Trial Outcomes & Findings for Evaluation of Vamorolone CYP3A4 Induction on Midazolam (a Sensitive CYP 3A4 Substrate) Pharmacokinetics (NCT NCT06689527)

NCT ID: NCT06689527

Last Updated: 2025-12-15

Results Overview

Area under the plasma concentration-time curve from 0 to the time of the last observed concentration (h\*pg/mL) on day 1 and day 14. The timepoints at which the data were collected to create the curve are as follows: predose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 10 hours postdose.

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

18 participants

Primary outcome timeframe

Day 1 and Day 14

Results posted on

2025-12-15

Participant Flow

Participant milestones

Participant milestones
Measure
Vamorolone/Midazolam
both Test Drug and Reference Drug are administered in this arm Vamorolone: Days 3 to 14: 6 mg/kg vamorolone once daily. Midazolam: Day 1 and 14: Single doses of 2.5 mg midazolam
Overall Study
STARTED
18
Overall Study
COMPLETED
18
Overall Study
NOT COMPLETED
0

Reasons for withdrawal

Withdrawal data not reported

Baseline Characteristics

This population only includes female participants.

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure
Vamorolone/Midazolam
n=18 Participants
both Test Drug (vamorolone) and Reference Drug (midazolam) are administered in this arm Vamorolone: Days 3 to 14: 6 mg/kg vamorolone once daily. Midazolam: Day 1 and 14: Single oral doses of 2.5 mg midazolam
Age, Continuous
38.2 years
STANDARD_DEVIATION 9.55 • n=18 Participants
Sex: Female, Male
Female
10 Participants
n=18 Participants
Sex: Female, Male
Male
8 Participants
n=18 Participants
Ethnicity (NIH/OMB)
Hispanic or Latino
0 Participants
n=18 Participants
Ethnicity (NIH/OMB)
Not Hispanic or Latino
18 Participants
n=18 Participants
Ethnicity (NIH/OMB)
Unknown or Not Reported
0 Participants
n=18 Participants
Race (NIH/OMB)
American Indian or Alaska Native
0 Participants
n=18 Participants
Race (NIH/OMB)
Asian
3 Participants
n=18 Participants
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
0 Participants
n=18 Participants
Race (NIH/OMB)
Black or African American
0 Participants
n=18 Participants
Race (NIH/OMB)
White
15 Participants
n=18 Participants
Race (NIH/OMB)
More than one race
0 Participants
n=18 Participants
Race (NIH/OMB)
Unknown or Not Reported
0 Participants
n=18 Participants
Region of Enrollment
Germany
18 participants
n=18 Participants
Height
170.5 cm
STANDARD_DEVIATION 10.55 • n=18 Participants
Weight
69.34 kg
STANDARD_DEVIATION 10.876 • n=18 Participants
BMI
23.81 kg/m2
STANDARD_DEVIATION 2.389 • n=18 Participants
Premenopausal/Postmenopausal Status
Premenopausal Status
8 Participants
n=10 Participants • This population only includes female participants.
Premenopausal/Postmenopausal Status
Postmenopausal Status
2 Participants
n=10 Participants • This population only includes female participants.

PRIMARY outcome

Timeframe: Day 1 and Day 14

Population: PK Set - Midazolam: a subset of the Safety Set and includes all subjects who completed the scheduled vamorolone and midazolam dosing and provided an evaluable midazolam PK profile on at least one of the following days Day 1 and Day 14. No vomiting should occur within 4 hours following midazolam and/or vamorolone administration. This PK set was used for PK concentration summary and PK parameter summary for midazolam and 1'-hydroxymidazolam.

Area under the plasma concentration-time curve from 0 to the time of the last observed concentration (h\*pg/mL) on day 1 and day 14. The timepoints at which the data were collected to create the curve are as follows: predose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 10 hours postdose.

