Trial Outcomes & Findings for A Comparison of the Pharmacokinetic Properties of ARN-75039 Tablets With Excipients to Neat ARN-75039 in Hydroxypropyl Methylcellulose (HPMC) Capsules in Healthy Adult Participants Under Fed Conditions (NCT NCT06911242)
NCT ID: NCT06911242
Last Updated: 2026-05-01
Results Overview
Area under the plasma concentration-time curve from time zero to 24 hours post-dose. Compare the pharmacokinetic (PK) properties of 300mg ARN-75039 with excipients in tablet form to 300mg neat ARN-75039 in HPMC capsules following oral administration under fed conditions.
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
16 participants
Primary outcome timeframe
From time zero (dose) to 24 hours post-dose.
Results posted on
2026-05-01
Participant Flow
Sixteen participants were enrolled, and none discontinued the study early or were excluded from analysis. All the informed consent forms (ICFs) were signed within the window from February 27, 2025 and March 11, 2025.
Two-period, two-sequence crossover (Sequence 1: A→B; Sequence 2: B→A). All 16 randomized participants completed both periods and contributed data to both formulations. Participant numbers shown per arm in the results represent treatment at the time of measurement (not unique participants).
Participant milestones
| Measure |
Sequence 1: Form A (Capsule), Then Form B (Tablet)
Participants received a single 300 mg ARN-75039 in capsule on first day of Day 1under fed conditions. After a washout period of 7 days, they then received a single 300mg (3x 100mg tablets) ARN-75039 tablet dose on Day 8, also administered under fed conditions. Following the dosing of the study drug on each treatment day (Day 1 and Day 8), fifteen venous blood samples were collected at regular time intervals.
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Sequence 2: Form B (Tablet), Then Form A (Capsule)
Participants first received 300 mg ARN-75039 tablet form (3x100mg tablets) on first day of Day 1under fed conditions. After a washout period of 7 days, they then received a single 300 mg ARN-75039 in capsule on Day 8, also administered under fed conditions. Following the dosing of the study drug on each treatment day (Day 1 and Day 8), fifteen venous blood samples were collected at regular time intervals.
|
|---|---|---|
|
First Intervention (day 1)
STARTED
|
8
|
8
|
|
First Intervention (day 1)
COMPLETED
|
8
|
8
|
|
First Intervention (day 1)
NOT COMPLETED
|
0
|
0
|
|
Washout (days 2 - 7)
STARTED
|
8
|
8
|
|
Washout (days 2 - 7)
COMPLETED
|
8
|
8
|
|
Washout (days 2 - 7)
NOT COMPLETED
|
0
|
0
|
|
Second Intervention (day 8)
STARTED
|
8
|
8
|
|
Second Intervention (day 8)
COMPLETED
|
8
|
8
|
|
Second Intervention (day 8)
NOT COMPLETED
|
0
|
0
|
Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
A Comparison of the Pharmacokinetic Properties of ARN-75039 Tablets With Excipients to Neat ARN-75039 in Hydroxypropyl Methylcellulose (HPMC) Capsules in Healthy Adult Participants Under Fed Conditions
Baseline characteristics by cohort
| Measure |
All Participants
n=16 Participants
All 16 randomized participants completed both periods of this two-period, two-sequence crossover study. Baseline characteristics represent assessments obtained prior to Period 1 dosing, and therefore apply to the entire cohort (N = 16). Baseline demographic values must not be interpreted as per-arm or per-period counts.
