Delving into the Latest Updates on PF-05230907 with Synapse

Overview

Basic Info

Drug Type

Recombinant coagulation factor

Synonyms

FXa, FXa-I16L, FXAI16L

+ [4]

Target

prothrombin

Action

modulators

Mechanism

prothrombin modulators(Prothrombin modulators)

Therapeutic Areas

Congenital DisordersHemic and Lymphatic DiseasesOther Diseases

Active Indication

Hemophilia B

Inactive Indication

Cerebral Hemorrhage

Originator Organization

Pfizer Inc.

Active Organization

The Children's Hospital of Philadelphia

Inactive Organization

Pfizer Inc.

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Login to view timeline

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).

Start Date01 Nov 2016

Sponsor / Collaborator

Pfizer Inc.

NCT02537002

/ CompletedPhase 1

A Phase 1, Randomized, Double-blind, Sponsor-open, Placebo-controlled, Single Ascending Dose Study To Evaluate The Safety, Tolerability, Pharmacokinetics And Pharmacodynamics Of An Intravenous Bolus Infusion Pf-05230907 In Healthy Japanese Subjects

The purpose of this study is the following:
* To determine the safety and tolerability of single ascending intravenous (IV) doses of PF-05230907 in healthy Japanese subjects.
* To characterize the PK profile of single ascending IV doses of PF-05230907 in healthy Japanese subjects.
* To characterize the PD profiles of single ascending IV doses of PF-05230907 in healthy Japanese subjects.
* To evaluate the immunogenicity of PF-05230907 in healthy Japanese subjects

Start Date01 Sep 2015

Sponsor / Collaborator

Pfizer Inc.

NCT01897142

/ CompletedPhase 1

A Phase 1, Randomized, Double-blind, Sponsor-open, Placebo-controlled, Single Ascending Dose Study To Evaluate The Safety, Tolerability, Pharmacokinetics And Pharmacodynamics Of Pf-05230907 In Healthy Subjects

The purpose of this study is to determine what the study drug does to the body, what the body does to the study drug, and if the study drug is safe and well tolerated when given to adult healthy volunteers.

Start Date01 Sep 2013

Sponsor / Collaborator

Pfizer Inc.

100 Clinical Results associated with PF-05230907

Login to view more data

100 Translational Medicine associated with PF-05230907

Login to view more data

100 Patents (Medical) associated with PF-05230907

Login to view more data

34

Literatures (Medical) associated with PF-05230907

15 Jun 2025·JOURNAL OF THE AMERICAN ACADEMY OF ORTHOPAEDIC SURGEONS

Ten-Year Trends in Venous Thromboembolism Prophylaxis at a High-Volume Arthroplasty Center

Article

Author: Austin, Matthew S. ; Lizcano, Juan D. ; Reddy, Yashas ; Baker, Colin M. ; Lizcano, Juan D ; Austin, Matthew S ; Sherman, Matthew B ; Baker, Colin M ; Sherman, Matthew B. ; Tarabichi, Saad

Introduction::

Venous thromboembolism (VTE) prophylaxis is the standard of care after total joint arthroplasty. However, there have been changes in the prevalence of certain medication classes used by institutions over time driven by the literature and national clinical practice guidelines. The purpose of this study was to analyze the patterns of VTE medications over the past 10 years at our institution.

Methods::

We identified 25,095 patients who underwent a primary total joint arthroplasty between 2012 and 2022. Medications for VTE prophylaxis included aspirin, warfarin, unfractioned heparin (UFH), low-molecular-weight heparin (LMWH), factor-Xa inhibitors (FXa), and antiplatelet agents different from aspirin and thrombin inhibitors. Tranexamic acid use was recorded. The rates of symptomatic VTE were calculated and categorized as deep vein thrombosis or pulmonary embolism.

