Trial Outcomes & Findings for A Study of Effect of Food and a Proton Pump Inhibitor on Selpercatinib (LY3527723) in Healthy Participants (NCT NCT05468164)
NCT ID: NCT05468164
Last Updated: 2025-09-19
Results Overview
PK: AUC0-t of Selpercatinib was reported.
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
20 participants
Primary outcome timeframe
Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.
Results posted on
2025-09-19
Participant Flow
A total of 20 participants were enrolled in this study. Participants were randomly assigned to 1 of 4 treatment sequences (ABCD, ABDC, BACD, and BADC). Treatment A was a single oral dose of 160 milligrams (mg) selpercatinib under fasting condition, Treatment B was a single oral dose of 160 mg selpercatinib under fed condition, (contd.)
(contd.) Treatment C was multiple daily oral doses of 40 mg omeprazole with a single oral dose of 160 mg selpercatinib co-administered under fasting conditions, and Treatment D was multiple daily oral doses of 40 mg omeprazole with 160 mg selpercatinib co-administered under fed condition.
Participant milestones
| Measure |
Treatment Sequence 1: ABCD
Participants received:
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 1 in fasted state.
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 2 in fed state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 3 in fasted state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 4 in fed state.
Periods 1 and 2, 2 and 3 were separated by a 7-day washout period. There was no washout between Periods 3 and 4.
|
Treatment Sequence 2: ABDC
Participants received:
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 1 in fasted state.
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 2 in fed state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 3 in fed state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 4 in fasted state.
Periods 1 and 2, 2 and 3 were separated by a 7-day washout period. There was no washout between Periods 3 and 4.
|
Treatment Sequence 3: BACD
Participants received:
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 1 in fed state.
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 2 in fasted state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 3 in fasted state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 4 in fed state.
Periods 1 and 2, 2 and 3 were separated by a 7-day washout period. There was no washout between Periods 3 and 4.
|
Treatment Sequence 3: BADC
Participants received:
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 1 in fed state.
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 2 in fasted state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 3 in fed state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 4 in fasted state.
Periods 1 and 2, 2 and 3 were separated by a 7-day washout period. There was no washout between Periods 3 and 4.
|
|---|---|---|---|---|
|
Treatment Period 1
STARTED
|
5
|
5
|
5
|
5
|
|
Treatment Period 1
Received At Least 1 Dose of Study Drug
|
5
|
5
|
5
|
5
|
|
Treatment Period 1
COMPLETED
|
5
|
5
|
5
|
5
|
|
Treatment Period 1
NOT COMPLETED
|
0
|
0
|
0
|
0
|
|
Treatment Period 2
STARTED
|
5
|
5
|
5
|
5
|
|
Treatment Period 2
Received At Least 1 Dose of Study Drug
|
5
|
5
|
5
|
5
|
|
Treatment Period 2
COMPLETED
|
5
|
5
|
5
|
5
|
|
Treatment Period 2
NOT COMPLETED
|
0
|
0
|
0
|
0
|
|
Treatment Period 3
STARTED
|
5
|
5
|
5
|
5
|
|
Treatment Period 3
Received At Least 1 Dose of Study Drug
|
5
|
5
|
5
|
5
|
|
Treatment Period 3
COMPLETED
|
5
|
5
|
5
|
5
|
|
Treatment Period 3
NOT COMPLETED
|
0
|
0
|
0
|
0
|
|
Treatment Period 4
STARTED
|
5
|
5
|
5
|
5
|
|
Treatment Period 4
Received At Least 1 Dose of Study Drug
|
5
|
5
|
5
|
4
|
|
Treatment Period 4
COMPLETED
|
5
|
5
|
5
|
4
|
|
Treatment Period 4
NOT COMPLETED
|
0
|
0
|
0
|
1
|
Reasons for withdrawal
| Measure |
Treatment Sequence 1: ABCD
Participants received:
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 1 in fasted state.
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 2 in fed state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 3 in fasted state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 4 in fed state.
Periods 1 and 2, 2 and 3 were separated by a 7-day washout period. There was no washout between Periods 3 and 4.
|
Treatment Sequence 2: ABDC
Participants received:
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 1 in fasted state.
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 2 in fed state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 3 in fed state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 4 in fasted state.
