Phase 1
N=16
A Study of Effects of Selpercatinib (LY3527723) on Repaglinide in Healthy Participants
Healthy
Bottom Line
View on ClinicalTrials.gov: NCT05469113 ↗Enrolled (actual)
16
Serious AEs
0.0%
Results posted
Dec 2025
Primary outcome: Primary: Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Repaglinide — 9.409; 26.87 nanogram*hour per milliliter (ng*h/mL)
Study Design & Population
- Study type
- Interventional
- Phase
- Phase 1
- Interventions
- Repaglinide (Drug); Selpercatinib (Drug)
- Age
- Adult · 18+ yrs
- Sex
- All
- Sponsor
- Eli Lilly and Company
- Primary completion
- Mar 2019
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Repaglinide |
9.409; 26.87 | — |
| PRIMARY PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Repaglinide |
10.15; 27.31 | — |
| PRIMARY PK: Percent of AUC0-inf Extrapolated (AUC%Extrap) of Repaglinide |
1.256; 1.258 | — |
| PRIMARY PK: Maximum Observed Concentration (Cmax) of Repaglinide |
6.600; 12.11 | — |
| PRIMARY PK: Time to Reach Maximum Observed Concentration (Tmax) of Repaglinide |
0.623; 0.854 | — |
| PRIMARY PK: Apparent Terminal Elimination Rate Constant (Kel) of Repaglindide |
0.2406; 0.2036 | — |
| PRIMARY PK: Apparent First-order Terminal Elimination Half-life (t½) of Repaglinide |
2.881; 3.405 | — |
| PRIMARY PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Repaglinide |
49.26; 18.31 | — |
| PRIMARY PK: Apparent Volume of Distribution During the Terminal Elimination Phase (Vz/F) of Repaglinide |
204.8; 89.92 | — |
| SECONDARY PK: Area Under the Concentration-time Curve, From Time 0 to the 12 Hour (AUC0-12) of Selpercatinib |
8424 | — |
| SECONDARY PK: Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib |
8396 | — |
| SECONDARY PK: Maximum Observed Concentration (Cmax) of Selpercatinib |
1476 | — |
| SECONDARY PK: Time to Reach Maximum Observed Concentration (Tmax) of Selpercatinib |
1.553 | — |
| SECONDARY PK: Area Under the Concentration-time Curve During a Dosing Interval (Tau) at Steady State (AUCtau) of Selpercatinib |
33960 | — |
| SECONDARY PK: Maximum Observed Concentration at Steady-state (Cmax,ss) of Selpertcatinib |
4082 | — |
| SECONDARY PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Selpercatinib |
983.2; 1509; 1664; 1842; 1971; 2039 | — |
| SECONDARY PK: Time to Reach Maximum Observed Concentration at Steady-state (Tmax,ss) of Selpercatinib |
1.888 | — |
| SECONDARY PK: Apparent Total Plasma Clearance at Steady State After Oral/Extravascular Administration (CL,ss/F) of Selpercatinib |
4.711 | — |
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.
Eligibility Criteria
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
Data sourced from ClinicalTrials.gov (NCT05469113). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.