Outcome measures

Outcome measures
Measure
Midazolam Alone on Day 1
n=18 Participants
Day 1: Single oral of midazolam dose 2.5 mg
Midazolam Co-administered With Vamorolone on Day 14.
n=18 Participants
Day 14: Single oral midazolam dose of 2.5mg + Single oral suspension vamorolone dose of 6mg/kg
Vamorolone on Day 11
Oral suspension of vamorolone 6 mg/kg
Vamorolone Alone on Day 13
Oral suspension of vamorolone 6 mg/kg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
No Treatment on Day 15
No drug administration; end of study treatment
AUC0-tlast of Midazolam
34331.8 h*pg/ml
Standard Deviation 11854.73
28619.6 h*pg/ml
Standard Deviation 11447.17

PRIMARY outcome

Timeframe: Day 1 and Day 14

Population: PK Set - Midazolam: a subset of the Safety Set and includes all subjects who completed the scheduled vamorolone and midazolam dosing and provided an evaluable midazolam PK profile on at least one of the following days Day 1 and Day 14. No vomiting should occur within 4 hours following midazolam and/or vamorolone administration. This PK set was used for PK concentration summary and PK parameter summary for midazolam and 1'-hydroxymidazolam

Area under the plasma concentration-time curve from zero to infinite time on day 1 and day 14. The timepoints at which the data were collected to create the curve are as follows: predose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 10 hours postdose and extrapolation to infinity.

Outcome measures

Outcome measures
Measure
Midazolam Alone on Day 1
n=18 Participants
Day 1: Single oral of midazolam dose 2.5 mg
Midazolam Co-administered With Vamorolone on Day 14.
n=17 Participants
Day 14: Single oral midazolam dose of 2.5mg + Single oral suspension vamorolone dose of 6mg/kg
Vamorolone on Day 11
Oral suspension of vamorolone 6 mg/kg
Vamorolone Alone on Day 13
Oral suspension of vamorolone 6 mg/kg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
No Treatment on Day 15
No drug administration; end of study treatment
AUC0-inf of Midazolam
38028.2 h*pg/mL
Standard Deviation 14556.59
30337.7 h*pg/mL
Standard Deviation 12238.52

PRIMARY outcome

Timeframe: Day 1 and Day 14

Population: PK Set - Midazolam: a subset of the Safety Set and includes all subjects who completed the scheduled vamorolone and midazolam dosing and provided an evaluable midazolam PK profile on at least one of the following days Day 1 and Day 14. No vomiting should occur within 4 hours following midazolam and/or vamorolone administration. This PK set was used for PK concentration summary and PK parameter summary for midazolam and 1'-hydroxymidazolam

maximum measured concentration of midazolam after administration of midazolam until the last collection time, i.e., 10 hours after dosing on day 1 and day 14

Outcome measures

Outcome measures
Measure
Midazolam Alone on Day 1
n=18 Participants
Day 1: Single oral of midazolam dose 2.5 mg
Midazolam Co-administered With Vamorolone on Day 14.
n=18 Participants
Day 14: Single oral midazolam dose of 2.5mg + Single oral suspension vamorolone dose of 6mg/kg
Vamorolone on Day 11
Oral suspension of vamorolone 6 mg/kg
Vamorolone Alone on Day 13
Oral suspension of vamorolone 6 mg/kg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
No Treatment on Day 15
No drug administration; end of study treatment
Cmax of Midazolam
15704 pg/ml
Standard Deviation 5495.3
13875 pg/ml
Standard Deviation 4995.2

PRIMARY outcome

Timeframe: Day 1 and Day 14

Population: PK Set - Midazolam: a subset of the Safety Set and includes all subjects who completed the scheduled vamorolone and midazolam dosing and provided an evaluable midazolam PK profile on at least one of the following days Day 1 and Day 14. No vomiting should occur within 4 hours following midazolam and/or vamorolone administration. This PK set was used for PK concentration summary and PK parameter summary for midazolam and 1'-hydroxymidazolam

Area under the plasma concentration-time curve from 0 to the time of the last observed concentration (h\*pg/mL) on day 1 and day 14. The timepoints at which the data were collected to create the curve are as follows: predose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 10 hours postdose.

