Trial Outcomes & Findings for A Study Comparing Two Formulations of Selpercatinib (LY3527723) in Healthy Participants (NCT NCT05089019)
NCT ID: NCT05089019
Last Updated: 2025-03-17
Results Overview
PK: Cmax of Selpercatinib
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
224 participants
Primary outcome timeframe
Day 1 and Day 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 192, 240, and 312 hours (h) postdose;
Results posted on
2025-03-17
Participant Flow
This study included a washout period of 14 days between doses of selpercatinib.
Participant milestones
| Measure |
Sequence 1 - Selpercatinib Reference/Test
Sequence 1: 160 mg selpercatinib (2 x 80 mg capsules) in Period 1, 160 mg selpercatinib (1 x 160 mg tablet) in Period 2.
|
Sequence 2 - Selpercatinib Test/Reference
Sequence 2: 160 mg selpercatinib (1 x 160 mg tablet) in Period 1, 160 mg Selpercatinib (2 x 80 mg capsules) in Period 2.
|
|---|---|---|
|
Period 1
STARTED
|
112
|
112
|
|
Period 1
Received at Least One Dose of Study Drug
|
112
|
112
|
|
Period 1
COMPLETED
|
112
|
111
|
|
Period 1
NOT COMPLETED
|
0
|
1
|
|
Washout Period
STARTED
|
112
|
111
|
|
Washout Period
COMPLETED
|
100
|
104
|
|
Washout Period
NOT COMPLETED
|
12
|
7
|
|
Period 2
STARTED
|
100
|
104
|
|
Period 2
Received at Least One Dose of Study Drug
|
100
|
104
|
|
Period 2
COMPLETED
|
95
|
101
|
|
Period 2
NOT COMPLETED
|
5
|
3
|
Reasons for withdrawal
| Measure |
Sequence 1 - Selpercatinib Reference/Test
Sequence 1: 160 mg selpercatinib (2 x 80 mg capsules) in Period 1, 160 mg selpercatinib (1 x 160 mg tablet) in Period 2.
|
Sequence 2 - Selpercatinib Test/Reference
Sequence 2: 160 mg selpercatinib (1 x 160 mg tablet) in Period 1, 160 mg Selpercatinib (2 x 80 mg capsules) in Period 2.
|
|---|---|---|
|
Period 1
Withdrawal by Subject
|
0
|
1
|
|
Washout Period
Adverse Event
|
3
|
4
|
|
Washout Period
Lost to Follow-up
|
1
|
0
|
|
Washout Period
Physician Decision
|
2
|
0
|
|
Washout Period
Withdrawal by Subject
|
6
|
3
|
|
Period 2
Adverse Event
|
4
|
2
|
|
Period 2
Lost to Follow-up
|
1
|
0
|
|
Period 2
Withdrawal by Subject
|
0
|
1
|
Baseline Characteristics
A Study Comparing Two Formulations of Selpercatinib (LY3527723) in Healthy Participants
Baseline characteristics by cohort
| Measure |
Sequence 1 - Selpercatinib Reference/Test
n=112 Participants
Sequence 1: 160 mg selpercatinib (2 x 80 mg capsules) Reference/160 mg selpercatinib (1 x 160 mg tablet) Test
|
Sequence 2: Selpercatinib Test/Reference
n=112 Participants
Sequence 2: 160 mg selpercatinib (1 x 160 mg tablet) Test/160 mg selpercatinib (2 x 80 mg capsules) Reference
|
Total
n=224 Participants
Total of all reporting groups
|
|---|---|---|---|
|
Age, Continuous
|
42.1 years
STANDARD_DEVIATION 12.3 • n=5 Participants
|
42.8 years
STANDARD_DEVIATION 12.4 • n=7 Participants
|
42.5 years
STANDARD_DEVIATION 12.3 • n=5 Participants
|
|
Sex: Female, Male
Female
|
53 Participants
n=5 Participants
|
53 Participants
n=7 Participants
|
106 Participants
n=5 Participants
|
|
Sex: Female, Male
Male
|
59 Participants
n=5 Participants
|
59 Participants
n=7 Participants
|
118 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Hispanic or Latino
|
35 Participants
n=5 Participants
|
36 Participants
n=7 Participants
|
71 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Not Hispanic or Latino
|
77 Participants
n=5 Participants
|
76 Participants
n=7 Participants
|
153 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
American Indian or Alaska Native
|
0 Participants
n=5 Participants
|
1 Participants
n=7 Participants
|
1 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Asian
|
6 Participants
n=5 Participants
|
4 Participants
n=7 Participants
|
10 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
|
1 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
1 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Black or African American
|
45 Participants
n=5 Participants
|
37 Participants
n=7 Participants
|
82 Participants
n=5 Participants
|
|
Race (NIH/OMB)
White
|
59 Participants
n=5 Participants
|
67 Participants
n=7 Participants
|
126 Participants
n=5 Participants
|
|
Race (NIH/OMB)
More than one race
|
1 Participants
n=5 Participants
|
3 Participants
n=7 Participants
|
4 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
|
Region of Enrollment
United States
|
112 participants
n=5 Participants
|
112 participants
n=7 Participants
|
224 participants
n=5 Participants
|
PRIMARY outcome
Timeframe: Day 1 and Day 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 192, 240, and 312 hours (h) postdose;Population: All participants who received at least 1 dose of Selpercatinib and have evaluable PK data.
