Healthy
Conditions
Keywords
Healthy Subjects
Brief summary
The purpose of this study is to assess the effect of omeprazole on the pharmacokinetics of dasatinib in healthy subjects and to assess the safety and tolerability of a single dose of dasatinib before and after 5 days of dosing with omeprazole in healthy subjects
Interventions
DRUGDasatinib + Omeprazole
Tablet/Capsule, Oral, (Dasatinib 100 mg)/(Omeprazole 40 mg), once daily, 7 days
Sponsors
Bristol-Myers Squibb
Study design
Allocation
NON_RANDOMIZED
Intervention model
SINGLE_GROUP
Primary purpose
SUPPORTIVE_CARE
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 50 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy subjects as determined by medical history, physical examination, ECGs, and clinical laboratory determinations
Exclusion criteria
* Women who are pregnant or breastfeeding * Prior exposure to dasatinib
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Dasatinib Pharmacokinetic (PK) Parameter: Maximum Observed Plasma Concentration (Cmax) | Day 1 and Day 6 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours post dose | Pharmacokinetics is a branch of pharmacology concerned with the rate at which drugs are absorbed, distributed, metabolized, and eliminated by the body. Cmax=maximum observed plasma concentration of dasatinib |
| Dasatinib PK Parameter Time of Maximum Observed Plasma Concentration(Tmax) | Day 1 and Day 6 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours post dose | Pharmacokinetics is a branch of pharmacology concerned with the rate at which drugs are absorbed, distributed, metabolized, and eliminated by the body. Tmax=time of maximum observed plasma concentration |
| Dasatinib PK Parameter: Plasma Half-Life (T-HALF) | Day 1 and Day 6 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours post dose | Pharmacokinetics is a branch of pharmacology concerned with the rate at which drugs are absorbed, distributed, metabolized, and eliminated by the body. T-Half=plasma half-life |
| Dasatinib PK Parameter: Area Under the Plasma Concentration-Time Curve From Time Zero to the Time of the Last Quantifiable Concentration (AUC[0-T]) | Day 1 and Day 6 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours post dose | area under the plasma concentration-time curve from time zero to the time of the last quantifiable concentration (AUC\[0-T\])for dasatinib |
| Dasatinib PK Parameters: Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinite Time (AUC[INF]) | Day 1 and Day 6 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours post dose | Pharmacokinetics is a branch of pharmacology concerned with the rate at which drugs are absorbed, distributed, metabolized, and eliminated by the body. AUC(INF)=area under the plasma concentration-time curve from time zero extrapolated to infinite time |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | At Informed Consent (within 21 days of Day 1) through Study Discharge (Day 7) | An AE is defined as any new untoward medical occurrence or worsening of a pre-existing medical condition in a patient or clinical investigation subject administered an investigational (medicinal) product and that does not necessarily have a causal relationship with this treatment. An SAE is any untoward medical occurrence that at any dose results in death, is life-threatening, requires inpatient hospitalization or causes prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, or is an important medical event. |
Countries
United States
Participant flow
Pre-assignment details
49 participants were enrolled in the study, and 35 discontinued before being treated (26 no longer met study criteria, 6 withdrew consent, 3 group full/not needed)
Participants by arm
| Arm | Count |
|---|---|
| Dasatinib/Omeprazole Day 1: 100-mg oral dasatinib; Days 2 through 6: 40-mg oral omeprazole; Day 6:100-mg oral dasatinib and 40-mg oral omeprazole | 14 |
| Total | 14 |
Withdrawals & dropouts
| Period | Reason | FG000 |
|---|---|---|
| Overall Study | Withdrawal by Subject | 1 |
Baseline characteristics
| Characteristic | Dasatinib/Omeprazole |
|---|---|
| Age Continuous | 37 years STANDARD_DEVIATION 6 |
| Body Mass Index (BMI) | 25.4 kg/m2 STANDARD_DEVIATION 2.9 |
| Race/Ethnicity, Customized Asian | 1 participants |
| Race/Ethnicity, Customized Black | 8 participants |
| Race/Ethnicity, Customized White | 5 participants |
| Sex: Female, Male Female | 1 Participants |
| Sex: Female, Male Male | 13 Participants |
Adverse events
| Event type | EG000 affected / at risk |
|---|---|
| deaths Total, all-cause mortality | — / — |
| other Total, other adverse events | 4 / 14 |
| serious Total, serious adverse events | 0 / 14 |
Outcome results
Primary
Dasatinib Pharmacokinetic (PK) Parameter: Maximum Observed Plasma Concentration (Cmax)
Pharmacokinetics is a branch of pharmacology concerned with the rate at which drugs are absorbed, distributed, metabolized, and eliminated by the body. Cmax=maximum observed plasma concentration of dasatinib
Time frame: Day 1 and Day 6 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours post dose
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Dasatinib (Day 1) | Dasatinib Pharmacokinetic (PK) Parameter: Maximum Observed Plasma Concentration (Cmax) | 65.58 ng/mL | Full Range 51 |
| Dasatinib + Omeprazole (Day 6) | Dasatinib Pharmacokinetic (PK) Parameter: Maximum Observed Plasma Concentration (Cmax) | 38.64 ng/mL | Full Range 76 |
Primary
