A Study of Effects of Selpercatinib (LY3527723) on Repaglinide in Healthy Participants

An Open-Label, Fixed-Sequence Study to Evaluate the Effect of Multiple Doses of LOXO-292 on the Single Dose Pharmacokinetics of Repaglinide in Healthy Adult Subjects

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT05469113

Enrollment

Registered

2022-07-21

Start date

2019-01-29

Completion date

2019-03-05

Last updated

2025-12-11

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy

Brief summary

The main purpose of this study is to assess the effect of selpercatinib on how fast repaglinide gets into the blood stream and how long it takes the body to remove it when administered in healthy participants. Information about safety and tolerability will be collected. The study will last up to 12 days.

Interventions

DRUGRepaglinide

Administered orally.

DRUGSelpercatinib

Administered orally.

Study design

Allocation

NON_RANDOMIZED

Intervention model

SEQUENTIAL

Primary purpose

BASIC_SCIENCE

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

18 Years to 55 Years

Healthy volunteers

Yes

Inclusion criteria

* Body mass index (BMI) ≥ 18.0 and ≤ 32.0 kilograms per meter squared (kg/m²) and had a minimum weight of at least 50 kg at screening * Have normal blood pressure, pulse rate, electrocardiogram (ECG), and blood and urine laboratory test results that are acceptable for the study * Hemoglobin (Hb) A1c value \< 6.5 % at screening and fasting glucose ≤ 126 mg/dL. * Males who are capable of fathering a child must agree to use one of the following methods of contraception from the time of the dose administration through 6 months after the last dose * Female of non-childbearing potential only or must have undergone sterilization procedures at least 6months prior to the first dosing

Exclusion criteria

* History or presence of diabetes or history of prior episode(s) of hypoglycemia. * Estimated creatinine clearance \<90 mL/min at Screening or Check-in (Day -1, Period 1) * Unable to refrain from or anticipates the use of any drug, including prescription and non prescription medications, herbal remedies, or vitamin supplements for 14 days prior to the first dosing and through EOT or ET. After first dosing, acetaminophen (up to 2 g per 24 hours) may be administered at the discretion of the PI or designee

Design outcomes

Primary

Measure	Time frame	Description
PK: Apparent Volume of Distribution During the Terminal Elimination Phase (Vz/F) of Repaglinide	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)	—
Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Repaglinide	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)	—
PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Repaglinide	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)	—
PK: Percent of AUC0-inf Extrapolated (AUC%Extrap) of Repaglinide	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)	—
PK: Maximum Observed Concentration (Cmax) of Repaglinide	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)	—
PK: Time to Reach Maximum Observed Concentration (Tmax) of Repaglinide	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)	—
PK: Apparent Terminal Elimination Rate Constant (Kel) of Repaglindide	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)	—
PK: Apparent First-order Terminal Elimination Half-life (t½) of Repaglinide	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)	—
PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Repaglinide	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)	PK: CL/F of Repaglinide

Secondary

Measure	Time frame
PK: Area Under the Concentration-time Curve During a Dosing Interval (Tau) at Steady State (AUCtau) of Selpercatinib	Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose)
PK: Area Under the Concentration-time Curve, From Time 0 to the 12 Hour (AUC0-12) of Selpercatinib	Period 2: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose)
PK: Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib	Period 2: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose)
PK: Maximum Observed Concentration (Cmax) of Selpercatinib	Period 2: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose)
PK: Time to Reach Maximum Observed Concentration (Tmax) of Selpercatinib	Period 2: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose)
PK: Maximum Observed Concentration at Steady-state (Cmax,ss) of Selpertcatinib	Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose)
PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib	Period 2: Predose at Day 1, Day 2, Day 3, Day 4, Day 5, Day 6, Day 7, Day 8, Day 9
PK: Time to Reach Maximum Observed Concentration at Steady-state (Tmax,ss) of Selpercatinib	Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose)
PK: Apparent Total Plasma Clearance at Steady State After Oral/Extravascular Administration (CL,ss/F) of Selpercatinib	Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose)

Countries

United States

Participant flow

Participants by arm

Arm	Count
All 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.	16
Total	16

Withdrawals & dropouts

Period	Reason	FG000	FG001
Period 2	Adverse Event	0	3

Baseline characteristics

Characteristic	All Participants
Age, Continuous	37.2 years STANDARD_DEVIATION 10.62
Ethnicity (NIH/OMB) Hispanic or Latino	9 Participants
Ethnicity (NIH/OMB) Not Hispanic or Latino	7 Participants
Ethnicity (NIH/OMB) Unknown or Not Reported	0 Participants
Race (NIH/OMB) American Indian or Alaska Native	0 Participants
Race (NIH/OMB) Asian	0 Participants
Race (NIH/OMB) Black or African American	1 Participants
Race (NIH/OMB) More than one race	0 Participants
Race (NIH/OMB) Native Hawaiian or Other Pacific Islander	0 Participants
Race (NIH/OMB) Unknown or Not Reported	0 Participants
Race (NIH/OMB) White	15 Participants
Region of Enrollment United States	16 Participants
Sex: Female, Male Female	3 Participants
Sex: Female, Male Male	13 Participants

