CompletedNCT05469113Updated Dec 11, 2025Results posted

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

A Phase 1 interventional study of Repaglinide and Selpercatinib in Healthy, sponsored by Eli Lilly and Company. Completed at 1 site in United States. Open to participants aged 18 Years to 55 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2025-12-11.

Sponsored by Eli Lilly and Company · Phase 1, Interventional, and Basic science

From the registry’s dates

Registered 3 years 5 months after the study started (first participant enrolled Jan 2019, registered Jul 2022).

Phase: Phase 1
Study type: Interventional
Enrollment: 16
Allocation: Non-randomized
Ages: 18 Years to 55 Years
Sex: All

Study 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.

Conditions studied

Healthy

In context

Lead sponsor

Eli Lilly and Company is the lead sponsor of 2,048 studies on the registry; 140 are open to participants now.

Of its 521 completed or terminated interventional studies of FDA-regulated products, 341 (65%) have results posted.

Counted across the registry records on this site, refreshed daily.

Who can participate

Ages eligible: 18 Years to 55 Years
Sexes eligible: All
Accepts 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

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

Study design

Phase: Phase 1
Primary purpose: Basic science
Allocation: Non-randomized
Intervention model: Sequential assignment
Masking: None (open label)
Enrollment: 16 participants (actual)

Study arms

Experimental
Period 1: Repaglinide
* Day 1: Participants received single dose of 0.5 mg repaglinide tablet.
Drug: Repaglinide
Experimental
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.
Drug: Repaglinide · Drug: Selpercatinib

Interventions

DrugRepaglinide
Administered orally.
DrugSelpercatinib
Administered orally.
Also known as: LY3527723, LOXO-292

What researchers measure

Primary outcomes

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

Secondary outcomes

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)
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)
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)
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)
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)
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)
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
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)
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)

Results

Posted Dec 11, 2025

Participant flow

Period 1

Participant flow — Period 1
Milestone	Period 1: Repaglinide	Period 2: Selpercatinib + Repaglinide
Started	16	0
Safety analysis population (received at least one dose of study drug)	16	0
Completed	16	0
Not completed	0	0

Period 2

Participant flow — Period 2
Milestone	Period 1: Repaglinide	Period 2: Selpercatinib + Repaglinide
Started	0	16
Safety analysis population (received at least one dose of study drug)	0	16
Completed	0	13
Not completed	0	3
Withdrew: Adverse event	0	3

Outcome measures

PrimaryPharmacokinetics (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)
Reported as:: Geometric mean · nanogram*hour per milliliter (ng*h/mL)

Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Repaglinide
nanogramhour per milliliter (ngh/mL)	Period 1: Repaglinide	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	9.409 ± 57.1	26.87 ± 53.2

PrimaryPK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) 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)
Reported as:: Geometric mean · nanogram*hour per milliliter (ng*h/mL)

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

PrimaryPK: Percent of AUC0-inf Extrapolated (AUC%Extrap) 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)
Reported as:: Geometric mean · percent AUC extrapolation

PK: Percent of AUC0-inf Extrapolated (AUC%Extrap) of Repaglinide
percent AUC extrapolation	Period 1: Repaglinide	Period 2: Selpercatinib + Repaglinide
PK: Percent of AUC0-inf Extrapolated (AUC%Extrap) of Repaglinide	1.256 ± 43.8	1.258 ± 85.8

PrimaryPK: Maximum Observed Concentration (Cmax) 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)
Reported as:: Geometric mean · nanogram per milliliter (ng/mL)

PK: Maximum Observed Concentration (Cmax) of Repaglinide
nanogram per milliliter (ng/mL)	Period 1: Repaglinide	Period 2: Selpercatinib + Repaglinide
PK: Maximum Observed Concentration (Cmax) of Repaglinide	6.600 ± 77.4	12.11 ± 42.7

PrimaryPK: Time to Reach Maximum Observed Concentration (Tmax) 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)
Reported as:: Geometric mean · hours

PK: Time to Reach Maximum Observed Concentration (Tmax) of Repaglinide
hours	Period 1: Repaglinide	Period 2: Selpercatinib + Repaglinide
PK: Time to Reach Maximum Observed Concentration (Tmax) of Repaglinide	0.623 ± 47.3	0.854 ± 42.5

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

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)
Reported as:: Geometric mean · One per hour (1/h)