PK: Cmax of Selpercatinib
Outcome measures
| Measure |
160 mg Selpercatinib (Reference)
n=209 Participants
160 milligram (mg) Selpercatinib (2 x 80 mg capsules) administered orally on Day 1 or Day 15 according to the randomization schedule.
|
160 mg Selpercatinib (Test)
n=206 Participants
160 mg Selpercatinib (tablet) administered orally according to the randomization schedule.
|
|---|---|---|
|
Pharmacokinetics (PK): Maximum Concentration (Cmax) of Selpercatinib
|
1520 nanograms per milliliter (ng/mL)
Geometric Coefficient of Variation 61
|
1350 nanograms per milliliter (ng/mL)
Geometric Coefficient of Variation 91
|
PRIMARY outcome
Timeframe: Day 1 and Day 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 192, 240, and 312 hours (h) postdose;Population: All participants who received at least one dose of selpercatinib and had evaluable PK data.
PK: AUC\[0-∞\] of Selpercatinib.
Outcome measures
| Measure |
160 mg Selpercatinib (Reference)
n=206 Participants
160 milligram (mg) Selpercatinib (2 x 80 mg capsules) administered orally on Day 1 or Day 15 according to the randomization schedule.
|
160 mg Selpercatinib (Test)
n=200 Participants
160 mg Selpercatinib (tablet) administered orally according to the randomization schedule.
|
|---|---|---|
|
PK: Area Under the Plasma Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Selpercatinib
|
20700 nanograms*hour per milliliter (ng*hr/mL)
Geometric Coefficient of Variation 45
|
19300 nanograms*hour per milliliter (ng*hr/mL)
Geometric Coefficient of Variation 51
|
PRIMARY outcome
Timeframe: Day 1 and Day 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 192, 240, and 312 hours (h) postdose;Population: All participants who received at least one dose of selpercatinib and had evaluable PK data.
PK: AUC\[0-tlast\] of Selpercatinib
Outcome measures
| Measure |
160 mg Selpercatinib (Reference)
n=206 Participants
160 milligram (mg) Selpercatinib (2 x 80 mg capsules) administered orally on Day 1 or Day 15 according to the randomization schedule.
|
160 mg Selpercatinib (Test)
n=204 Participants
160 mg Selpercatinib (tablet) administered orally according to the randomization schedule.
|
|---|---|---|
|
Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Measured Concentration Value (AUC[0-tlast]) of Selpercatinib
|
20200 ng*hr/mL
Geometric Coefficient of Variation 47
|
18100 ng*hr/mL
Geometric Coefficient of Variation 65
|
Adverse Events
160 mg Selpercatinib (2 x 80 mg Reference)
Serious events: 0 serious events
Other events: 0 other events
Deaths: 0 deaths
160 mg Selpercatinib (1 x 160 mg Test)
Serious events: 0 serious events
Other events: 0 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
Adverse event data not reported
Additional Information
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place
Restriction type: GT60