Adverse events

Event type	EG000 affected / at risk	EG001 affected / at risk	EG002 affected / at risk
deaths Total, all-cause mortality	0 / 16	0 / 16	0 / 13
other Total, other adverse events	7 / 16	7 / 16	11 / 13
serious Total, serious adverse events	0 / 16	0 / 16	0 / 13

Outcome results

Primary

Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Repaglinide

Time frame: 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.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Repaglinide	9.409 nanogramhour per milliliter (ngh/mL)	Geometric Coefficient of Variation 57.1
Period 2: Selpercatinib + Repaglinide	Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Repaglinide	26.87 nanogramhour per milliliter (ngh/mL)	Geometric Coefficient of Variation 53.2

Primary

PK: Apparent First-order Terminal Elimination Half-life (t½) of Repaglinide

Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	PK: Apparent First-order Terminal Elimination Half-life (t½) of Repaglinide	2.881 hours	Geometric Coefficient of Variation 27.9
Period 2: Selpercatinib + Repaglinide	PK: Apparent First-order Terminal Elimination Half-life (t½) of Repaglinide	3.405 hours	Geometric Coefficient of Variation 36.2

Primary

PK: Apparent Terminal Elimination Rate Constant (Kel) of Repaglindide

Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	PK: Apparent Terminal Elimination Rate Constant (Kel) of Repaglindide	0.2406 One per hour (1/h)	Geometric Coefficient of Variation 27.9
Period 2: Selpercatinib + Repaglinide	PK: Apparent Terminal Elimination Rate Constant (Kel) of Repaglindide	0.2036 One per hour (1/h)	Geometric Coefficient of Variation 36.2

Primary

PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Repaglinide

PK: CL/F of Repaglinide

Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Repaglinide	49.26 Liter per Hour (L/h)	Geometric Coefficient of Variation 51.3
Period 2: Selpercatinib + Repaglinide	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

Primary

PK: Apparent Volume of Distribution During the Terminal Elimination Phase (Vz/F) of Repaglinide

Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	PK: Apparent Volume of Distribution During the Terminal Elimination Phase (Vz/F) of Repaglinide	204.8 Liter (L)	Geometric Coefficient of Variation 53.6
Period 2: Selpercatinib + Repaglinide	PK: Apparent Volume of Distribution During the Terminal Elimination Phase (Vz/F) of Repaglinide	89.92 Liter (L)	Geometric Coefficient of Variation 64.9

Primary

PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Repaglinide

Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Repaglinide	10.15 nanogramhour per milliliter (ngh/mL)	Geometric Coefficient of Variation 51.3
Period 2: Selpercatinib + Repaglinide	PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Repaglinide	27.31 nanogramhour per milliliter (ngh/mL)	Geometric Coefficient of Variation 53.6

Primary

PK: Maximum Observed Concentration (Cmax) of Repaglinide

Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	PK: Maximum Observed Concentration (Cmax) of Repaglinide	6.600 nanogram per milliliter (ng/mL)	Geometric Coefficient of Variation 77.4
Period 2: Selpercatinib + Repaglinide	PK: Maximum Observed Concentration (Cmax) of Repaglinide	12.11 nanogram per milliliter (ng/mL)	Geometric Coefficient of Variation 42.7

Primary

PK: Percent of AUC0-inf Extrapolated (AUC%Extrap) of Repaglinide

Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	PK: Percent of AUC0-inf Extrapolated (AUC%Extrap) of Repaglinide	1.256 percent AUC extrapolation	Geometric Coefficient of Variation 43.8
Period 2: Selpercatinib + Repaglinide	PK: Percent of AUC0-inf Extrapolated (AUC%Extrap) of Repaglinide	1.258 percent AUC extrapolation	Geometric Coefficient of Variation 85.8

Primary

PK: Time to Reach Maximum Observed Concentration (Tmax) of Repaglinide

Population: All participants who complied sufficiently with the protocol and displayed an evaluable PK profile for this outcome.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	PK: Time to Reach Maximum Observed Concentration (Tmax) of Repaglinide	0.623 hours	Geometric Coefficient of Variation 47.3
Period 2: Selpercatinib + Repaglinide	PK: Time to Reach Maximum Observed Concentration (Tmax) of Repaglinide	0.854 hours	Geometric Coefficient of Variation 42.5