Outcome measures

Outcome measures
Measure
Midazolam Alone on Day 1
n=18 Participants
Day 1: Single oral of midazolam dose 2.5 mg
Midazolam Co-administered With Vamorolone on Day 14.
n=18 Participants
Day 14: Single oral midazolam dose of 2.5mg + Single oral suspension vamorolone dose of 6mg/kg
Vamorolone on Day 11
Oral suspension of vamorolone 6 mg/kg
Vamorolone Alone on Day 13
Oral suspension of vamorolone 6 mg/kg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
No Treatment on Day 15
No drug administration; end of study treatment
AUC0-tlast of 1'-Hydroxymidazolam
11019.7 h*pg/ml
Standard Deviation 4377.21
12669.0 h*pg/ml
Standard Deviation 5085.13

PRIMARY outcome

Timeframe: Day 1 and Day 14

Population: PK Set - Midazolam: a subset of the Safety Set and includes all subjects who completed the scheduled vamorolone and midazolam dosing and provided an evaluable midazolam PK profile on at least one of the following days Day 1 and Day 14. No vomiting should occur within 4 hours following midazolam and/or vamorolone administration. This PK set was used for PK concentration summary and PK parameter summary for midazolam and 1'-hydroxymidazolam

Area under the plasma concentration-time curve from 0 to the infinite time (h\*pg/mL) on day 1 and Day 14. The timepoints at which the data were collected to create the curve are as follows: predose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 10 hours postdose and extrapolation to infinity.

Outcome measures

Outcome measures
Measure
Midazolam Alone on Day 1
n=18 Participants
Day 1: Single oral of midazolam dose 2.5 mg
Midazolam Co-administered With Vamorolone on Day 14.
n=18 Participants
Day 14: Single oral midazolam dose of 2.5mg + Single oral suspension vamorolone dose of 6mg/kg
Vamorolone on Day 11
Oral suspension of vamorolone 6 mg/kg
Vamorolone Alone on Day 13
Oral suspension of vamorolone 6 mg/kg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
No Treatment on Day 15
No drug administration; end of study treatment
AUC-inf of 1'-Hydroxymidazolam
11592.1 h*pg/ml
Standard Deviation 4592.86
13211.4 h*pg/ml
Standard Deviation 5225.69

PRIMARY outcome

Timeframe: Day 1 and Day 14

Population: PK Set - Midazolam: a subset of the Safety Set and includes all subjects who completed the scheduled vamorolone and midazolam dosing and provided an evaluable midazolam PK profile on at least one of the following days Day 1 and Day 14. No vomiting should occur within 4 hours following midazolam and/or vamorolone administration. This PK set was used for PK concentration summary and PK parameter summary for midazolam and 1'-hydroxymidazolam

maximum measured concentration of 1'-Hydroxymidazolam after administration of midazolam until the last collection time, i.e., 10 hours after dosing

Outcome measures

Outcome measures
Measure
Midazolam Alone on Day 1
n=18 Participants
Day 1: Single oral of midazolam dose 2.5 mg
Midazolam Co-administered With Vamorolone on Day 14.
n=18 Participants
Day 14: Single oral midazolam dose of 2.5mg + Single oral suspension vamorolone dose of 6mg/kg
Vamorolone on Day 11
Oral suspension of vamorolone 6 mg/kg
Vamorolone Alone on Day 13
Oral suspension of vamorolone 6 mg/kg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
No Treatment on Day 15
No drug administration; end of study treatment
Cmax of 1'-Hydroxymidazolam
5846 pg/ml
Standard Deviation 2748.8
7920 pg/ml
Standard Deviation 3988.6

SECONDARY outcome

Timeframe: Day 1 and Day 14

Population: PK Set - Midazolam: a subset of the Safety Set and includes all subjects who completed the scheduled vamorolone and midazolam dosing and provided an evaluable midazolam PK profile on at least one of the following days Day 1 and Day 14. No vomiting should occur within 4 hours following midazolam and/or vamorolone administration. This PK set was used for PK concentration summary and PK parameter summary for midazolam and 1'-hydroxymidazolam

