Deviation 7.9
|
56.4 ng/mL
Standard Deviation 15.0
|
35.2 ng/mL
Standard Deviation 18.8
|
76.3 ng/mL
Standard Deviation 26.7
|
86.4 ng/mL
Standard Deviation 27.1
|
129 ng/mL
Standard Deviation 35
|
126 ng/mL
Standard Deviation 50
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 27Population: All subjects with evaluable concentrations
Time to maximum observed concentration for M3 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
Tmax for M3
|
2 hr
Interval 2.0 to 4.0
|
3 hr
Interval 2.0 to 6.0
|
3 hr
Interval 2.0 to 4.0
|
4 hr
Interval 2.0 to 4.0
|
4 hr
Interval 2.0 to 4.0
|
4 hr
Interval 2.0 to 6.0
|
4 hr
Interval 2.0 to 6.0
|
2 hr
Interval 2.0 to 4.0
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 27Population: All subjects with evaluable concentrations
Area under the plasma concentration versus time curve from hour 0 to the last measurable concentration for M3 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
AUC0-t for M3
|
335 ng*hr/mL
Standard Deviation 84
|
239 ng*hr/mL
Standard Deviation 90
|
617 ng*hr/mL
Standard Deviation 163
|
386 ng*hr/mL
Standard Deviation 183
|
891 ng*hr/mL
Standard Deviation 259
|
1150 ng*hr/mL
Standard Deviation 462
|
1640 ng*hr/mL
Standard Deviation 664
|
1640 ng*hr/mL
Standard Deviation 767
|
SECONDARY outcome
Timeframe: 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose on Day 27Population: All subjects with evaluable concentrations
Apparent terminal elimination half-life for M3 metabolite of lomitapide
Outcome measures
| Measure |
Japanese 10 mg
n=10 Participants
Japanese Subjects who received 10 mg Lomitapide
|
Caucasian 10 mg
n=10 Participants
Caucasian Subjects who received 10 mg Lomitapide
|
Japanese 20 mg
n=6 Participants
Japanese Subjects who received 20 mg Lomitapide
|
Caucasian 20 mg
n=6 Participants
Caucasian Subjects who received 20 mg Lomitapide
|
Japanese 40 mg
n=6 Participants
Japanese Subjects who received 40 mg Lomitapide
|
Caucasian 40 mg
n=6 Participants
Caucasian Subjects who received 40 mg Lomitapide
|
Japanese 60 mg
n=6 Participants
Japanese Subjects who received 60 mg Lomitapide
|
Caucasian 60 mg
n=6 Participants
Caucasian Subjects who received 60 mg Lomitapide
|
|---|---|---|---|---|---|---|---|---|
|
t1/2 for M3
|
54.4 hr
Standard Deviation 11.0
|
44.3 hr
Standard Deviation 7.2
|
40.4 hr
Standard Deviation 6.9
|
55.4 hr
Standard Deviation 11.5
|
41.6 hr
Standard Deviation 8.6
|
39.3 hr
Standard Deviation 7.6
|
54.9 hr
Standard Deviation 17.4
|
41.8 hr
Standard Deviation 9.3
|
Adverse Events
Placebo - Japanese Patients
Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths
Placebo - Caucasian Patients
Serious events: 0 serious events
Other events: 6 other events
Deaths: 0 deaths
Cohort 1- Japanese Patients
Serious events: 0 serious events
Other events: 4 other events
Deaths: 0 deaths
Cohort 1 - Caucasian Patients
Serious events: 0 serious events
Other events: 6 other events
Deaths: 0 deaths
Cohort 2 - Japanese Patients
Serious events: 0 serious events
Other events: 3 other events
Deaths: 0 deaths
Cohort 2 - Caucasian Patients
Serious events: 0 serious events
Other events: 4 other events
Deaths: 0 deaths
Cohort 3 - Japanese Patients
Serious events: 0 serious events
Other events: 5 other events
Deaths: 0 deaths
Cohort 3 - Caucasian Patients
Serious events: 0 serious events
Other events: 6 other events
Deaths: 0 deaths
Cohort 4 - Japanese Patients
Serious events: 0 serious events
Other events: 6 other events
Deaths: 0 deaths
Cohort 4 - Caucasian Patients
Serious events: 0 serious events
Other events: 6 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Placebo - Japanese Patients
