Trial Outcomes & Findings for A Relative Bioavailability Study of Selpercatinib (LY3527723) in Healthy Participants (NCT NCT05136404)
NCT ID: NCT05136404
Last Updated: 2025-03-17
Results Overview
PK: Cmax of Selpercatinib
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
42 participants
Primary outcome timeframe
Days 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours (h) postdose
Results posted on
2025-03-17
Participant Flow
Participant milestones
| Measure |
Selpercatinib Sequence A:
Period 1: 20 milligram (mg) Selpercatinib capsule single oral dose administered orally on Day 1.
Period 2: 20 mg per milliliter (mL) Selpercatinib Powder for Oral suspension (PFOS) single oral suspension dose on Day 8.
Period 3: 20 mg/mL Selpercatinib Ready to Use (RTU) single oral suspension on Day 15.
Selpercatinib: Administered orally
|
Selpercatinib Sequence B
Period 1: 20 mg/mL Selpercatinib RTU single oral suspension on Day 1.
Period 2: 20 mg Selpercatinib capsule single oral dose administered orally on Day 8.
Period 3: 20 mg/mL PFOS single oral suspension dose on Day 15.
Selpercatinib: Administered orally
|
Selpercatinib Sequence C
Period 1: 20 mg/mL PFOS single oral suspension dose on Day 1.
Period 2: 20 mg/mL Selpercatinib RTU single oral suspension on Day 8.
Period 3: 20 mg Selpercatinib capsule single oral dose administered orally on Day 15.
Selpercatinib: Administered orally
|
|---|---|---|---|
|
Period 1
STARTED
|
14
|
14
|
14
|
|
Period 1
Received atLeast One Dose of Study Drug
|
14
|
14
|
14
|
|
Period 1
COMPLETED
|
14
|
13
|
13
|
|
Period 1
NOT COMPLETED
|
0
|
1
|
1
|
|
Period 2
STARTED
|
14
|
13
|
13
|
|
Period 2
COMPLETED
|
14
|
13
|
12
|
|
Period 2
NOT COMPLETED
|
0
|
0
|
1
|
|
Period 3
STARTED
|
14
|
13
|
12
|
|
Period 3
COMPLETED
|
14
|
13
|
11
|
|
Period 3
NOT COMPLETED
|
0
|
0
|
1
|
Reasons for withdrawal
| Measure |
Selpercatinib Sequence A:
Period 1: 20 milligram (mg) Selpercatinib capsule single oral dose administered orally on Day 1.
Period 2: 20 mg per milliliter (mL) Selpercatinib Powder for Oral suspension (PFOS) single oral suspension dose on Day 8.
Period 3: 20 mg/mL Selpercatinib Ready to Use (RTU) single oral suspension on Day 15.
Selpercatinib: Administered orally
|
Selpercatinib Sequence B
Period 1: 20 mg/mL Selpercatinib RTU single oral suspension on Day 1.
Period 2: 20 mg Selpercatinib capsule single oral dose administered orally on Day 8.
Period 3: 20 mg/mL PFOS single oral suspension dose on Day 15.
Selpercatinib: Administered orally
|
Selpercatinib Sequence C
Period 1: 20 mg/mL PFOS single oral suspension dose on Day 1.
Period 2: 20 mg/mL Selpercatinib RTU single oral suspension on Day 8.
Period 3: 20 mg Selpercatinib capsule single oral dose administered orally on Day 15.
Selpercatinib: Administered orally
|
|---|---|---|---|
|
Period 1
Adverse Event
|
0
|
1
|
1
|
|
Period 2
Inappropriate Behavior
|
0
|
0
|
1
|
|
Period 3
Adverse Event
|
0
|
0
|
1
|
Baseline Characteristics
A Relative Bioavailability Study of Selpercatinib (LY3527723) in Healthy Participants
Baseline characteristics by cohort
| Measure |
20 mg Selpercatinib
n=42 Participants
Participants were randomized to 1 of 3 treatment sequences and will receive single doses of 20 mg Selpercatinib on each of Days 1, 8, and 15 as either the RTU suspension, the PFOS, or the capsule.
Sequence A: Period 1: 20 milligram (mg) Selpercatinib capsule single oral dose administered orally on Day 1. Period 2: 20 mg per milliliter (mL) Selpercatinib Powder for Oral suspension (PFOS) single oral suspension dose on Day 8. Period 3: 20 mg/mL Selpercatinib Ready to Use (RTU) single oral suspension on Day 15.
Sequence B: Period 1: 20 mg/mL Selpercatinib RTU single oral suspension on Day 1. Period 2: 20 mg Selpercatinib capsule single oral dose administered orally on Day 8. Period 3: 20 mg/mL PFOS single oral suspension dose on Day 15.
