Trial Outcomes & Findings for A Study of Effects of Selpercatinib (LY3527723) on Repaglinide in Healthy Participants (NCT NCT05469113)
NCT ID: NCT05469113
Last Updated: 2025-12-11
Results Overview
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
16 participants
Primary outcome timeframe
Period 1: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose); Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose)
Results posted on
2025-12-11
Participant Flow
Participant milestones
| Measure |
Period 1: Repaglinide
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
Period 2: Selpercatinib + Repaglinide
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
|---|---|---|
|
Period 1
STARTED
|
16
|
0
|
|
Period 1
Safety Analysis Population (Received at Least One Dose of Study Drug)
|
16
|
0
|
|
Period 1
COMPLETED
|
16
|
0
|
|
Period 1
NOT COMPLETED
|
0
|
0
|
|
Period 2
STARTED
|
0
|
16
|
|
Period 2
Safety Analysis Population (Received at Least One Dose of Study Drug)
|
0
|
16
|
|
Period 2
COMPLETED
|
0
|
13
|
|
Period 2
NOT COMPLETED
|
0
|
3
|
Reasons for withdrawal
| Measure |
Period 1: Repaglinide
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
Period 2: Selpercatinib + Repaglinide
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
|---|---|---|
|
Period 2
Adverse Event
|
0
|
3
|
Baseline Characteristics
A Study of Effects of Selpercatinib (LY3527723) on Repaglinide in Healthy Participants
Baseline characteristics by cohort
| Measure |
All Participants
n=16 Participants
* Period 1: Participants received single dose of 0.5 mg Repaglinide tablet on Day 1.
* Period 2: Participants received 160 mg Selpercatinib capsule twice daily (BID) from Day 1-10, and on Day 10 it was co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
|---|---|
|
Age, Continuous
|
37.2 years
STANDARD_DEVIATION 10.62 • n=9 Participants
|
|
Sex: Female, Male
Female
|
3 Participants
n=9 Participants
|
|
Sex: Female, Male
Male
|
13 Participants
n=9 Participants
|
|
Ethnicity (NIH/OMB)
Hispanic or Latino
|
9 Participants
n=9 Participants
|
|
Ethnicity (NIH/OMB)
Not Hispanic or Latino
|
7 Participants
n=9 Participants
|
|
Ethnicity (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=9 Participants
|
|
Race (NIH/OMB)
American Indian or Alaska Native
|
0 Participants
n=9 Participants
|
|
Race (NIH/OMB)
Asian
|
0 Participants
n=9 Participants
|
|
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
|
0 Participants
n=9 Participants
|
|
Race (NIH/OMB)
Black or African American
|
1 Participants
n=9 Participants
|
|
Race (NIH/OMB)
White
|
15 Participants
n=9 Participants
|
|
Race (NIH/OMB)
More than one race
|
0 Participants
n=9 Participants
|
|
Race (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=9 Participants
|
|
Region of Enrollment
United States
|
16 Participants
n=9 Participants
|
PRIMARY outcome
Timeframe: Period 1: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose); Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome.
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
n=13 Participants
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=16 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Repaglinide
|
26.87 nanogram*hour per milliliter (ng*h/mL)
Geometric Coefficient of Variation 53.2
|
9.409 nanogram*hour per milliliter (ng*h/mL)
Geometric Coefficient of Variation 57.1
|
PRIMARY outcome
Timeframe: Period 1: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose); Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome.
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
n=13 Participants
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=15 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Repaglinide
|
27.31 nanogram*hour per milliliter (ng*h/mL)
Geometric Coefficient of Variation 53.6
|
10.15 nanogram*hour per milliliter (ng*h/mL)
Geometric Coefficient of Variation 51.3
|
PRIMARY outcome
Timeframe: Period 1: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose); Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome.
