Trial Outcomes & Findings for Safety, Pharmacokinetics and Efficacy Study of QCC374 in PAH Patients (NCT NCT02927366)

NCT ID: NCT02927366

Last Updated: 2021-01-05

Results Overview

The efficacy of 16 weeks of QCC374 administration in subjects with Pulmonary Arterial Hypertension (PAH) was assessed by measuring changes from baseline in Pulmonary Vascular Resistance (PVR). PVR is derived from the CO measurement in dyn·s/cm5 and can be calculated as 80 multiplied by (Mean Arterial Pressure - Mean Pulmonary Artery Wedge Pressure) divided by Cardiac Output. A higher negative number in Pulmonary Vascular Resistance indicates improvement. Only descriptive analysis performed.

Recruitment status

TERMINATED

Study phase

PHASE2

Target enrollment

8 participants

Primary outcome timeframe

Baseline, Week 16 (Day 111)

Results posted on

2021-01-05

Participant Flow

This study was conducted in 5 centers in 4 countries: Germany (2), Korea (1), UK (1) and USA (1).

Part 1 consisted of 8 subjects, randomized in a 6:2 ratio to QCC374 or placebo. The planned bid dose levels in Part 1 were 0.03 mg, 0.06 mg and 0.12 mg. Subjects began dosing at 0.03 mg bid.

Participant milestones

Participant milestones
Measure
QCC374
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Overall Study
STARTED
6
2
Overall Study
Pharmacodynamic (PD) Analysis Set
6
2
Overall Study
Pharmacokinetic (PK) Analysis Set
4
0
Overall Study
COMPLETED
4
2
Overall Study
NOT COMPLETED
2
0

Reasons for withdrawal

Reasons for withdrawal
Measure
QCC374
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Overall Study
Adverse Event
1
0
Overall Study
Patient schedule
1
0

Baseline Characteristics

Safety, Pharmacokinetics and Efficacy Study of QCC374 in PAH Patients

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure
QCC374
n=6 Participants
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
n=2 Participants
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Total
n=8 Participants
Total of all reporting groups
Age, Continuous
41.0 Years
STANDARD_DEVIATION 14.62 • n=99 Participants
57.5 Years
STANDARD_DEVIATION 9.19 • n=107 Participants
45.1 Years
STANDARD_DEVIATION 14.93 • n=206 Participants
Sex: Female, Male
Female
5 Participants
n=99 Participants
2 Participants
n=107 Participants
7 Participants
n=206 Participants
Sex: Female, Male
Male
1 Participants
n=99 Participants
0 Participants
n=107 Participants
1 Participants
n=206 Participants
Race/Ethnicity, Customized
Asian
1 Participants
n=99 Participants
0 Participants
n=107 Participants
1 Participants
n=206 Participants
Race/Ethnicity, Customized
White
5 Participants
n=99 Participants
2 Participants
n=107 Participants
7 Participants
n=206 Participants
Ethiology of Pulmonary Arterial Hypertension (PAH)
Family PAH
1 Participants
n=99 Participants
0 Participants
n=107 Participants
1 Participants
n=206 Participants
Ethiology of Pulmonary Arterial Hypertension (PAH)
Idiopathic PAH
4 Participants
n=99 Participants
1 Participants
n=107 Participants
5 Participants
n=206 Participants
Ethiology of Pulmonary Arterial Hypertension (PAH)
PAH associated with Connective Tissue Disease
1 Participants
n=99 Participants
0 Participants
n=107 Participants
1 Participants
n=206 Participants
Ethiology of Pulmonary Arterial Hypertension (PAH)
PAH induced by Drug/Toxin
0 Participants
n=99 Participants
1 Participants
n=107 Participants
1 Participants
n=206 Participants
Time from Pulmonary Arterial Hypertension (PAH) diagnosis
2.985 Years
n=99 Participants
9.201 Years
n=107 Participants
4.966 Years
n=206 Participants

PRIMARY outcome

Timeframe: Baseline, Week 16 (Day 111)

Population: Participants from the Pharmacodynamic (PD) analysis set, defined as all randomized participants who received at least one dose of study drug and one evaluable PD assessment, with data available for analysis were considered.

