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Safety and Tolerability of PF-05230907 in Intracerebral Hemorrhage

Phase 1
Terminated
Conditions
Intracerebral Hemorrhage
Interventions
Biological: PF-05230907
Registration Number
NCT02687191
Lead Sponsor
Pfizer
Brief Summary

This study employs a modified continual reassessment method (mCRM) design to estimate the maximum tolerated dose (MTD) of PF-05230907, defined as a target toxicity rate of 15% based on treatment emergent thromboembolic and/or ischemic events (TIEs). The mCRM design utilizes Bayesian methodology to continuously learn the dose-toxicity relationship, which is characterized by a parametric model.

Subjects with a diagnosis of ICH (determined by computed tomography) will be enrolled in cohorts of 3. The total length of time planned for study participation is approximately 3 months; 6.0 hours for screening, a single dose administration with a 4-day minimum hospital confinement period and follow-up visits through Day 91.

Severity of adverse events (AEs) and serious adverse events (SAEs) will be graded according to the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 4.03. All subjects who receive PF-05230907 are evaluable for TIEs. The determination of MTD using mCRM modeling will be based on TIEs which occur through 7 days post-dose (Day 8).

Detailed Description

Not available

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
21
Inclusion Criteria
  • ICH as documented by CT scan within 6.0 hours of symptom onset
  • Baseline ICH volume > 5mL and < 60 mL
Exclusion Criteria
  • Deep coma (Glasgow Coma Scale < 6)
  • Modified Rankin Score > 3 prior to ICH onset
  • Known history of schemic, vaso-occlusive or thrombotic events within 6 months prior to screening
  • Known prothrombotic disorders
  • Known secondary ICH related to aneurysm, arteriovenous malformation, subarachnoid hemorrhage, trauma, or other causes. CT angiography, MR, or other diagnostic studies obtained as part of the standard of care may be used to assess eligibility.
  • Known use of oral anticoagulant(s)
  • Known use of low-molecular weight heparin or heparin

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
PF-05230907 (Cohort 15)PF-05230907PF-05230907 IV bolus injection
PF-05230907 (Cohort 4)PF-05230907PF-05230907 IV bolus injection
PF-05230907 (Cohort 8)PF-05230907PF-05230907 IV bolus injection
PF-05230907 (Cohort 2)PF-05230907PF-05230907 IV bolus injection
PF-05230907 (Cohort 1)PF-05230907PF-05230907 IV bolus injection
PF-05230907 (Cohort 3)PF-05230907PF-05230907 IV bolus injection
PF-05230907 (Cohort 5)PF-05230907PF-05230907 IV bolus injection
PF-05230907 (Cohort 6)PF-05230907PF-05230907 IV bolus injection
PF-05230907 (Cohort 9)PF-05230907PF-05230907 IV bolus injection
PF-05230907 (Cohort 10)PF-05230907PF-05230907 IV bolus injection
PF-05230907 (Cohort 11)PF-05230907PF-05230907 IV bolus injection
PF-05230907 (Cohort 14)PF-05230907PF-05230907 IV bolus injection
PF-05230907 (Cohort 12)PF-05230907PF-05230907 IV bolus injection
PF-05230907 (Cohort 13)PF-05230907PF-05230907 IV bolus injection
PF-05230907 (Cohort 7)PF-05230907PF-05230907 IV bolus injection
Primary Outcome Measures
NameTimeMethod
Number of Participants With Treatment-Emergent Thromboembolic and/or Ischemic Events (TIEs)Day 1 through day of discharge (Day 8)

Thromboembolic and/or ischemic events (TIEs) were defined as any of the following events: disseminated intravascular coagulation (Grade \[Gr\]\>=3); acute coronary syndrome (Gr \>=3); cardiac arrest (Gr \>=4); myocardial infarction (Gr \>=3); Cardiac troponin I increased (Gr 3); ischemia cerebrovascular (Gr \>=1 and associated with lesion\[s\]); portal vein thrombosis (Gr \>=2); ischemic stroke (Gr \>=1 and associated with lesion\[s\]); transient ischemic attacks (Gr 2); purpura (Gr \>=2); superior vena cava syndrome (Gr \>=1); thromboembolic event (Gr \>=2); visceral arterial ischemia (Gr \>=2); peripheral arterial ischemia (Gr \>=3). TIEs were graded based on Common Terminology Criteria for Adverse Events (CTCAE) version 4.03. For the respective event to count as a treatment-emergent TIE, onset or worsening of the event must have occurred following treatment with PF-05230907 and during the interval between Day 1 dosing through Day 8.

Number of Participants With Treatment-Emergent Serious Adverse Events (SAEs)Day 1 through follow-up visit (Day 43)

A serious adverse event (SAE) was any untoward medical occurrence at any dose that: resulted in death; or was life threatening (immediate risk of death); or required inpatient hospitalization or prolongation of existing hospitalization; or resulted in persistent or significant disability/incapacity (substantial disruption of the ability to conduct normal life functions); or resulted in congenital anomaly/birth defect. Any such events occurring following the start of treatment or increasing in severity were counted as treatment-emergent.

Number of Participants With Treatment-Emergent Adverse Events (AEs)Day 1 through day of discharge (Day 8)

An adverse event (AE) was any untoward medical occurrence in a participant who received study treatment without regard to possibility of causal relationship. For the respective event to count as a treatment-emergent AE, onset or worsening of the event must have occurred following treatment with PF-05230907 and during the interval between Day 1 dosing through Day 8.

Change From Baseline for Body TemperatureBaseline (pre-dose), Day 1 (5 and 45 minutes [min] post-dose), Day 2, Day 3, Day 4, Day 8/discharge

Body temperature was measured by oral, tympanic, axillary or temporal method.

