Integrilin (eptifibatide) / Takeda - LARVOL DELTA

A murine monoclonal antibody to integrin αIIbβ3 that inhibits protein disulfide isomerase binding to platelets and platelet aggregation (ASH 2025) - "Eptifibatide, which induces αIIbβ3 to adopt the extended-open conformation, alsoincreased the speed and amount of 21C11 bound to platelets... mAb R21C11 binding to platelet αIIbβ3: 1. Inhibits exogenous PDI binding to platelets. 2."

Preclinical • Cardiovascular • Hematological Disorders • Thrombosis

Efficacy and safety of adjunctive eptifibatide or argatroban versus control for acute ischemic stroke: A systematic review and network meta-analysis of randomized control trials (ASH 2025) - "Introduction: Acute ischemic stroke is a major cause of disability and mortality, with treatment mainlylimited to intravenous alteplase thrombolysis. Functional Independence (mRS 0-1): Eptifibatide showed superior odds versus control (OR 1.12 [0.65-1.95]) and Argatroban (OR 1.82 [0.61-5.45]), with wide confidence intervals. Argatroban versus controlyielded OR 1.05 [0.59-1.86], indicating uncertainty. Bayesian analysis showed minimal effect for Controlversus Argatroban = -0.046 [-0.65, 0.59], and slight advantage for Control versus Eptifibatide = 0.205 [-0.37, 0.78], with uncertainty."

Retrospective data • Review • Cardiovascular • Cerebral Hemorrhage • CNS Disorders • Hematological Disorders • Ischemic stroke

Administration of eptifibatide as rescue therapy during mechanical thrombectomy in acute ischemic stroke. (PubMed, Front Neurol) - "The use of eptifibatide is an effective and safe procedure in technically more difficult cases of MT. It enables a similar degree of recanalization to be achieved without increasing the risk of SICH."

Journal • Cardiovascular • Cerebral Hemorrhage • CNS Disorders • Hematological Disorders • Ischemic stroke

Procedural eptifibatide administration as an alternative to preprocedural dual antiplatelet therapy for patients undergoing flow diversion procedures: case series and review of the literature. (PubMed, J Neurointerv Surg) - "Intraprocedural eptifibatide may be an acceptable alternative to preprocedural DAPT to achieve platelet inhibition for FD procedures. This protocol did not result in peripheral or neurological hemorrhagic complications and was associated with a very low incidence of post-procedure diffusion lesions."

Journal • Cardiovascular • Hematological Disorders

The Impact of Cangrelor in the UK for the Treatment of STEMI Patients with Gastric Absorption Issues Undergoing Percutaneous Coronary Intervention. (PubMed, J Clin Med) - "Oral P2Y12 inhibitors (clopidogrel, prasugrel, and ticagrelor), glycoprotein IIb/IIIa inhibitors (eptifibatide and tirofiban), and aspirin and heparin alone were included as base case comparators. The introduction of cangrelor is estimated to lead to 314 fewer hospital days and 190 clinical events avoided over 5 years. Introducing cangrelor to STEMI patients with gastric absorption issues undergoing PCI in the UK is estimated to generate a small cost saving and reduced length of stay for some patients."

Journal • Cardiovascular • Myocardial Infarction

Prophylactic Intra-Arterial Eptifibatide in Stent-Assisted Coiling and Flow Diverter Treatment of Cerebral Aneurysms: A Single-Center Retrospective Analysis. (PubMed, J Clin Med) - "No hemorrhagic complications were recorded. Prophylactic low-dose intra-arterial Eptifibatide demonstrated a favorable safety profile, potentially reducing thrombotic complications without substantially increasing hemorrhagic risk."