PK: Apparent Terminal Elimination Rate Constant (Kel) of Repaglindide
One per hour (1/h)	Period 1: Repaglinide	Period 2: Selpercatinib + Repaglinide
PK: Apparent Terminal Elimination Rate Constant (Kel) of Repaglindide	0.2406 ± 27.9	0.2036 ± 36.2

PrimaryPK: Apparent First-order Terminal Elimination Half-life (t½) 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)
Reported as:: Geometric mean · hours

PK: Apparent First-order Terminal Elimination Half-life (t½) of Repaglinide
hours	Period 1: Repaglinide	Period 2: Selpercatinib + Repaglinide
PK: Apparent First-order Terminal Elimination Half-life (t½) of Repaglinide	2.881 ± 27.9	3.405 ± 36.2

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

PK: CL/F 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)
Reported as:: Geometric mean · Liter per Hour (L/h)

PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Repaglinide
Liter per Hour (L/h)	Period 1: Repaglinide	Period 2: Selpercatinib + Repaglinide
PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Repaglinide	49.26 ± 51.3	18.31 ± 53.6

PrimaryPK: Apparent Volume of Distribution During the Terminal Elimination Phase (Vz/F) 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)
Reported as:: Geometric mean · Liter (L)

PK: Apparent Volume of Distribution During the Terminal Elimination Phase (Vz/F) of Repaglinide
Liter (L)	Period 1: Repaglinide	Period 2: Selpercatinib + Repaglinide
PK: Apparent Volume of Distribution During the Terminal Elimination Phase (Vz/F) of Repaglinide	204.8 ± 53.6	89.92 ± 64.9

SecondaryPK: 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)
Reported as:: Geometric mean · ng*h/mL

PK: Area Under the Concentration-time Curve, From Time 0 to the 12 Hour (AUC0-12) of Selpercatinib
ng*h/mL	Period 2: Selpercatinib + Repaglinide
PK: Area Under the Concentration-time Curve, From Time 0 to the 12 Hour (AUC0-12) of Selpercatinib	8424 ± 56.6

SecondaryPK: 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)
Reported as:: Geometric mean · ng*h/mL

PK: Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib
ng*h/mL	Period 2: Selpercatinib + Repaglinide
PK: Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib	8396 ± 56.7

SecondaryPK: 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)
Reported as:: Geometric mean · ng/mL

PK: Maximum Observed Concentration (Cmax) of Selpercatinib
ng/mL	Period 2: Selpercatinib + Repaglinide
PK: Maximum Observed Concentration (Cmax) of Selpercatinib	1476 ± 66.3

SecondaryPK: 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)
Reported as:: Geometric mean · hours

PK: Time to Reach Maximum Observed Concentration (Tmax) of Selpercatinib
hours	Period 2: Selpercatinib + Repaglinide
PK: Time to Reach Maximum Observed Concentration (Tmax) of Selpercatinib	1.553 ± 25.9

SecondaryPK: 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)
Reported as:: Geometric mean · ng*h/mL

PK: Area Under the Concentration-time Curve During a Dosing Interval (Tau) at Steady State (AUCtau) of Selpercatinib
ng*h/mL	Period 2: Selpercatinib + Repaglinide
PK: Area Under the Concentration-time Curve During a Dosing Interval (Tau) at Steady State (AUCtau) of Selpercatinib	33960 ± 45.0

SecondaryPK: 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)
Reported as:: Geometric mean · ng/mL

PK: Maximum Observed Concentration at Steady-state (Cmax,ss) of Selpertcatinib
ng/mL	Period 2: Selpercatinib + Repaglinide
PK: Maximum Observed Concentration at Steady-state (Cmax,ss) of Selpertcatinib	4082 ± 40.8

SecondaryPK: 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
Reported as:: Mean · ng/mL

PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib
ng/mL	Period 2: Selpercatinib + Repaglinide
Day 1	983.2 ± 225.43
Day 2	1509 ± 362.03
Day 3	1664 ± 529.60
Day 4	1842 ± 657.65
Day 5	1971 ± 642.36
Day 6	2039 ± 780.35
Day 7	2160 ± 771.22
Day 8	2034 ± 635.04
Day 9	2085 ± 762.09

SecondaryPK: 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)
Reported as:: Geometric mean · hours

