Healthy ParticipantsPhase 1NCT05032690
Evaluation of the Relative Bioavailability of Bosutinib Capsules Under Fed Condition and Estimation of Food Effect on Orally Administered Bosutinib Capsule
A Phase 1 study testing Bosutinib capsule and Bosutinib in people with Healthy Participants, run by Pfizer at 1 site in Belgium.
Trial summary
This study is intended to estimate the bioavailability of a single 100 mg bosutinib capsules relative to four 25 mg capsules under fed condition in adult healthy participants and to estimate the effect of a high-fat, high-calorie meal on the bioavailability of a single 100 mg capsule of bosutinib relative to fasted… Read more about this study
- Who is it for?
- Ages 18 to 55 yearsHealthy volunteers can take part
- Conditions the study is for
- Healthy Participants
- What is being tested?
- Bosutinib capsule and Bosutinib
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 32 participants
- Where
- 1 siteBelgium
- Study dates
- 19 Jan 2022to 25 Jun 2022
- Phase
- Phase 1
- Are there results?
- Yes, posted in the registrySummary in the doctors' view
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 55 years
- All sexes
- Healthy volunteers accepted
- Adult
Who may be able to join
- Female participants of non-childbearing potential and/or male participants must be 18 to 55 years of age, inclusive, at the time of signing the informed consent document (ICD)
- participants who are overtly healthy as determined by medical evaluation including a detailed medical history, complete physical examination, vital signs which include BP and pulse rate measurement, clinical laboratory tests, and electrocardiogram (ECG).
- Participants who are willing and able to comply with all scheduled visits, treatment plan, laboratory tests, lifestyle considerations, and other study procedures
Who cannot join
- Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurological, dermatological, or allergic disease.
- Any condition possibly affecting drug absorption (eg, gastrectomy, cholecystectomy).
- History of human immunodeficiency virus (HIV) infection, hepatitis B, or hepatitis C; positive testing for HIV, HBsAg,hepatitis B surface antigen (HBcAb) or hepatitis C antibody (HCVAb).
- Participants with ANY of the following abnormalities in clinical laboratory tests at screening, as assessed by the study-specific laboratory and confirmed by a single repeat test, if deemed necessary:
- estimated glomerular filtration rate (eGFR) (Chronic Kidney Disease Epidemiology Collaboration [CKD-EPI]) <90 mL/min/1.73 m2;
- aspartate aminotransferase (AST) or alanine aminotransferase (ALT) level >upper limit of normal (ULN);
- Serum (total and direct) bilirubin level > ULN; participants with a history of Gilbert's syndrome may have direct bilirubin measured and would be eligible for this study provided the direct bilirubin level is <= ULN;
- Amylase and lipase level > ULN.
Trial locations and contacts
1 site in 1 country.
Belgium1 site
Pfizer Clinical Research Unit - Brussels
Brussels, Bruxelles-capitale, Région de, B-1070
About this study
Official title: A PHASE 1, RANDOMIZED, OPEN-LABEL, 3-PERIOD, 4-SEQUENCE, CROSSOVER, SINGLE-DOSE STUDY TO COMPARE THE BIOAVAILABILITY OF ORALLY ADMINISTERED BOSUTINIB CAPSULES AND TO ESTIMATE THE EFFECT OF FOOD ON BOSUTINIB CAPSULE
This study is intended to estimate the bioavailability of a single 100 mg bosutinib capsules relative to four 25 mg capsules under fed condition in adult healthy participants and to estimate the effect of a high-fat, high-calorie meal on the bioavailability of a single 100 mg capsule of bosutinib relative to fasted condition in adults healthy participants. The comparisons will be performed using the pharmacokinetic parameters that define the rate and extend of absorption (Cmax, AUC). Statistical analyses will be performed after the administration of a single 100 mg dose under fed condition as the Reference treatment and the four 25 mg capsules as the Test treatment for the first comparison, and after administration of a single 100 mg dose under fasted condition as the Reference treatment and the 100 mg capsule under fed condition as the Test treatment for the second comparison.