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
n=13 Participants
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=15 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Percent of AUC0-inf Extrapolated (AUC%Extrap) of Repaglinide
|
1.258 percent AUC extrapolation
Geometric Coefficient of Variation 85.8
|
1.256 percent AUC extrapolation
Geometric Coefficient of Variation 43.8
|
PRIMARY outcome
Timeframe: Period 1: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose); Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
n=13 Participants
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=16 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Maximum Observed Concentration (Cmax) of Repaglinide
|
12.11 nanogram per milliliter (ng/mL)
Geometric Coefficient of Variation 42.7
|
6.600 nanogram per milliliter (ng/mL)
Geometric Coefficient of Variation 77.4
|
PRIMARY outcome
Timeframe: Period 1: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose); Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome.
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
n=13 Participants
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=16 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Time to Reach Maximum Observed Concentration (Tmax) of Repaglinide
|
0.854 hours
Geometric Coefficient of Variation 42.5
|
0.623 hours
Geometric Coefficient of Variation 47.3
|
PRIMARY outcome
Timeframe: Period 1: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose); Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome.
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
n=13 Participants
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=15 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Apparent Terminal Elimination Rate Constant (Kel) of Repaglindide
|
0.2036 One per hour (1/h)
Geometric Coefficient of Variation 36.2
|
0.2406 One per hour (1/h)
Geometric Coefficient of Variation 27.9
|
PRIMARY outcome
Timeframe: Period 1: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose); Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome.
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
n=13 Participants
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=15 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Apparent First-order Terminal Elimination Half-life (t½) of Repaglinide
|
3.405 hours
Geometric Coefficient of Variation 36.2
|
2.881 hours
Geometric Coefficient of Variation 27.9
|
PRIMARY outcome
Timeframe: Period 1: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose); Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome.
PK: CL/F of Repaglinide
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
n=13 Participants
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=15 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Repaglinide
|
18.31 Liter per Hour (L/h)
Geometric Coefficient of Variation 53.6
|
49.26 Liter per Hour (L/h)
Geometric Coefficient of Variation 51.3
|
PRIMARY outcome
Timeframe: Period 1: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose); Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome.
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
n=13 Participants
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=15 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Apparent Volume of Distribution During the Terminal Elimination Phase (Vz/F) of Repaglinide
|
89.92 Liter (L)
Geometric Coefficient of Variation 64.9
|
204.8 Liter (L)
Geometric Coefficient of Variation 53.6
|
SECONDARY outcome
Timeframe: Period 2: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile.
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=16 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Area Under the Concentration-time Curve, From Time 0 to the 12 Hour (AUC0-12) of Selpercatinib
|
—
|
8424 ng*h/mL
Geometric Coefficient of Variation 56.6
|
SECONDARY outcome
Timeframe: Period 2: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile.
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=16 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib
|
—
|
8396 ng*h/mL
Geometric Coefficient of Variation 56.7
|
SECONDARY outcome
Timeframe: Period 2: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile.
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=16 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Maximum Observed Concentration (Cmax) of Selpercatinib
|
—
|
1476 ng/mL
Geometric Coefficient of Variation 66.3
|
SECONDARY outcome
Timeframe: Period 2: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile.
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=16 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Time to Reach Maximum Observed Concentration (Tmax) of Selpercatinib
|
—
|
1.553 hours
Geometric Coefficient of Variation 25.9
|
SECONDARY outcome
Timeframe: Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile.
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=13 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Area Under the Concentration-time Curve During a Dosing Interval (Tau) at Steady State (AUCtau) of Selpercatinib
|
—
|
33960 ng*h/mL
Geometric Coefficient of Variation 45.0
|
SECONDARY outcome
Timeframe: Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile.
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=13 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Maximum Observed Concentration at Steady-state (Cmax,ss) of Selpertcatinib
|
—
|
4082 ng/mL
Geometric Coefficient of Variation 40.8
|
SECONDARY outcome
Timeframe: Period 2: Predose at Day 1, Day 2, Day 3, Day 4, Day 5, Day 6, Day 7, Day 8, Day 9Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome. 'Number analyzed' signifies participants with available data at specified timepoints.