|
|---|---|
|
Age, Continuous
|
37.7 years
STANDARD_DEVIATION 5.96 • n=14 Participants
|
|
Sex: Female, Male
Female
|
7 Participants
n=14 Participants
|
|
Sex: Female, Male
Male
|
9 Participants
n=14 Participants
|
|
Race (NIH/OMB)
American Indian or Alaska Native
|
0 Participants
n=14 Participants
|
|
Race (NIH/OMB)
Asian
|
0 Participants
n=14 Participants
|
|
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
|
0 Participants
n=14 Participants
|
|
Race (NIH/OMB)
Black or African American
|
7 Participants
n=14 Participants
|
|
Race (NIH/OMB)
White
|
9 Participants
n=14 Participants
|
|
Race (NIH/OMB)
More than one race
|
0 Participants
n=14 Participants
|
|
Race (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=14 Participants
|
|
Ethnicity (NIH/OMB)
Hispanic or Latino
|
12 Participants
n=14 Participants
|
|
Ethnicity (NIH/OMB)
Not Hispanic or Latino
|
4 Participants
n=14 Participants
|
|
Ethnicity (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=14 Participants
|
|
Weight
|
74.1 kg
STANDARD_DEVIATION 9.96 • n=14 Participants
|
|
Height
|
167.8 cm
STANDARD_DEVIATION 7.48 • n=14 Participants
|
|
Body Mass Index (BMI)
|
26.4 kg/m^2
STANDARD_DEVIATION 3.61 • n=14 Participants
|
PRIMARY outcome
Timeframe: From time zero (dose) to time of last quantifiable concentration. Period 1: 0 to 144 hours; Period 2: 0 to 168 hours.Population: Safety/PK population included all participants who received at least 1 dose of ARN-75039.
Area Under the Plasma-drug Concentration Time Curve from time zero to time of last quantifiable concentration. Compare the pharmacokinetic (PK) properties of 300mg ARN-75039 with excipients in tablet form to 300mg neat ARN-75039 in HPMC capsules following oral administration under fed conditions.
Outcome measures
| Measure |
ARN-75039 Form A (HPMC Capsule)
n=16 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
ARN-75039 Form B (Tablet With Excipients)
n=16 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
|---|---|---|
|
AUC0-t
|
9450 h*ng/ml
Standard Deviation 3230
|
8990 h*ng/ml
Standard Deviation 3060
|
PRIMARY outcome
Timeframe: From time zero (dose) to 24 hours post-dose.Population: Safety/PK population included all participants who received at least 1 dose of ARN-75039.
Area under the plasma concentration-time curve from time zero to 24 hours post-dose. Compare the pharmacokinetic (PK) properties of 300mg ARN-75039 with excipients in tablet form to 300mg neat ARN-75039 in HPMC capsules following oral administration under fed conditions.
Outcome measures
| Measure |
ARN-75039 Form A (HPMC Capsule)
n=16 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
ARN-75039 Form B (Tablet With Excipients)
n=16 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
|---|---|---|
|
AUC0-24
|
6150 h*ng/ml
Standard Deviation 2120
|
5820 h*ng/ml
Standard Deviation 1980
|
PRIMARY outcome
Timeframe: From time zero (dose) extrapolated to infinity. Time frame is from 0 to Tlast + extrapolation from C last to infinity time, where concentration is equal to 0.Population: Safety/PK population included all participants who received at least 1 dose of ARN-75039.
Area under plasma concentration-time curve from time zero to infinity. Compare the pharmacokinetic (PK) properties of 300mg ARN-75039 with excipients in tablet form to 300mg neat ARN-75039 in HPMC capsules following oral administration under fed conditions.
Outcome measures
| Measure |
ARN-75039 Form A (HPMC Capsule)
n=4 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
ARN-75039 Form B (Tablet With Excipients)
n=7 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
|---|---|---|
|
AUC0-∞
|
11800 h*ng/ml
Standard Deviation 2570
|
9700 h*ng/ml
Standard Deviation 2770
|
PRIMARY outcome
Timeframe: From time 0 (dose) through 168 hours post-dose.Population: Safety/PK population included all participants who received at least 1 dose of ARN-75039.
Maximum observed plasma concentration. Compare the pharmacokinetic (PK) properties of 300mg ARN-75039 with excipients in tablet form to 300mg neat ARN-75039 in HPMC capsules following oral administration under fed conditions.