Secondary

PK: Apparent Total Plasma Clearance at Steady State After Oral/Extravascular Administration (CL,ss/F) of Selpercatinib

Time frame: 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.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	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

Secondary

PK: Area Under the Concentration-time Curve During a Dosing Interval (Tau) at Steady State (AUCtau) of Selpercatinib

Time frame: 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.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	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

Secondary

PK: Area Under the Concentration-time Curve, From Time 0 to the 12 Hour (AUC0-12) of Selpercatinib

Time frame: 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.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	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

PK: Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib

Time frame: 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.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	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

PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib

Time frame: Period 2: Predose at Day 1, Day 2, Day 3, Day 4, Day 5, Day 6, Day 7, Day 8, Day 9

Population: 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.

Arm	Measure	Group	Value (MEAN)	Dispersion
Period 1: Repaglinide	PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib	Day 1	983.2 ng/mL	Standard Deviation 225.43
Period 1: Repaglinide	PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib	Day 2	1509 ng/mL	Standard Deviation 362.03
Period 1: Repaglinide	PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib	Day 4	1842 ng/mL	Standard Deviation 657.65
Period 1: Repaglinide	PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib	Day 5	1971 ng/mL	Standard Deviation 642.36
Period 1: Repaglinide	PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib	Day 6	2039 ng/mL	Standard Deviation 780.35
Period 1: Repaglinide	PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib	Day 7	2160 ng/mL	Standard Deviation 771.22
Period 1: Repaglinide	PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib	Day 8	2034 ng/mL	Standard Deviation 635.04
Period 1: Repaglinide	PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib	Day 9	2085 ng/mL	Standard Deviation 762.09
Period 1: Repaglinide	PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib	Day 3	1664 ng/mL	Standard Deviation 529.6

Secondary

PK: Maximum Observed Concentration at Steady-state (Cmax,ss) of Selpertcatinib

Time frame: 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.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	PK: Maximum Observed Concentration at Steady-state (Cmax,ss) of Selpertcatinib	4082 ng/mL	Geometric Coefficient of Variation 40.8

Secondary

PK: Maximum Observed Concentration (Cmax) of Selpercatinib

Time frame: 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.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	PK: Maximum Observed Concentration (Cmax) of Selpercatinib	1476 ng/mL	Geometric Coefficient of Variation 66.3

Secondary

PK: Time to Reach Maximum Observed Concentration at Steady-state (Tmax,ss) of Selpercatinib

Time frame: 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.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	PK: Time to Reach Maximum Observed Concentration at Steady-state (Tmax,ss) of Selpercatinib	1.888 hours	Geometric Coefficient of Variation 29.6

Secondary

PK: Time to Reach Maximum Observed Concentration (Tmax) of Selpercatinib

Time frame: 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.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Period 1: Repaglinide	PK: Time to Reach Maximum Observed Concentration (Tmax) of Selpercatinib	1.553 hours	Geometric Coefficient of Variation 25.9

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026

A Study of Effects of Selpercatinib (LY3527723) on Repaglinide in Healthy Participants

Conditions

Brief summary

Related papers

Interventions

Sponsors

Study design

Eligibility

Inclusion criteria

Exclusion criteria

Design outcomes

Primary

Secondary

Countries

Participant flow

Participants by arm

Withdrawals & dropouts

Baseline characteristics

Adverse events

Outcome results

Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Repaglinide

PK: Apparent First-order Terminal Elimination Half-life (t½) of Repaglinide

PK: Apparent Terminal Elimination Rate Constant (Kel) of Repaglindide

PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Repaglinide

PK: Apparent Volume of Distribution During the Terminal Elimination Phase (Vz/F) of Repaglinide

PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Repaglinide

PK: Maximum Observed Concentration (Cmax) of Repaglinide

PK: Percent of AUC0-inf Extrapolated (AUC%Extrap) of Repaglinide

PK: Time to Reach Maximum Observed Concentration (Tmax) of Repaglinide

PK: Apparent Total Plasma Clearance at Steady State After Oral/Extravascular Administration (CL,ss/F) of Selpercatinib

PK: Area Under the Concentration-time Curve During a Dosing Interval (Tau) at Steady State (AUCtau) of Selpercatinib

PK: Area Under the Concentration-time Curve, From Time 0 to the 12 Hour (AUC0-12) of Selpercatinib

PK: Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib

PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib

PK: Maximum Observed Concentration at Steady-state (Cmax,ss) of Selpertcatinib

PK: Maximum Observed Concentration (Cmax) of Selpercatinib

PK: Time to Reach Maximum Observed Concentration at Steady-state (Tmax,ss) of Selpercatinib

PK: Time to Reach Maximum Observed Concentration (Tmax) of Selpercatinib