Change From Baseline for Supine Pulse RateBaseline (pre-dose), Day 1 (5 and 45 minutes [min] post-dose), Day 2, Day 3, Day 4, Day 8/discharge

The use of an automated device for measuring pulse rate was acceptable, although, when done manually, pulse rate was measured in the brachial/radial artery for at least 30 seconds.

Number of Participants With Changes From Baseline in Physical ExaminationBaseline (pre-dose), Day 2, Day 3, Day 4, Day 8/discharge

Comprehensive and targeted physical examinations included general appearance, HEENT (head, eyes, ears, nose and throat), skin, heart (auscultation), lungs (auscultation), abdomen (palpitation and auscultation), and extremities with attention to swelling, general or localized tenderness, entire leg or calf swelling, edema, and collateral superficial veins. The results of the comprehensive and targeted physical examinations were combined to evaluate the changes from baseline through Day 8 (or discharge) for each site parameter according to the categories: positive change (abnormal to normal); no change (normal to normal or abnormal to abnormal); negative change (normal to abnormal). Parameters with at least 1 participant meeting the positive/negative change from baseline criteria are presented here.

Number of Participants With Treatment-Emergent Laboratory AbnormalitiesDay 1 through Day 8 (or discharge) for D-dimer laboratory test and urinalysis; Day 1 through Day 4 for all other laboratory tests

Laboratory safety parameters included hematology, blood chemistry, prothrombin time/international normalized ratio (PT/INR), fibrinogen, antithrombin III (ATIII), Protein S level, Protein C activity, cardiac troponin I, D-dimer, and urinalysis. The number of participants with laboratory test abnormalities meeting specified criteria without regard to baseline abnormality was assessed. Any abnormalities occurring after the administration of treatment and increasing in severity from baseline value were counted as treatment-emergent.

Change From Baseline for Supine Respiratory RateBaseline (pre-dose), Day 1 (5 and 45 minutes [min] post-dose), Day 2, Day 3, Day 4, Day 8/discharge

Respiratory rate was measured after 5 minutes rest in supine position by observing and counting the respirations of the participant for 30 seconds and multiplied by 2. The use of an automated device for measuring respiratory rate was acceptable.

Change From Baseline for Supine Systolic and Diastolic Blood PressureBaseline (pre-dose), Day 1 (5 and 45 minutes [min] post-dose), Day 2, Day 3, Day 4, Day 8/discharge

Supine blood pressure (BP, systolic and diastolic) was measured with the participant's arm supported at the level of the heart and recorded to the nearest milliliters of mercury (mmHg) after 5 minutes of rest whenever possible and as permitted by the participant's medical condition.

Number of Participants With Electrocardiogram (ECG) Qualitative ResultsBaseline (pre-dose), Day 2, Day 4, Day 8/discharge

The electrocardiogram (ECG) results over time were compared to baseline and assessed by the investigator as "less abnormal", "no significant change", or "more abnormal".

Secondary Outcome Measures
NameTimeMethod
Number of Participants With Anti-Drug Antibody (ADA) ProductionDay 1 up to follow-up visit (Day 43 and/or Day 91)

Participants with anti-drug antibody (ADA) production were those with at least 1 positive result from Day 1 through follow-up visit (Day 43 and/or Day 91). ADA positive: titer value \>=1.88.

Number of Participants With Depletion of Coagulation Factor XBaseline (pre-dose), Day 43, Day 91

Depletion of coagulation factor X was defined as \>50% reduction relative to baseline (pre-dose).

Maximum Changes From Baseline for Activated Partial Thromboplastin Time (aPTT)Baseline (pre-dose), Day 2

Maximum changes from baseline were calculated for activated partial thromboplastin time (aPTT) after dosing with PF-05230907 through Day 2.

Maximum Changes From Baseline for Prothrombin Fragment 1+2 (PF1+2)Baseline (pre-dose), Day 2

Maximum changes from baseline were calculated for prothrombin fragment 1+2 (PF1+2) after dosing with PF-05230907 through Day 2.

Number of Participants With Neutralizing Antibody (NAb) ProductionDay 1 up to follow-up visit (Day 43 and/or Day 91)

ADA positive samples were planned to be further characterized for neutralizing antibody (NAb). Participants with NAb production were those with at least 1 positive result from Day 1 through follow-up visit (Day 43 and/or Day 91). As all ADA samples were negative (titer value \<1.88), NAb analysis was not conducted.

Trial Locations

Locations (13)

Barnes Jewish Hospital

🇺🇸

Saint Louis, Missouri, United States

The Ohio State University Wexner Medical Center

🇺🇸

Columbus, Ohio, United States

James Cancer Hospital and Solove Research Institute

🇺🇸

Columbus, Ohio, United States

Martha Morehouse Medical Plaza

🇺🇸

Columbus, Ohio, United States

The Ottawa Hospital

🇨🇦

Ottawa, Ontario, Canada

Montreal Neurological Institute and Hospital

🇨🇦

Montreal, Quebec, Canada

Hospital Universitari Germans Trias i Pujol

🇪🇸

Badalona, Barcelona, Spain

Hospital Clínico Universitario de Santiago de Compostela, Area Neurovascular-Neurologia

🇪🇸

Santiago de Compostela, LA Coruna, Spain

Hospital Universitario Ramon y Cajal

🇪🇸

Madrid, Spain

Hospital Universitari Dr. Josep Trueta IDIBGI, Department Neurology

🇪🇸

Girona, Spain

Hospital Vall d'Hebron, Unidad de Ictus

🇪🇸

Barcelona, Spain

University College Hospital

🇬🇧

London, United Kingdom

Washington University,

🇺🇸

Saint Louis, Missouri, United States

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