Outcome measures
| Measure |
ARN-75039 Form A (HPMC Capsule)
n=16 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
ARN-75039 Form B (Tablet With Excipients)
n=16 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
|---|---|---|
|
Cmax
|
847 ng/ml
Standard Deviation 266
|
828 ng/ml
Standard Deviation 226
|
PRIMARY outcome
Timeframe: From time 0 (dose) through 168 hours post-dose.Population: Safety/PK population included all participants who received at least 1 dose of ARN-75039.
Time to reach Cmax
Outcome measures
| Measure |
ARN-75039 Form A (HPMC Capsule)
n=16 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
ARN-75039 Form B (Tablet With Excipients)
n=16 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
|---|---|---|
|
Tmax
|
4 h
Full Range 2-6 • Interval 2.0 to 6.0
|
3.5 h
Full Range 2-4.1 • Interval 2.0 to 4.1
|
PRIMARY outcome
Timeframe: From time 0 (dose) through 168 hours post-dose (terminal elimination phase).Population: Safety/PK population included all participants who received at least 1 dose of ARN-75039.
Half-life
Outcome measures
| Measure |
ARN-75039 Form A (HPMC Capsule)
n=11 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
ARN-75039 Form B (Tablet With Excipients)
n=11 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
|---|---|---|
|
t1/2
|
141 h
Standard Deviation 52.4
|
120 h
Standard Deviation 49.1
|
PRIMARY outcome
Timeframe: From time 0 (dose) through 168 hours post-dose (derived from the concentration-time profile).Population: Safety/PK population included all participants who received at least 1 dose of ARN-75039.
Apparent clearance after extravascular administration.
Outcome measures
| Measure |
ARN-75039 Form A (HPMC Capsule)
n=4 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
ARN-75039 Form B (Tablet With Excipients)
n=7 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
|---|---|---|
|
CL/F
|
26.4 L/h
Standard Deviation 5.99
|
35 L/h
Standard Deviation 17.1
|
PRIMARY outcome
Timeframe: From time 0 (dose) through 168 hours post-dose (derived from the concentration-time profile).Population: Safety/PK population included all participants who received at least 1 dose of ARN-75039.
Apparent volume of distribution during the terminal phase after extravascular administration.
Outcome measures
| Measure |
ARN-75039 Form A (HPMC Capsule)
n=4 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
ARN-75039 Form B (Tablet With Excipients)
n=7 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
|---|---|---|
|
Vz/F
|
3820 L
Standard Deviation 1290
|
4810 L
Standard Deviation 2270
|
SECONDARY outcome
Timeframe: From first dose through approximately 7 days after the last dose (includes washout); with Day 36 follow-up phone call to assess for any adverse events (AEs).Population: From first dose through approximately 7 days after the last dose (includes washout); with Day 36 follow-up phone call to assess for any AEs.
Type and frequency of treatment-emergent adverse events (TEAEs).
Outcome measures
| Measure |
ARN-75039 Form A (HPMC Capsule)
n=16 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
ARN-75039 Form B (Tablet With Excipients)
n=16 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
|---|---|---|
|
Participants With ≥1 TEAE
|
0 Participant count
|
3 Participant count
|
SECONDARY outcome
Timeframe: From first dose through approximately 7 days after the last dose (includes washout); with Day 36 follow-up phone call to assess for any adverse events (AEs).Population: From first dose through approximately 7 days after the last dose (includes washout); with Day 36 follow-up phone call to assess for any AEs.
Type and frequency of treatment-emergent serious adverse events (TESAEs).
Outcome measures
| Measure |
ARN-75039 Form A (HPMC Capsule)
n=16 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
ARN-75039 Form B (Tablet With Excipients)
n=16 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
|---|---|---|
|
Participants With ≥1 TESAE
|
0 Participant count
|
0 Participant count
|
SECONDARY outcome
Timeframe: From first dose through approximately 7 days after the last dose (includes washout); with Day 36 follow-up phone call to assess for any adverse events (AEs).Population: From first dose through approximately 7 days after the last dose (includes washout); with Day 36 follow-up phone call to assess for any AEs.
