A Study of Effects of Selpercatinib (LY3527723) on Repaglinide in Healthy Participants
Study Details
Study Description
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.
| Condition or Disease | Intervention/Treatment | Phase |
|---|---|---|
| Phase 1 |
Study Design
Arms and Interventions
| Arm | Intervention/Treatment |
|---|---|
| Experimental: Repaglinide - Period 1 Single dose of repaglinide administered orally. |
Drug: Repaglinide
Administered orally.
|
| Experimental: Selpercatinib and repaglinide - Period 2 Multiple doses of selpercatinib along with single dose of repaglinide administered orally. There will be a 24-hour washout period between Period 1 and 2. |
Drug: Repaglinide
Administered orally.
Drug: Selpercatinib
Administered orally.
Other Names:
|
Outcome Measures
Primary Outcome Measures
- Pharmacokinetics (PK): Area under the concentration-time curve, from time 0 to the last observed non-zero concentration (AUC0-t) of Repaglinide [Pre-dose up to 16 hours postdose]
PK: AUC0-t of Repaglinide
- PK: Area under the concentration-time curve from time 0 extrapolated to infinity (AUC0-inf) of Repaglinide [Pre-dose up to 16 hours post-dose]
PK: AUC0-inf of Repaglinide
- PK: Percent of AUC0-inf extrapolated (AUC%extrap) of Repaglinide [Pre-dose up to 16 hours post-dose]
PK: AUC%extrap of Repaglinide
- PK: Maximum observed concentration (Cmax) of Repaglinide [Pre-dose up to 16 hours post-dose]
PK: Cmax of Repaglinide
- PK: Time to reach Cmax (Tmax) of Repaglinide [Pre-dose up to 16 hour post-dose]
PK: Tmax of Repaglinide
- PK: Apparent first-order terminal elimination rate constant (Kel) of Repaglindide [Pre-dose up to 16 hour post-dose]
PK: Kel of Repaglindide
- PK: Apparent first-order terminal elimination half-life (t½) of Repaglinide [Pre-dose up to 16 hour post-dose]
PK: t½ of Repaglinide
- PK: Apparent total plasma clearance after oral (extravascular) administration (CL/F) of Repaglinide [Pre-dose up to 16 hour post-dose]
PK: CL/F of Repaglinide
- PK: Apparent volume of distribution during the terminal elimination phase after oral (extravascular) administration (Vz/F) of Repaglinide [Pre-dose up to 16 hour post-dose]
PK: (Vz/F) of Repaglinide
Secondary Outcome Measures
- PK: Area under the concentration-time curve, from time 0 to the 12 hour timepoint (AUC0-12) of Selpercatinib (Day 1 of Period 2) [Pre-morning dose up to 12 hours following the morning dose]
PK: 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 (Day 1 of Period 2) [Pre-morning dose up to 12 hours following the morning dose]
PK: AUC0-t of Selpercatinib
- PK: Maximum observed concentration (Cmax) of Selpercatinib (Day 1 of Period 2) [Pre-morning dose up to 12 hours following the morning dose]
PK: Cmax of Selpercatinib
- PK: Time to reach Cmax (Tmax) of Selpercatinib (Day 1 of Period 2) [Pre-morning dose up to 12 hours following the morning dose]
PK: Tmax of Selpercatinib
- PK: Area under the concentration-time curve during a dosing interval (tau) at steady state (AUCtau) of Selpercatinib (Day 10 of Period 2) [Pre-morning dose up to 12 hours following the morning dose]
PK: AUCtau of Selpercatinib
- PK: Maximum observed concentration at steady-state (Cmax,ss) of Selpertcatinib (Day 10 of Period 2) [Pre-morning dose up to 12 hours following the morning dose]
PK: Cmax,ss of Selpertcatinib
- PK: Concentration observed at the end of the dosing interval (Ctrough) of Selpercatinib (Day 10 of Period 2) [Pre-morning dose]
PK: Ctrough of Selpercatinib
- PK: Time to reach Cmax,ss (Tmax,ss) of Selpercatinib (Day 10 of Period 2) [Pre-morning dose up to 12 hours following the morning dose]
PK: Tmax,ss of Selpercatinib
- PK: Apparent total plasma clearance after oral (extravascular) administration(CL,ss/F) of Selpercatinib (Day 10 of Period 2) [Pre-morning dose up to 12 hours following the morning dose]
PK: CL,ss/F of Selpercatinib
Eligibility Criteria
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
Contacts and Locations
Locations
| Site | City | State | Country | Postal Code | |
|---|---|---|---|---|---|
| 1 | Celerion | Tempe | Arizona | United States | 85283 |
Sponsors and Collaborators
- Eli Lilly and Company
- Loxo Oncology, Inc.
Investigators
- Study Director: 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), Eli Lilly and Company
Study Documents (Full-Text)
None provided.More Information
Publications
None provided.- 17754
- J2G-OX-JZJS
- LOXO-RET-18026