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Apixaban

Phase 3

Deep Vein Thrombosis | Small molecule | Cardiovascular |Bristol-Myers Squibb Company|Last Updated: Oct 3, 2022

Success Probability

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Trial Design

RandomizedDouble-BlindACTIVE_CONTROLLEDDMC
Total Trials2
Total Enrollment8,628

FDA Designations

No designations recorded

Clinical trial landscape

Apixaban · 25 trials · 21 indications

Phase 3 8Phase 2 7Phase 1 10
NCT02369653A Study of the Safety and Effectiveness of Apixaban in Preventing Blood Clots in Children With Leukemia Who Have a Central Venous Catheter and Are Treated With AsparaginaseLymphoma
COMPLETED512 Analytics
NCT00643201Efficacy and Safety Study of Apixaban for the Treatment of Deep Vein Thrombosis or Pulmonary EmbolismVenous Thrombosis
COMPLETED5,614 Analytics
NCT00633893Efficacy and Safety Study of Apixaban for Extended Treatment of Deep Vein Thrombosis or Pulmonary EmbolismVenous Thrombosis
COMPLETED2,711 Analytics
NCT00496769A Phase III Study of Apixaban in Patients With Atrial FibrillationAtrial Fibrillation
COMPLETED6,421 Analytics
NCT00457002Study of Apixaban for the Prevention of Thrombosis-related Events in Patients With Acute Medical IllnessVenous Thrombosis
COMPLETED6,758 Analytics
NCT00452530Study of an Investigational Drug for the Prevention of Thrombosis-related Events Following Knee Replacement SurgeryDeep Vein Thrombosis
COMPLETED3,221 Analytics
NCT00423319Study of an Investigational Drug for the Prevention of Thrombosis-related Events Following Hip Replacement Surgery (ADVANCE-3)Deep Vein Thrombosis
COMPLETED5,407 Analytics
NCT00412984Apixaban for the Prevention of Stroke in Subjects With Atrial FibrillationAtrial Fibrillation
COMPLETED20,976 Analytics
PHASE3COMPLETED
A Study of the Safety and Effectiveness of Apixaban in Preventing Blood Clots in Children With Leukemia Who Have a Central Venous Catheter and Are Treated With Asparaginase
LymphomaUnlock trial analytics
PHASE3COMPLETED
Efficacy and Safety Study of Apixaban for the Treatment of Deep Vein Thrombosis or Pulmonary Embolism
Venous ThrombosisUnlock trial analytics
PHASE3COMPLETED
Efficacy and Safety Study of Apixaban for Extended Treatment of Deep Vein Thrombosis or Pulmonary Embolism
Venous ThrombosisUnlock trial analytics
PHASE3COMPLETED
A Phase III Study of Apixaban in Patients With Atrial Fibrillation
Atrial FibrillationUnlock trial analytics
PHASE3COMPLETED
Study of Apixaban for the Prevention of Thrombosis-related Events in Patients With Acute Medical Illness
Venous ThrombosisUnlock trial analytics
PHASE3COMPLETED
Study of an Investigational Drug for the Prevention of Thrombosis-related Events Following Knee Replacement Surgery
Deep Vein ThrombosisUnlock trial analytics
PHASE3COMPLETED
Study of an Investigational Drug for the Prevention of Thrombosis-related Events Following Hip Replacement Surgery (ADVANCE-3)
Deep Vein ThrombosisUnlock trial analytics
PHASE3COMPLETED
Apixaban for the Prevention of Stroke in Subjects With Atrial Fibrillation
Atrial FibrillationUnlock trial analytics

Study Endpoints

Primary Endpoints

The Number of Participants With Non-Fatal DVT, PE, and CVST, and VTE-Related-Death
From first dose up to approximately 40 days after first dose

The number of participants with non-fatal deep vein thromboses (DVT) (including asymptomatic and symptomatic), pulmonary embolism (PE), cerebral venous sinus thrombosis (CVST); and venous thromboembolism (VTE) related-death objectively confirmed by a blinded, independent adjudication committee. Symptomatic events are included during the intended treatment period. Asymptomatic events are included from scans up to Day 40.

The Number of Participants With Adjudicated Major Bleeding
From first dose up to approximately 34 days after first dose

The number of participants with major bleeding adjudicated by a blinded, independent adjudication committee. Adjudicated major bleeding is defined as bleeding that satisfies one or more of the following criteria: 1. fatal bleeding 2. clinically overt bleeding associated with a decrease in hemoglobin of at least 20g/L (ie, 2g/dL) in a 24-hour period 3. bleeding that is retroperitoneal, pulmonary, intracranial, or otherwise involves the CNS; and/or 4. bleeding that requires surgical intervention in an operating suite, including interventional radiology.

Incidence of Adjudicated Composite of Symptomatic, Recurrent Venous Thromboembolism (VTE) or VTE-Related Death During 6 Months of Treatment
Day 1 to Week 24 + 2 Days or 355 days (Discontinued Early)

VTE: nonfatal deep vein thrombosis (DVT) or nonfatal pulmonary embolism (PE). All events were adjudicated by an ICAC blinded to treatment. DVT assessed by compression ultrasound and/or venography; PE assessed by spiral computed tomography scanning, pulmonary angiography, and/or ventilation/perfusion lung scan. Event rate (proportion of participants): n/N (n=number of participants with observation; N=total number of efficacy evaluable participants). Intended treatment period: longer of the dosing period plus 2 days (completed treatment) or 355 days (discontinued early). Composite endpoint: events at any time from randomization until end of intended treatment, regardless whether drug treatment was received. All randomized participants with a non-missing primary endpoint were summarized. Missing endpoint = outcomes which could not be documented on or after study Day 154. Participants were categorized to the assigned group regardless of the treatment actually received (intent-to-treat).

