Destabilization of PF4-antigenic complexes in heparin-induced thrombocytopenia

L Lubica Rauova (4Hematology Division, Children’s Hospital of Philadelphia, Philadelphia, PA) K Khalil Bdeir (University of Pennsylvania Perelman School of Medicine, Philadelphia, Pennsylvania, United States) A Ann H. Rux (3Department of Pathology and Laboratory Medicine, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA) M Manu Thomas Kalathottukaren (4Department of Pathology and Laboratory Medicine, Center for Blood Research and Life Sciences Institute, The University of British Columbia, Vancouver, Canada) J Jenna Oberg (Children's Hospital of Philadelphia, Philadelphia, Pennsylvania, United States) C Chanel C. La (4Department of Pathology and Laboratory Medicine, Center for Blood Research and Life Sciences Institute, The University of British Columbia, Vancouver, Canada) D David T. E. Lim (4Department of Pathology and Laboratory Medicine, Center for Blood Research and Life Sciences Institute, The University of British Columbia, Vancouver, Canada) V Vincent Hayes (1Hematology Division, Children’s Hospital of Philadelphia, Philadelphia, PA) G Gavin T. Koma (1Hematology Division, Children’s Hospital of Philadelphia, Philadelphia, PA) A Amrita Sarkar (Children's Hospital of Philadelphia, Philadelphia, Pennsylvania, United States) M Mortimer Poncz J Jayachandran N. Kizhakkedathu (4Department of Pathology and Laboratory Medicine, Center for Blood Research and Life Sciences Institute, The University of British Columbia, Vancouver, Canada) D Douglas B. Cines (Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania, Philadelphia, Pennsylvania, United States)

Abstract

Abstract Heparin-induced thrombocytopenia (HIT) is initiated by antibodies that recognize large antigenic complexes composed of multiple molecules of cationic platelet factor 4 (PF4) and polyanions such as unfractionated heparin (UFH) that bind to each other primarily through electrostatic interactions. We asked whether the formation and stability of these HIT antigenic or ultralarge immune complexes (ULICs) would be inhibited by biocompatible synthetic polycationic molecules shown previously to dissociate UFH from antithrombin III and to inhibit polyphosphates. Members of this family of molecules, designated universal heparin reversal agents (UHRAs), inhibited formation and dissociated preformed ultralarge PF4-UFH (antigenic) complexes (ULCs), dissociated ULICs composed of the HIT-like monoclonal antibody KKO and ULCs, blocked binding of human HIT immunoglobulin G antibodies to PF4/heparin, binding of KKO to platelets, KKO-induced adhesion of platelets to activated human endothelium under flow, and microvascular thrombosis induced by KKO in a mouse model of HIT. These data suggest that UHRAs might provide a rationale intervention that acts at an early step in the pathogenesis of HIT to enhance the benefits and lessen the risks of nonheparin anticoagulants. Destabilization of immune complexes using polycationic inhibitors might also find a role in management of other polyanion PF4-antibody–mediated conditions, including vaccine-induced thrombocytopenia/thrombosis, postviral, and autoimmune HIT.

Article Details

Journal Blood
Volume / Issue Vol. 145, Issue 25
Published June 19, 2025
Pages 3030-3040
ISSN 0006-4971
Publisher Elsevier BV

Journal Info

Blood

Elsevier BV

ISSN: 0006-4971 Health Sciences

Authors (13)

L

Lubica Rauova

4Hematology Division, Children’s Hospital of Philadelphia, Philadelphia, PA

K

Khalil Bdeir

University of Pennsylvania Perelman School of Medicine, Philadelphia, Pennsylvania, United States

A

Ann H. Rux

3Department of Pathology and Laboratory Medicine, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA

M

Manu Thomas Kalathottukaren

4Department of Pathology and Laboratory Medicine, Center for Blood Research and Life Sciences Institute, The University of British Columbia, Vancouver, Canada

J

Jenna Oberg

Children's Hospital of Philadelphia, Philadelphia, Pennsylvania, United States

C

Chanel C. La

4Department of Pathology and Laboratory Medicine, Center for Blood Research and Life Sciences Institute, The University of British Columbia, Vancouver, Canada

D

David T. E. Lim

4Department of Pathology and Laboratory Medicine, Center for Blood Research and Life Sciences Institute, The University of British Columbia, Vancouver, Canada

V

Vincent Hayes

1Hematology Division, Children’s Hospital of Philadelphia, Philadelphia, PA

G

Gavin T. Koma

1Hematology Division, Children’s Hospital of Philadelphia, Philadelphia, PA

A

Amrita Sarkar

Children's Hospital of Philadelphia, Philadelphia, Pennsylvania, United States

M

Mortimer Poncz

J

Jayachandran N. Kizhakkedathu

4Department of Pathology and Laboratory Medicine, Center for Blood Research and Life Sciences Institute, The University of British Columbia, Vancouver, Canada

D

Douglas B. Cines

Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania, Philadelphia, Pennsylvania, United States