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

Eli Lilly and Company16 enrolled

Overview

The main purpose of this study is to assess the effect of selpercatinib on how fast midazolam 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 about 6 weeks, inclusive of screening period.

Study Type

INTERVENTIONAL

Allocation

NON_RANDOMIZED

Purpose

BASIC_SCIENCE

Masking

NONE

Enrollment

Conditions

Healthy

Interventions

MidazolamDRUG

Administered orally.

SelpercatinibDRUG

Administered orally.

Eligibility

Sex: ALLMin age: 18 YearsMax age: 55 YearsHealthy volunteers:

Medical Language ↔ Plain English

Inclusion Criteria : * Male and 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days or any other type of medical research judged to be incompatible with this study * Have previously participated or withdrawn from this study * Have or used to have health problems or laboratory test results or ECG readings that, in the opinion of the doctor, could make it unsafe to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

Locations (1)

Celerion

Tempe, Arizona, United States

Outcomes

Primary Outcomes

Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Midazolam and Its Metabolite 1-hydroxymidazolam (1-OH-midazolam)

PK: PK: AUC0-t of midazolam and its metabolite 1-OH-midazolam was reported.

Time frame: Period 1: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24 hours post dose); Period 2: Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24 hours post dose)

PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Midazolam and Its Metabolite 1-OH-midazolam

PK: PK: AUC0-inf of midazolam and its metabolite 1-OH-midazolam was reported.

PK: Percent of AUC0-inf Extrapolated (AUC%Extrap) of Midazolam and Its Metabolite 1-OH-midazolam

PK: PK: AUC%extrap of midazolam and its metabolite 1-OH-midazolam was reported.

PK: Maximum Observed Concentration (Cmax) of Midazolam and Its Metabolite 1-OH-midazolam

PK: Cmax of midazolam and its metabolite 1-OH-midazolam was reported.

PK: Time to Reach Maximum Observed Concentration (Tmax) of Midazolam and Its Metabolite 1-OH-midazolam

PK: Tmax of midazolam and its metabolite 1-OH-midazolam was reported.

Data from ClinicalTrials.gov

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Secondary Outcomes

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

PK: AUC0-12 of Selpercatinib was reported.

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

PK: AUC0-tau of Selpercatinib was reported.

Time frame: Period 2: Day 9 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose); Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24 hours post dose)

PK: Maximum Observed Concentration (Cmax) of Selpercatinib

PK: Cmax of Selpercatinib was reported.

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 at Steady-state (Cmax,ss) of Selpercatinib

PK: Cmax,ss of Selpercatinib was reported.

Time frame: Period 2: Day 9 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose); Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24 hours post dose)

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

PK: Ctrough of Selpercatinib was reported.

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 (Tmax) of Selpercatinib

PK: tmax of Selpercatinib was reported.

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 at Steady-state (Tmax,ss) of Selpercatinib

PK: Tmax,ss of Selpercatinib was reported.

Time frame: Period 2: Day 9 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose); Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24 hours post dose)

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

PK: CL,ss/F of Selpercatinib was reported.

Time frame: Period 2: Day 9 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post dose); Day 10 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24 hours post dose)