Periods 1 and 2, 2 and 3 were separated by a 7-day washout period. There was no washout between Periods 3 and 4.
|
Treatment Sequence 3: BACD
Participants received:
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 1 in fed state.
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 2 in fasted state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 3 in fasted state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 4 in fed state.
Periods 1 and 2, 2 and 3 were separated by a 7-day washout period. There was no washout between Periods 3 and 4.
|
Treatment Sequence 3: BADC
Participants received:
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 1 in fed state.
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 2 in fasted state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 3 in fed state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 4 in fasted state.
Periods 1 and 2, 2 and 3 were separated by a 7-day washout period. There was no washout between Periods 3 and 4.
|
|---|---|---|---|---|
|
Treatment Period 4
Adverse Event
|
0
|
0
|
0
|
1
|
Baseline Characteristics
A Study of Effect of Food and a Proton Pump Inhibitor on Selpercatinib (LY3527723) in Healthy Participants
Baseline characteristics by cohort
| Measure |
Treatment Sequence 1: ABCD
n=5 Participants
Participants received:
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 1 in fasted state.
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 2 in fed state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 3 in fasted state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 4 in fed state.
Periods 1 and 2, 2 and 3 were separated by a 7-day washout period. There was no washout between Periods 3 and 4.
|
Treatment Sequence 2: ABDC
n=5 Participants
Participants received:
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 1 in fasted state.
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 2 in fed state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 3 in fed state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 4 in fasted state.
Periods 1 and 2, 2 and 3 were separated by a 7-day washout period. There was no washout between Periods 3 and 4.
|
Treatment Sequence 3: BACD
n=5 Participants
Participants received:
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 1 in fed state.
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 2 in fasted state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 3 in fasted state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 4 in fed state.
Periods 1 and 2, 2 and 3 were separated by a 7-day washout period. There was no washout between Periods 3 and 4.
|
Treatment Sequence 3: BADC
n=5 Participants
Participants received:
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 1 in fed state.
* Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 2 in fasted state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 3 in fed state.
* Multiple daily oral doses of 40 mg omeprazole administered from Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 4 in fasted state.
Periods 1 and 2, 2 and 3 were separated by a 7-day washout period. There was no washout between Periods 3 and 4.
|
Total
n=20 Participants
Total of all reporting groups
|
|---|---|---|---|---|---|
|
Age, Continuous
|
45.0 years
STANDARD_DEVIATION 6.82 • n=5 Participants
|
38.2 years
STANDARD_DEVIATION 6.50 • n=7 Participants
|
41.8 years
STANDARD_DEVIATION 10.35 • n=5 Participants
|
38.4 years
STANDARD_DEVIATION 7.44 • n=4 Participants
|
40.9 years
STANDARD_DEVIATION 7.82 • n=21 Participants
|
|
Sex: Female, Male
Female
|
3 Participants
n=5 Participants
|
2 Participants
n=7 Participants
|
2 Participants
n=5 Participants
|
3 Participants
n=4 Participants
|
10 Participants
n=21 Participants
|
|
Sex: Female, Male
Male
|
2 Participants
n=5 Participants
|
3 Participants
n=7 Participants
|
3 Participants
n=5 Participants
|
2 Participants
n=4 Participants
|
10 Participants
n=21 Participants
|
|
Ethnicity (NIH/OMB)
Hispanic or Latino
|
5 Participants
n=5 Participants
|
4 Participants
n=7 Participants
|
5 Participants
n=5 Participants
|
5 Participants
n=4 Participants
|
19 Participants
n=21 Participants
|
|
Ethnicity (NIH/OMB)
Not Hispanic or Latino
|
0 Participants
n=5 Participants
|
1 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
1 Participants
n=21 Participants
|
|
Ethnicity (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
0 Participants
n=21 Participants
|
|
Race (NIH/OMB)
American Indian or Alaska Native
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
0 Participants
n=21 Participants
|
|
Race (NIH/OMB)
Asian
|
0 Participants
n=5 Participants
|
1 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
1 Participants
n=21 Participants
|
|
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
0 Participants
n=21 Participants
|
|
Race (NIH/OMB)
Black or African American
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
0 Participants
n=21 Participants
|
|
Race (NIH/OMB)
White
|
5 Participants
n=5 Participants
|
4 Participants
n=7 Participants
|
5 Participants
n=5 Participants
|
5 Participants
n=4 Participants
|
19 Participants
n=21 Participants
|
|
Race (NIH/OMB)
More than one race
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
0 Participants
n=21 Participants
|
|
Race (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
0 Participants
n=21 Participants
|
|
Region of Enrollment
United States
|
5 Participants
n=5 Participants
|
5 Participants
n=7 Participants
|
5 Participants
n=5 Participants
|
5 Participants
n=4 Participants
|
20 Participants
n=21 Participants
|
PRIMARY outcome
Timeframe: Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.Population: All participants who received at least one dose of study drug and had evaluable PK data.