Adjudicated Composite of Symptomatic, Recurrent Venous Thromboembolism (VTE) or All-Cause Death During the Intended Treatment Period - Randomized Population With Imputation
Day 1 up to 12 Months

VTE included: nonfatal deep vein thrombosis (DVT) or nonfatal pulmonary embolism (PE). All index events, DVT and/or PE were adjudicated/confirmed by a central independent adjudication committee blinded to treatment. DVT assessed by compression ultrasound and/or venography; PE assessed by spiral computed tomography scanning, pulmonary angiography, and/or ventilation/perfusion lung scan. Event rate (proportion of participants with event) calculated as n/N (n=number of events; N=number of participants). Intended treatment period: longer of the dosing period plus 2 days (completed treatment) or 355 days (discontinued early). Composite endpoint included events at any time from randomization until end of the intended treatment period, regardless whether drug treatment was received. For missing endpoint data, participants were imputed as having had a primary efficacy outcome event.

Adjudicated Composite of Symptomatic, Recurrent Venous Thromboembolism (VTE) or All-Cause Death During the Intended Treatment Period - Randomized Population Without Imputation
Day 1 up to 12 months

VTE included: nonfatal DVT or nonfatal PE. Event rate (proportion of participants with event) calculated as n/N (n=number of events; N=number of participants). Intended treatment period: longer of the dosing period plus 2 days (completed treatment) or 355 days (discontinued early). Composite endpoint included events at any time from randomization until end of the intended treatment period, regardless whether drug treatment was received. No imputation was done for these endpoints; participants who had an event during the intended treatment period were counted. Confidence interval (CI) for single event rate was calculated based on the Wald asymptotic confidence limits.

Event Rate of Stroke/Systemic Embolism During the Intended-treatment Period
Randomization to efficacy cutoff date of May 28, 2010 (date revised following cessation of study for superior efficacy)

Event rate=percent of participants with an event divided by the total participants in the arm. Intended-treatment period=date of randomization to the efficacy cutoff date, which was to be the date on which at least 226 unrefuted original primary efficacy events occurred (date revised to May 28, 2010 following cessation of study for superior efficacy.)

Incidence of Composite of Adjudicated Total Venous Thromboembolism (VTE) and VTE-related Death During the Intended Treatment Period - Primary Efficacy Population
Intended Treatment Period

VTE: nonfatal pulmonary embolism (PE), symptomatic deep vein thrombosis (DVT), or asymptomatic proximal DVT detected by ultrasound. VTE-related death: fatal PE or sudden death for which VTE could not be excluded as a cause. Intended Treatment Period=period that started on day of randomization: period ended (for treated) at latter of a) 2 days after last dose of study drug and b) 32 days after first dose of study drug; period ended (for not treated) 32 days after randomization. A bilateral compression ultrasound (CUS) was performed between Days 5 and 14 for detection of asymptomatic proximal DVT unless a symptomatic VTE was confirmed prior. CUS was also performed on Day 30 ± 2 except for those participants who had a confirmed symptomatic VTE or proximal asymptomatic DVT prior to that time. All efficacy events were adjudicated by the Independent Central Adjudication Committee (ICAC). Event rate (%): n/N\*100 (n=number with observation; N=total efficacy evaluable participants).

Incidence of Major Bleeding During the Treatment Period in Treated Participants
Day 1, first dose of study drug, to last dose of study drug plus 2 days

Major bleeding was adjudicated by an ICAC using criteria from the International Society on Thrombosis and Hemostasis (ISTH) and was defined as acute clinically overt bleeding: associated with a fall in hemoglobin of 2 grams per deciliter (g/dL) or more, or leading to a transfusion of 2 or more units of packed red blood cells or 1000 milliliters (mL) or more of whole blood, or bleeding in a critical site or bleeding which is fatal. Incidence determined by Event Rate (%): n/N\*100 (n=number with observation; N=total efficacy evaluable participants).

Incidence of Clinically Relevant Non-Major (CRNM) Bleeding During the Treatment Period in Treated Participants
Day 1, first dose of study drug, to last dose of study drug plus 2 days

Bleeding was adjudicated by an ICAC using criteria from the ISTH. CRNM bleeding: acute clinically overt bleeding compromising hemodynamics; leading to hospitalization; traumatic subcutaneous hematoma; intramuscular hematoma; epistaxis that lasted for more than 5 minutes, was repetitive or led to an intervention; spontaneous gingival bleeding; spontaneous hematuria; macroscopic gastrointestinal hemorrhage (including at least 1 episode of melena or hematemesis, if clinically apparent with positive results on a fecal occult-blood test); rectal blood loss. Treatment Period=includes measurements or events with onset from first dose of study drug through 2 days after the last dose of study drugs for bleeding endpoints. Incidence determined by Event Rate (%): n/N\*100 (n=number with observation; N=total efficacy evaluable participants).

Incidence of Composite of Major or Clinically Relevant Non-Major (CRNM) Bleeding During the Treatment Period in Treated Participants
Day 1, first dose of study drug, to last dose of study drug plus 2 days

Bleeding was adjudicated by an ICAC using criteria from the ISTH. Major bleeding: acute clinically overt bleeding: associated with a fall in hemoglobin of 2 g/dL or more, or leading to a transfusion of 2 or more units of packed red blood cells or 1000 mL or more of whole blood, or bleeding in a critical site or bleeding which is fatal. CRNM bleeding: acute clinically overt bleeding compromising hemodynamics; leading to hospitalization; traumatic subcutaneous hematoma; intramuscular hematoma; epistaxis that lasted for more than 5 minutes, was repetitive or led to an intervention; spontaneous gingival bleeding; spontaneous hematuria; macroscopic gastrointestinal hemorrhage; rectal blood loss. Treatment Period=onset from first dose of study drug through 2 days after last dose of study drugs. Incidence: Event Rate (%): n/N\*100 (n=number with observation; N=total efficacy evaluable participants).

Incidence of All Bleeding During the Treatment Period in Treated Participants
Day 1, first dose of drug to last dose of drug plus 2 days

Bleeding was adjudicated by an ICAC using criteria from the ISTH. Treatment Period=includes measurements or events with onset from first dose of study drug through 2 days after the last dose of study drugs, for bleeding endpoints. Incidence determined by Event Rate (%): n/N\*100 (n=number with observation; N=total efficacy evaluable participants).