The efficacy of 16 weeks of QCC374 administration in subjects with Pulmonary Arterial Hypertension (PAH) was assessed by measuring changes from baseline in Pulmonary Vascular Resistance (PVR). PVR is derived from the CO measurement in dyn·s/cm5 and can be calculated as 80 multiplied by (Mean Arterial Pressure - Mean Pulmonary Artery Wedge Pressure) divided by Cardiac Output. A higher negative number in Pulmonary Vascular Resistance indicates improvement. Only descriptive analysis performed.

Outcome measures

Outcome measures
Measure
QCC374
n=6 Participants
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
n=2 Participants
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Change From Baseline in Pulmonary Vascular Resistance (PVR) at Week 16 (Day 111)
PVR at Screening-Ratio to Baseline
1.00 dyn*s/cm5
Standard Deviation 0.000
1.00 dyn*s/cm5
Standard Deviation 0.000
Change From Baseline in Pulmonary Vascular Resistance (PVR) at Week 16 (Day 111)
PVR at Day 111-Ratio to Baseline
1.07 dyn*s/cm5
Standard Deviation 0.274
1.05 dyn*s/cm5
Standard Deviation 0.073

SECONDARY outcome

Timeframe: Baseline, Day 28, Day 56, Day 84 and Day 111

Population: Participants from the Pharmacodynamic (PD) analysis set, defined as all randomized participants who received at least one dose of study drug and one evaluable PD assessment, with data available for analysis were considered.

The Six Minute Walk Test measures the distance an individual is able to walk over a total of six minutes on a hard, flat surface. The goal is for the individual to walk as far as possible in six minutes. The individual is able to self-pace and rest as needed as they traverse back and forth along a marked walkway. Only descriptive analysis performed.

Outcome measures

Outcome measures
Measure
QCC374
n=6 Participants
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
n=2 Participants
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Change From Baseline in Six Minute Walk Distance (6MWD) Over Time
Chge from BL at Day 111
13.25 Meter
Standard Deviation 25.002
14.00 Meter
Standard Deviation 9.192
Change From Baseline in Six Minute Walk Distance (6MWD) Over Time
Baseline
443.83 Meter
Standard Deviation 47.942
458.50 Meter
Standard Deviation 111.723
Change From Baseline in Six Minute Walk Distance (6MWD) Over Time
Chge from BL at Day 28
-7.17 Meter
Standard Deviation 20.651
9.75 Meter
Standard Deviation 13.789
Change From Baseline in Six Minute Walk Distance (6MWD) Over Time
Chge from BL at Day 56
-11.60 Meter
Standard Deviation 19.562
14.50 Meter
Standard Deviation 19.799
Change From Baseline in Six Minute Walk Distance (6MWD) Over Time
Chge from BL at Day 84
-4.25 Meter
Standard Deviation 21.956
12.50 Meter
Standard Deviation 16.971

SECONDARY outcome

Timeframe: Baseline, Week 16 (Day 111)

Population: Participants from the Pharmacodynamic (PD) analysis set, defined as all randomized participants who received at least one dose of study drug and one evaluable PD assessment, with data available for analysis were considered.

The Right Heart Catheterization (RHC) assessment was performed to assess several hemodynamic variables in pulmonary hypertension, including Cardiac Output (CO). All hemodynamic parameters were assessed when the patient was in a stable hemodynamic rest state (as demonstrated by three consecutive CO measurements within 10% of each other) while the patient was breathing ambient air or oxygen. CO was measured in triplicate using the thermodilution technique. Direct Fick could be used only after discussion and approval by the Sponsor. In all cases, the same technique was to be used at baseline and week 16. . A higher positive number in Cardiac Output indicates improvement. Only descriptive analysis performed.