PK: AUC0-t of Selpercatinib was reported.
Outcome measures
| Measure |
Treatment A: 160 mg Selpercatinib (Fasted)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib administered in a fasted state.
|
Treatment B: 160 mg Selpercatinib (Fed)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib administered in a fed state.
|
Treatment C: 160 mg Selpercatinib + 40 mg Omeprazole (Fasted)
n=19 Participants
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fasted state.
|
Treatment D: 160 mg Selpercatinib + 40 mg Omeprazole (Fed)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fed state.
|
|---|---|---|---|---|
|
Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib
|
26160 nanogram*hour per milliliter (ng*h/mL)
Geometric Coefficient of Variation 38.9
|
28400 nanogram*hour per milliliter (ng*h/mL)
Geometric Coefficient of Variation 20.4
|
7973 nanogram*hour per milliliter (ng*h/mL)
Geometric Coefficient of Variation 161.9
|
26570 nanogram*hour per milliliter (ng*h/mL)
Geometric Coefficient of Variation 14.1
|
PRIMARY outcome
Timeframe: Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.Population: All participants who received at least one dose of study drug and had evaluable PK data.
PK: AUC0-inf of Selpercatinib was reported.
Outcome measures
| Measure |
Treatment A: 160 mg Selpercatinib (Fasted)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib administered in a fasted state.
|
Treatment B: 160 mg Selpercatinib (Fed)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib administered in a fed state.
|
Treatment C: 160 mg Selpercatinib + 40 mg Omeprazole (Fasted)
n=19 Participants
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fasted state.
|
Treatment D: 160 mg Selpercatinib + 40 mg Omeprazole (Fed)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fed state.
|
|---|---|---|---|---|
|
PK: Area Under the Concentration-time Curve, From Time 0 Extrapolated to Infinity (AUC0-inf) of Selpercatinib
|
26280 ng*h/mL
Geometric Coefficient of Variation 38.9
|
28530 ng*h/mL
Geometric Coefficient of Variation 20.4
|
8256 ng*h/mL
Geometric Coefficient of Variation 143.3
|
26770 ng*h/mL
Geometric Coefficient of Variation 13.8
|
PRIMARY outcome
Timeframe: Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.Population: All participants who received at least one dose of study drug and had evaluable PK data.
PK: AUC%extrap of Selpercatinib was reported.
Outcome measures
| Measure |
Treatment A: 160 mg Selpercatinib (Fasted)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib administered in a fasted state.
|
Treatment B: 160 mg Selpercatinib (Fed)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib administered in a fed state.
|
Treatment C: 160 mg Selpercatinib + 40 mg Omeprazole (Fasted)
n=19 Participants
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fasted state.
|
Treatment D: 160 mg Selpercatinib + 40 mg Omeprazole (Fed)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fed state.
|
|---|---|---|---|---|
|
PK: Percent of AUC0-inf Extrapolated (AUC%Extrap) of Selpercatinib
|
0.4468 percentage of AUC0-inf extrapolated
Standard Deviation 0.14909
|
0.4541 percentage of AUC0-inf extrapolated
Standard Deviation 0.22000
|
3.065 percentage of AUC0-inf extrapolated
Standard Deviation 7.5841
|
0.7158 percentage of AUC0-inf extrapolated
Standard Deviation 0.46382
|
PRIMARY outcome
Timeframe: Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.Population: All participants who received at least one dose of study drug and had evaluable PK data.
PK: Cmax of Selpercatinib was reported.
