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A Relative Bioavailability Study of Selpercatinib (LY3527723) in Healthy Participants

An Open-Label, Randomized Study to Evaluate the Relative Bioavailability of Selpercatinib in 3 Formulations for Pediatric Use

Status
Completed
Phases
Phase 1
Study type
Interventional
Source
ClinicalTrials.gov
Registry ID
NCT05136404
Enrollment
42
Registered
2021-11-29
Start date
2021-12-03
Completion date
2022-03-14
Last updated
2025-03-17

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy

Brief summary

The main purpose of this study is to compare the amount of selpercatinib that gets into the blood stream and how long it takes the body to get rid of it, when given as three different formulations in adult healthy participants. The information about any adverse effects experienced will be collected and the tolerability of selpercatinib will also be evaluated. The study may last up to 59 days including the 28 days of screening period.

Interventions

DRUGSelpercatinib

Administered orally

Sponsors

Eli Lilly and Company
CollaboratorINDUSTRY
Loxo Oncology, Inc.
Lead SponsorINDUSTRY

Study design

Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
BASIC_SCIENCE
Masking
NONE

Eligibility

Sex/Gender
ALL
Age
21 Years to No maximum
Healthy volunteers
Yes

Inclusion criteria

* Participants who are overtly healthy as determined by medical evaluation including medical history, physical examination, and vital signs * Body mass index (BMI) within the range 18.0 to 35.0 kilograms per meter squared (kg/m²)

Exclusion criteria

* Have a history of allergic reactions to medications or food products * Have a clinically significant abnormality of blood pressure and/or pulse rate as determined by the investigator * Clinically significant abnormalities on ECG as determined by the investigator or prolongation of the QTcB or QTcF \>450 msec at screening * Have clinically significant active cardiovascular disease or history of myocardial infarction within 6 months prior to the planned start of selpercatinib * Have a history or presence of cardiovascular, respiratory, renal, gastrointestinal, endocrine, hematological, or neurological disorders capable of significantly altering the absorption, metabolism, or elimination of drugs; of constituting a risk when taking the investigational product; or of interfering with the interpretation of data. Appendectomy, splenectomy, and cholecystectomy are considered as acceptable * Use of H2 blockers, proton pump inhibitors, and other drugs that affect selpercatinib exposure within 7 days of screening * Are intending to use over-the-counter or prescription medication, including dietary supplements, within 14 days prior to dosing and until study discharge (apart from occasional acetaminophen (≤2 g/24 hours), hormonal contraception, or hormone replacement therapy)

Design outcomes

Primary

MeasureTime frameDescription
Pharmacokinetics (PK): Maximum Concentration (Cmax) of SelpercatinibDays 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours (h) postdosePK: Cmax of Selpercatinib
PK: Area Under the Plasma Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of SelpercatinibDays 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 h postdosePK AUC\[0-∞\] of Selpercatinib
PK: Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Measured Concentration Value (AUC[0-tlast]) of SelpercatinibDays 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 h postdosePK: AUC\[0-tlast\] of Selpercatinib
PK: Time to Maximum Observed Concentration (Tmax) of SelpercatinibDays 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 h postdosePK: Tmax of Selpercatinib

Countries

United States

Participant flow

Participants by arm

ArmCount
20 mg Selpercatinib
Participants were randomized to 1 of 3 treatment sequences and will receive single doses of 20 mg Selpercatinib on each of Days 1, 8, and 15 as either the RTU suspension, the PFOS, or the capsule. Sequence A: Period 1: 20 milligram (mg) Selpercatinib capsule single oral dose administered orally on Day 1. Period 2: 20 mg per milliliter (mL) Selpercatinib Powder for Oral suspension (PFOS) single oral suspension dose on Day 8. Period 3: 20 mg/mL Selpercatinib Ready to Use (RTU) single oral suspension on Day 15. Sequence B: Period 1: 20 mg/mL Selpercatinib RTU single oral suspension on Day 1. Period 2: 20 mg Selpercatinib capsule single oral dose administered orally on Day 8. Period 3: 20 mg/mL PFOS single oral suspension dose on Day 15. Sequence C: Period 1: 20 mg/mL PFOS single oral suspension dose on Day 1. Period 2: 20 mg/mL Selpercatinib RTU single oral suspension on Day 8. Period 3: 20 mg Selpercatinib capsule single oral dose administered orally on Day 15.
42
Total42

Withdrawals & dropouts

PeriodReasonFG000FG001FG002
Period 1Adverse Event011
Period 2Inappropriate Behavior001
Period 3Adverse Event001