Journal • Retrospective data • Cardiovascular • Hematological Disorders • Thrombosis • Vascular Neurology

αIIbβ3-dependent platelet procoagulant activity promotes pulmonary arterial thrombosis triggered by circulating tissue factor. (PubMed, Thromb Res) - "Notably, pretreatment of mice with annexin A5 or eptifibatide also completely abrogated thromboplastin-induced iPAT...Our study provides in vivo evidence that cTF contributes to the development of iPAT. We demonstrate that the prothrombotic effect of cTF is dependent on platelet-αIIbβ3 signaling, which enhances platelet procoagulant activity, leading to accelerated coagulation and development of iPAT."

Journal • Cardiovascular • Hematological Disorders • Thrombosis • ANXA5

αIIbβ3-Dependent Platelet Procoagulant Activity Promotes Pulmonary Arterial Thrombosis Triggered By Blood-Borne Tissue Factor (ASH 2024) - "We examined the impact of coagulation inhibition with heparin, platelet αIIbβ3 inhibition using eptifibatide, and phosphatidylserine (PS) blocking with annexin A5 (ANX) on circulating TF-induced PAT in WT mice...We demonstrate that TF's action is dependent on platelet αIIbβ3 signaling, which promotes platelet procoagulant activity, accelerates coagulation and leads to PAT. Both our models have potential applications in investigating the molecular determinants of PAT associated with various pulmonary disorders, and in evaluating the efficacy of new antithrombotic drugs."

Asthma • Cardiovascular • Chronic Obstructive Pulmonary Disease • Genetic Disorders • Hematological Disorders • Immunology • Infectious Disease • Pulmonary Disease • Respiratory Diseases • Sickle Cell Disease • Thrombosis • ANXA5 • ITGA2

"Letter to The Editor: Can Eptifibatide Rewrite the NSTEMI Story? (Eptifibatide vs. Standard Care for NSTEMI: A 5-Year Analysis of Major Adverse Cardiovascular Events)". (PubMed, Catheter Cardiovasc Interv) - No abstract available

Adverse events • Journal • Cardiovascular

SAFETY PROFILE OF INTEGRILIN (EPTIFIBATIDE) USED IN ENDOVASCULAR THERAPY OF ACUTE ISCHAEMIC STROKE (WSC 2025) - "The use of integrilin in MT patients was associated with lower rates of ICH, with no difference in sICH and mortality rates."

Clinical • Atherosclerosis • Cardiovascular • Cerebral Hemorrhage • Hematological Disorders • Ischemic stroke • Thrombosis

OPTIMAL INTRAPROCEDURAL ANTIPLATELET STRATEGY DURING RESCUE STENTING FOR REFRACTORY LARGE VESSEL OCCLUSION: A SUB-STUDY OF THE RESISTANT REGISTRY (WSC 2025) - "Antiplatelet regimens were classified as intravenous (IV-APT) (cangrelor, tirofiban, eptifibatide, abciximab), single oral (aspirin, clopidogrel, ticagrelor), or dual oral therapy. ConclusionsIntraprocedural intravenous antiplatelet therapy was associated with improved procedural success and reduced re-occlusion without a significant impact on hemorrhagic or functional outcomes. These findings support the procedural safety of IV antiplatelets and highlight their potential benefit in optimizing reperfusion outcomes during rescue stenting."

Cerebral Hemorrhage • CNS Disorders • Hematological Disorders

Can Eptifibatide Rewrite the NSTEMI Story? (Eptifibatide vs. Standard Care for NSTEMI: A 5-Year Analysis of Major Adverse Cardiovascular Events). (PubMed, Catheter Cardiovasc Interv) - "Eptifibatide showed no significant effect on MACE or survival in NSTEMI patients undergoing PCI. Further research is needed to explore its role in high-risk subgroups."

Adverse events • Journal • Acute Coronary Syndrome • Cardiovascular • Coronary Artery Disease • Myocardial Infarction

Potent Inhibition of Arterial Thrombosis and Venous Thrombogenesis Subject to Adequate Hemostasis via Disrupting β3/Src Interaction in Platelets. (PubMed, Thromb Haemost) - "In vitro and in vivo studies demonstrated that C109 and C116 effectively suppress thrombosis at levels comparable to high doses of the αIIbβ3 antagonist integrilin, without elevating bleeding risk. In the Stenosis Model, C109 and C116 significantly reduced venous thrombogenesis by suppressing platelet activation and neutrophil extracellular trap formation. Additionally, C109 displayed favorable PK properties and robust metabolic stability.These findings identify promising small molecules that inhibit thrombosis while maintaining hemostasis, providing new avenues for safer and more effective clinical management."