- Conditions
- Healthy Participants
- Being tested
- Bosutinib capsule, Bosutinib
- Keywords
- Bioavailability, Food Effect, Bosutinib, Maximum Observed Plasma Concentration (Cmax), Area Under the Curve (AUC)
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
Bosutinib capsuleDrug
Bosutinib four 25 mg capsule taken after a high-fat and high calorie breakfast
Bosutinib capsuleDrug
Bosutinib 100 mg capsule taken after a high-fat and high calorie breakfast
BosutinibDrug
Bosutinib 100 mg capsule taken after an overnight fast of at least 10 hours
Bosutinib capsuleDrug
Bosutinib 100 mg capsule taken after a high-fat and high-calorie breakfast
| Study group | Role | What they receive |
|---|---|---|
| Treatment B: Bosutinib four 25 mg capsule after meal | Experimental | Bosutinib four 25 mg capsule taken after a high-fat and high-calorie breakfast for comparison 1 Receives: Drug: Bosutinib capsule |
| Treatment A: Bosutinib 100 mg capsule after meal (active comparator) | Active comparator | Bosutinib 100 mg capsule taken after a high-fat and high-calorie breakfast for comparison 1 Receives: Drug: Bosutinib capsule |
| Treatment A: Bosutinib 100 mg capsule after meal (experimental) | Experimental | Bosutinib 100 mg capsule taken after a high-fat and high-calorie breakfast for comparison 2 Receives: Drug: Bosutinib capsule |
| Treatment C: Bosutinib 100 mg capsule after fasting | Active comparator | Bosutinib 100 mg capsule taken after an overnight fast of at least 10 hours for comparison 2 Receives: Drug: Bosutinib |
What is being measured
The primary outcome is the main question the study is designed to answer.
Area Under the Concentration-time Curve From Time 0 to Infinity (AUCinf) for Bosutinib
AUCinf was calculated as [AUClast+(Clast*/kel)], where AUClast is the area under the plasma concentration-time profile from time 0 to the time of the Clast, Clast is the last quantifiable concentration, Clast* is the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis, and kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve. The geometric coefficient of variation was reported as percentage
Measured: Predose (0 hour) and at 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, and 144 hours post bosutinib dose
Maximum Observed Plasma Concentration (Cmax) for Bosutinib
Cmax was the maximum observed plasma concentration. The geometric coefficient of variation was reported as percentage.
Measured: Predose (0 hour) and at 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, and 144 hours post bosutinib dose
Secondary outcomes (7)
Area Under the Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration (AUClast) for Bosutinib
AUClast was the area under the concentration-time curve from time 0 to the time of the last quantifiable concentration.
Measured: Predose (0 hour) and at 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, and 144 hours post bosutinib dose
Time for Cmax (Tmax) of Bosutinib
Tmax was the time to reach maximum observed plasma concentration and was observed directly from data as time of the first occurrence.
Measured: Predose (0 hour) and at 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, and 144 hours post bosutinib dose
Apparent Clearance After Oral Dose (CL/F) of Bosutinib
CL/F was the apparent clearance after oral dose and was determined as dose/AUCinf. The geometric coefficient of variation was reported as percentage.
Measured: Predose (0 hour) and at 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, and 144 hours post bosutinib dose
Apparent Volume of Distribution After Oral Dose (Vz/F) of Bosutinib
Vz/F was the apparent volume of distribution after oral dose. It was determined as dose/(AUCinf × kel), where kel was the terminal elimination phase rate constant calculated by a linear regression of the log-linear concentration time curve. The geometric coefficient of variation was reported as percentage.
Measured: Predose (0 hour) and at 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, and 144 hours post bosutinib dose
Terminal Elimination Half-Life (t1/2) of Bosutinib
t½ was the terminal elimination plasma half-life. It was determined as Loge(2)/kel, where kel was the terminal elimination phase rate constant calculated by a linear regression of the log-linear concentration-time curve.
Measured: Predose (0 hour) and at 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, and 144 hours post bosutinib dose
Number of Participants With Laboratory Abnormalities (Without Regard to Baseline Abnormality)
Laboratory tests included hematology tests, chemistry tests, and urinalysis tests. Laboratory parameters with at least 1 occurrence meeting the pre-defined criteria are reported for this outcome measure.
Measured: On Days 4, 5, 7 of Periods 1 and 2 for all participants, on Period 3 Days 4, 5, 7 for participants who were assigned to treatment sequences A=>B=>C and B=>A=>C, and at early termination/discontinuation (if applicable)
Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
TEAEs are those with initial onset or that worsen in severity after the first dose of the study medication. All AEs in the table below were TEAEs. An SAE is any untoward medical occurrence at any dose that: results in death; is life threatening (immediate risk of death); requires inpatient hospitalization or prolongation of existing hospitalization; results in persistent or significant disability/incapacity (substantial disruption of the ability to conduct normal life functions); results in congenital anomaly/birth defect; or that is considered to be an important medical event. Severe AEs were defined as AEs that interfered significantly with participant's usual function. Both SAEs and severe AEs were according to the investigator's assessment.
Measured: Post first dose on Period 1 Day 1 up to 28 days post the last dose of study intervention (up to a maximum of 75 days)
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted2 Sep 2021
- Study start19 Jan 2022
- Primary completion25 Jun 2022
- Study completion25 Jun 2022
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Posted resultsParticipant flow, outcome measures and adverse events reported by the sponsor.