Rate of Adjudicated Venous Thromboembolic Event-related and All-cause Deaths With Onset During the Intended-treatment Period
Day of randomization to later of 2 days after last dose or 14 days after first dose; 14 days after randomization for those who did not receive study drug

Event rate=Number of events divided by the number of patients evaluated. Intended treatment period starts on the day of randomization, and for those who received study drug, ends at the later of 2 days after last dose or 14 days after the first dose of study drug; for randomized patients who did not receive study drug, the period ends 14 days after randomization.Venous thromboembolic event (VTE)=nonfatal pulmonary embolism (PE), symptomatic deep vein thrombosis (DVT), or asymptomatic proximal DVT detected by ultrasound. VTE-related death=fatal PE or sudden death for which VTE could not be excluded as a cause.

Rate of Composite of Adjudicated Venous Thromboembolic Event (VTE)-Related (Pulmonary Embolism and Symptomatic and Asymptomatic Deep Vein Thrombosis[DVT]) and All-cause Death During the Intended Treatment Period
Day 1 (first dose of study drug) to later of 2 days after last dose or 38 days after first dose

Event rate=Number of events divided by the number of patients evaluated. A mandatory bilateral ascending contrast venogram was to be obtained on Day 35 (± 3). Patients with confirmed symptomatic DVT at any time, or asymptomatic DVT upon venography, were to receive treatment for DVT according to the investigator's standard of care. Signs and symptoms suggestive of VTE included, but were not limited to: 1) lower extremity DVT: erythema, warmth, pain, swelling, tenderness; and 2) PE: pleuritic chest pain, dyspnea, cough, hemoptysis, syncope, light-headedness/dizziness, tachypnea, and tachycardia. Intended Treatment Period started on day of randomization and, for patients who received treatment, ended at the later of 2 days after last dose of study drug or 38 days after the first dose (presurgery) of study drug. For randomized patients who did not receive study drug, the period ended 38 days after randomization.

Number of Participants With First Event of Ischemic/Unspecified Stroke, Hemorrhagic Stroke, or Systemic Embolism (SE) During the Intended Treatment Period
Time to first event in "Intended Treatment Period": started on day of randomization, ended at efficacy cut-off date (date target number of primary efficacy events [448] was expected to have occurred; set to 30-Jan-2011, prior to unblinding).

All suspected efficacy events were adjudicated by the Central Events Committee (CEC). Diagnosis of stroke=the nontraumatic focal neurological deficit lasting at least 24 hours, and includes ischemic stroke, hemorrhagic stroke, ischemic stroke with hemorrhagic conversion, stroke of uncertain type, and retinal ischemic event (embolism, infarction). Diagnosis of SE=clinical history consistent with an acute loss of blood flow to a peripheral artery (or arteries), supported by evidence of embolism from surgical specimens, autopsy, angiography, vascular imaging, or other objective testing.

Rate of Adjudicated Stroke or Systemic Embolism (SE) During the Intended Treatment Period
"Intended Treatment Period" started on the day of randomization and ended at the efficacy cut-off date (date on which it was expected that the target number of primary efficacy events [448] would have occurred; set to 30-Jan-2011, prior to unblinding).

Rate=Number of adjudicated stroke or SE events per 100 patient years. Diagnosis of stroke=the nontraumatic focal neurological deficit lasting at least 24 hours, and includes ischemic stroke, hemorrhagic stroke, ischemic stroke with hemorrhagic conversion, stroke of uncertain type, and retinal ischemic event (embolism, infarction). Diagnosis of SE=clinical history consistent with an acute loss of blood flow to a peripheral artery (or arteries), supported by evidence of embolism from surgical specimens, autopsy, angiography, vascular imaging, or other objective testing.

Composite of Adjudicated Major or Clinically Relevant Non-Major (CRNM) Bleeding Events
From first dose to 2 days after last dose (Up to approximately 12 months)

The number of participants with adjudicated major or CRNM bleeding events per the Perinatal and Paediatric Haemostasis Subcommittee of International Society on Thrombosis and Haemostasis (ISTH) criteria. Events are adjudicated by a blinded, independent events adjudication committee (EAC). Major bleeding satisfies one or more of the following criteria: fatal bleeding, clinically overt bleeding associated with a decrease in hemoglobin of at least 20 g/L (i.e., 2 g/dL) in a 24-hour period, bleeding that is retroperitoneal, pulmonary, intracranial, or otherwise involves the CNS, or bleeding that requires surgical intervention in an operating suite, including interventional radiology. CRNM bleeding satisfies one or both of the following criteria: overt bleeding for which blood product is administered and not directly attributable to the subject's underlying medical condition or bleeding that requires medical or surgical intervention to restore hemostasis, other than in an operating room.

AUC0-T apixaban
48 hours

Anti-Xa activity values (IIU/mL) will be converted to apixaban concentration data (ng/mL) based on the previously demonstrated linear relationship (e.g. Frost et al., 2014 - PMID: 24697979). The area under the curve (AUC) between administration (time 0) and the last measurable data point (AUC0-T) will be calculated with the 'Lin up/Log down' trapezoidal method. The AUCT-∞ will be obtained from the last measureable concentration divided by λ, and will be summed with AUC0-T to obtain AUC0-∞ (total exposure). the slope (λ) of the terminal phase of the concentration-time profile will be determined by log-linear regression on the appropriate number (typically at least 3) of data points. The terminal (elimination) half-life (t1/2, λ) will be calculated from Ln(2)/λ.

Cmax
48 hours

Apixaban concentration-time profiles will be generated and observed values for the descriptive PK parameter Cmax (peak plasma concentration) will be determined directly from the time-concentration curve

Tmax
48 hours

Apixaban concentration-time profiles will be generated and observed values for the descriptive PK parameter time to Cmax (Tmax)) will be determined directly from the time-concentration curve

Number of Participants With Incidence of Major Bleeding
Day 1 post-op/standard of care first medication dose to day 90 (+/-14 days) post-op/standard of care

The International Society on Thrombosis and Hemostasis criteria (ISTH) will be used to assess incidence of major bleeding. Participants were monitored for up to 90 days. This is the number of participants who have had at least one major bleeding incidence during the time of observation.