Outcome measures
| Measure |
Treatment A: 160 mg Selpercatinib (Fasted)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib administered in a fasted state.
|
Treatment B: 160 mg Selpercatinib (Fed)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib administered in a fed state.
|
Treatment C: 160 mg Selpercatinib + 40 mg Omeprazole (Fasted)
n=19 Participants
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fasted state.
|
Treatment D: 160 mg Selpercatinib + 40 mg Omeprazole (Fed)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fed state.
|
|---|---|---|---|---|
|
PK: Maximum Observed Concentration (Cmax) of Selpercatinib
|
2024 nanograms per milliliter (ng/mL)
Geometric Coefficient of Variation 60.4
|
1745 nanograms per milliliter (ng/mL)
Geometric Coefficient of Variation 20.9
|
251.5 nanograms per milliliter (ng/mL)
Geometric Coefficient of Variation 263.9
|
1023 nanograms per milliliter (ng/mL)
Geometric Coefficient of Variation 24.7
|
PRIMARY outcome
Timeframe: Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.Population: All participants who received at least one dose of study drug and had evaluable PK data.
PK: Tmax of Selpercatinib was reported.
Outcome measures
| Measure |
Treatment A: 160 mg Selpercatinib (Fasted)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib administered in a fasted state.
|
Treatment B: 160 mg Selpercatinib (Fed)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib administered in a fed state.
|
Treatment C: 160 mg Selpercatinib + 40 mg Omeprazole (Fasted)
n=19 Participants
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fasted state.
|
Treatment D: 160 mg Selpercatinib + 40 mg Omeprazole (Fed)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fed state.
|
|---|---|---|---|---|
|
PK: Time to Reach Cmax (Tmax) of Selpercatinib
|
1.502 hours (h)
Interval 1.0 to 24.0
|
3.997 hours (h)
Interval 2.01 to 6.0
|
2.501 hours (h)
Interval 1.5 to 23.97
|
6.011 hours (h)
Interval 3.0 to 23.93
|
PRIMARY outcome
Timeframe: Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.Population: All participants who received at least one dose of study drug and had evaluable PK data.
PK: Kel of Selpercatinib was reported.
Outcome measures
| Measure |
Treatment A: 160 mg Selpercatinib (Fasted)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib administered in a fasted state.
|
Treatment B: 160 mg Selpercatinib (Fed)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib administered in a fed state.
|
Treatment C: 160 mg Selpercatinib + 40 mg Omeprazole (Fasted)
n=19 Participants
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fasted state.
|
Treatment D: 160 mg Selpercatinib + 40 mg Omeprazole (Fed)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fed state.
|
|---|---|---|---|---|
|
PK: Apparent First Order Terminal Elimination Rate Constant (Kel) of Selpercatinib
|
0.02445 1/hour
Standard Deviation 0.0058755
|
0.02282 1/hour
Standard Deviation 0.0047476
|
0.02207 1/hour
Standard Deviation 0.0095909
|
0.02214 1/hour
Standard Deviation 0.0077557
|
PRIMARY outcome
Timeframe: Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.Population: All participants who received at least one dose of study drug and had evaluable PK data.
PK: CL/F of Selpercatinib was reported.
Outcome measures
| Measure |
Treatment A: 160 mg Selpercatinib (Fasted)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib administered in a fasted state.
|
Treatment B: 160 mg Selpercatinib (Fed)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib administered in a fed state.
|
Treatment C: 160 mg Selpercatinib + 40 mg Omeprazole (Fasted)
n=19 Participants
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fasted state.
|
Treatment D: 160 mg Selpercatinib + 40 mg Omeprazole (Fed)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fed state.
|
|---|---|---|---|---|
|
PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Selpercatinib
|
6.585 Liters/hour
Standard Deviation 3.2392
|
5.717 Liters/hour
Standard Deviation 1.1560
|
50.45 Liters/hour
Standard Deviation 135.82
|
6.031 Liters/hour
Standard Deviation 0.81650
|
PRIMARY outcome
Timeframe: Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.Population: All participants who received at least one dose of study drug and had evaluable PK data.
PK: t½ of Selpercatinib was reported.