Results::

Venous thromboembolism rates decreased from 1.1% in 2012 to 0.2% in 2022 and ranged between 0.4% and 1.2% during the ten-year period. Although VTE incidence decreased in the past 4 years, an isolated increase was noted in 2021(1%). In 2012, the use of aspirin, warfarin, FXa, and UFH were 52.1%, 30.7%, 0%, and 16.2%, respectively, whereas in 2022, the rates for the same medications were 83.3%, 0.3%, 10.4%, and 1.8%, respectively. The use of LMWH, thrombin inhibitors, and other antiplatelet agents had minimal variation, and none of these medications surpassed 5% during this period. The aspirin dose changed from 325 mg in 2012 (96.5%) to 81 mg in 2022 (98.8%). Similarly, TXA use increased from 30.8% in 2012 to 84.9% in 2022.

Conclusion::

In the past 10 years, our institution has transitioned from warfarin, UFH, and high-dose aspirin to low-dose aspirin and FXa, exhibiting acceptably low deep vein thrombosis and diminishing pulmonary embolism rates during that time.

20 Jul 2021·Investigative ophthalmology & visual scienceQ2 · MEDICINE

Activated Blood Coagulation Factor X (FXa) Contributes to the Development of Traumatic PVR Through Promoting RPE Epithelial-Mesenchymal Transition

Q2 · MEDICINE

ArticleOA

Author: Zhao, Xiao ; Yang, Xueli ; Wang, Xiaohong ; Liao, Mengyu ; Dong, Xue ; You, Caiyun ; Huang, Bo ; Yan, Hua ; Du, Mei ; Han, Han ; Song, Yinting

Purpose:

Uncontrolled coagulation reactions contribute to pathological fibroproliferation in several organs, and yet their role in proliferative vitreoretinopathy (PVR) remains to be elucidated. In this study, we evaluated the profibrotic effects of FXa in RPE cells and in a mouse model of PVR.

Methods:

FXa levels in the eyes of traumatic PVR patients and rabbit models of mechanical ocular trauma was measured by ELISA and immunohistochemistry. FXa-induced RPE EMT was assessed by examining cell proliferation, migration, tight junction changes, and expression of fibrotic markers. For in vivo study, FXa was injected into dispase-injured eyes, then intraocular fibrosis was evaluated by histological analysis and Western blotting. The therapeutic effect of FXa inhibitor was also examined in PVR mouse models.

Results:

Vitreous FXa were higher in patients with traumatic PVR compared to patients with macular hole. Moreover, expressions of FXa and PAR1 were found in the epiretinal membranes from traumatic PVR patients. Vitreous FXa were markedly increased after mechanical ocular trauma in rabbits. In vitro, FXa stimulated RPE EMT characterized as ZO-1 disruption, compromised cell polarity, and increased fibronectin expressions. Co-injection of FXa and dispase in mice induced more severely damaged retinal structures, and increased α-SMA expressions than FXa or dispase treatment alone. Oral FXa or thrombin inhibitors significantly blocked intraocular fibrosis in PVR mouse models. FXa promoted phospho-activation of p38 in ARPE19 cells, which was dependent on PAR1. Moreover, TGF-βR inhibitor also significantly alleviated FXa-induced intraocular fibrosis in mice.

Conclusions:

FXa promotes intraocular fibrosis in mice via mechanisms involving RPE activation.

01 Apr 2021·Archives of orthopaedic and trauma surgeryQ3 · MEDICINE

Outcome of older hip fracture patients on anticoagulation: a comparison of vitamin K-antagonists and Factor Xa inhibitors

Q3 · MEDICINE

Article

Author: Jacobs, M ; Bail, H ; Gosch, M ; Grueninger, S ; Wicklein, S

INTRODUCTION:

Older hip fracture patients are still challenging in daily clinical practice. Due to the high prevalence of osteoporosis and atrial fibrillation in this age group, the number of fragility fracture patients under oral anticoagulation (OAC) increases. The outcome is still disappointing, short- and long-term mortality and morbidity is high. The impact of pre-existing OAC is not yet clear, especially regarding new OAC drugs like Factor Xa inhibitors (FXa). The purpose of our study was to compare the short-term outcome of older hip fracture patients, without OAC (controls), on Vitamin K antagonists (VKA) and on FXa.