Number of Participants With Incidence of Clinically Relevant Non Major Bleeding Events
Day 1 post-op/standard of care first dose of medication to day 90 (+/- 14 days) post-op/standard of care

Participants were monitored for up to 90 days. This is the number of participants with bleeding events that did not meet the ISTH criteria but still required intervention. This is the number of participants who had at least one non-major bleeding event during the time of observation.

Number of Participants With Composite of Confirmed Major Bleeding and Clinically Relevant Nonmajor (CRNM) Bleeding
From first dose to 2 days following last dose of study drug

Major bleeding was defined as clinically overt bleeding accompanied by 1 or more of the following: * A decrease in hemoglobin of 20 g/L or more or * Required transfusion of 2 or more units of packed red blood cells or whole blood, or * Occurred in a critical site * Contributed to death. CRNM bleeding was defined as bleeding that did not meet the criteria for major bleeding but that, in routine clinical practice, would be considered relevant and not trivial by a patient and physician. Such bleeding satisfied a priori criteria defined by the ICAC, including: * Skin hematoma * Epistaxis that lasted for longer than 5 minutes, was repetitive, or led to an intervention * Hematuria that was macroscopic and either spontaneous or lasted for longer than 24 hours after instrumentation of the urogenital tract * Any other bleeding type that was considered to have clinical consequences.

Event Rate of Composite of Adjudicated Major Bleeding and Clinically Relevant Non-Major Bleeding During the Treatment Period- Treated Participants With Placebo or Apixaban Low Doses
From first dose of study drug (Day 1) to last dose plus 2 days, up to Year 2 of the Study

Bleeding was assessed using the International Society on Thrombosis and Hemostasis (ISTH) guidelines. Events were adjudicated by the Clinical Events Committee (CEC). Event rate was number of participants with events divided by the number of participants treated, measured as a percentage (%). The primary outcome is based on data for the placebo and 2 apixaban low-dose groups (2.5 mg BID and 10 mg QD) combined across Phase A and Phase B. The analyses of Phase B data across all doses of apixaban are secondary because of the premature termination of the apixaban high-dose groups (10mg BID, 20mg QD) and the resulting lower duration of exposure for these groups.

The composite of symptomatic recurrent venous thromboembolism (i.e., recurrent deep-vein thrombosis or fatal or non-fatal pulmonary embolism and deterioration of the thrombotic burden as assessed by repeat bilateral
compression ultrasound and perfusion lung scan.
Determine the dose-response relationship among the 3 QD and 3 BID doses of BMS-562247 on the composite endpoint of adjudicated VTE events and all-cause death in subjects treated with study medication for 12 +/-2 days following surgery
throughout the study
Maximum observed concentration (Cmax)
Days 1-11
Area under the plasma concentration-time curve from time zero extrapolated to infinite time (AUC(INF))
Days 1-11
Area under the plasma concentration-time curve from time zero to the time of the last quantifiable concentration (AUC(0-T))
Days 1-11
Adjusted Geometric Mean of Maximum Observed Plasma Concentration (Cmax) of Apixaban
Days 1, 5, and 9 predose and 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 24, 36, 48, 60 and 72 hours post dose

Maximum observed plasma concentration (Cmax) measured in nanograms per milliliter (ng/mL)

Adjusted Geometric Mean of Area Under the Plasma Concentration-time Curve (AUC) From Time Zero Extrapolated to Infinite Time [AUC(INF)] of Apixaban
Days 1, 5, and 9 predose and 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 24, 36, 48, 60, and 72 hours post dose

Area Under the Plasma Concentration-time Curve (AUC) From Time of Zero Extrapolated to Infinite Time (INF) \[AUC (INF)\] is measured as nanograms multiplied by hours per milliliter (ng\*h/mL)

Adjusted Geometric Mean of Area Under the Plasma Concentration-time Curve (AUC) From Time Zero to the Time of the Last Quantifiable Concentration [AUC(0-T)] of Apixaban
Days 1, 5, and 9 predose and 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 24, 36, 48, 60, and 72 hours post dose

Area Under the Plasma Concentration-time Curve (AUC) From Time Zero to the Last Quantifiable Concentration \[AUC (0-T)\] is measured as nanograms multiplied by hours per milliliter (ng\*h/mL)

Pharmacodynamic (PD) Parameter: Adjusted Mean Change in Endogenous Thrombin Potential (ETP) From Day 4 Pre-Infusion (PCC or Placebo) Baseline at Day 4, 30 Minutes Post Infusion of PCC or Placebo
Day 4 at 3 hours post apixaban dose and prior to infusion (Pre-infusion Baseline), Day 4 at 30 minutes post infusion (PCC or Placebo)

ETP was evaluated using a Thrombin Generation Assay (TGA), a validated automated ex vivo assay performed on platelet-poor plasma samples and based on the automated, calibrated thrombin generation method: thrombin formation was triggered with recombinant tissue factor and phospholipids. Thrombin concentration in each sample was calculated over time by measuring the cleavage of a fluorogenic substrate in the context of a paired calibration sample. Dedicated software (Thrombinoscope, Thrombinoscope B.V., Maastricht, The Netherlands) performed the calculations and derived ETP as area under the curve from the resulting "thrombogram" curve. Pre-infusion baseline= sample on Day 4, 3 hours post apixaban dose (just prior to IV infusion of PCC or placebo). Samples on Day 4 were obtained at 0 (pre-dose), 0.5, 1, 2, 3 hours post apixaban dose and at 0.5, 1, 2, 4, 6, 9, 21, 45, and 69 hours post infusion (PCC or Placebo) in each treatment period. ETP was measured as nanomolar\*minute (nM\*min).