Time to reach observed maximal concentration of midazolam after administration of midazolam until the last collection time, i.e., 10 hours after administration on day 1 and day 14

Outcome measures

Outcome measures
Measure
Midazolam Alone on Day 1
n=18 Participants
Day 1: Single oral of midazolam dose 2.5 mg
Midazolam Co-administered With Vamorolone on Day 14.
n=18 Participants
Day 14: Single oral midazolam dose of 2.5mg + Single oral suspension vamorolone dose of 6mg/kg
Vamorolone on Day 11
Oral suspension of vamorolone 6 mg/kg
Vamorolone Alone on Day 13
Oral suspension of vamorolone 6 mg/kg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
No Treatment on Day 15
No drug administration; end of study treatment
Tmax of Midazolam
0.500 h
Interval 0.25 to 1.52
0.500 h
Interval 0.25 to 2.02

SECONDARY outcome

Timeframe: Day 1 and Day 14

Population: PK Set - Midazolam: a subset of the Safety Set and includes all subjects who completed the scheduled vamorolone and midazolam dosing and provided an evaluable midazolam PK profile on at least one of the following days Day 1 and Day 14. No vomiting should occur within 4 hours following midazolam and/or vamorolone administration. This PK set was used for PK concentration summary and PK parameter summary for midazolam and 1'-hydroxymidazolam

The apparent clearance measures how quickly a drug leaves the body, considering how much reaches it after being taken orally. It was calculated using the formula: Dose/AUCinf on day 1 and day 14. The timepoints used were as follows: predose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 hours on day 1 and day 14

Outcome measures

Outcome measures
Measure
Midazolam Alone on Day 1
n=18 Participants
Day 1: Single oral of midazolam dose 2.5 mg
Midazolam Co-administered With Vamorolone on Day 14.
n=17 Participants
Day 14: Single oral midazolam dose of 2.5mg + Single oral suspension vamorolone dose of 6mg/kg
Vamorolone on Day 11
Oral suspension of vamorolone 6 mg/kg
Vamorolone Alone on Day 13
Oral suspension of vamorolone 6 mg/kg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
No Treatment on Day 15
No drug administration; end of study treatment
CL/F of Midazolam
78.80 L/h
Standard Deviation 45.683
93.27 L/h
Standard Deviation 31.471

SECONDARY outcome

Timeframe: Day 1 and Day 14

Population: PK Set - Midazolam: a subset of the Safety Set and includes all subjects who completed the scheduled vamorolone and midazolam dosing and provided an evaluable midazolam PK profile on at least one of the following days Day 1 and Day 14. No vomiting should occur within 4 hours following midazolam and/or vamorolone administration. This PK set was used for PK concentration summary and PK parameter summary for midazolam and 1'-hydroxymidazolam

Vz/F is the ratio of the volume of distribution of a drug to its bioavailability. It describes how widely the drug is distributed in the body after oral administration. It was calculated based on the terminal phase (ℷz)using the formula: Dose /ℷz.AUCinf on day 1 and day 14. The timepoints were as follows: predose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 hours.

Outcome measures

Outcome measures
Measure
Midazolam Alone on Day 1
n=18 Participants
Day 1: Single oral of midazolam dose 2.5 mg
Midazolam Co-administered With Vamorolone on Day 14.
n=17 Participants
Day 14: Single oral midazolam dose of 2.5mg + Single oral suspension vamorolone dose of 6mg/kg
Vamorolone on Day 11
Oral suspension of vamorolone 6 mg/kg
Vamorolone Alone on Day 13
Oral suspension of vamorolone 6 mg/kg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
No Treatment on Day 15
No drug administration; end of study treatment
Vz/F of Midazolam
311.0 L
Standard Deviation 110.54
414.3 L
Standard Deviation 123.97