MATERIALS AND METHODS:

The study is a retrospective case-control study including patients older than 70 years who sustained hip fractures caused by an inadequate trauma and treated at a level 1 trauma center from February 2017 to June 2018. Patient's information was taken from patient's charts. 102 cases were analysed, 61 controls, 41 on OAC (15 on VKA and 26 on FXa). As outcome parameter we defined mortality, perioperative complications, bleeding, need of blood supplements, delay of surgery, length of stay, and a combined outcome parameter (mortality, myocardial infarction, stroke, thromboembolic events, blood preservations, re-vision surgery, major bleeding and decline of hemoglobin).

RESULTS:

Eight patients died during hospital stay, in-hospital mortality was 7.8%. The highest mortality rate was found in patients on VKA (20%), compared to patients on FXa (3.8%) and controls (6.6%). However, mortality rate did not differ significantly within the groups. The combined endpoint was significantly more frequently seen in patients on OAC compared to controls (p = 0.006). No difference was observed between patients on VKA or FXa. Mean time to surgery and LOS was significantly longer in patients on OAC compared to controls. No significant differences were seen between VKA and FXa.

CONCLUSIONS:

In our study OAC was significantly associated with worse outcome compared to controls. Marginal differences were observed between patients on FXa or VKA. Further studies involving a higher number of patients are necessary to confirm our results. At that time, some our results have to interpreted carefully and need confirmation.

100 Deals associated with PF-05230907

Login to view more data

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Cerebral Hemorrhage	Phase 1	United States	Pfizer Inc.	01 Nov 2016
Cerebral Hemorrhage	Phase 1	Canada	Pfizer Inc.	01 Nov 2016
Cerebral Hemorrhage	Phase 1	Spain	Pfizer Inc.	01 Nov 2016
Cerebral Hemorrhage	Phase 1	United Kingdom	Pfizer Inc.	01 Nov 2016
Hemophilia B	Preclinical	United States	The Children's Hospital of Philadelphia	16 Nov 2008

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02687191 (Pubmed \| Cochrane Database Syst Rev \| Stroke) Manual	Phase 1	Cerebral Hemorrhage	21	PF-05230907	frwdomllkn(sbjklwploc) = thromboembolic or ischemic events occurred in the 30 μg/kg dose group 2patirnt pssrueegyj (adzjvitsod )	Positive	01 Jan 2021
NCT02687191 (CTgov)	Phase 1	Cerebral Hemorrhage	21	PF-05230907 (PF-05230907 5 Microgram Per Kilogram (mcg/kg))	ghyijlqfab = ttptpauhoj lfplmajstt (ffswmdibge, idnijepflx - phiooullia) View more	-	17 Apr 2019
NCT02687191 (CTgov)	Phase 1	Cerebral Hemorrhage	21	PF-05230907 (PF-05230907 8 mcg/kg)	ghyijlqfab = fteoyffszo lfplmajstt (ffswmdibge, wpmssrjqbk - ksuhgohqzb) View more	-	17 Apr 2019

Login to view more data

Translational Medicine

Boost your research with our translational medicine data.

login

or

view full example data

Boost your research with our translational medicine data.

Deal

Boost your decision using our deal data.

login

or

view full example data

Boost your decision using our deal data.

Core Patent

Boost your research with our Core Patent data.

login

or

view full example data

Boost your research with our Core Patent data.

Clinical Trial

Identify the latest clinical trials across global registries.

login

or

view full example data

Identify the latest clinical trials across global registries.

Approval

Accelerate your research with the latest regulatory approval information.

login

or

view full example data

Accelerate your research with the latest regulatory approval information.

Biosimilar

Competitive landscape of biosimilars in different countries/locations. Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3.

login

or

view full example data