PD Parameter: Adjusted Mean Change in Endogenous Thrombin Potential (ETP) From Day 1 Pre-Dose Apixaban Baseline at Day 4, 30 Minutes Post Infusion of PCC or Placebo
Day 1 pre-dose apixaban (pre-apixaban Baseline), Day 4 at 30 minutes post infusion (PCC or Placebo)

ETP was evaluated using a Thrombin Generation Assay (TGA), a validated automated ex vivo assay performed on platelet-poor plasma samples and based on the automated, calibrated thrombin generation method: thrombin formation was triggered with recombinant tissue factor and phospholipids. Thrombin concentration in each sample was calculated over time by measuring the cleavage of a fluorogenic substrate in the context of a paired calibration sample. A dedicated software program (Thrombinoscope, Thrombinoscope B.V., Maastricht, The Netherlands) performed the calculations and derived ETP as area under the curve from the resulting "thrombogram" curve. Pre-dose Apixaban baseline was Day 1 pre-dose (0 hour). Samples on Day 4 were obtained at 0, 0.5, 1, 2, 3 hours post apixaban dose and at 0.5, 1, 2, 4, 6, 9, 21, 45, and 69 hours post infusion (PCC or Placebo) in each treatment period.

Estimated area under the plasma concentration-time curve [AUC(INF)] of Apixaban
Up to 26 hours, post dose (from Day 1 to Day 2)
Maximum estimated plasma concentration (Cmax) of Apixaban
Up to 26 hours, post dose (from Day 1 to Day 2)
Estimated time at which maximum plasma concentration occurs (Tmax) of Apixaban
Up to 26 hours, post dose (from Day 1 to Day 2)
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 for each intervention

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 for each intervention

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 for each intervention

AUC(0-T) is measured in nanogram hours per milliliter (ng\*h/mL)

Adjusted Geometric Mean Maximum Observed Plasma Concentration (Cmax) of Apixaban
Day 1 (0 h, 0.25h, 0.50h, 1h, 2h, 3h, 4h, 5h, 6h, 9h, 12h, 24h, 36h, 48h, 60h, and 72h post dose) in Periods 1, 2 and 3

Samples of plasma from participants were obtained at the following times: 0 hour (h) and post dose at 0.25h, 0.50h, 1h, 2h, 3h, 4h, 5h, 6h, 9h, 12h, 24h, 36h, 48h, 60h, and 72h. Apixaban was assayed using a validated Liquid chromatography tandem mass spectrometry (LC-MS/MS) method during the period of known analyte stability. Maximum observed plasma concentration (Cmax) was measured in nanograms per milliliter (ng/mL).

Geometric Mean of Maximum Observed Plasma Concentration (Cmax) of Single 5mg Oral Dose of Apixaban
24 hours pre-dose to 72 hours post-dose

Maximum observed plasma concentration (Cmax) was measured by plasma concentration of apixaban over time. The geometric means are reported in nanograms per milliliter (ng/mL).

Geometric Mean of Maximum Observed Plasma Concentration (Cmax) of Metabolite BMS-730823
From 24 hours pre-dose to 72 hours post-dose

Maximum observed plasma concentration (Cmax) was measured by plasma concentration of BMS-730823 over time. The geometric means are reported in nanograms per milliliter (ng/mL).

Geometric Mean of Area Under the Concentration-time Curve From Time Zero to Time of the Last Quantifiable Concentration (AUC(0-T)) of Single 5mg Oral Dose of Apixaban
24 hours pre-dose to 72 hours post-dose

Area under the concentration-time curve from time zero to time of the last quantifiable concentration (AUC(0-T)) was measured by plasma concentration of apixaban over time. The geometric means are reported in nanogram hours per milliliter (ng\*h/mL).

Geometric Mean of Area Under the Concentration-time Curve From Time Zero to Time of the Last Quantifiable Concentration (AUC(0-T)) of Metabolite BMS-730823
From 24 hours pre-dose to 72 hours post-dose

Area under the concentration-time curve from time zero to time of the last quantifiable concentration (AUC(0-T)) was measured by plasma concentration of BMS-730823 over time. The geometric means are reported in nanogram hours per milliliter (ng\*h/mL).

Geometric Mean of Area Under the Concentration-time Curve From Time Zero Extrapolated to Infinite Time (AUC(INF)) of Single 5mg Oral Dose of Apixaban
From 24 hours pre-dose to 72 hours post-dose

The area under the concentration-time curve from time zero extrapolated to infinite time (AUC(INF)) was measured by plasma concentration of apixaban over time. The geometric means are reported in nanogram hours per milliliter (ng\*h/mL).

Geometric Mean of Area Under the Concentration-time Curve From Time Zero Extrapolated to Infinite Time (AUC(INF)) of BMS-730823
24 hours pre-dose to 72 hours post-dose

The area under the concentration-time curve from time zero extrapolated to infinite time (AUC(INF)) was measured by plasma concentration of BMS-730823 over time. The geometric means are reported in nanogram hours per milliliter (ng\*h/mL).

Mean Plasma Terminal Half-life (T-Half) of Single 5mg Oral Dose of Apixaban
From 24 hours pre-dose to 72 hours post-dose

Plasma terminal half-life (T-Half) for apixaban was derived from plasma concentrations versus time data. Means were reported in hours.

Mean Plasma Terminal Half-life (T-Half) of BMS-730823
24 hours pre-dose to 72 hours post-dose

Mean plasma terminal half-life (T-Half) for BMS-730823 was derived from plasma concentrations versus time data.

Median Time of Maximum Observed Plasma Concentration (Tmax) of a Single 5 mg Oral Dose of Apixaban
From 24 hours pre-dose to 72 hours post-dose

Time of maximum observed plasma concentration (Tmax) for apixaban was derived from plasma concentrations versus time data. Medians were reported in hours.

Median Time of Maximum Observed Plasma Concentration (Tmax) of Metabolite BMS-730823
From 24 hours pre-dose to 72 hours post-dose

Time of maximum observed plasma concentration (Tmax) for BMS-730823 was derived from plasma concentrations versus time data. Medians were reported in hours.

Geometric Mean of Area Under the Plasma Concentration-Time Curve From 2 to 6 Hours (AUC(2-6)) for Apixaban
2 to 6 hours post-dose

Area under the plasma concentration-time curve from 2 hours to 6 hours (AUC(2-6) for Apixaban was measured in participants with ESRD during dialysis in Period 1 only. Geometric Means were reported in nanogram hours per milliliter (ng\*hr/mL) and were determined from blood samples both entering and exiting the dialyzer.