Outcome measures

Outcome measures
Measure
QCC374
n=6 Participants
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
n=2 Participants
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Change From Baseline in Cardiac Output (CO) at Week 16 (Day 111)
Average Cardiac Output at Baseline
4.33 L/min
Standard Deviation 1.527
3.61 L/min
Standard Deviation 0.085
Change From Baseline in Cardiac Output (CO) at Week 16 (Day 111)
Average Cardiac Output at Day 111
4.46 L/min
Standard Deviation 0.937
3.79 L/min
Standard Deviation 0.191
Change From Baseline in Cardiac Output (CO) at Week 16 (Day 111)
Cardiac Output 1 at Baseline
4.38 L/min
Standard Deviation 1.491
3.61 L/min
Standard Deviation 0.127
Change From Baseline in Cardiac Output (CO) at Week 16 (Day 111)
Cardiac Output 1 at Day 111
4.58 L/min
Standard Deviation 1.002
3.69 L/min
Standard Deviation 0.311
Change From Baseline in Cardiac Output (CO) at Week 16 (Day 111)
Cardiac Output 2 at Baseline
3.96 L/min
Standard Deviation 1.588
3.60 L/min
Standard Deviation 0.000
Change From Baseline in Cardiac Output (CO) at Week 16 (Day 111)
Cardiac Output 2 at Day 111
4.33 L/min
Standard Deviation 0.993
3.89 L/min
Standard Deviation 0.233
Change From Baseline in Cardiac Output (CO) at Week 16 (Day 111)
Cardiac Output 3 at Baseline
3.98 L/min
Standard Deviation 1.340
3.61 L/min
Standard Deviation 0.127
Change From Baseline in Cardiac Output (CO) at Week 16 (Day 111)
Cardiac Output 3 at Day 111
4.40 L/min
Standard Deviation 1.238
3.79 L/min
Standard Deviation 0.028

SECONDARY outcome

Timeframe: Baseline, Week 16 (Day 111)

Population: Participants from the Pharmacodynamic (PD) analysis set, defined as all randomized participants who received at least one dose of study drug and one evaluable PD assessment, with data available for analysis were considered.

The Right Heart Catheterization (RHC) assessment was performed to assess several hemodynamic variables in pulmonary hypertension, including Cardiac Index. All hemodynamic parameters were assessed when the patient was in a stable hemodynamic rest state (as demonstrated by three consecutive CO measurements within 10% of each other) while the patient was breathing ambient air or oxygen. A higher negative number in Cardiac Index indicates improvement. Only descriptive analysis performed.

Outcome measures

Outcome measures
Measure
QCC374
n=6 Participants
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
n=2 Participants
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Change From Baseline in Cardiac Index at Week 16 (Day 111)
Cardiac Index at Baseline
2.45 L/min/m2
Standard Deviation 0.794
2.15 L/min/m2
Standard Deviation 0.070
Change From Baseline in Cardiac Index at Week 16 (Day 111)
Cardiac Index at Day 111
2.54 L/min/m2
Standard Deviation NA
NA: Not estimable due to insufficient number of participants with events

SECONDARY outcome

Timeframe: Baseline, Week 16 (Day 111)

Population: Participants from the Pharmacodynamic (PD) analysis set, defined as all randomized participants who received at least one dose of study drug and one evaluable PD assessment, with data available for analysis were considered.

The Right Heart Catheterization (RHC) assessment was performed to assess several hemodynamic variables in pulmonary hypertension, including mean Pulmonary Capillary Wedge Pressure (PCWP). All hemodynamic parameters were assessed when the patient was in a stable hemodynamic rest state (as demonstrated by three consecutive CO measurements within 10% of each other) while the patient was breathing ambient air or oxygen. Pressure measurements were made in the PA, PA wedge, right ventricle (RV) and right atrium (RA) and determined at the end of normal expiration. The PCWP was recorded as the mean of three measurements. Only descriptive analysis performed.