PK: Time to Reach Maximum Observed Concentration at Steady-state (Tmax,ss) of Selpercatinib
hours	Period 2: Selpercatinib + Repaglinide
PK: Time to Reach Maximum Observed Concentration at Steady-state (Tmax,ss) of Selpercatinib	1.888 ± 29.6

SecondaryPK: 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)
Reported as:: Geometric mean · Liter per Hours (L/h)

PK: Apparent Total Plasma Clearance at Steady State After Oral/Extravascular Administration (CL,ss/F) of Selpercatinib
Liter per Hours (L/h)	Period 2: Selpercatinib + Repaglinide
PK: Apparent Total Plasma Clearance at Steady State After Oral/Extravascular Administration (CL,ss/F) of Selpercatinib	4.711 ± 45.0

Adverse events

Collected over Baseline to Follow-up (up to Day 2 for Period 1; up to Day 11 for Period 2). Non-serious events are listed at a 0% frequency threshold.

Adverse event summary by group
Group	Deaths	Serious	Other
Period 1: Repaglinide (Day 1)	0/16 (0%)	0/16 (0%)	7/16 (43.8%)
Period 2: Selpercatinib (Day 1 to Day 9)	0/16 (0%)	0/16 (0%)	7/16 (43.8%)
Period 2: Selpercatinib + Repaglinide (Day 10)	0/13 (0%)	0/13 (0%)	11/13 (84.6%)

Most frequent other events

Showing 10 of 16

Most frequent other events
Event	Period 1: Repaglinide (Day 1)	Period 2: Selpercatinib (Day 1 to Day 9)	Period 2: Selpercatinib + Repaglinide (Day 10)
Blood glucose decreasedInvestigations	5/16	0/16	8/13
HypoglycaemiaMetabolism and nutrition disorders	1/16	0/16	3/13
HeadacheNervous system disorders	0/16	2/16	2/13
PainGeneral disorders	0/16	0/16	1/13
NauseaGastrointestinal disorders	0/16	0/16	1/13
CoughRespiratory, thoracic and mediastinal disorders	0/16	0/16	1/13
Electrocardiogram QT prolongedInvestigations	0/16	1/16	0/13
DizzinessNervous system disorders	0/16	1/16	0/13
TremorNervous system disorders	1/16	0/16	0/13
FatigueGeneral disorders	0/16	1/16	0/13

Baseline characteristics

All participants who received at least one dose of study drug.

Age, Continuous
Age, Continuous(years)	All Participants
Mean	37.2 ± 10.62

Sex: Female, Male
Sex: Female, Male(Participants)	All Participants
Female	3
Male	13

Ethnicity (NIH/OMB)
Ethnicity (NIH/OMB)(Participants)	All Participants
Hispanic or Latino	9
Not Hispanic or Latino	7
Unknown or Not Reported	0

Race (NIH/OMB)
Race (NIH/OMB)(Participants)	All Participants
American Indian or Alaska Native	0
Asian	0
Native Hawaiian or Other Pacific Islander	0
Black or African American	1
White	15
More than one race	0
Unknown or Not Reported	0

Region of Enrollment
Region of Enrollment(Participants)	All Participants
United States	16

Study locations

1 site

Celerion
Tempe, Arizona 85283, United States

References and documents

Study documents

Study protocol · Feb 20, 2019
Statistical analysis plan · Mar 22, 2019

Documents are hosted by the registry — open the source record to download them.

Individual participant data

Plan to share: No

Updates

Tracking since Sep 25, 2026

No changes since tracking began. The registry record was last updated on Dec 11, 2025, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗

Registry details

Key details

Study ID: NCT05469113
Lead sponsor: Eli Lilly and Company
Collaborators: Loxo Oncology, Inc.
Responsible party: Sponsor
First posted: Jul 21, 2022
Start date: Jan 29, 2019
Primary completion: Mar 5, 2019
Completion: Mar 5, 2019
Results posted: Dec 11, 2025
Last update: Dec 11, 2025

Study contacts

Call 1-877-CTLILLY (1-877-285-4559) or 1-317-615-4559 Mon - Fri 9 AM - 5 PM Eastern time (UTC/GMT - 5 hours, EST)

study director · Eli Lilly and Company

Oversight

Data monitoring committee: No
FDA-regulated drug: Yes
FDA-regulated device: No

View the source record on ClinicalTrials.gov ↗

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Eli Lilly and Company

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