Geometric Mean of Area Under the Plasma Concentration-Time Curve From 2 to 6 Hours (AUC(2-6)) for BMS-730823
2 to 6 hours post-dose

Area under the plasma concentration-time curve from 2 hours to 6 hours (AUC(2-6) for BMS-730823 was measured in participants with ESRD during dialysis in Period 1 only. Geometric Means were reported in nanogram hours per milliliter (ng\*hr/mL) and were determined from blood samples both entering and exiting the dialyzer.

Mean Percent Dose of Apixaban Recovered in Urine (%UR)
24 hours pre-dose to 72 hours post-dose

The percent dose recovered in urine was calculated by dividing the cumulative amount of unchanged apixaban excreted in urine from the time of dose up to 72 hours post-dose by the apixaban dose administered.

Mean Percent Dose of Apixaban Recovered in Dialysate (%DR)
2 to 6 hours post-dose

Percent dose of Apixaban recovered in dialysate (%DR) was calculated by dividing the cumulative amount of apixaban excreted in each dialysate collection over 2-6 hours (DR(2-6)) by the apixaban dose. %DR was recorded only in period 1.

Mean Renal Clearance (CLR) of Apixaban
24 hours pre-dose to 72 hours post-dose

Renal clearance (CLR) was calculated by dividing the cumulative amount of apixaban excreted in urine by the respective cumulative plasma AUC over the same urine collection interval. Geometric means were reported in milliliters per minute (mL/min).

Mean Renal Clearance (CLR) of BMS-730823
24 hours pre-dose to 72 hours post-dose

Renal clearance (CLR) was calculated by dividing the cumulative amount of BMS-730823 excreted in urine by the respective cumulative plasma AUC over the same urine collection interval. Geometric means were reported in milliliters per minute (mL/min).

Mean Hemodialysis Clearance (CLD) of Apixaban
2 to 6 hours post-dose

Hemodialysis clearance (CLD) was calculated by dividing the cumulative amount of apixaban excreted in dialysate by the respective cumulative plasma AUC over the same dialysate collection interval (AUC(2-6) entering). CLD measurements occurred only in period 1. Geometric means were reported in milliliters per minute (mL/min).

Mean Hemodialysis Clearance (CLD) of BMS-730823
2 to 6 hours post-dose

Hemodialysis clearance (CLD) was calculated by dividing the cumulative amount of BMS-730823 excreted in dialysate by the respective cumulative plasma AUC over the same dialysate collection interval (AUC(2-6) entering). CLD measurements occurred only in period 1. Geometric means were reported in milliliters per minute (mL/min).

Percentage of Apixaban Extracted During Hemodialysis
2 to 6 hours post-dose

The percentage of apixaban extracted during hemodialysis (extraction ratio) was calculated using the formula \[plasma AUC(2-6) exiting - AUC(2-6) entering\] / \[AUC(2-6) entering\] and converted to a percentage. The extraction ratio was measured in period 1 only, and was reported as a percentage.

Percentage of BMS-730823 Extracted During Hemodialysis
2 to 6 hours post-dose

The percentage of BMS-730823 extracted during hemodialysis (extraction ratio) was calculated using the formula \[plasma AUC(2-6)exiting - AUC(2-6)entering\] / \[AUC(2-6) entering\] and converted to a percentage. The extraction ratio was measured in period 1 only, and was reported as a percentage.

Apixaban and Atenolol plasma concentration
Days 1-13

Blood samples for Atenolol PK were collected on days 1-3 of each period (Treatment B and C). Blood samples for Apixaban PK were collected on days 1-4 of each period (Treatment A and C)

Apixaban and Digoxin plasma concentration
Days 8-21

Blood samples for Digoxin were collected on Days 8, 9, 10, 11, 18, 19, 20 \& 21 Urine samples for Digoxin were collected for 24 hours post dose on Days 10 \& 20. Blood samples for Apixaban concentration were collected on Days 18-20

Secondary Endpoints

The Number of Participants With Non-fatal Asymptomatic Deep Vein Thromboses (DVT)
From first dose up to approximately 40 days after first dose
The Number of Participants With Non-fatal Symptomatic Deep Vein Thromboses (DVT)
From first dose up to approximately 34 days after first dose
The Number of Participants With Non-fatal Pulmonary Embolism (PE)
From first dose up to approximately 34 days after first dose
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelPARALLEL
PurposePREVENTION