Outcome measures

Outcome measures
Measure
QCC374
n=6 Participants
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
n=2 Participants
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Change From Baseline in Pulmonary Capillary Wedge Pressure (PCWP) at Week 16 (Day 111)
PCWP at Baseline
8.67 mmHg
Standard Deviation 1.366
9.50 mmHg
Standard Deviation 0.707
Change From Baseline in Pulmonary Capillary Wedge Pressure (PCWP) at Week 16 (Day 111)
PCWP at Day 111
11.75 mmHg
Standard Deviation 5.188
9.50 mmHg
Standard Deviation 0.707

SECONDARY outcome

Timeframe: Baseline, Week 16 (Day 111)

Population: Participants from the Pharmacodynamic (PD) analysis set, defined as all randomized participants who received at least one dose of study drug and one evaluable PD assessment, with data available for analysis were considered.

The Right Heart Catheterization (RHC) assessment was performed to assess several hemodynamic variables in pulmonary hypertension, including Systemic Vascular Resistance (SVR). All hemodynamic parameters were assessed when the patient was in a stable hemodynamic rest state (as demonstrated by three consecutive CO measurements within 10% of each other) while the patient was breathing ambient air or oxygen. SVR is derived from the CO measurement in dyn·s/cm5 and can be calculated as 80 multiplied by (Mean Arterial Pressure - Mean Venous Pressure or CVP)) divided by Cardiac Output. A higher negative number in Mean Systemic Vascular Resistance indicates improvement. Only descriptive analysis performed.

Outcome measures

Outcome measures
Measure
QCC374
n=6 Participants
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
n=2 Participants
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Change From Baseline in Systemic Vascular Resistance (SVR) at Week 16 (Day 111)
SVR at Baseline
1133.31 dynes*Sec*cm5
Standard Deviation 410.336
1425.89 dynes*Sec*cm5
Standard Deviation 633.723
Change From Baseline in Systemic Vascular Resistance (SVR) at Week 16 (Day 111)
SVR at Day 111
1285.50 dynes*Sec*cm5
Standard Deviation 465.983
1240.00 dynes*Sec*cm5
Standard Deviation 274.357

SECONDARY outcome

Timeframe: Baseline, Week 16 (Day 111)

Population: Participants from the Pharmacodynamic (PD) analysis set, defined as all randomized participants who received at least one dose of study drug and one evaluable PD assessment, with data available for analysis were considered.

Key Right Ventricular (RV) function endpoints such as RV fractional area change (RV FAC) and RV Free Wall Average Peak Long Strain (RV FWPLS) were assessed with echocardiography. A higher number in RV FAC and a lower number in RV FWPLS indicate an improvement. Only descriptive analysis performed.

Outcome measures

Outcome measures
Measure
QCC374
n=5 Participants
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
n=2 Participants
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Change From Baseline in RV Fractional Area Change and RV Free Wall Average Peak Long Strain at Week 16 (Day 111) Using Echocardiography
RV FWPLS at Baseline
12.68 Percentage
Standard Deviation 3.534
16.30 Percentage
Standard Deviation NA
NA: Not estimable due to insufficient number of participants with events
Change From Baseline in RV Fractional Area Change and RV Free Wall Average Peak Long Strain at Week 16 (Day 111) Using Echocardiography
RV FAC at Baseline
20.17 Percentage
Standard Deviation 8.717
30.05 Percentage
Standard Deviation 7.050
Change From Baseline in RV Fractional Area Change and RV Free Wall Average Peak Long Strain at Week 16 (Day 111) Using Echocardiography
RV FAC at Day 111
20.70 Percentage
Standard Deviation 5.091
26.20 Percentage
Standard Deviation NA
NA: Not estimable due to insufficient number of participants with events
Change From Baseline in RV Fractional Area Change and RV Free Wall Average Peak Long Strain at Week 16 (Day 111) Using Echocardiography
RV FWPLS at Day 111
7.85 Percentage
Standard Deviation 2.758

SECONDARY outcome

Timeframe: Baseline, Week 16 (Day 111)

Population: Participants from the Pharmacodynamic (PD) analysis set, defined as all randomized participants who received at least one dose of study drug and one evaluable PD assessment, with data available for analysis were considered.

