A Study of Selpercatinib (LY3527723) in Healthy Participants

Study Overview
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Brief Summary
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The main purpose of this study is to determine how safe and how well tolerated selpercatinib is when given as oral doses to healthy participants. The study will also assess how fast selpercatinib gets into the blood stream and how long it takes the body to remove it. The study will last up to about 6 weeks, inclusive of screening period.

Official Title
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A Phase I, Single-Ascending Dose Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of LOXO-292 in Healthy Adult Subjects

Conditions
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Healthy

Intervention / Treatment
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* Drug: Selpercatinib


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: Female participants of non-childbearing potential who are agreeable to take birth control measures until study completion 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 Exclusion Criteria: Are currently participating in or completed a clinical trial within the last 30 days or any other type of medical research judged to be incompatible with this study Have previously participated or withdrawn from this study Have or used to have health problems or laboratory test results or ECG readings that, in the opinion of the doctor, could make it unsafe to participate, or could interfere with understanding the results of the study Had blood loss of more than 500 milliliters (mL) within the previous 30 days of study screening Require treatment with inducers or inhibitors of cytochrome P450 (CYP) CYP3A within 14 days before the first dose of study drug through the end of Period 2

Ages Eligible for Study
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Minimum Age: 18 Years
Maximum Age: 55 Years

Sexes Eligible for Study
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All

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

Primary Purpose: Basic Science
Allocation: Non-Randomized
Intervention Model: Sequential Assignment
Masking: None (Open Label)


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: Selpercatinib Cohort 1<br>Selpercatinib administered orally. | Drug: Selpercatinib<br>* Administered orally.<br>* Other names: LOXO-292;|
| Experimental: Selpercatinib Cohort 2<br>Selpercatinib administered orally. | Drug: Selpercatinib<br>* Administered orally.<br>* Other names: LOXO-292;|
| Experimental: Selpercatinib Cohort 3<br>Selpercatinib administered orally. | Drug: Selpercatinib<br>* Administered orally.<br>* Other names: LOXO-292;|

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Number of Participants with One or More Serious Adverse Event(s) (SAEs) Considered by the Investigator to be Related to Study Drug Administration | A summary of SAEs and other non-serious adverse events (AEs), regardless of causality, will be reported in the Reported Adverse Events module | Baseline through Day 8 | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Pharmacokinetics (PK): Area under the concentration-time curve, from time 0 to the last observed non-zero concentration (AUC0-t) of Selpercatinib | PK: AUC0-t of Selpercatinib | Pre-dose up to 168 hour post-dose | 
| PK: Area under the concentration-time curve, from time 0 to Hour 24 (AUC0-24) of Selpercatinib | PK: AUC0-24 of Selpercatinib | Pre-dose up to 168 hour post-dose | 
| PK: Area under the concentration-time curve from time 0 extrapolated to infinity (AUC0-inf) of Selpercatinib | PK: AUC0-inf of Selpercatinib | Pre-dose up to 168 hour post-dose | 
| PK: Percent of AUC0-inf extrapolated (AUC%extrap) of Selpercatinib | PK: AUC%extrap of Selpercatinib | Pre-dose up to 168 hour post-dose | 
| PK: Apparent total plasma clearance after oral (extravascular) administration (CL/F) of Selpercatinib | PK: CL/F of Selpercatinib | Pre-dose up to 168 hour post-dose | 
| PK: Maximum observed concentration (Cmax) of Selpercatinib | PK: Cmax of Selpercatinib | Pre-dose up to 168 hour post-dose | 
| PK: Time to reach Cmax (Tmax) of Selpercatinib | PK: Tmax of Selpercatinib | Pre-dose up to 168 hour post-dose | 
| PK: Apparent first-order terminal elimination rate constant (Kel) of Selpercatinib | PK: Kel of Selpercatinib | Pre-dose up to 168 hour post-dose | 
| PK: Apparent volume of distribution during the terminal elimination phase (Vz/F) of Selpercatinib | PK: Vz/F of Selpercatinib | Pre-dose up to 168 hour post-dose |