n=8 participants at risk
8 Japanese patients will receive placebo, across the cohorts.
(2 at each cohort)
|
Placebo - Caucasian Patients
n=8 participants at risk
8 Caucasian patients will receive placebo, across the cohorts.
(2 at each cohort)
|
Cohort 1- Japanese Patients
n=10 participants at risk
10 Japanese subjects will receive 10 mg of lomitapide.
|
Cohort 1 - Caucasian Patients
n=10 participants at risk
10 Caucasian subjects will receive 10 mg of lomitapide.
|
Cohort 2 - Japanese Patients
n=6 participants at risk
6 Japanese subjects will receive 20 mg of lomitapide.
|
Cohort 2 - Caucasian Patients
n=6 participants at risk
6 Caucasian subjects will receive 20 mg of lomitapide.
|
Cohort 3 - Japanese Patients
n=6 participants at risk
6 Japanese subjects will receive 40 mg of lomitapide.
|
Cohort 3 - Caucasian Patients
n=6 participants at risk
6 Caucasian subjects will receive 40 mg of lomitapide.
|
Cohort 4 - Japanese Patients
n=6 participants at risk
6 Japanese subjects will receive 60 mg of lomitapide.
|
Cohort 4 - Caucasian Patients
n=6 participants at risk
6 Caucasian subjects will receive 60 mg of lomitapide.
|
|---|---|---|---|---|---|---|---|---|---|---|
|
Gastrointestinal disorders
Abdominal Discomfort
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
0.00%
0/10
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
33.3%
2/6 • Number of events 2
|
0.00%
0/6
|
|
Gastrointestinal disorders
Abdominal Distension
|
12.5%
1/8 • Number of events 1
|
0.00%
0/8
|
0.00%
0/10
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
33.3%
2/6 • Number of events 2
|
66.7%
4/6 • Number of events 4
|
50.0%
3/6 • Number of events 3
|
83.3%
5/6 • Number of events 5
|
|
Gastrointestinal disorders
Abdominal Pain
|
12.5%
1/8 • Number of events 1
|
12.5%
1/8 • Number of events 1
|
10.0%
1/10 • Number of events 1
|
30.0%
3/10 • Number of events 3
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
16.7%
1/6 • Number of events 1
|
33.3%
2/6 • Number of events 2
|
|
Gastrointestinal disorders
Abdominal Pain Upper
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
|
Gastrointestinal disorders
Change of Bowel Movement
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
10.0%
1/10 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
|
Gastrointestinal disorders
Constipation
|
0.00%
0/8
|
12.5%
1/8 • Number of events 1
|
0.00%
0/10
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
|
Gastrointestinal disorders
Diarrhoea
|
0.00%
0/8
|
12.5%
1/8 • Number of events 1
|
10.0%
1/10 • Number of events 1
|
10.0%
1/10 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
33.3%
2/6 • Number of events 2
|
66.7%
4/6 • Number of events 4
|
50.0%
3/6 • Number of events 3
|
|
Gastrointestinal disorders
Dyspepsia
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
|
Gastrointestinal disorders
Mouth Ulceration
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
20.0%
2/10 • Number of events 2
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
|
Gastrointestinal disorders
Nausea
|
0.00%
0/8
|
0.00%
0/8
|
20.0%
2/10 • Number of events 2
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
33.3%
2/6 • Number of events 2
|
16.7%
1/6 • Number of events 1
|
66.7%
4/6 • Number of events 4
|
66.7%
4/6 • Number of events 4
|
|
Gastrointestinal disorders
Toothache
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
10.0%
1/10 • Number of events 1
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
|
Gastrointestinal disorders
Vomiting
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
16.7%
1/6 • Number of events 1
|
33.3%
2/6 • Number of events 2
|
16.7%
1/6 • Number of events 1
|
|
General disorders
Catheter Site Related Reaction
|
0.00%
0/8
|
12.5%
1/8 • Number of events 1
|
0.00%
0/10
|
10.0%
1/10 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
|
General disorders
Fatigue
|
0.00%
0/8
|
0.00%
0/8
|
20.0%
2/10 • Number of events 2
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
|
General disorders
Thirst
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