SECONDARY outcome

Timeframe: Day 1 and Day 14

Population: PK Set - Midazolam: a subset of the Safety Set and includes all subjects who completed the scheduled vamorolone and midazolam dosing and provided an evaluable midazolam PK profile on at least one of the following days Day 1 and Day 14. No vomiting should occur within 4 hours following midazolam and/or vamorolone administration. This PK set was used for PK concentration summary and PK parameter summary for midazolam and 1'-hydroxymidazolam

Elimination half-life is the amount of time it takes for the concentration of the drug (midazolam) in the body to decrease by half after administration on day 1 and day 14. The collection times were predose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 hours.

Outcome measures

Outcome measures
Measure
Midazolam Alone on Day 1
n=18 Participants
Day 1: Single oral of midazolam dose 2.5 mg
Midazolam Co-administered With Vamorolone on Day 14.
n=18 Participants
Day 14: Single oral midazolam dose of 2.5mg + Single oral suspension vamorolone dose of 6mg/kg
Vamorolone on Day 11
Oral suspension of vamorolone 6 mg/kg
Vamorolone Alone on Day 13
Oral suspension of vamorolone 6 mg/kg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
No Treatment on Day 15
No drug administration; end of study treatment
t1/2 of Midazolam
2.980 h
Standard Deviation 0.7003
3.305 h
Standard Deviation 0.8752

SECONDARY outcome

Timeframe: Day 1 and Day 14

Population: PK Set - Midazolam: a subset of the Safety Set and includes all subjects who completed the scheduled vamorolone and midazolam dosing and provided an evaluable midazolam PK profile on at least one of the following days Day 1 and Day 14. No vomiting should occur within 4 hours following midazolam and/or vamorolone administration. This PK set was used for PK concentration summary and PK parameter summary for midazolam and 1'-hydroxymidazolam

Time to reach observed maximal concentration of 1'-Hydroxymidazolam after administration of midazolam until the last collection time, i.e., 10 hours after dosing on day 1 and day 14

Outcome measures

Outcome measures
Measure
Midazolam Alone on Day 1
n=18 Participants
Day 1: Single oral of midazolam dose 2.5 mg
Midazolam Co-administered With Vamorolone on Day 14.
n=18 Participants
Day 14: Single oral midazolam dose of 2.5mg + Single oral suspension vamorolone dose of 6mg/kg
Vamorolone on Day 11
Oral suspension of vamorolone 6 mg/kg
Vamorolone Alone on Day 13
Oral suspension of vamorolone 6 mg/kg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
No Treatment on Day 15
No drug administration; end of study treatment
Tmax of 1'-Hydroxymidazolam
0.500 h
Interval 0.25 to 1.52
0.500 h
Interval 0.5 to 2.02

SECONDARY outcome

Timeframe: Day 1 and Day 14

Population: PK Set - Midazolam: a subset of the Safety Set and includes all subjects who completed the scheduled vamorolone and midazolam dosing and provided an evaluable midazolam PK profile on at least one of the following days Day 1 and Day 14. No vomiting should occur within 4 hours following midazolam and/or vamorolone administration. This PK set was used for PK concentration summary and PK parameter summary for midazolam and 1'-hydroxymidazolam

Elimination half-life is the amount of time it takes for the concentration of the drug (1'-Hydroxymidazolam) in the body to decrease by half on day 1 and day 14. The collection times were predose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 hours.

