Bioavailability of Bosutinib Administered as Capsule Contents Mixed With Applesauce or Yogurt Relative to Intact Capsules Under Fed Condition

NCT04916769 | Completed Phase 1 Results FDA Drug

• 2 other identifiers: B18710632021-000500-38
• Study Type: interventional
• Target: 18
• Locations: 1 country
• Sites: 1

Brief Summary

This study is intended to estimate the relative bioavailability of a single 500 mg dose of bosutinib when administered as capsule contents mixed with applesauce or yogurt to intact capsules under fed condition in adult healthy participants. The comparisons will be performed using the pharmacokinetic parameters that define the rate and extent of absorption, those are Cmax and AUC. Statistical analyses will be performed comparing these parameters calculated after administration of a single 500 mg dose with the intact capsule formulation (100 mg x 5) as the Reference treatment and the capsule contents mixed with applesauce or yogurt (100 mg x 5) as the Test treatments.

Conditions

Healthy Participants

Keywords

Bioavailability; bosutinib; Maximum Observed Plasma Concentration (Cmax); Area Under the Curve (AUC)

Outcome Measures

Primary Outcomes (2)

• 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.

  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.

  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

  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 to Reach Maximum Observed Plasma Concentration (Tmax) for Bosutinib

  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) for Bosutinib

  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) for Bosutinib

  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 Phase Half-life (t½ ) for Bosutinib

  Predose (0 hour) and at 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, and 144 hours post bosutinib dose

Study Arms (3)

Bosutinib capsule contents mixed with applesauce

EXPERIMENTAL

Bosutinib capsule contents mixed with applesauce to healthy participants

Drug: Bosutinib capsule

Bosutinib capsule contents mixed with yogurt

EXPERIMENTAL

Bosutinib capsule contents mixed with yogurt to healthy participants

Drug: Bosutinib capsule

Bosutinib intact capsules

ACTIVE COMPARATOR

Bosutinib intact capsules to healthy participants

Drug: Bosutinib capsule

Interventions

Bosutinib capsule DRUG

500 mg dose of bosutinib capsule contents mixed with applesauce

Bosutinib capsule contents mixed with applesauce

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Female participants of non childbearing potential and/or male participants must be 18 to 54 years of age, inclusive, at the time of signing the informed consent document (ICD).
• Capable of giving signed informed consent as described in Appendix 1, which includes compliance with the requirements and restrictions listed in the ICD and in this protocol.

You may not qualify if:

• 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.
• 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 levels \> ULN.

Sponsors & Collaborators

• Pfizer: lead

Study Sites (1)

Pfizer Clinical Research Unit - Brussels

Brussels, Bruxelles-capitale, Région de, B-1070, Belgium

Location

Related Links

• To obtain contact information for a study center near you, click here.

MeSH Terms

Interventions

bosutinib

Results Point of Contact

• Title: Pfizer ClinicalTrials.gov Call Center
• Organization: Pfizer, Inc.

ClinicalTrials.gov_Inquiries@pfizer.com

1-800-718-1021

Study Officials

• Pfizer CT.gov Call Center

  Pfizer

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: Yes
• Restriction Type: OTHER
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: A Phase 1, open-label, randomized, single dose, 3-period, 6-sequence, crossover study in healthy participants

Study Record Dates

• First Submitted: June 1, 2021
• First Posted: June 8, 2021
• Study Start: August 13, 2021
• Primary Completion: January 27, 2022
• Study Completion: January 27, 2022
• Last Updated: November 7, 2024
• Results First Posted: November 7, 2024

Record last verified: 2024-11

Data Sharing

• IPD Sharing: Will not share

Locations

BE (1)