Healthy
Conditions
Brief summary
The purposes of this study are to determine: * If there are any differences in the amount of baricitinib in the blood/body when taken in two different forms. * How a high-fat, high-calorie meal affects the amount of baricitinib in the blood/body. * The safety and tolerability of baricitinib. The study has two parts. Individuals will participate in only one part. Participants will be admitted to the clinical research unit (CRU) and will be discharged from the CRU following the completion of 3 overnight stays. Each part of this study will last from 8-10 days, not including screening. Follow-up will occur 7 to 14 days after the last dose of baricitinib.
Interventions
DRUGBaricitinib suspension
Administered orally
DRUGBaricitinib tablet
Administered orally
Sponsors
Eli Lilly and Company
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
* Are overtly healthy males or females, as determined by medical history and physical examination * Women not of child-bearing potential * Have a body mass index (BMI) of 18.5 to 29.9 kilograms per meter squared (kg/m²) inclusive, at screening
Exclusion criteria
* Have received live vaccine(s) within 3 months of screening, or intend to during the study * Have a current or recent history (less than \[\<\] 30 days prior to screening and/or \<45 days prior to Day -1 in Period 1) of a clinically significant bacterial, fungal parasitic, viral (not including rhinopharyngitis), or mycobacterial infection
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Baricitinib Following a Single Oral Dose | Predose, 0.25 hour (hr), 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 9 hr, 12 hr, 24 hr, 36 hr, 48 hr postdose | PK: Cmax of baricitinib after a single oral dose |
| PK: Area Under the Concentration Versus Time Curve From Time Zero to the Last Time Point With a Measurable Concentration (AUC[0-tlast]) of Baricitinib Following a Single Oral Dose | Predose, 0.25 hour (hr), 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 9 hr, 12 hr, 24 hr, 36 hr, 48 hr postdose | PK: AUC(0-tlast) of Baricitinib, measured in hour times nanogram per milliliter (ng\*hr/mL) |
| PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-∞]) of Baricitinib Following a Single Oral Dose | Predose, 0.25 hour (hr), 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 9 hr, 12 hr, 24 hr, 36 hr, 48 hr postdose | PK: AUC(0-∞) of Baricitinib |
Countries
Singapore
Participant flow
Participants by arm
| Arm | Count |
|---|---|
| Part A:All Participants All participants who received study drug during Part A. | 24 |
| Part B: All Participants All participants who received study drug during Part B. | 18 |
| Total | 42 |
Baseline characteristics
| Characteristic | Part A:All Participants | Part B: All Participants | Total |
|---|---|---|---|
| Age, Continuous | 39.9 years STANDARD_DEVIATION 8.5 | 41.1 years STANDARD_DEVIATION 11.3 | 40.4 years STANDARD_DEVIATION 9.7 |
| Body Mass Index (BMI) | 24.14 kilograms per meter squared (kg/m^2) STANDARD_DEVIATION 2.55 | 25.36 kilograms per meter squared (kg/m^2) STANDARD_DEVIATION 3.03 | 24.5 kilograms per meter squared (kg/m^2) STANDARD_DEVIATION 2.8 |
| Ethnicity (NIH/OMB) Hispanic or Latino | 0 Participants | 0 Participants | 0 Participants |
| Ethnicity (NIH/OMB) Not Hispanic or Latino | 24 Participants | 18 Participants | 42 Participants |
| Ethnicity (NIH/OMB) Unknown or Not Reported | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) American Indian or Alaska Native | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Asian | 24 Participants | 17 Participants | 41 Participants |
| Race (NIH/OMB) Black or African American | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) More than one race | 0 Participants | 1 Participants | 1 Participants |
| Race (NIH/OMB) Native Hawaiian or Other Pacific Islander | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Unknown or Not Reported | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) White | 0 Participants | 0 Participants | 0 Participants |
| Region of Enrollment Singapore | 24 Participants | 18 Participants | 42 Participants |
| Sex: Female, Male Female | 1 Participants | 0 Participants | 1 Participants |
| Sex: Female, Male Male | 23 Participants | 18 Participants | 41 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk | EG002 affected / at risk | EG003 affected / at risk | EG004 affected / at risk |
|---|---|---|---|---|---|
| deaths Total, all-cause mortality | 0 / 24 | 0 / 24 | 0 / 24 | 0 / 18 | 0 / 18 |
| other Total, other adverse events | 2 / 24 | 1 / 24 | 4 / 24 | 1 / 18 | 5 / 18 |
| serious Total, serious adverse events | 0 / 24 | 0 / 24 | 0 / 24 | 0 / 18 | 0 / 18 |
Outcome results
Primary
Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Baricitinib Following a Single Oral Dose
PK: Cmax of baricitinib after a single oral dose
Time frame: Predose, 0.25 hour (hr), 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 9 hr, 12 hr, 24 hr, 36 hr, 48 hr postdose
Population: All participants who received at least 1 dose of study drug and had evaluable PK parameters.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A: Baricitinib T1 | Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Baricitinib Following a Single Oral Dose | 49.8 nanograms per milliliter (ng/mL) | Geometric Coefficient of Variation 21 |