Outcome measures

Outcome measures
Measure
Midazolam Alone on Day 1
n=18 Participants
Day 1: Single oral of midazolam dose 2.5 mg
Midazolam Co-administered With Vamorolone on Day 14.
n=18 Participants
Day 14: Single oral midazolam dose of 2.5mg + Single oral suspension vamorolone dose of 6mg/kg
Vamorolone on Day 11
Oral suspension of vamorolone 6 mg/kg
Vamorolone Alone on Day 13
Oral suspension of vamorolone 6 mg/kg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
No Treatment on Day 15
No drug administration; end of study treatment
t1/2 of 1'-Hydroxymidazolam
2.215 h
Standard Deviation 0.4131
2.122 h
Standard Deviation 0.3770

SECONDARY outcome

Timeframe: Day 3, Day 4, Day 7, Day 11, Day 13, Day 14

Population: PK-Set Vamorolone: This analysis set is a subset of the safety set and includes all subjects who completed at least one scheduled vamorolone dose without vomiting within 4 hours immediately following that vamorolone administration and provided at least one valid PK concentration data for vamorolone. This PK set was used for PK concentration summary and PK parameter summary for vamorolone

Concentration measurements taken just before the first administration of vamorolone on day 3, and at the end of each vamorolone dosing interval before the next dose on days 4, 7, 11, 13, and 14.

Outcome measures

Outcome measures
Measure
Midazolam Alone on Day 1
n=18 Participants
Day 1: Single oral of midazolam dose 2.5 mg
Midazolam Co-administered With Vamorolone on Day 14.
n=18 Participants
Day 14: Single oral midazolam dose of 2.5mg + Single oral suspension vamorolone dose of 6mg/kg
Vamorolone on Day 11
n=18 Participants
Oral suspension of vamorolone 6 mg/kg
Vamorolone Alone on Day 13
n=18 Participants
Oral suspension of vamorolone 6 mg/kg
Vamorolone Coadministrated With Midazolam on Day 14
n=18 Participants
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
Vamorolone Coadministrated With Midazolam on Day 14
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
No Treatment on Day 15
No drug administration; end of study treatment
Predose Concentration (Ctrough) of Vamorolone
9.397 ng/ml
Standard Deviation 20.182
3.486 ng/ml
Standard Deviation 5.0864
3.816 ng/ml
Standard Deviation 5.1055
2.070 ng/ml
Standard Deviation 2.5436
1.303 ng/ml
Standard Deviation 1.5972

SECONDARY outcome

Timeframe: Day 1, Day 3, Day 4, Day 7, Day 11, Day 14, Day 15

Population: Safety Set: All subjects assigned to study treatment and who received at least 1 dose of study treatment. Subjects were analyzed according to the treatment they actually received.

Urinary 6β-hydroxycortisol to cortisol ratio is used as in vivo biomarkers for CYP3A4 activity. The impact of vamorlone on adrenal suppression could result in alterations in urinary cortisol and 6-β-hydroxycortisol levels.. Thus, the 6-β-hydroxycortisol to cortisol ratio is an unreliable measure of vamorolone's CYP3A4 induction potential.

Outcome measures

Outcome measures
Measure
Midazolam Alone on Day 1
n=17 Participants
Day 1: Single oral of midazolam dose 2.5 mg
Midazolam Co-administered With Vamorolone on Day 14.
n=18 Participants
Day 14: Single oral midazolam dose of 2.5mg + Single oral suspension vamorolone dose of 6mg/kg
Vamorolone on Day 11
n=11 Participants
Oral suspension of vamorolone 6 mg/kg
Vamorolone Alone on Day 13
n=11 Participants
Oral suspension of vamorolone 6 mg/kg
Vamorolone Coadministrated With Midazolam on Day 14
n=10 Participants
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
Vamorolone Coadministrated With Midazolam on Day 14
n=5 Participants
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
No Treatment on Day 15
n=14 Participants
No drug administration; end of study treatment
Urinary 6β-hydroxycortisol to Cortisol Ratio
3.496 ratio
Standard Deviation 1.4406
2.856 ratio
Standard Deviation 1.1187
4.739 ratio
Standard Deviation 0.95864
5.518 ratio
Standard Deviation 1.4118
5.234 ratio
Standard Deviation 1.4441
5.388 ratio
Standard Deviation 0.99344
6.571 ratio
Standard Deviation 2.6256

SECONDARY outcome

Timeframe: Day 1, Day 3, Day 4, Day 7, Day 11, Day 14, Day 15

Population: Safety Set: All subjects assigned to study treatment and who received at least 1 dose of study treatment. Subjects were analyzed according to the treatment they actually received.