Key Right Ventricular (RV) function endpoints such as Tei Index were assessed with echocardiography. The RV Tei index is using both systolic and diastolic time intervals to evaluate the overall global dysfunction of the right ventricle in PAH patients. A lower number in RV Tei Index indicates an improvement. Only descriptive analysis performed.

Outcome measures

Outcome measures
Measure
QCC374
n=5 Participants
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
n=2 Participants
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Change From Baseline in RV Tei Index at Week 16 (Day 111) Using Echocardiography
RV Tei Index at Baseline
0.92 Index
Standard Deviation 0.260
0.88 Index
Standard Deviation 0.361
Change From Baseline in RV Tei Index at Week 16 (Day 111) Using Echocardiography
RV Tei Index at Day 111
0.89 Index
Standard Deviation 0.099
0.89 Index
Standard Deviation 0.078

SECONDARY outcome

Timeframe: Baseline, Week 16 (Day 111)

Population: Participants from the Pharmacodynamic (PD) analysis set, defined as all randomized participants who received at least one dose of study drug and one evaluable PD assessment, with data available for analysis were considered.

Key Right Ventricular (RV) function endpoints such as Tricuspid Annular Peak Systolic Velocity (TA S') were assessed with echocardiography. Only descriptive analysis performed.

Outcome measures

Outcome measures
Measure
QCC374
n=5 Participants
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
n=2 Participants
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Change From Baseline in Tricuspid Annular Peak Systolic Velocity (TA S') at Week 16 (Day 111) Using Echocardiography
TA S' at Baseline
11.23 cm/s
Standard Deviation 1.723
9.50 cm/s
Standard Deviation 0.990
Change From Baseline in Tricuspid Annular Peak Systolic Velocity (TA S') at Week 16 (Day 111) Using Echocardiography
TA S' at Day 111
9.73 cm/s
Standard Deviation 1.069
13.20 cm/s
Standard Deviation NA
NA: Not estimable due to insufficient number of participants with events

SECONDARY outcome

Timeframe: Baseline, Week 16 (Day 111)

Population: Participants from the Pharmacodynamic (PD) analysis set, defined as all randomized participants who received at least one dose of study drug and one evaluable PD assessment, with data available for analysis were considered.

Key Right Ventricular (RV) function endpoints such as Tricuspid Annular Plane Sys Excursion (TAPSE) were assessed with echocardiography. A higher number in TAPSE indicates an improvement. Only descriptive analysis performed.

Outcome measures

Outcome measures
Measure
QCC374
n=5 Participants
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
n=2 Participants
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Change From Baseline in Tricuspid Annular Plane Sys Excursion (TAPSE) at Week 16 (Day 111) Using Echocardiography
TAPSE at Day 111
1.79 cm
Standard Deviation 0.511
1.76 cm
Standard Deviation NA
NA: Not estimable due to insufficient number of participants with events
Change From Baseline in Tricuspid Annular Plane Sys Excursion (TAPSE) at Week 16 (Day 111) Using Echocardiography
TAPSE at Baseline
1.88 cm
Standard Deviation 0.313
1.27 cm
Standard Deviation 0.170

SECONDARY outcome

Timeframe: Day 1 and 112 (0.00, 0.05, 0.15, 0.30, 1.00, 2.00, 4.00, 8.00 and 12.00 hours post-dose))

Population: Participants from the Pharmacokinetic (PK) analysis set, defined as all randomized participants who received at least one dose of study drug and one evaluable PK concentration measurement, with data available for analysis were considered.

Cmax is the maximum (peak) observed plasma drug concentration after single dose administration. PK parameters were calculated from plasma concentration-time data using non-compartmental methods. Only descriptive analysis performed.