Baseline characteristics

Characteristic20 mg Selpercatinib
Age, Continuous42.0 years
STANDARD_DEVIATION 9.7
Ethnicity (NIH/OMB)
Hispanic or Latino
20 Participants
Ethnicity (NIH/OMB)
Not Hispanic or Latino
22 Participants
Ethnicity (NIH/OMB)
Unknown or Not Reported
0 Participants
Race (NIH/OMB)
American Indian or Alaska Native
1 Participants
Race (NIH/OMB)
Asian
1 Participants
Race (NIH/OMB)
Black or African American
11 Participants
Race (NIH/OMB)
More than one race
0 Participants
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
0 Participants
Race (NIH/OMB)
Unknown or Not Reported
0 Participants
Race (NIH/OMB)
White
29 Participants
Region of Enrollment
United States
42 Participants
Sex: Female, Male
Female
13 Participants
Sex: Female, Male
Male
29 Participants

Adverse events

Event typeEG000
affected / at risk
EG001
affected / at risk
EG002
affected / at risk
deaths
Total, all-cause mortality
0 / 390 / 410 / 41
other
Total, other adverse events
0 / 390 / 410 / 41
serious
Total, serious adverse events
0 / 390 / 410 / 41

Outcome results

Primary

Pharmacokinetics (PK): Maximum Concentration (Cmax) of Selpercatinib

PK: Cmax of Selpercatinib

Time frame: Days 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours (h) postdose

Population: All participants who received at least one dose of Selpercatinib and have evaluable pharmacokinetic (PK) data.

ArmMeasureValue (GEOMETRIC_MEAN)Dispersion
20 mg Selpercatinib Capsule (Reference)Pharmacokinetics (PK): Maximum Concentration (Cmax) of Selpercatinib176 nanograms per milliliter (ng/mL)Geometric Coefficient of Variation 64.2
20 mg Selpercatinib RTU Suspension (Test)Pharmacokinetics (PK): Maximum Concentration (Cmax) of Selpercatinib174 nanograms per milliliter (ng/mL)Geometric Coefficient of Variation 36.9
20 mg/mL PFOS (Test)Pharmacokinetics (PK): Maximum Concentration (Cmax) of Selpercatinib180 nanograms per milliliter (ng/mL)Geometric Coefficient of Variation 39.8
90% CI: [0.937, 1.08]Mixed Models Analysis
90% CI: [0.968, 1.11]Mixed Models Analysis
Primary

PK: Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Measured Concentration Value (AUC[0-tlast]) of Selpercatinib

PK: AUC\[0-tlast\] of Selpercatinib

Time frame: Days 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 h postdose

Population: All participants who received at least one dose of study drug and had evaluable PK data.

ArmMeasureValue (GEOMETRIC_MEAN)Dispersion
20 mg Selpercatinib Capsule (Reference)PK: Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Measured Concentration Value (AUC[0-tlast]) of Selpercatinib2180 ng*hr/mLGeometric Coefficient of Variation 36.9
20 mg Selpercatinib RTU Suspension (Test)PK: Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Measured Concentration Value (AUC[0-tlast]) of Selpercatinib2160 ng*hr/mLGeometric Coefficient of Variation 31.6
20 mg/mL PFOS (Test)PK: Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Measured Concentration Value (AUC[0-tlast]) of Selpercatinib2190 ng*hr/mLGeometric Coefficient of Variation 30.8
90% CI: [0.972, 1.06]Mixed Models Analysis
90% CI: [0.992, 1.08]Mixed Models Analysis
Primary

PK: Area Under the Plasma Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Selpercatinib

PK AUC\[0-∞\] of Selpercatinib

Time frame: Days 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 h postdose

Population: All participants who received at least one dose of selpercatinib and have evaluable PK data.

ArmMeasureValue (GEOMETRIC_MEAN)Dispersion
20 mg Selpercatinib Capsule (Reference)PK: Area Under the Plasma Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Selpercatinib2540 nanogram*hour per milliliter (ng*hr/mL)Geometric Coefficient of Variation 28
20 mg Selpercatinib RTU Suspension (Test)PK: Area Under the Plasma Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Selpercatinib2410 nanogram*hour per milliliter (ng*hr/mL)Geometric Coefficient of Variation 29
20 mg/mL PFOS (Test)PK: Area Under the Plasma Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Selpercatinib2490 nanogram*hour per milliliter (ng*hr/mL)Geometric Coefficient of Variation 27
90% CI: [0.953, 1.03]Mixed Models Analysis
90% CI: [0.982, 1.06]Mixed Models Analysis
Primary

PK: Time to Maximum Observed Concentration (Tmax) of Selpercatinib

PK: Tmax of Selpercatinib

Time frame: Days 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 h postdose

Population: All participants who received at least one dose of study drug and had evaluable PK data.

ArmMeasureValue (MEDIAN)
20 mg Selpercatinib Capsule (Reference)PK: Time to Maximum Observed Concentration (Tmax) of Selpercatinib1.50 h
20 mg Selpercatinib RTU Suspension (Test)PK: Time to Maximum Observed Concentration (Tmax) of Selpercatinib1.50 h
20 mg/mL PFOS (Test)PK: Time to Maximum Observed Concentration (Tmax) of Selpercatinib1.50 h
p-value: 0.472890% CI: [-0.5, 0]Sign test
p-value: 0.014290% CI: [-0.5, 0]Sign test

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026