Journal • Cardiovascular • Hematological Disorders • Thrombosis

Thrombolysis Alone vs With Argatroban or Eptifibatide: A Prespecified Subgroup Analysis of the MOST Trial. (PubMed, Neurology) - P3 | "Outcomes in patients treated with IVT-O were not improved by adding either argatroban or eptifibatide. Increased bleeding was not observed, but mortality was higher in both investigational arms. Limitations included small sample size in the argatroban subgroup."

Clinical • Journal • Cardiovascular • Hematological Disorders • Ischemic stroke

The inhibitory effect of antiplatelet drugs on spontaneous platelet aggregation on glass surfaces: an analysis based on microscopic three-dimensional topography. (PubMed, J Thromb Thrombolysis) - "Ticagrelor, eptifibatide, and tirofiban dose-dependently decreased both Vol and CS-area...GPIb-IX-von Willebrand factor (vWF) inhibitors (4 μM) and indomethacin (4 μM) significantly reduced both Vol and CS-area, with a smaller reduction in CS-area compared to Vol. In patients, aspirin alone significantly reduced Vol, while clopidogrel, aspirin combined with clopidogrel, and Xuesaitong significantly decreased both Vol and CS-area. Our novel analytical strategy is capable of distinguishing the pharmacological effects of various antiplatelet agents without the need for exogenous agonists, suggesting that this system may aid in the determination of the appropriate type and dose of the antiplatelet agent in the clinical setting."

Journal

Safety and Efficacy of Intracranial Stenting in Acute Stroke Patients Using a Pharmacological Treatment Protocol Including Low-Dose Intra-arterial Eptifibatide-A Single-center Retrospective Analysis. (PubMed, Clin Neuroradiol) - "In cases of MT requiring EICS, the administration of low-dose intra-arterial Eptifibatide immediately post-stenting, in addition to post-procedure dual anti-platelet therapy, demonstrated high recanalization rates with a favorable safety profile."

Journal • Retrospective data • Cardiovascular • Cerebral Hemorrhage • CNS Disorders • Hematological Disorders • Ischemic stroke • Thrombosis

Intravenous Argatroban or Eptifibatide in Patients Undergoing Mechanical Thrombectomy: A Subgroup Analysis of the MOST Randomized Clinical Trial. (PubMed, JAMA Neurol) - P3 | "Future investigations of these agents as intravenous adjuncts to thrombectomy should focus on populations who are ineligible for intravenous thrombolysis. ClinicalTrials.gov Identifier: NCT03735979."

Clinical • Journal • Cardiovascular • Cerebral Hemorrhage • CNS Disorders • Hematological Disorders • Ischemic stroke

Ecstasy-Induced Acute Myocardial Infarction Unraveled by Multimodality Imaging. (PubMed, Cureus) - "Left heart catheterization showed mild obstructive coronary disease with red thrombus in the proximal left anterior descending (LAD) artery seen on optical coherence tomography (OCT) and with note of improvement and decrease in thrombus burden on repeat coronary angiogram the next day after starting the patient on eptifibatide. Cardiac magnetic resonance imaging (CMR) showed a small-sized infarct involving the apical inferior, apical lateral, and basal septum, with myocardial edema at the apex and septum, and a note of a small apical clot. He improved significantly during his course and was maintained on ticagrelor, apixaban, and atorvastatin."