Outcome measures
| Measure |
Treatment A: 160 mg Selpercatinib (Fasted)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib administered in a fasted state.
|
Treatment B: 160 mg Selpercatinib (Fed)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib administered in a fed state.
|
Treatment C: 160 mg Selpercatinib + 40 mg Omeprazole (Fasted)
n=19 Participants
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fasted state.
|
Treatment D: 160 mg Selpercatinib + 40 mg Omeprazole (Fed)
n=20 Participants
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fed state.
|
|---|---|---|---|---|
|
PK: Apparent First-order Terminal Elimination Half-life (t½) of Selpercatinib
|
29.801 h
Standard Deviation 6.6155
|
31.641 h
Standard Deviation 6.5273
|
37.288 h
Standard Deviation 16.0167
|
35.841 h
Standard Deviation 14.7170
|
Adverse Events
Treatment A: 160 mg Selpercatinib (Fasted)
Serious events: 0 serious events
Other events: 3 other events
Deaths: 0 deaths
Treatment B: 160 mg Selpercatinib (Fed)
Serious events: 0 serious events
Other events: 6 other events
Deaths: 0 deaths
Treatment C: 160 mg Selpercatinib + 40 mg Omeprazole (Fasted)
Serious events: 0 serious events
Other events: 7 other events
Deaths: 0 deaths
Treatment D: 160 mg Selpercatinib + 40 mg Omeprazole (Fed)
Serious events: 0 serious events
Other events: 8 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Treatment A: 160 mg Selpercatinib (Fasted)
n=20 participants at risk
Participants received a single oral dose of 160 mg selpercatinib administered in a fasted state.
|
Treatment B: 160 mg Selpercatinib (Fed)
n=20 participants at risk
Participants received a single oral dose of 160 mg selpercatinib administered in a fed state.
|
Treatment C: 160 mg Selpercatinib + 40 mg Omeprazole (Fasted)
n=19 participants at risk
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fasted state.
|
Treatment D: 160 mg Selpercatinib + 40 mg Omeprazole (Fed)
n=20 participants at risk
Participants received a single oral dose of 160 mg selpercatinib along with multiple daily oral doses of 40 mg omeprazole administered in a fed state.
|
|---|---|---|---|---|
|
Gastrointestinal disorders
Abdominal discomfort
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/19 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
10.0%
2/20 • Number of events 5 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Gastrointestinal disorders
Abdominal pain lower
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.3%
1/19 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Gastrointestinal disorders
Abdominal pain upper
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.3%
1/19 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Gastrointestinal disorders
Dyspepsia
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
10.0%
2/20 • Number of events 2 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/19 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.0%
1/20 • Number of events 2 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Gastrointestinal disorders
Flatulence
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/19 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
10.0%
2/20 • Number of events 2 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Investigations
Alanine aminotransferase increased
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.3%
1/19 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.0%
1/20 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Investigations
Blood creatine phosphokinase increased
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.3%
1/19 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Investigations
Weight decreased
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.3%
1/19 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.0%
1/20 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Metabolism and nutrition disorders
Hypertriglyceridaemia
|
5.0%
1/20 • Number of events 2 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.3%
1/19 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.0%
1/20 • Number of events 3 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Nervous system disorders
Headache
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
15.8%
3/19 • Number of events 4 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
10.0%
2/20 • Number of events 2 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Skin and subcutaneous tissue disorders
Pruritus generalised
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.3%
1/19 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Investigations
Blood alkaline phosphatase increased
|
5.0%
1/20 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.0%
1/20 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/19 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.0%
1/20 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Musculoskeletal and connective tissue disorders
Muscle spasms
|
5.0%
1/20 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/19 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Investigations
Amylase increased
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.0%
1/20 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/19 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Investigations
Lipase increased
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.0%
1/20 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/19 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Respiratory, thoracic and mediastinal disorders
Epistaxis
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.0%
1/20 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/19 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Respiratory, thoracic and mediastinal disorders
Nasal congestion
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.0%
1/20 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/19 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Respiratory, thoracic and mediastinal disorders
Nasal inflammation
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.0%
1/20 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/19 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Respiratory, thoracic and mediastinal disorders
Rhinorrhoea
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.0%
1/20 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/19 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
|
Respiratory, thoracic and mediastinal disorders
Throat irritation
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
5.0%
1/20 • Number of events 1 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/19 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
0.00%
0/20 • Baseline to End of Follow-up (Up To 39 Days)
All participants who received at least one dose of study drug. Per pre-specified analysis, adverse events were analyzed and reported based on the assigned study treatment.
|
Additional Information
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place
Restriction type: GT60