| Part A: Baricitinib T2 | Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Baricitinib Following a Single Oral Dose | 49.6 nanograms per milliliter (ng/mL) | Geometric Coefficient of Variation 24 |
| Part A: Baricitinib R | Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Baricitinib Following a Single Oral Dose | 47.8 nanograms per milliliter (ng/mL) | Geometric Coefficient of Variation 25 |
| Part B: Baricitinib TF Fasted | Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Baricitinib Following a Single Oral Dose | 47.9 nanograms per milliliter (ng/mL) | Geometric Coefficient of Variation 22 |
| Part B: Baricitinib TF Fed | Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Baricitinib Following a Single Oral Dose | 32.5 nanograms per milliliter (ng/mL) | Geometric Coefficient of Variation 22 |
Comparison: Bioequivalence of single 4 mg dose of baricitinib as the suspension formulation with (T1) water compared to the commercial tablet (R).95% CI: [0.946, 1.15]
Comparison: Bioequivalence of single 4 mg dose of baricitinib as the suspension formulation without (T2) water compared to the commercial tablet (R).95% CI: [0.944, 1.14]
Comparison: Bioequivalence of single 4 mg dose of baricitinib as fasted vs fed.95% CI: [0.617, 0.74]
Primary
PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-∞]) of Baricitinib Following a Single Oral Dose
PK: AUC(0-∞) of Baricitinib
Time frame: Predose, 0.25 hour (hr), 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 9 hr, 12 hr, 24 hr, 36 hr, 48 hr postdose
Population: All participants who received at least 1 dose of study drug and had evaluable PK parameters.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A: Baricitinib T1 | PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-∞]) of Baricitinib Following a Single Oral Dose | 319 ng*hr/mL | Geometric Coefficient of Variation 19 |
| Part A: Baricitinib T2 | PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-∞]) of Baricitinib Following a Single Oral Dose | 319 ng*hr/mL | Geometric Coefficient of Variation 17 |
| Part A: Baricitinib R | PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-∞]) of Baricitinib Following a Single Oral Dose | 319 ng*hr/mL | Geometric Coefficient of Variation 17 |
| Part B: Baricitinib TF Fasted | PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-∞]) of Baricitinib Following a Single Oral Dose | 284 ng*hr/mL | Geometric Coefficient of Variation 22 |
| Part B: Baricitinib TF Fed | PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-∞]) of Baricitinib Following a Single Oral Dose | 282 ng*hr/mL | Geometric Coefficient of Variation 21 |
Comparison: Bioequivalence of single 4 mg dose of baricitinib as the suspension formulation with (T1) water compared to the commercial tablet (R).95% CI: [0.996, 1.03]
Comparison: Bioequivalence of single 4 mg dose of baricitinib as the suspension formulation with (T1) water compared to the commercial tablet (R).95% CI: [0.966, 1.03]
Comparison: Bioequivalence of single 4 mg dose of baricitinib as fasted vs fed.95% CI: [0.941, 1.02]
Primary
PK: Area Under the Concentration Versus Time Curve From Time Zero to the Last Time Point With a Measurable Concentration (AUC[0-tlast]) of Baricitinib Following a Single Oral Dose
PK: AUC(0-tlast) of Baricitinib, measured in hour times nanogram per milliliter (ng\*hr/mL)
Time frame: Predose, 0.25 hour (hr), 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 9 hr, 12 hr, 24 hr, 36 hr, 48 hr postdose
Population: All participants who received at least 1 dose of study drug and had evaluable PK parameters.
| Arm | Measure | Value (GEOMETRIC_LEAST_SQUARES_MEAN) | Dispersion |
|---|---|---|---|
| Part A: Baricitinib T1 | PK: Area Under the Concentration Versus Time Curve From Time Zero to the Last Time Point With a Measurable Concentration (AUC[0-tlast]) of Baricitinib Following a Single Oral Dose | 314 ng*hr/mL | Geometric Coefficient of Variation 19 |
| Part A: Baricitinib T2 | PK: Area Under the Concentration Versus Time Curve From Time Zero to the Last Time Point With a Measurable Concentration (AUC[0-tlast]) of Baricitinib Following a Single Oral Dose | 315 ng*hr/mL | Geometric Coefficient of Variation 17 |
| Part A: Baricitinib R | PK: Area Under the Concentration Versus Time Curve From Time Zero to the Last Time Point With a Measurable Concentration (AUC[0-tlast]) of Baricitinib Following a Single Oral Dose | 216 ng*hr/mL | Geometric Coefficient of Variation 18 |
| Part B: Baricitinib TF Fasted | PK: Area Under the Concentration Versus Time Curve From Time Zero to the Last Time Point With a Measurable Concentration (AUC[0-tlast]) of Baricitinib Following a Single Oral Dose | 281 ng*hr/mL | Geometric Coefficient of Variation 22 |
| Part B: Baricitinib TF Fed | PK: Area Under the Concentration Versus Time Curve From Time Zero to the Last Time Point With a Measurable Concentration (AUC[0-tlast]) of Baricitinib Following a Single Oral Dose | 273 ng*hr/mL | Geometric Coefficient of Variation 20 |
Comparison: Bioequivalence of single 4 mg dose of baricitinib as the suspension formulation with (T1) water compared to the commercial tablet (R).95% CI: [0.963, 1.03]
Comparison: Bioequivalence of s single 4 mg dose of baricitinib as the suspension formulation without (T2) water compared to the commercial tablet (R).95% CI: [0.995, 1.03]
Comparison: Bioequivalence of single 4 mg dose of baricitinib as fasted vs fed.95% CI: [0.936, 1.01]