Journal • Cardiovascular • Myocardial Infarction • Thrombosis

Selective inhibition of ERO1α with M6766, a novel small-molecule inhibitor, prevents arterial thrombosis and ischemic stroke in mice. (PubMed, Mol Ther) - "Although eptifibatide, an αIIbβ3 antagonist, effectively blocks arterial thrombosis, it prolongs bleeding times at therapeutic doses. Our findings suggest that ERO1α inhibition is a promising anti-thrombotic strategy with potential advantages over current therapies."

Journal • Preclinical • Cardiovascular • Hematological Disorders • Ischemic stroke • Thrombosis • ERO1A • STIM1

Eptifibatide as an adjuvant therapy to thrombolysis versus thrombolysis alone in stroke management: a systematic review and meta-analysis of randomized controlled trials. (PubMed, J Thromb Thrombolysis) - "Eptifibatide as an adjunct to rt-PA does not significantly impact functional independence, mortality, or sICH risk in AIS. Larger studies are needed to clarify its potential benefits and risks."

Journal • Retrospective data • Review • Cardiovascular • Cerebral Hemorrhage • CNS Disorders • Hematological Disorders • Ischemic stroke

Loss of the interaction linking the aIIb K514 to the ß3 E500 leads to constitutive aIIbß3 activation (ISTH 2025) - "Eptifibatide induced a significant increase of AP5 and LIBS2 binding to some mutants (Fig 1C, D). Table or Figure Upload"

Histidine-rich Glycoprotein Modulates Platelet Adhesion by Competing with vWF for Binding GPIba (ISTH 2025) - "Fluorescently labelled HRG bound to resting human or mouse platelets in the presence of eptifibatide with a Kd =1.4 ± 0.2 µM and Kd =1.1 ± 0.3 µM, and vWF competed with IC50 values of 2.3 ± 0.3 U/mL and 3.1 ± 0.4 U/mL, respectively...Under flow conditions, 2 µM HRG significantly (P < 0.001) reduced vWF-mediated platelet string formation on histamine-activated endothelium from 37 ± 4 to 7 ± 2 strings/field at 5 minutes. Table or Figure Upload"

A microfluidic model of thromboinflammation integrating platelet secretion fibrin formation and NETosis in flowing human blood suitable for testing potential therapies (ISTH 2025) - "The following treatments were tested: glenzocimab (anti-GPVI), eptifibatide (anti-GPIIbIIIa), FXII900 (FXIIa inhibitor), and anti-tissue factor antibody. Hyperglycemia led to an exacerbation and acceleration of platelet activation, coagulation, and channel occlusion, in association with a marked formation of neutrophil extracellular traps. Combined inhibition of GPVI and FXIIa, or PPACK inhibition of thrombin, fully prevented platelet secretion and subsequent fibrin formation in both normoglycemic and hyperglycemic conditions, as well as NETosis in hyperglycemic conditions."

Cardiovascular • Diabetes • Inflammation • Ischemic stroke • ANXA5

Development of a novel point-of-care device to monitor arterial thrombosis (ISTH 2025) - "The POC was sensitive to antiplatelet agents Acetyl-Salicylic Acid, 2-MeSAMPS and eptifibatide, showing an increase in end volume, a proxy for occlusion time, after treatment (p<0.001, Figure 2B). The novel POC device provides a unique endpoint that is uncorrelated with PFA-100 results (Figure 2C/D). Table or Figure Upload"

Cardiovascular • Hematological Disorders • Myocardial Infarction • Thrombosis

Identification of an ERO1a-specific inhibitor as a novel anti-thrombotic agent (ISTH 2025) - "In contrast, eptifibatide (5 μg/g mouse, an αIIbβ3 antagonist) prolongs both TTO and tail bleeding times. Intravital microscopy demonstrates that compared to the vehicle control, M6766 (0.3 μg/g mouse) significantly inhibits platelet accumulation but not adhesion at sites of laser-induced cremaster arteriolar injury in mice. In addition, intravenous injection of M6766 into mice reduces infarct volume in ischemic stroke induced by transient middle cerebral artery injury."

CNS Disorders • Ischemic stroke • Oncology • Thrombosis • Vascular Neurology • ERO1A