Outcome measures

Outcome measures
Measure
QCC374
n=4 Participants
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Maximum Observed Plasma Concentration (Cmax) for QCC374 and Its Metabolite QCM441
QCC374: Day 1, Dose Level 0.03 mg
101 pg/mL
Geometric Coefficient of Variation 15.7
Maximum Observed Plasma Concentration (Cmax) for QCC374 and Its Metabolite QCM441
QCC374: Day 112, Dose Level 0.06 mg
461 pg/mL
Geometric Coefficient of Variation NA
NA: Not estimable due to insufficient number of participants with events
Maximum Observed Plasma Concentration (Cmax) for QCC374 and Its Metabolite QCM441
QCC374: Day 112, Dose Level 0.12 mg
406 pg/mL
Geometric Coefficient of Variation NA
NA: Not estimable due to insufficient number of participants with events
Maximum Observed Plasma Concentration (Cmax) for QCC374 and Its Metabolite QCM441
QCM441: Day 1, Dose Level 0.03 mg
346 pg/mL
Geometric Coefficient of Variation 32.4
Maximum Observed Plasma Concentration (Cmax) for QCC374 and Its Metabolite QCM441
QCM441: Day 112, Dose Level 0.06 mg
2350 pg/mL
Geometric Coefficient of Variation NA
NA: Not estimable due to insufficient number of participants with events
Maximum Observed Plasma Concentration (Cmax) for QCC374 and Its Metabolite QCM441
QCM441: Day 112, Dose Level 0.12 mg
3610 pg/mL
Geometric Coefficient of Variation NA
NA: Not estimable due to insufficient number of participants with events

SECONDARY outcome

Timeframe: Day 1 and 112 (0.00, 0.05, 0.15, 0.30, 1.00, 2.00, 4.00, 8.00 and 12.00 hours post-dose))

Population: Participants from the Pharmacokinetic (PK) analysis set, defined as all randomized participants who received at least one dose of study drug and one evaluable PK concentration measurement, with data available for analysis were considered.

Tmax is the time to reach maximum plasma concentration after single dose administration. PK parameters were calculated from plasma concentration-time data using non-compartmental methods. Only descriptive analysis performed.

Outcome measures

Outcome measures
Measure
QCC374
n=4 Participants
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Time to Reach the Maximum Plasma Concentration (Tmax) for QCC374 and Its Metabolite QCM441
QCC374: Day 1, Dose Level 0.03 mg
0.159 hour
Interval 0.083 to 0.267
Time to Reach the Maximum Plasma Concentration (Tmax) for QCC374 and Its Metabolite QCM441
QCC374: Day 112, Dose Level 0.06 mg
0.00 hour
Interval 0.0 to 0.0
Time to Reach the Maximum Plasma Concentration (Tmax) for QCC374 and Its Metabolite QCM441
QCC374: Day 112, Dose Level 0.12 mg
0.517 hour
Interval 0.517 to 0.517
Time to Reach the Maximum Plasma Concentration (Tmax) for QCC374 and Its Metabolite QCM441
QCM441: Day 1, Dose Level 0.03 mg
3.99 hour
Interval 3.85 to 8.0
Time to Reach the Maximum Plasma Concentration (Tmax) for QCC374 and Its Metabolite QCM441
QCM441: Day 112, Dose Level 0.06 mg
1.00 hour
Interval 1.0 to 1.0
Time to Reach the Maximum Plasma Concentration (Tmax) for QCC374 and Its Metabolite QCM441
QCM441: Day 112, Dose Level 0.12 mg
4.02 hour
Interval 4.02 to 4.02

SECONDARY outcome

Timeframe: Day 1 and 112 (0.00, 0.05, 0.15, 0.30, 1.00, 2.00, 4.00, 8.00 and 12.00 hours post-dose))

Population: Participants from the Pharmacokinetic (PK) analysis set, defined as all randomized participants who received at least one dose of study drug and one evaluable PK concentration measurement, with data available for analysis were considered.