Sequence C: Period 1: 20 mg/mL PFOS single oral suspension dose on Day 1. Period 2: 20 mg/mL Selpercatinib RTU single oral suspension on Day 8. Period 3: 20 mg Selpercatinib capsule single oral dose administered orally on Day 15.
|
|---|---|
|
Age, Continuous
|
42.0 years
STANDARD_DEVIATION 9.7 • n=5 Participants
|
|
Sex: Female, Male
Female
|
13 Participants
n=5 Participants
|
|
Sex: Female, Male
Male
|
29 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Hispanic or Latino
|
20 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Not Hispanic or Latino
|
22 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
American Indian or Alaska Native
|
1 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Asian
|
1 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Black or African American
|
11 Participants
n=5 Participants
|
|
Race (NIH/OMB)
White
|
29 Participants
n=5 Participants
|
|
Race (NIH/OMB)
More than one race
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=5 Participants
|
|
Region of Enrollment
United States
|
42 Participants
n=5 Participants
|
PRIMARY outcome
Timeframe: Days 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours (h) postdosePopulation: All participants who received at least one dose of Selpercatinib and have evaluable pharmacokinetic (PK) data.
PK: Cmax of Selpercatinib
Outcome measures
| Measure |
20 mg Selpercatinib Capsule (Reference)
n=38 Participants
20 mg Selpercatinib capsule administered orally.
|
20 mg Selpercatinib RTU Suspension (Test)
n=41 Participants
20 mg/mL Selpercatinib RTU administered orally.
|
20 mg/mL PFOS (Test)
n=41 Participants
20 mg/mL PFOS administered orally.
|
|---|---|---|---|
|
Pharmacokinetics (PK): Maximum Concentration (Cmax) of Selpercatinib
|
176 nanograms per milliliter (ng/mL)
Geometric Coefficient of Variation 64.2
|
174 nanograms per milliliter (ng/mL)
Geometric Coefficient of Variation 36.9
|
180 nanograms per milliliter (ng/mL)
Geometric Coefficient of Variation 39.8
|
PRIMARY outcome
Timeframe: Days 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 h postdosePopulation: All participants who received at least one dose of selpercatinib and have evaluable PK data.
PK AUC\[0-∞\] of Selpercatinib
Outcome measures
| Measure |
20 mg Selpercatinib Capsule (Reference)
n=36 Participants
20 mg Selpercatinib capsule administered orally.
|
20 mg Selpercatinib RTU Suspension (Test)
n=41 Participants
20 mg/mL Selpercatinib RTU administered orally.
|
20 mg/mL PFOS (Test)
n=40 Participants
20 mg/mL PFOS administered orally.
|
|---|---|---|---|
|
PK: Area Under the Plasma Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Selpercatinib
|
2540 nanogram*hour per milliliter (ng*hr/mL)
Geometric Coefficient of Variation 28.0
|
2410 nanogram*hour per milliliter (ng*hr/mL)
Geometric Coefficient of Variation 29.0
|
2490 nanogram*hour per milliliter (ng*hr/mL)
Geometric Coefficient of Variation 27.0
|
PRIMARY outcome
Timeframe: Days 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 h postdosePopulation: All participants who received at least one dose of study drug and had evaluable PK data.
PK: AUC\[0-tlast\] of Selpercatinib
Outcome measures
| Measure |
20 mg Selpercatinib Capsule (Reference)
n=38 Participants
20 mg Selpercatinib capsule administered orally.
|
20 mg Selpercatinib RTU Suspension (Test)
n=41 Participants
20 mg/mL Selpercatinib RTU administered orally.
|
20 mg/mL PFOS (Test)
n=41 Participants
20 mg/mL PFOS administered orally.
|
|---|---|---|---|
|
PK: Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Measured Concentration Value (AUC[0-tlast]) of Selpercatinib
|
2180 ng*hr/mL
Geometric Coefficient of Variation 36.9
|
2160 ng*hr/mL
Geometric Coefficient of Variation 31.6
|
2190 ng*hr/mL
Geometric Coefficient of Variation 30.8
|
PRIMARY outcome
Timeframe: Days 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 h postdosePopulation: All participants who received at least one dose of study drug and had evaluable PK data.
PK: Tmax of Selpercatinib
Outcome measures
| Measure |
20 mg Selpercatinib Capsule (Reference)
n=38 Participants
20 mg Selpercatinib capsule administered orally.
|
20 mg Selpercatinib RTU Suspension (Test)
n=41 Participants
20 mg/mL Selpercatinib RTU administered orally.
|
20 mg/mL PFOS (Test)
n=41 Participants
20 mg/mL PFOS administered orally.
|
|---|---|---|---|
|
PK: Time to Maximum Observed Concentration (Tmax) of Selpercatinib
|
1.50 h
Interval 1.0 to 24.02
|
1.50 h
Interval 1.0 to 3.0
|
1.50 h
Interval 1.0 to 3.5
|
Adverse Events
Selpercatinib Sequence A:
Serious events: 0 serious events
Other events: 0 other events
Deaths: 0 deaths
Selpercatinib Sequence B:
Serious events: 0 serious events
Other events: 0 other events
Deaths: 0 deaths
Selpercatinib Sequence C:
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