Phase 1
Completed N=30
Bioavailability of Apixaban Sprinkle Compared to Apixaban Capsules
Healthy Volunteers
Source: ClinicalTrials.gov NCT03509883 ↗
Enrolled (actual)
30
Serious AEs
0.0%
Results posted
Jan 2020
Primary outcomePrimary: Concentration as Measured by Maximum Observed Plasma Concentration (Cmax) — 77.4; 99.3 ng/mL
Summary
The purpose of this study is to evaluate the absorption of apixaban (BMS-562247) into the bloodstream of healthy volunteers, when administered as sprinkle capsules compared to tablets. Eligible participants will be randomly assigned to 1 of 2 treatment sequences and will receive a single oral dose of apixaban twice during the course of the study.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Concentration as Measured by Maximum Observed Plasma Concentration (Cmax) |
77.4; 99.3 | — |
| PRIMARY AUC (0-T) - Area Under the Plasma Concentration-time Curve From Time Zero to Time of Last Quantifiable Concentration |
695.9; 769.2 | — |
| PRIMARY AUC (INF) - Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinite Time |
714.7; 787.9 | — |
| SECONDARY Tmax - Time of Maximum Observed Plasma Concentration |
2.30; 0.98 | — |
| SECONDARY T-Half - Terminal Plasma Half Life. |
8.81; 7.91 | — |
| SECONDARY Frel - Relative Bioavailability |
110.24 | — |
| SECONDARY Number of Participants With Adverse Events Regardless of Causality, Serious Adverse Events and Adverse Events Leading to Discontinuation |
7; 3; 0; 0; 0; 0 | — |
| SECONDARY Physical Measurement - Height |
173.23; 165.86 | — |
| SECONDARY Physical Measurement - Weight |
78.09; 165.86; 77.83; 71.47; 76.15; 70.64 | — |
| SECONDARY Physical Measurement - Body Mass Index (BMI) |
22.96; 25.85; 25.87; 25.84; 25.31; 25.55 | — |
| SECONDARY Number of Participants With a Given Clinical Laboratory Abnormality |
0; 0; 0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Out-of Range Vital Signs: Blood Pressure |
0; 0; 0; 0; 0; 1 | — |
| SECONDARY Number of Participants With Out-of Range Vital Signs: Heart Rate (Bpm) |
0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Out-of Range Vital Signs: Respiration Rate |
1; 1; 0; 0; 1; 1 | — |
| SECONDARY Number of Participants With Out-of Range Vital Signs: Temperature |
0; 0; 0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Out-of Range ECG Evaluations |
30; 30; 0; 0; 29; 30 | — |
Eligibility Criteria
Inclusion Criteria
- Signed informed consent form.
- Healthy male and female participants determined by no clinically significant deviation from normal in medical history, physical examination, 12-lead ECGs (electrocardiograms), vital signs and clinical laboratory determinations.
- Women of childbearing potential (WOCBP) must have negative serum pregnancy tests (performed at screening and Day 1), must not be breastfeeding, and must agree to follow instructions for method(s) of contraception for duration of treatment with study drug apixaban, and for a total of 33 days after last dose of apixaban.
- Males sexually active with women of childbearing potential must agree to follow instructions for method(s) of contraception for duration of treatment with study drug apixaban, and for a total of 93 days after the last dose of apixaban; and must be willing to refrain from sperm donation during this time.
- Body mass index (BMI) of 18.0 to 30.0 kg/m², inclusive. Body mass index = weight (kg)/[height(m)]².
Exclusion Criteria
- History of chronic headaches (occurring 15 days or more a month) over the previous 3 months.
- History of gastroesophageal reflux disease, dyspepsia, protracted nausea, or chronic diarrhea.
- History or evidence of abnormal bleeding or coagulation disorders, hypermenorrhea, intracranial hemorrhage, or abnormal bleeding or coagulation disorders.
- Inability to comply with restrictions and prohibited treatments (e.g. women currently taking hormonal contraception).
- Use of tobacco- or nicotine-containing products (e.g. cigarettes, pipes, cigars, chewing tobacco, nicotine patches, nicotine lozenges, nicotine gum) within 6 months prior to study drug administration.
- Donation of blood to a blood bank or in a clinical study (except screening or follow-up visit) within 4 weeks of study drug administration (within 2 weeks for plasma only).
Other protocol defined inclusion/exclusion criteria could apply.
Data sourced from ClinicalTrials.gov (NCT03509883). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.