AUClast is the area under the plasma concentration-time curve from time zero to the last measurable concentration sampling time. PK parameters were calculated from plasma concentration-time data using non-compartmental methods. Only descriptive analysis performed.

Outcome measures

Outcome measures
Measure
QCC374
n=4 Participants
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Area Under the Plasma Concentration-time Curve From 0 to the Last Measurable Concentration (AUClast) for QCC374 and Its Metabolite QCM441
QCC374: Day 1, Dose Level 0.03 mg
128 h*pg/mL
Geometric Coefficient of Variation 14.3
Area Under the Plasma Concentration-time Curve From 0 to the Last Measurable Concentration (AUClast) for QCC374 and Its Metabolite QCM441
QCC374: Day 112, Dose Level 0.06 mg
638 h*pg/mL
Geometric Coefficient of Variation NA
NA: Not estimable due to insufficient number of participants with events
Area Under the Plasma Concentration-time Curve From 0 to the Last Measurable Concentration (AUClast) for QCC374 and Its Metabolite QCM441
QCC374: Day 112, Dose Level 0.12 mg
883 h*pg/mL
Geometric Coefficient of Variation NA
NA: Not estimable due to insufficient number of participants with events
Area Under the Plasma Concentration-time Curve From 0 to the Last Measurable Concentration (AUClast) for QCC374 and Its Metabolite QCM441
QCM441: Day 1, Dose Level 0.03 mg
2590 h*pg/mL
Geometric Coefficient of Variation 22.8
Area Under the Plasma Concentration-time Curve From 0 to the Last Measurable Concentration (AUClast) for QCC374 and Its Metabolite QCM441
QCM441: Day 112, Dose Level 0.06 mg
17700 h*pg/mL
Geometric Coefficient of Variation NA
NA: Not estimable due to insufficient number of participants with events
Area Under the Plasma Concentration-time Curve From 0 to the Last Measurable Concentration (AUClast) for QCC374 and Its Metabolite QCM441
QCM441: Day 112, Dose Level 0.12 mg
33800 h*pg/mL
Geometric Coefficient of Variation NA
NA: Not estimable due to insufficient number of participants with events

SECONDARY outcome

Timeframe: Day 1 and 112 (0.00, 0.05, 0.15, 0.30, 1.00, 2.00, 4.00, 8.00 and 12.00 hours post-dose))

Population: Participants from the Pharmacokinetic (PK) analysis set, defined as all randomized participants who received at least one dose of study drug and one evaluable PK concentration measurement, with data available for analysis were considered.

AUCtau is the area under the plasma concentration-time curve from time zero to the end of the dosing interval. PK parameters were calculated from plasma concentration-time data using non-compartmental methods. Only descriptive analysis performed.

Outcome measures

Outcome measures
Measure
QCC374
n=4 Participants
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Area Under the Plasma Concentration Time Curve From 0 to the End of a Dosing Interval (AUCtau) for QCC374 and Its Metabolite QCM441
QCC374: Day 1, Dose Level 0.03 mg
148 h*pg/mL
Geometric Coefficient of Variation 15.5
Area Under the Plasma Concentration Time Curve From 0 to the End of a Dosing Interval (AUCtau) for QCC374 and Its Metabolite QCM441
QCC374: Day 112, Dose Level 0.06 mg
638 h*pg/mL
Geometric Coefficient of Variation NA
NA: Not estimable due to insufficient number of participants with events
Area Under the Plasma Concentration Time Curve From 0 to the End of a Dosing Interval (AUCtau) for QCC374 and Its Metabolite QCM441
QCC374: Day 112, Dose Level 0.12 mg
910 h*pg/mL
Geometric Coefficient of Variation NA
NA: Not estimable due to insufficient number of participants with events
Area Under the Plasma Concentration Time Curve From 0 to the End of a Dosing Interval (AUCtau) for QCC374 and Its Metabolite QCM441
QCM441: Day 1, Dose Level 0.03 mg
2600 h*pg/mL
Geometric Coefficient of Variation 40.6
Area Under the Plasma Concentration Time Curve From 0 to the End of a Dosing Interval (AUCtau) for QCC374 and Its Metabolite QCM441
QCM441: Day 112, Dose Level 0.06 mg
17700 h*pg/mL
Geometric Coefficient of Variation NA
NA: Not estimable due to insufficient number of participants with events
Area Under the Plasma Concentration Time Curve From 0 to the End of a Dosing Interval (AUCtau) for QCC374 and Its Metabolite QCM441
QCM441: Day 112, Dose Level 0.12 mg
33800 h*pg/mL
Geometric Coefficient of Variation NA
NA: Not estimable due to insufficient number of participants with events