|
Injury, poisoning and procedural complications
Arthropod Bite
|
0.00%
0/8
|
0.00%
0/8
|
10.0%
1/10 • Number of events 1
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
|
Investigations
Hepatic Enzyme Increased
|
0.00%
0/8
|
0.00%
0/8
|
10.0%
1/10 • Number of events 1
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
|
Metabolism and nutrition disorders
Decreased Appetite
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
10.0%
1/10 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
33.3%
2/6 • Number of events 2
|
|
Musculoskeletal and connective tissue disorders
Arthralgia
|
0.00%
0/8
|
0.00%
0/8
|
10.0%
1/10 • Number of events 1
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
|
Musculoskeletal and connective tissue disorders
Back Pain
|
0.00%
0/8
|
0.00%
0/8
|
10.0%
1/10 • Number of events 1
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
|
Musculoskeletal and connective tissue disorders
Muscle Spasms
|
0.00%
0/8
|
12.5%
1/8 • Number of events 1
|
0.00%
0/10
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
|
Musculoskeletal and connective tissue disorders
Pain in Extremity
|
0.00%
0/8
|
12.5%
1/8 • Number of events 1
|
0.00%
0/10
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
|
Musculoskeletal and connective tissue disorders
Musculoskeletal Chest Pain
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
10.0%
1/10 • Number of events 1
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
|
Nervous system disorders
Headache
|
12.5%
1/8 • Number of events 1
|
0.00%
0/8
|
10.0%
1/10 • Number of events 1
|
20.0%
2/10 • Number of events 2
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
33.3%
2/6 • Number of events 2
|
0.00%
0/6
|
0.00%
0/6
|
33.3%
2/6 • Number of events 2
|
|
Nervous system disorders
Paraesthesia
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
0.00%
0/10
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
|
Nervous system disorders
VIITH Nerve Paralysis
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
|
Psychiatric disorders
Insomnia
|
0.00%
0/8
|
0.00%
0/8
|
10.0%
1/10 • Number of events 1
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
|
Renal and urinary disorders
Pollakiuria
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
10.0%
1/10 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
|
Respiratory, thoracic and mediastinal disorders
Dyspnoea
|
0.00%
0/8
|
25.0%
2/8 • Number of events 2
|
0.00%
0/10
|
0.00%
0/10
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
|
Respiratory, thoracic and mediastinal disorders
Nasal Congestion
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
50.0%
3/6 • Number of events 3
|
0.00%
0/6
|
0.00%
0/6
|
|
Respiratory, thoracic and mediastinal disorders
Upper Respiratory Tract Infection
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
10.0%
1/10 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
33.3%
2/6 • Number of events 2
|
0.00%
0/6
|
0.00%
0/6
|
|
Skin and subcutaneous tissue disorders
Rash
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
0.00%
0/10
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
|
Vascular disorders
Dizziness
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
10.0%
1/10 • Number of events 1
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
|
Vascular disorders
Epistaxis
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
0.00%
0/10
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
|
Vascular disorders
Haematochezia
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
|
Vascular disorders
Syncope
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/10
|
0.00%
0/10
|
0.00%
0/6
|
0.00%
0/6
|
16.7%
1/6 • Number of events 1
|
0.00%
0/6
|
0.00%
0/6
|
0.00%
0/6
|
Additional Information
Alison Long, MD - VP Clinical
Aegerion Pharmaceuticals, Inc.
Phone: 8572425142
Email: [email protected]
Results disclosure agreements
- Principal investigator is a sponsor employee Described in the contract.
- Publication restrictions are in place
Restriction type: OTHER