Dasatinib PK Parameter: Area Under the Plasma Concentration-Time Curve From Time Zero to the Time of the Last Quantifiable Concentration (AUC[0-T])
area under the plasma concentration-time curve from time zero to the time of the last quantifiable concentration (AUC\[0-T\])for dasatinib
Time frame: Day 1 and Day 6 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours post dose
| Arm | Measure | Value (GEOMETRIC_MEAN) |
|---|---|---|
| Dasatinib (Day 1) | Dasatinib PK Parameter: Area Under the Plasma Concentration-Time Curve From Time Zero to the Time of the Last Quantifiable Concentration (AUC[0-T]) | 249.46 ng∙h/mL |
| Dasatinib + Omeprazole (Day 6) | Dasatinib PK Parameter: Area Under the Plasma Concentration-Time Curve From Time Zero to the Time of the Last Quantifiable Concentration (AUC[0-T]) | 137.49 ng∙h/mL |
Primary
Dasatinib PK Parameter: Plasma Half-Life (T-HALF)
Pharmacokinetics is a branch of pharmacology concerned with the rate at which drugs are absorbed, distributed, metabolized, and eliminated by the body. T-Half=plasma half-life
Time frame: Day 1 and Day 6 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours post dose
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| Dasatinib (Day 1) | Dasatinib PK Parameter: Plasma Half-Life (T-HALF) | 4.00 hours | Standard Deviation 1.35 |
| Dasatinib + Omeprazole (Day 6) | Dasatinib PK Parameter: Plasma Half-Life (T-HALF) | 4.29 hours | Standard Deviation 1.62 |
Primary
Dasatinib PK Parameters: Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinite Time (AUC[INF])
Pharmacokinetics is a branch of pharmacology concerned with the rate at which drugs are absorbed, distributed, metabolized, and eliminated by the body. AUC(INF)=area under the plasma concentration-time curve from time zero extrapolated to infinite time
Time frame: Day 1 and Day 6 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours post dose
| Arm | Measure | Value (GEOMETRIC_MEAN) |
|---|---|---|
| Dasatinib (Day 1) | Dasatinib PK Parameters: Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinite Time (AUC[INF]) | 265.40 ng∙h/mL |
| Dasatinib + Omeprazole (Day 6) | Dasatinib PK Parameters: Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinite Time (AUC[INF]) | 152.84 ng∙h/mL |
Primary
Dasatinib PK Parameter Time of Maximum Observed Plasma Concentration(Tmax)
Pharmacokinetics is a branch of pharmacology concerned with the rate at which drugs are absorbed, distributed, metabolized, and eliminated by the body. Tmax=time of maximum observed plasma concentration
Time frame: Day 1 and Day 6 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours post dose
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| Dasatinib (Day 1) | Dasatinib PK Parameter Time of Maximum Observed Plasma Concentration(Tmax) | 0.75 hours |
| Dasatinib + Omeprazole (Day 6) | Dasatinib PK Parameter Time of Maximum Observed Plasma Concentration(Tmax) | 1.00 hours |
Secondary
Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations
An AE is defined as any new untoward medical occurrence or worsening of a pre-existing medical condition in a patient or clinical investigation subject administered an investigational (medicinal) product and that does not necessarily have a causal relationship with this treatment. An SAE is any untoward medical occurrence that at any dose results in death, is life-threatening, requires inpatient hospitalization or causes prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, or is an important medical event.
Time frame: At Informed Consent (within 21 days of Day 1) through Study Discharge (Day 7)
| Arm | Measure | Group | Value (NUMBER) |
|---|---|---|---|
| Dasatinib (Day 1) | Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | SAE | 0 Participants |
| Dasatinib (Day 1) | Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | Number of Participants with ≥1 AE | 3 Participants |
| Dasatinib (Day 1) | Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | Death | 0 Participants |
| Dasatinib (Day 1) | Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | Discontinuation due to AEs | 0 Participants |
| Dasatinib + Omeprazole (Day 6) | Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | Discontinuation due to AEs | 0 Participants |
| Dasatinib + Omeprazole (Day 6) | Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | SAE | 0 Participants |
| Dasatinib + Omeprazole (Day 6) | Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | Number of Participants with ≥1 AE | 2 Participants |
| Dasatinib + Omeprazole (Day 6) | Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | Death | 0 Participants |
| Dasatinib + Omeprazole (Day 6) | Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | Death | 0 Participants |
| Dasatinib + Omeprazole (Day 6) | Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | Number of Participants with ≥1 AE | 2 Participants |
| Dasatinib + Omeprazole (Day 6) | Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | SAE | 0 Participants |
| Dasatinib + Omeprazole (Day 6) | Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | Discontinuation due to AEs | 0 Participants |
| All Participants | Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | Death | 0 Participants |
| All Participants | Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | Number of Participants with ≥1 AE | 4 Participants |
| All Participants | Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | Discontinuation due to AEs | 0 Participants |
| All Participants | Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations | SAE | 0 Participants |