Adverse Events

QCC374

Serious events: 1 serious events
Other events: 6 other events
Deaths: 0 deaths

Placebo

Serious events: 0 serious events
Other events: 1 other events
Deaths: 0 deaths

Serious adverse events

Serious adverse events
Measure
QCC374
n=6 participants at risk
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
n=2 participants at risk
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Nervous system disorders
Syncope
16.7%
1/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
0.00%
0/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.

Other adverse events

Other adverse events
Measure
QCC374
n=6 participants at risk
Adult patients with pulmonary arterial hypertension (PAH) on QCC374. All patients were initiated at 0.03 mg BID (Day 1-3), and were up-titrated to next higher dose 0.06 mg BID (Day 4) and increased to 0.12 mg BID (Day 7-14).
Placebo
n=2 participants at risk
Adult patients with pulmonary arterial hypertension (PAH) on placebo matching to QCC374 doses (0.03 mg BID (Day 1-3), 0.06 mg BID (Day 4) and 0.12 mg BID (Day 7-14)).
Gastrointestinal disorders
Dental Caries
0.00%
0/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
50.0%
1/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
Gastrointestinal disorders
Diarrhoea
33.3%
2/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
0.00%
0/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
Gastrointestinal disorders
Dyspepsia
16.7%
1/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
0.00%
0/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
Gastrointestinal disorders
Gastrointestinal Disorder
16.7%
1/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
0.00%
0/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
Gastrointestinal disorders
Gastrooesophageal Reflux Disease
16.7%
1/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
0.00%
0/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
Gastrointestinal disorders
Nausea
50.0%
3/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
0.00%
0/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
Gastrointestinal disorders
Vomiting
16.7%
1/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
0.00%
0/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
General disorders
Hangover
0.00%
0/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
50.0%
1/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
Infections and infestations
Gastroenteritis
16.7%
1/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
0.00%
0/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
Infections and infestations
Nasopharyngitis
33.3%
2/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
50.0%
1/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
Infections and infestations
Otitis Media
16.7%
1/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
0.00%
0/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
Musculoskeletal and connective tissue disorders
Pain In Extremity
16.7%
1/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
0.00%
0/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
Musculoskeletal and connective tissue disorders
Pain In Jaw
33.3%
2/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
0.00%
0/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
Nervous system disorders
Dysgeusia
16.7%
1/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
0.00%
0/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
Nervous system disorders
Head Discomfort
16.7%
1/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
0.00%
0/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
Nervous system disorders
Headache
83.3%
5/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
0.00%
0/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
Skin and subcutaneous tissue disorders
Erythema
16.7%
1/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
0.00%
0/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
Vascular disorders
Flushing
50.0%
3/6 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.
0.00%
0/2 • Adverse Events and Serious Adverse Events were collected for the maximum duration of participants' treatment exposure plus any follow up period, approximately 5 months.

Additional Information

Study Director

Novartis Pharmaceuticals

Phone: 862-778-8300

Results disclosure agreements

  • Principal investigator is a sponsor employee The terms and conditions of Novartis' agreements with its investigators may vary. However, Novartis does not prohibit any investigator from publishing. Any publications from a single-site are postponed until the publication of the pooled data (ie, data from all sites) in the clinical trial.
  • Publication restrictions are in place

Restriction type: OTHER