- Other trials for Healthy ParticipantsStudies of the same condition, open and under way.
- More trials run by PfizerThe sponsor's other registered studies.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Basic science
- Allocation
- Randomised
- Intervention model
- Crossover
- Model description
- A Phase 1, open-label, randomized, single dose, 3-period, 4 sequence, crossover study in healthy participants
- Masking
- None (open label)
- Enrolment
- 32 participants (actual)
Sponsor and investigators
- Lead sponsor
- Pfizer
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
- Investigators
- Pfizer CT.gov Call Center, Study director, Pfizer
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT05032690
- Sponsor's protocol ID
- B1871062
- Other IDs
- 2021-004911-24
- Status last verified
- May 2024
- First submitted
- 27 Aug 2021
- Last updated
- 20 Sep 2024
- Results posted
- Yes, on ClinicalTrials.gov
- FDA-regulated drug
- Yes
- FDA-regulated device
- No
- Individual data sharing
- No: Pfizer will provide access to individual de-identified participant data and related study documents (e.g. protocol, Statistical Analysis Plan (SAP), Clinical Study Report (CSR)) upon request from qualified researchers, and subject to certain criteria, conditions, and exceptions. Further details on Pfizer's data sharing criteria and process for requesting access can be found at: https://www.pfizer.com/science/clinical\_trials/trial\_data\_and\_results/data\_requests.
Study at a glance
From the registry record, last updated by the sponsor on 20 Sep 2024. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- A PHASE 1, RANDOMIZED, OPEN-LABEL, 3-PERIOD, 4-SEQUENCE, CROSSOVER, SINGLE-DOSE STUDY TO COMPARE THE BIOAVAILABILITY OF ORALLY ADMINISTERED BOSUTINIB CAPSULES AND TO ESTIMATE THE EFFECT OF FOOD ON BOSUTINIB CAPSULE
- ClinicalTrials.gov ID
- NCT05032690
- Acronym / sponsor ID
- B1871062
- Conditions
- Healthy Participants
- Keywords
- Bioavailability, Food Effect, Bosutinib, Maximum Observed Plasma Concentration (Cmax), Area Under the Curve (AUC)
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 32 participants (actual)
- Lead sponsor
- PfizerIndustry (pharma, biotech, devices)
- Study start
- 19 Jan 2022 (actual)
- Primary completion
- 25 Jun 2022 (actual)
- Study completion
- 25 Jun 2022 (actual)
- First posted
- 2 Sep 2021 (actual)
- Results
- Posted 20 Sep 2024
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
This study is intended to estimate the bioavailability of a single 100 mg bosutinib capsules relative to four 25 mg capsules under fed condition in adult healthy participants and to estimate the effect of a high-fat, high-calorie meal on the bioavailability of a single 100 mg capsule of bosutinib relative to fasted condition in adults healthy participants. The comparisons will be performed using the pharmacokinetic parameters that define the rate and extend of absorption (Cmax, AUC). Statistical analyses will be performed after the administration of a single 100 mg dose under fed condition as the Reference treatment and the four 25 mg capsules as the Test treatment for the first comparison, and after administration of a single 100 mg dose under fasted condition as the Reference treatment and the 100 mg capsule under fed condition as the Test treatment for the second comparison.
Study design
- Primary purpose
- Basic science
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Number of arms
- 4
- Model description
- A Phase 1, open-label, randomized, single dose, 3-period, 4 sequence, crossover study in healthy participants
| Arm | Type | Receives |
|---|---|---|
| Treatment B: Bosutinib four 25 mg capsule after meal | Experimental | Drug: Bosutinib capsuleBosutinib four 25 mg capsule taken after a high-fat and high-calorie breakfast for comparison 1 |
| Treatment A: Bosutinib 100 mg capsule after meal (active comparator) | Active comparator | Drug: Bosutinib capsuleBosutinib 100 mg capsule taken after a high-fat and high-calorie breakfast for comparison 1 |
| Treatment A: Bosutinib 100 mg capsule after meal (experimental) | Experimental | Drug: Bosutinib capsuleBosutinib 100 mg capsule taken after a high-fat and high-calorie breakfast for comparison 2 |
| Treatment C: Bosutinib 100 mg capsule after fasting | Active comparator | Drug: BosutinibBosutinib 100 mg capsule taken after an overnight fast of at least 10 hours for comparison 2 |
Who may qualify
- Ages
- 18 to 55 years
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (3 listed)
- Female participants of non-childbearing potential and/or male participants must be 18 to 55 years of age, inclusive, at the time of signing the informed consent document (ICD)
- participants who are overtly healthy as determined by medical evaluation including a detailed medical history, complete physical examination, vital signs which include BP and pulse rate measurement, clinical laboratory tests, and electrocardiogram (ECG).