Treatment Arms

ArmTypeDescription
ApixabanEXPERIMENTALChildren aged 1 to \<18 years weighing 6 to \<35 kg randomized to apixaban will receive a fixed dose apixaban based on body weight tier twice a day for approximately 28 days. Children aged 1 to \<18 years weighing ≥ 35 kg will receive 2.5 mg of apixaban twice a day for approximately 28 days. Subjects ≥ 5 years may be administered either 2.5-mg, 0.5-mg tablets or oral solution apixaban. Subjects \< 5years and \< 35 kg may be administered 0.5-mg tablets only
No systemic anticoagulant prophylaxisPLACEBO_COMPARATORNo systemic anticoagulant prophylaxis
Enoxaparin + WarfarinEXPERIMENTALEnoxaparin: solution, subcutaneous, 1 mg/kg Q12h until international normalized ratio (INR) ≥2.
1EXPERIMENTAL2.5 mg
2EXPERIMENTAL5.0 mg
3ACTIVE_COMPARATOR0 mg
Acetylasalicylic acidACTIVE_COMPARATOR -
Arm 1EXPERIMENTALWhile hospitalized, Apixaban plus Placebo Apixaban (Tablets, Oral, 2.5 mg), Placebo (Syringes, SC) After hospital discharge, Apixaban Apixaban (Tablets, Oral, 2.5 mg)
Arm 2ACTIVE_COMPARATORWhile hospitalized, Enoxaparin plus Placebo Enoxaparin (Syringes, SC, 40 mg), Placebo (Tablets, Oral) After hospital discharge: Placebo Placebo (Tablets, Oral)
Apixaban, 2.5 mg BID + PlaceboEXPERIMENTALParticipants received apixaban, 2.5-mg tablets twice daily (BID), plus a matching enoxaparin-placebo injection 12 (±3) hours prior to hip-replacement surgery through 11 (±2) days after the day of surgery.
Enoxaparin, 40 mg QD + PlaceboACTIVE_COMPARATORParticipants received enoxaparin, 40-mg subcutaneous injection once daily (QD), plus a matching apixaban-placebo tablet 12 (±3) hours prior to hip-replacement surgery through 11 (±2) days after the day of surgery.
Apixaban, 2.5 mg BID plus placeboACTIVE_COMPARATORParticipants received apixaban, 2.5 mg twice daily (BID), as oral tablets, and matching enoxaparin-placebo injection once daily (QD)
Enoxaparin, 40 mg QD plus placeboEXPERIMENTALParticipants received enoxaparin, 40 mg QD subcutaneously, and matching apixaban-placebo tablets BID
LMWH/VKAACTIVE_COMPARATOR -
Part A : postdialysis low doseEXPERIMENTALInterdialytic kinetics of low dose (2.5 mg apixaban) post-dialysis
Part A: ipostdialysis high doseEXPERIMENTALInterdialytic kinetics of high dose (5 mg apixaban) post-dialysis
Part B : predialysis low doseEXPERIMENTALIntra- and interrdialytic kinetics of low (2.5 mg) apixaban pre-dialysis
Part B : predialysis high doseEXPERIMENTALIntra- and interrdialytic kinetics of high (5 mg) apixaban pre-dialysis
Oral apixabanEXPERIMENTALOral apixaban 2.5 mg tablet twice daily for 28 days post-surgery
Subcutaneous enoxaparinACTIVE_COMPARATORSubcutaneous enoxaparin 40mg once daily (QD) for 28 days post-surgery.
Cohort 1: PlaceboPLACEBO_COMPARATORParticipants received placebo tablets once daily
Cohort 1: Apixaban, 5 mgPLACEBO_COMPARATORParticipants received apixaban as tablet, 5 mg, once daily
Cohort 1: Apixaban, 10 mgACTIVE_COMPARATORParticipants received apixaban as tablet, 10 mg, once daily
Cohort 1: Apixaban, 20 mgACTIVE_COMPARATORParticipants received apixaban as tablet, 20 mg, once daily
Cohort 2: PlaceboPLACEBO_COMPARATORParticipants in this cohort were admitted to the trial following the addition of a protocol amendment (Amendment 5), which removed the prohibition of inclusion of patients receiving chemotherapy with concomitant antiangiogenic therapy with bevacizumab. Patients received placebo once daily.
Cohort 2: Apixaban, 5 mgACTIVE_COMPARATORParticipants in this cohort were admitted to the trial following the addition of a protocol amendment (Amendment 5), which removed the prohibition of inclusion of patients receiving chemotherapy with concomitant antiangiogenic therapy with bevacizumab. Patients received apixaban as tablet, 5 mg, once daily.
A1ACTIVE_COMPARATOR -
A2EXPERIMENTAL -
A3PLACEBO_COMPARATOR -
A4EXPERIMENTAL -
A5EXPERIMENTALApixaban: 10 mg, QD PLUS Enoxaparin Placebo
A6EXPERIMENTALApixaban: 20 mg, QD PLUS Enoxaparin Placebo
E1ACTIVE_COMPARATOREnoxaparin: 30 mg PLUS Apixaban Placebo
W1ACTIVE_COMPARATORWarfarin: 5 mg tablets dose titrated to a targeted INR of 1.8 to 3.0
Apixaban and ClarithromycinEXPERIMENTAL -
Apixaban, 10 mg (whole tablets)EXPERIMENTALParticipants received a single dose of apixaban, 10 mg, given orally as 2 5-mg whole commercial tablets (reference)
Apixaban, 10 mg (crushed and suspended in water)EXPERIMENTALParticipants received a single dose of apixaban, 10 mg, given by mouth as 2 5-mg whole commercial tablets crushed and suspended in 30 mL of water
Apixaban, 10 mg (crushed and mixed with applesauce)EXPERIMENTALParticipants received a single dose of 10 mg, given by mouth as 2 5-mg apixaban commercial tablets crushed and mixed with 30 g of applesauce
Treatment A: Apixaban + Placebo (Saline solution)EXPERIMENTALApixaban 10 mg Tablet orally \[Day 1-Day 3: twice daily (BID), Day 4: Single Dose (SD)\] followed 3hr later by Saline solution (placebo) 0 IU/kg infusion for 30 min Intravenously
Treatment B: Apixaban + Cofact (4-Factor PCC)EXPERIMENTALApixaban 10 mg Tablet orally \[Day 1-Day 3: twice daily (BID), Day 4: Single Dose (SD)\] followed 3hr later by a Cofact (4-Factor PCC) 50 IU/kg infusion for 30 min Intravenously
Treatment C: Apixaban + Beriplex P/N (4-Factor PCC)EXPERIMENTALApixaban 10 mg Tablet orally \[Day 1-Day 3: twice daily (BID), Day 4: Single Dose (SD)\] followed 3hr later by a Beriplex P/N (4-Factor PCC) 50 IU/kg infusion for 30 min Intravenously
Group 1: Apixaban (low dose)EXPERIMENTAL -
Group 2A: Apixaban (low dose)EXPERIMENTAL -
Group 2B: Apixaban (low dose)EXPERIMENTAL -
Group 3: Apixaban (low dose)EXPERIMENTAL -
Group 4: Apixaban (low dose)EXPERIMENTAL -
Group 5: Apixaban (low dose)EXPERIMENTAL -
Group 2A (higher dose): Apixaban (low dose)EXPERIMENTAL -
Arm A-ApixabanEXPERIMENTALSolution Apixaban 5 mg ( 0.4 mg/ml oral solution x 12.5 ml) through mouth or oral syringe
Arm B-ApixabanEXPERIMENTALOral Solution Apixaban 5 mg single dose (0.4 mg/mL oral solution x 12.5 mL) after 180 mL of Boost Plus®, followed by 60 mL of Boost Plus® via same NGT
Arm C-ApixabanEXPERIMENTALSingle dose crushed Apixaban tablet 5 mg (5 mg tablet crushed and suspended in 60 mL Dextrose 5% in water (D5W)) through NGT
Arm A: ApixabanEXPERIMENTALSingle dose Apixaban 5 mg (0.4 mg/mL x 12.5 mL) oral solution via oral syringe
Arm B: ApixabanEXPERIMENTALSingle dose Apixaban 5 mg (0.4 mg/mL x 12.5 mL) oral solution via nasogastric tube (NGT) immediately followed by 60 mL of D5W via NGT
Arm C: ApixabanEXPERIMENTALSingle dose Apixaban 5 mg (0.4 mg/mL x 12.5 mL) oral solution via NGT immediately followed by 60 mL of infant formula via NGT
Group A: ApixabanEXPERIMENTAL -
Group B: ApixabanEXPERIMENTAL -
Treatment A: Apixaban tabletEXPERIMENTALApixaban Film coated Tablet Single dose 10 mg orally
Treatment B: Apixaban oral solutionEXPERIMENTALApixaban Solution Single dose 10 mg orally
Treatment A: ApixabanEXPERIMENTALApixaban tablet by mouth on specified day
Treatment B: AtenololEXPERIMENTALAtenolol tablet by mouth on specified day
Treatment C: Apixaban and AtenololEXPERIMENTALApixaban and Atenolol tablets by mouth on specified day
Treatment A: DigoxinEXPERIMENTALDigoxin tablet by mouth on specified days
Treatment B: Apixaban and DigoxinEXPERIMENTALApixaban and Digoxin tablets by mouth on specified days

