NCT05338476

Brief Summary

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.

Trial Health

87
On Track

Trial Health Score

Automated assessment based on enrollment pace, timeline, and geographic reach

Enrollment
16

participants targeted

Target at below P25 for phase_1 healthy

Timeline
Completed

Started Jul 2018

Shorter than P25 for phase_1 healthy

Geographic Reach
1 country

1 active site

Status
completed

Health score is calculated from publicly available data and should be used for screening purposes only.

Trial Relationships

Click on a node to explore related trials.

Study Timeline

Key milestones and dates

Study Start

First participant enrolled

July 12, 2018

Completed
20 days until next milestone

Primary Completion

Last participant's last visit for primary outcome

August 1, 2018

Completed
2 months until next milestone

Study Completion

Last participant's last visit for all outcomes

September 18, 2018

Completed
3.6 years until next milestone

First Submitted

Initial submission to the registry

April 19, 2022

Completed
2 days until next milestone

First Posted

Study publicly available on registry

April 21, 2022

Completed
3.5 years until next milestone

Results Posted

Study results publicly available

October 20, 2025

Completed
Last Updated

October 20, 2025

Status Verified

October 1, 2025

Enrollment Period

20 days

First QC Date

April 19, 2022

Results QC Date

September 1, 2025

Last Update Submit

October 1, 2025

Conditions

Healthy

Outcome Measures

Primary Outcomes (9)

  • 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.

    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.

    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: 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.

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

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

    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: 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.

    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: Apparent Terminal Elimination Rate Constant (Kel) of Midazolam and Its Metabolite 1-OH-midazolam

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

    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: Apparent Terminal Elimination Half-life (t½) of Midazolam and Its Metabolite 1-OH-midazolam

    PK: t½ of midazolam and its metabolite 1-OH-midazolam was reported.

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

    PK: CL/F of midazolam was reported.

    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: Apparent Volume of Distribution During the Terminal Elimination Phase (Vz/F) of Midazolam

    PK: Vz/F of midazolam was reported.

    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)

Secondary Outcomes (8)

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

    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

    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

    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

    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

    Period 2: Predose at Day 1, Day 2, Day 3, Day 4, Day 5, Day 6, Day 7, Day 8, Day 9

  • +3 more secondary outcomes

Study Arms (2)

Period 1: Midazolam

EXPERIMENTAL

* Day 1: Participants received single oral dose of 2 milligram (mg) midazolam syrup.

Drug: Midazolam

Period 2: Selpercatinib + Midazolam

EXPERIMENTAL

* Day 1 to Day 9: Participants received 160 mg Selpercatinib capsules twice daily (BID). * Day 10: Participant received 160 mg Selpercatinib capsules BID co-administered with a single oral dose of 2 mg midazolam syrup on the morning of Day 10.

Drug: MidazolamDrug: Selpercatinib

Interventions

MidazolamDRUG

Administered orally.

Period 1: MidazolamPeriod 2: Selpercatinib + Midazolam
SelpercatinibDRUG

Administered orally.

Also known as: LY3527723, LOXO-292
Period 2: Selpercatinib + Midazolam

Eligibility Criteria

Age18 Years - 55 Years
Sexall
Healthy VolunteersYes
Age GroupsAdult (18-64)

You may qualify if:

  • 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

You may not qualify if:

  • 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

Contact the study team to confirm eligibility.

Sponsors & Collaborators

Study Sites (1)

Celerion

Tempe, Arizona, 85283, United States

Location

MeSH Terms

Interventions

Midazolamselpercatinib

Intervention Hierarchy (Ancestors)

BenzodiazepinesBenzazepinesHeterocyclic Compounds, 2-RingHeterocyclic Compounds, Fused-RingHeterocyclic Compounds

Results Point of Contact

Title
Chief Medical Officer
Organization
Eli Lilly and Company
ClinicalTrials.gov@lilly.com
08005455979

Study Officials

  • 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 DIRECTOR

Publication Agreements

PI is Sponsor Employee
No
Restriction Type
GT60
Restrictive Agreement
Yes

Study Design

Study Type
interventional
Phase
phase 1
Allocation
NON RANDOMIZED
Masking
NONE
Purpose
BASIC SCIENCE
Intervention Model
SEQUENTIAL
Sponsor Type
INDUSTRY
Responsible Party
SPONSOR

Study Record Dates

First Submitted

April 19, 2022

First Posted

April 21, 2022

Study Start

July 12, 2018

Primary Completion

August 1, 2018

Study Completion

September 18, 2018

Last Updated

October 20, 2025

Results First Posted

October 20, 2025

Record last verified: 2025-10

Data Sharing

IPD Sharing
Will not share

Locations

US(1)