Healthy
Conditions
Keywords
Selpercatinib, Food, Pharmacokinetics
Brief summary
The main purpose of this study is to learn about how food affects selpercatinib in healthy participants. The selpercatinib will be administered in fed and fasted states. Participation could last about 7 weeks.
Interventions
DRUGSelpercatinib
Administered orally.
Sponsors
Eli Lilly and Company
Loxo Oncology, Inc.
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
21 Years to 65 Years
Healthy volunteers
Yes
Inclusion criteria
* Participants who are overtly healthy as determined by medical evaluation including medical history, physical examination, vital signs and clinical laboratory tests.
Exclusion criteria
* 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.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Pharmacokinetics(PK): Area Under the Plasma Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Selpercatinib | PK: Day 1 and Day 8: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, and 72 hours (h) postdose; | PK: 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 Selpercatinib | PK: Day 1 and Day 8: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, and 72 hours (h) postdose; | PK: AUC\[0-tlast\] of Selpercatinib |
| PK: Maximum Concentration (Cmax) of Selpercatinib | PK: Day 1 and Day 8: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, and 72 hours (h) postdose; | PK: Cmax of Selpercatinib. |
Countries
Singapore
Participant flow
Participants by arm
| Arm | Count |
|---|---|
| Selpercatinib 160 mg Selpercatinib will be administered orally on Day 1 in fasted state or fed state and on Day 8 in fed state or fasted state. | 46 |
| Total | 46 |
Withdrawals & dropouts
| Period | Reason | FG000 | FG001 |
|---|---|---|---|
| Period 1 | Physician Decision | 0 | 1 |
| Period 1 | Withdrawal by Subject | 1 | 0 |
Baseline characteristics
| Characteristic | Selpercatinib |
|---|---|
| Age, Continuous | 40.6 years STANDARD_DEVIATION 9.2 |
| Ethnicity (NIH/OMB) Hispanic or Latino | 0 Participants |
| Ethnicity (NIH/OMB) Not Hispanic or Latino | 46 Participants |
| Ethnicity (NIH/OMB) Unknown or Not Reported | 0 Participants |
| Race (NIH/OMB) American Indian or Alaska Native | 0 Participants |
| Race (NIH/OMB) Asian | 45 Participants |
| Race (NIH/OMB) Black or African American | 0 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 | 1 Participants |
| Region of Enrollment Singapore | 46 Participants |
| Sex: Female, Male Female | 10 Participants |
| Sex: Female, Male Male | 36 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk |
|---|---|---|
| deaths Total, all-cause mortality | 0 / 45 | 0 / 45 |
| other Total, other adverse events | 29 / 45 | 21 / 45 |
| serious Total, serious adverse events | 0 / 45 | 0 / 45 |
Outcome results
Primary
Pharmacokinetics(PK): Area Under the Plasma Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Selpercatinib
PK: AUC\[0-∞\] of Selpercatinib'
Time frame: PK: Day 1 and Day 8: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, and 72 hours (h) postdose;
Population: All participants who received doses of study drug on Day 1 and Day 8 and had evaluable PK data.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Selpercatinib Fasted (Reference) | Pharmacokinetics(PK): Area Under the Plasma Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Selpercatinib | 23400 nanogram * hour per milliliter (ng*hr/mL | Geometric Coefficient of Variation 32 |
| Selpercatinib Fed (Test) | Pharmacokinetics(PK): Area Under the Plasma Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Selpercatinib | 22500 nanogram * hour per milliliter (ng*hr/mL | Geometric Coefficient of Variation 44 |
90% CI: [0.876, 1.03]
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: PK: Day 1 and Day 8: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, and 72 hours (h) postdose;
Population: All participants who received doses of study drug on Day 1 and Day 8 and had evaluable PK data.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Selpercatinib Fasted (Reference) | PK: Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Measured Concentration Value (AUC[0-tlast]) of Selpercatinib | 22700 ng*hr/mL | Geometric Coefficient of Variation 32 |
| Selpercatinib Fed (Test) | PK: Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Measured Concentration Value (AUC[0-tlast]) of Selpercatinib | 21700 ng*hr/mL | Geometric Coefficient of Variation 46 |
90% CI: [0.869, 1.04]
Primary
PK: Maximum Concentration (Cmax) of Selpercatinib
PK: Cmax of Selpercatinib.
Time frame: PK: Day 1 and Day 8: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, and 72 hours (h) postdose;
Population: All participants who received doses of study drug on Day 1 and Day 8 and had evaluable PK data.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Selpercatinib Fasted (Reference) | PK: Maximum Concentration (Cmax) of Selpercatinib | 1840 nanograms per milliliter (ng/mL) | Geometric Coefficient of Variation 39 |
| Selpercatinib Fed (Test) | PK: Maximum Concentration (Cmax) of Selpercatinib | 1540 nanograms per milliliter (ng/mL) | Geometric Coefficient of Variation 45 |
90% CI: [0.744, 0.925]