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=16 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib
Day 1
|
—
|
983.2 ng/mL
Standard Deviation 225.43
|
|
PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib
Day 2
|
—
|
1509 ng/mL
Standard Deviation 362.03
|
|
PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib
Day 3
|
—
|
1664 ng/mL
Standard Deviation 529.60
|
|
PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib
Day 4
|
—
|
1842 ng/mL
Standard Deviation 657.65
|
|
PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib
Day 5
|
—
|
1971 ng/mL
Standard Deviation 642.36
|
|
PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib
Day 6
|
—
|
2039 ng/mL
Standard Deviation 780.35
|
|
PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib
Day 7
|
—
|
2160 ng/mL
Standard Deviation 771.22
|
|
PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib
Day 8
|
—
|
2034 ng/mL
Standard Deviation 635.04
|
|
PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib
Day 9
|
—
|
2085 ng/mL
Standard Deviation 762.09
|
SECONDARY outcome
Timeframe: Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome.
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=13 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Time to Reach Maximum Observed Concentration at Steady-state (Tmax,ss) of Selpercatinib
|
—
|
1.888 hours
Geometric Coefficient of Variation 29.6
|
SECONDARY outcome
Timeframe: Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose)Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile.
Outcome measures
| Measure |
Period 2: Selpercatinib + Repaglinide
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
Period 1: Repaglinide
n=13 Participants
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
|---|---|---|
|
PK: Apparent Total Plasma Clearance at Steady State After Oral/Extravascular Administration (CL,ss/F) of Selpercatinib
|
—
|
4.711 Liter per Hours (L/h)
Geometric Coefficient of Variation 45.0
|
Adverse Events
Period 1: Repaglinide (Day 1)
Serious events: 0 serious events
Other events: 7 other events
Deaths: 0 deaths
Period 2: Selpercatinib (Day 1 to Day 9)
Serious events: 0 serious events
Other events: 7 other events
Deaths: 0 deaths
Period 2: Selpercatinib + Repaglinide (Day 10)
Serious events: 0 serious events
Other events: 11 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Period 1: Repaglinide (Day 1)
n=16 participants at risk
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
|
Period 2: Selpercatinib (Day 1 to Day 9)
n=16 participants at risk
* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsule twice daily (BID).
|
Period 2: Selpercatinib + Repaglinide (Day 10)
n=13 participants at risk
* Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 0.5 mg Repaglinide tablet on the morning of Day 10.
|
|---|---|---|---|
|
Investigations
Blood glucose decreased
|
31.2%
5/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
61.5%
8/13 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
|
Investigations
Electrocardiogram QT prolonged
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
6.2%
1/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/13 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
|
Nervous system disorders
Headache
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
12.5%
2/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
15.4%
2/13 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
|
Nervous system disorders
Dizziness
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
6.2%
1/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/13 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
|
Nervous system disorders
Tremor
|
6.2%
1/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/13 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
|
Metabolism and nutrition disorders
Hypoglycaemia
|
6.2%
1/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
23.1%
3/13 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
|
General disorders
Fatigue
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
6.2%
1/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/13 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
|
General disorders
Pain
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
7.7%
1/13 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
|
Musculoskeletal and connective tissue disorders
Back pain
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
6.2%
1/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/13 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
|
Musculoskeletal and connective tissue disorders
Myalgia
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
6.2%
1/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/13 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
|
Cardiac disorders
Palpitations
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
6.2%
1/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/13 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
|
Eye disorders
Vision blurred
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
6.2%
1/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/13 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
|
Gastrointestinal disorders
Nausea
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
7.7%
1/13 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
|
Psychiatric disorders
Insomnia
|
6.2%
1/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/13 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
|
Respiratory, thoracic and mediastinal disorders
Cough
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
7.7%
1/13 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
|
Vascular disorders
Hypertension
|
0.00%
0/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
6.2%
1/16 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
0.00%
0/13 • Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2)
Safety analysis population: All participants who received at least one dose of study drug. * 2 participants discontinued the study on Day 3, and 1 participant discontinued study on Day 8 after receiving the Selpercatinib dose in Period 2. Therefore, safety analysis population for Period 2: Selpercatinib + Repaglinide (Day 10) treatment includes only the remaining 13 participants.
|
Additional Information
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place
Restriction type: GT60