Type and frequency of study drug-related \>Grade 1 TEAEs
Outcome measures
| Measure |
ARN-75039 Form A (HPMC Capsule)
n=16 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
ARN-75039 Form B (Tablet With Excipients)
n=16 Participants
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
|---|---|---|
|
Participants With Study Drug-related TEAEs of Grade >1
|
0 Participant count
|
0 Participant count
|
Adverse Events
ARN-75039 Form A (HPMC Capsule)
Serious events: 0 serious events
Other events: 0 other events
Deaths: 0 deaths
ARN-75039 Form B (Tablet With Excipients)
Serious events: 0 serious events
Other events: 3 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
ARN-75039 Form A (HPMC Capsule)
n=16 participants at risk
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
ARN-75039 Form B (Tablet With Excipients)
n=16 participants at risk
This was a 2-period, randomized cross-over study with two sequences (A→B and B→A) separated by a 7-day washout. Results are presented per intervention (Form A vs Form B) aggregating all participants exposed to each intervention. For safety, AEs are attributed to the treatment received at AE onset; AEs occurring during washout are attributed to the prior treatment.
|
|---|---|---|
|
Cardiac disorders
Sinus tachycardia
|
0.00%
0/16 • From first dose through approximately 7 days after the last dose (includes washout); with Day 36 follow-up phone call to assess for any adverse events (AEs)
AEs were collected from informed consent through approximately 7 days after the last study drug administration (including washout). TEAEs are those with onset on/after first dose through \~7 days after last dose; events during washout are attributed to the prior treatment. Participants were contacted on Day 36 for AE follow-up.
|
6.2%
1/16 • From first dose through approximately 7 days after the last dose (includes washout); with Day 36 follow-up phone call to assess for any adverse events (AEs)
AEs were collected from informed consent through approximately 7 days after the last study drug administration (including washout). TEAEs are those with onset on/after first dose through \~7 days after last dose; events during washout are attributed to the prior treatment. Participants were contacted on Day 36 for AE follow-up.
|
|
Nervous system disorders
Headache
|
0.00%
0/16 • From first dose through approximately 7 days after the last dose (includes washout); with Day 36 follow-up phone call to assess for any adverse events (AEs)
AEs were collected from informed consent through approximately 7 days after the last study drug administration (including washout). TEAEs are those with onset on/after first dose through \~7 days after last dose; events during washout are attributed to the prior treatment. Participants were contacted on Day 36 for AE follow-up.
|
6.2%
1/16 • From first dose through approximately 7 days after the last dose (includes washout); with Day 36 follow-up phone call to assess for any adverse events (AEs)
AEs were collected from informed consent through approximately 7 days after the last study drug administration (including washout). TEAEs are those with onset on/after first dose through \~7 days after last dose; events during washout are attributed to the prior treatment. Participants were contacted on Day 36 for AE follow-up.
|
|
Skin and subcutaneous tissue disorders
Rash macular
|
0.00%
0/16 • From first dose through approximately 7 days after the last dose (includes washout); with Day 36 follow-up phone call to assess for any adverse events (AEs)
AEs were collected from informed consent through approximately 7 days after the last study drug administration (including washout). TEAEs are those with onset on/after first dose through \~7 days after last dose; events during washout are attributed to the prior treatment. Participants were contacted on Day 36 for AE follow-up.
|
6.2%
1/16 • From first dose through approximately 7 days after the last dose (includes washout); with Day 36 follow-up phone call to assess for any adverse events (AEs)
AEs were collected from informed consent through approximately 7 days after the last study drug administration (including washout). TEAEs are those with onset on/after first dose through \~7 days after last dose; events during washout are attributed to the prior treatment. Participants were contacted on Day 36 for AE follow-up.
|
Additional Information
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place