The plasma concentration of 4-β-hydroxycholesterol is used as an in vivo marker to assess CYP3A4 induction activity

Outcome measures

Outcome measures
Measure
Midazolam Alone on Day 1
n=18 Participants
Day 1: Single oral of midazolam dose 2.5 mg
Midazolam Co-administered With Vamorolone on Day 14.
n=18 Participants
Day 14: Single oral midazolam dose of 2.5mg + Single oral suspension vamorolone dose of 6mg/kg
Vamorolone on Day 11
n=18 Participants
Oral suspension of vamorolone 6 mg/kg
Vamorolone Alone on Day 13
n=18 Participants
Oral suspension of vamorolone 6 mg/kg
Vamorolone Coadministrated With Midazolam on Day 14
n=18 Participants
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
Vamorolone Coadministrated With Midazolam on Day 14
n=18 Participants
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
No Treatment on Day 15
n=18 Participants
No drug administration; end of study treatment
Plasma 4β-hydroxycholesterol Level
40.75 ng/ml
Standard Deviation 44.696
41.51 ng/ml
Standard Deviation 34.890
40.36 ng/ml
Standard Deviation 33.582
45.53 ng/ml
Standard Deviation 34.426
38.87 ng/ml
Standard Deviation 20.366
36.73 ng/ml
Standard Deviation 19.713
38.93 ng/ml
Standard Deviation 19.328

Adverse Events

Midazolam Alone on Day 1

Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths

Vamorolone Alone on Day 3 to Day 13

Serious events: 0 serious events
Other events: 8 other events
Deaths: 0 deaths

Vamorolone Coadministrated With Midazolam on Day 14

Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Other adverse events
Measure
Midazolam Alone on Day 1
n=18 participants at risk
Single oral midazolam dose 2.5mg
Vamorolone Alone on Day 3 to Day 13
n=18 participants at risk
Oral suspension of vamorolone 6 mg/kg
Vamorolone Coadministrated With Midazolam on Day 14
n=18 participants at risk
Oral suspension of vamorolone 6 mg/kg coadministrated with single oral of midazolam dose 2.5 mg
General disorders
Fatigue
5.6%
1/18 • Number of events 2 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
Nervous system disorders
Headache
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
5.6%
1/18 • Number of events 2 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
5.6%
1/18 • Number of events 1 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
Psychiatric disorders
Initial Insomnia
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
16.7%
3/18 • Number of events 3 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
Investigations
ALT increased
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
5.6%
1/18 • Number of events 1 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
Investigations
Amylase increased
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
5.6%
1/18 • Number of events 1 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
Investigations
Lipase Increased
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
5.6%
1/18 • Number of events 1 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
Eye disorders
Foreign body sensation in eyes
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
5.6%
1/18 • Number of events 1 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
Gastrointestinal disorders
Dyspepsia
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
5.6%
1/18 • Number of events 1 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
Infections and infestations
Nasopharyngitis
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
5.6%
1/18 • Number of events 1 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
Respiratory, thoracic and mediastinal disorders
Nasal Discomfort
5.6%
1/18 • Number of events 1 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
5.6%
1/18 • Number of events 1 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.
0.00%
0/18 • All AEs and SAEs were collected from signing the informed consent until the safety follow-up visit on Day 28 i.e., approximately 2 weeks after the last midazolam administration/early discontinuation visit. After the conclusion of the study, investigators did not actively seek AEs and SAEs. All SAEs had to be recorded and reported to the sponsor or designee within 24 hours. Investigators had to report any SADR (SAE considered related to the IMP) to the sponsor.

Additional Information

Shabir Hasham MD, Chief Medical Officer

Santhera Pharmaceuticals LTD

Phone: +41 79 520 95 18

Results disclosure agreements

  • Principal investigator is a sponsor employee
  • Publication restrictions are in place