Interventions

NameTypeDescription
ApixabanDRUG -
No systemic anticoagulant prophylaxisOTHER -
EnoxaparinDRUGsolution, subcutaneous, 1 mg/kg Q12h until International normalized ratio (INR) ≥2.
warfarinDRUGtablets, oral, dosing to target INR range between 2.0 - 3.0, once daily, 6 months
Placebo for apixabanDRUGtablets, oral, 10 mg tablets, twice daily, for 7 days followed by placebo for apixaban 5 mg tablets, twice daily, 6 months
Placebo for enoxaparinDRUGsolution, subcutaneous, 1 mg/kg Q12h until sham INR ≥2.
Placebo for warfarinDRUGtablets, oral, dosing to target sham INR range between 2.0 - 3.0, once daily, 6 months
PlaceboDRUGTablets, Oral, twice daily, 12 months
Acetylsalicylic acidDRUGTablets, oral, 81-324 mg, once daily, up to 156 weeks
Enoxaparin-matching placeboDRUGAdministered once daily by subcutaneous injection
Apixaban-matching placeboDRUGOral tablet administered twice daily
Vitamin K Antagonist (VKA)DRUGSpecified dose on specified days
Low Molecular Weight Heparin (LMWH)DRUGSpecified dose on specified days
Oral apixabanDRUGTo evaluate the incidence of major bleeding (including CRNM bleeding) events in women undergoing surgery for gynecologic cancer with apixaban 2.5 mg BID compared to current standard of care, subcutaneous enoxaparin 40 mg QD for 28 days post surgery.
Subcutaneous enoxaparinDRUGTo evaluate the incidence of major bleeding (including CRNM bleeding) events in women undergoing surgery for gynecologic cancer with apixaban 2.5 mg BID compared to current standard of care, subcutaneous enoxaparin 40 mg QD for 28 days post surgery.
Enoxaparin PlaceboDRUGInjection, SQ, BID, 12 +/- 2 days
Apixaban PlaceboDRUGTablets, Oral, BID, 12 +/- 2 days
ClarithromycinDRUGMultiple-dose clarithromycin and single-dose Apixaban
Cofact (4-Factor PCC)DRUG -
Beriplex P/N (4-Factor PCC)DRUG -
Placebo (Saline solution)DRUG -
Boost PlusDIETARY_SUPPLEMENT -
AtenololDRUG -
DigoxinDRUG -
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Eligibility Criteria

Age Range1 Year to 17 Years
SexALL
Healthy VolunteersNo
Study Sites96

For more information regarding BMS clinical trial participation, please visit www.BMSStudyConnect.com Inclusion Criteria: * New diagnosis of de novo ALL, lymphomas (T or B cell), or mixed-phenotype acute leukemia * Planned 3-4 drug systemic induction chemotherapy with a corticosteroid, vincristine...

Countries:United StatesAustraliaBelgiumCanadaCzechiaHungaryMexicoNew ZealandPolandPuerto RicoRussiaSouth KoreaArgentinaAustriaBrazilChileChinaDenmarkFranceGermanyHong KongIndiaIsraelItalyMalaysiaNorwayPortugalRomaniaSingaporeSouth AfricaSpainUkraineUnited KingdomPhilippinesColombiaFinlandGreeceIndonesiaSwedenTaiwanTurkey (Türkiye)NetherlandsPeruJapanSwitzerland
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Frequently asked questions about Apixaban

What is Apixaban used for?

Apixaban is an investigational small molecule being studied for anticoagulation in conditions including venous thrombosis, pulmonary embolism, deep-vein thrombosis, and acute coronary syndrome. It is also being evaluated in healthy subjects and in patients with end-stage renal disease. Apixaban is not approved and remains in clinical development.

Who makes Apixaban?

Apixaban is being developed by Bristol-Myers Squibb Company, traded on the New York Stock Exchange under the ticker BMY. The company is conducting clinical trials to evaluate the drug's safety and efficacy for various cardiovascular indications.

What phase is Apixaban in?

Apixaban is in Phase 2 clinical development. Although some completed trials were Phase 1 and Phase 3, the drug's current development stage is Phase 2. Apixaban is investigational and has not been approved by regulatory authorities.

What clinical trials is Apixaban in?

Apixaban has completed four clinical trials. NCT00097357 studied the drug in subjects undergoing elective total knee replacement surgery for venous thrombosis and pulmonary embolism. NCT00633893 evaluated extended treatment of deep-vein thrombosis or pulmonary embolism. NCT02262520 and NCT02262533 were Phase 1 drug interaction studies in healthy subjects.

Is Apixaban the same as BMS-562247?

Yes, Apixaban is also known as BMS-562247. In clinical trials, the drug has been referred to by this alternative name, such as in NCT00097357, which studied BMS-562247 in subjects undergoing elective total knee replacement surgery.