- Participants who are willing and able to comply with all scheduled visits, treatment plan, laboratory tests, lifestyle considerations, and other study procedures
Key exclusion criteria (8 listed)
- Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurological, dermatological, or allergic disease.
- Any condition possibly affecting drug absorption (eg, gastrectomy, cholecystectomy).
- History of human immunodeficiency virus (HIV) infection, hepatitis B, or hepatitis C; positive testing for HIV, HBsAg,hepatitis B surface antigen (HBcAb) or hepatitis C antibody (HCVAb).
- Participants with ANY of the following abnormalities in clinical laboratory tests at screening, as assessed by the study-specific laboratory and confirmed by a single repeat test, if deemed necessary:
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| Bosutinib capsuleBosutinib four 25 mg capsule taken after a high-fat and high calorie breakfast | Drug | Treatment B: Bosutinib four 25 mg capsule after meal |
| Bosutinib capsuleBosutinib 100 mg capsule taken after a high-fat and high calorie breakfast | Drug | Treatment A: Bosutinib 100 mg capsule after meal (active comparator) |
| BosutinibBosutinib 100 mg capsule taken after an overnight fast of at least 10 hours | Drug | Treatment C: Bosutinib 100 mg capsule after fasting |
| Bosutinib capsuleBosutinib 100 mg capsule taken after a high-fat and high-calorie breakfast | Drug | Treatment A: Bosutinib 100 mg capsule after meal (experimental) |
Primary outcome
Area Under the Concentration-time Curve From Time 0 to Infinity (AUCinf) for Bosutinib
Time frame: Predose (0 hour) and at 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, and 144 hours post bosutinib dose
AUCinf was calculated as [AUClast+(Clast*/kel)], where AUClast is the area under the plasma concentration-time profile from time 0 to the time of the Clast, Clast is the last quantifiable concentration, Clast* is the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis, and kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve. The geometric coefficient of variation was reported as percentage
Maximum Observed Plasma Concentration (Cmax) for Bosutinib
Time frame: Predose (0 hour) and at 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, and 144 hours post bosutinib dose
Cmax was the maximum observed plasma concentration. The geometric coefficient of variation was reported as percentage.
7 secondary outcomes
Area Under the Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration (AUClast) for Bosutinib
Time frame: Predose (0 hour) and at 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, and 144 hours post bosutinib dose
Time for Cmax (Tmax) of Bosutinib
Time frame: Predose (0 hour) and at 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, and 144 hours post bosutinib dose
Apparent Clearance After Oral Dose (CL/F) of Bosutinib
Time frame: Predose (0 hour) and at 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, and 144 hours post bosutinib dose
Apparent Volume of Distribution After Oral Dose (Vz/F) of Bosutinib
Time frame: Predose (0 hour) and at 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, and 144 hours post bosutinib dose
Terminal Elimination Half-Life (t1/2) of Bosutinib
Time frame: Predose (0 hour) and at 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, and 144 hours post bosutinib dose
Number of Participants With Laboratory Abnormalities (Without Regard to Baseline Abnormality)
Time frame: On Days 4, 5, 7 of Periods 1 and 2 for all participants, on Period 3 Days 4, 5, 7 for participants who were assigned to treatment sequences A=>B=>C and B=>A=>C, and at early termination/discontinuation (if applicable)
Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
Time frame: Post first dose on Period 1 Day 1 up to 28 days post the last dose of study intervention (up to a maximum of 75 days)
Results and safety
Loading the posted results from ClinicalTrials.gov…
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 20 Sep 2024.
- Posted resultsParticipant flow, baseline, all outcome measures and adverse events.
- To obtain contact information for a study center near you, click here.Link provided by the sponsor.
- Individual participant dataSharing planned: No. Pfizer will provide access to individual de-identified participant data and related study documents (e.g. protocol, Statistical Analysis Plan (SAP), Clinical Study Report (CSR)) upon request from qualified researchers, and subject to certain criteria, conditions, and exceptions. Further details on Pfizer's data sharing criteria and process for requesting access can be found at: https://www.pfizer.com/science/clinical_trials/trial_data_and_results/data_requests.
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Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
Pfizer CT.gov Call Center study director
Pfizer
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing Bosutinib capsule and Bosutinib in people with Healthy Participants, run by Pfizer at 1 site in Belgium.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 3 inclusion and 8 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 20 Sep 2024. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 1 site in Belgium. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
Yes. Results are posted in the registry (first posted 20 Sep 2024). A summary is in the For doctors view, and the full results are on ClinicalTrials.gov.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Area Under the Concentration-time Curve From Time 0 to Infinity (AUCinf) for Bosutinib (time frame: Predose (0 hour) and at 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, and 144 hours post bosutinib dose). The study lists 2 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 20 Sep 2024.