Phase 1 Bioavailability Study of Apixaban Solution Formulation Relative to Apixaban Tablets in Healthy Subjects

Phase 1

Completed

• Conditions: Healthy Volunteers
• Interventions: Drug: Apixaban

• Registration Number: NCT02034565
• Lead Sponsor: Bristol-Myers Squibb

Brief Summary

The purpose of this study is to assess the oral bioavailability of Apixaban solution formulation (Treatment B, 10 mg as 25 mL x 0.4 mg/mL) relative to Apixaban tablets (Treatment A, 10 mg as 2 x 5 mg tablets) in healthy subjects.

Detailed Description

Not available

Study Timeline

• Study Start: 2010-02
• Primary Completion: 2010-03
• Study Completion: 2010-03
• Study First Submitted: 2014-01-10
• Study First Submitted QC: 2014-01-10
• Study First Posted: 2014-01-13
• Status Verified: 2016-07
• Results First Submitted: 2016-07-07
• Results First Submitted QC: 2016-07-07
• Last Update Submitted: 2016-07-07
• Results First Posted: 2016-08-22
• Last Update Posted: 2016-08-22

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 48

Inclusion Criteria

• Healthy subjects as determined by no clinically significant deviation from normal in medical history, physical examination, ECGs, and clinical laboratory determinations

Exclusion Criteria

• Any significant acute or chronic medical illness or relevant trauma (e.g., history of chronic hypertension, bacterial endocarditis, hemorrhagic stroke, motor vehicle accident resulting in significant head trauma or internal injuries)
• History or evidence of abnormal bleeding or coagulation disorder (e.g., easy bruising or gingival bleeding, prolonged bleeding after dental extraction, postpartum, or after trauma, wounds or surgery)

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
Treatment A: Apixaban tablet	Apixaban	Apixaban Film coated Tablet Single dose 10 mg orally
Treatment B: Apixaban oral solution	Apixaban	Apixaban Solution Single dose 10 mg orally

Primary Outcome Measures

Name	Time	Method
Adjusted Geometric Mean of the Maximum Observed Plasma Concentration (Cmax) of Apixaban	Pre-dose and 0.25, 0.50, 1, 2, 3, 4, 5, 6, 9, 12, 24, 36, 48, 60, 72 hours post-dose per intervention	Serial blood samples for pharmacokinetic analysis were collected at selected times up to 72 hours after each dose. Maximum observed plasma concentration (Cmax) is measured in nanograms per milliliter (ng/mL)
Adjusted Geometric Mean of the Area Under the Plasma Concentration-Time Curve (AUC) From Time Zero Extrapolated to Infinite Time AUC(INF) of Apixaban	Pre-dose and 0.25, 0.50, 1, 2, 3, 4, 5, 6, 9, 12, 24, 36, 48, 60, 72 hours post-dose per intervention	Serial blood samples for pharmacokinetic analysis were collected at selected times up to 72 hours after each dose. AUC(INF) is measured in nanogram hours per milliliter (ng\*h/mL)
Adjusted Geometric Mean of the Area Under the Plasma Concentration-Time Curve From Time Zero to the Time of the Last Quantifiable Concentration [AUC(0-T)] of Apixaban	Pre-dose and 0.25, 0.50, 1, 2, 3, 4, 5, 6, 9, 12, 24, 36, 48, 60, 72 hours post-dose per intervention	Serial blood samples for pharmacokinetic analysis were collected at selected times up to 72 hours after each dose. AUC(0-T) is measured in nanogram hours per milliliter (ng\*h/mL)

Secondary Outcome Measures

Name	Time	Method
Number of Participants With Serious Adverse Events (SAEs), Treatment-Related Adverse Events (AEs), Deaths or Discontinuation of Study Drug Due to AEs	Day 1 to 30 days after last dose of study drug	AE=any new unfavorable symptom, sign or disease or worsening of a preexisting condition that may not have a causal relationship with treatment. SAE=a medical event that at any dose results in death, persistent or significant disability/incapacity or drug dependency/abuse; is life-threatening, an important medical event or a congenital anomaly/birth defect; or requires or prolongs hospitalization. Treatment-related=having certain, probable, possible or missing relationship to study drug. Death=during the study and up to 28 days past study discontinuation. The select AEs were determined using the Medical Dictionary for Regulatory Activities (MedDRA, v13).
Number of Participants With Marked Laboratory Abnormalities	Pre-study screen (Day -1) to Day 8 or day of study discharge	Clinical laboratory tests were performed pre-study and at selected times throughout the study. Marked laboratory abnormalities were defined as laboratory assessments meeting the following investigator-specified criteria: Leukocytes \< 0.9\* lower limits of normal (LLN), absolute neutrophils + bands \<= 1.500 10\*3 cells/microliter, white blood cells (WBC) urine value \>= 2+. These laboratory abnormalities were not considered clinically significant and therefore not adverse events.

Trial Locations

Locations (1)

Mds Pharma Services; 🇺🇸 Neptune, New Jersey, United States