Delving into the Latest Updates on Eptifibatide with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Eptifibatide (INN), Integrelin, Intrifiban

+ [8]

Target

GP IIb/IIIa

Action

antagonists

Mechanism

GP IIb/IIIa antagonists(Integrin alpha-IIb/beta-3 antagonists)

Therapeutic Areas

Nervous System DiseasesCardiovascular DiseasesOther Diseases

Active Indication

Angina, UnstableNon-St Elevated Myocardial InfarctionAcute Coronary Syndrome+ [1]

Inactive Indication

ST Elevation Myocardial Infarction

Originator Organization

Millennium Pharmaceuticals, Inc.

Active Organization

Jiangsu Hansoh Pharmaceutical Co., Ltd.Accord Healthcare SLUGlaxoSmithKline (Ireland) Ltd.

+ [1]

Inactive Organization

Merck Sharp & Dohme Corp.Schering-Plough Corp.

GSK Plc

Drug Highest PhaseApproved

First Approval Date

United States (18 May 1998),

Acute Coronary SyndromeMyocardial Infarction

Regulation-

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Structure/Sequence

Molecular FormulaC35H49N11O9S2

InChIKeyCZKPOZZJODAYPZ-LROMGURASA-N

CAS Registry188627-80-7

Sequence Code 13855361

Source: *****

Current therapies to treat excessive bleeding are associated with significant complications, which may outweigh their benefits. Red blood cell-derived microparticles (RMPs) are a promising hemostatic agent. Previous studies demonstrated that they reduce bleeding in animal models, correct coagulation defects in patient blood, and have an excellent safety profile. However, their exact mechanism of action is not known. We investigated the potential role of RMPs on primary and secondary hemostasis.

Methods:

To evaluate the effects of RMPs, prepared using high-pressure extrusion, on primary hemostasis, we employed platelet aggregometry with platelet inhibitors, eptifibatide, and ticagrelor, with and without RMPs. To evaluate their effects on secondary hemostasis, we employed thromboelastography with plasma deficient in factors VII, VIII, IX, XI, and XII with and without RMPs.

Results:

We found that RMPs significantly increased collagen-induced platelet aggregation. However, there were no significant differences with and without RMP in the presence of the platelet inhibitors, indicating that RMPs may work through these receptors, either directly or indirectly. For secondary hemostasis, RMPs significantly decreased clotting times for plasma deficient in factors VII, VIII, IX, and XI but not in XII.

Conclusions:

Our results indicate that RMPs enhance primary hemostasis and both pathways of secondary hemostasis.

04 Feb 2025·Journal of the American Heart Association

Comparative Effects of Glenzocimab and Eptifibatide on Bleeding Severity in 2 Mouse Models of Intracranial Hemorrhage

Article

Author: Zemali, Fatima ; Pascal, Eloïse ; Mavouna, Sabrina ; Dupont, Sébastien ; Bourrienne, Marie‐Charlotte ; Desilles, Jean‐Philippe ; Nieswandt, Bernhard ; Cogo, Adrien ; Solo Nomenjanahary, Mialitiana ; Mazighi, Mikael ; Boulaftali, Yacine ; Perrot, Astride ; Loyau, Stéphane ; Ho‐Tin‐Noé, Benoît ; Ollivier, Véronique ; Lebas, Héloïse ; Camerer, Eric ; Jandrot‐Perrus, Martine ; Farkh, Carine

Background:

Antiplatelet drugs represent potential candidates for protecting the penumbral microcirculation during cerebral ischemia and improving the benefits of arterial recanalization in ischemic stroke. Yet while the efficacy of such adjuvant strategies has been shown to be highly time dependent, antiplatelet therapy at the acute phase of ischemic stroke cannot be envisioned until the diagnosis of stroke and its ischemic nature have been confirmed because of the presumed risk of worsening bleeding in case of intracranial hemorrhage (ICH). Here, we investigated this risk for 2 antiplatelet drugs currently being tested in clinical trials for ischemic stroke, glenzocimab and eptifibatide, in 2 mouse models of ICH.

Methods and Results:

The severity of ICH was assessed in mice humanized for glycoprotein VI treated or not with glenzocimab or eptifibatide at effective dose, in a model of primary ICH caused by unilateral striatal injection of collagenase type VII, and in a model of hyperglycemia‐induced hemorrhagic transformation of cerebral ischemia–reperfusion injury. Glenzocimab had no impact on bleeding severity in either model of ICH. Conversely, eptifibatide caused a significant increase in intracranial bleeding in both models, and a drastic increase in death after hyperglycemia‐induced hemorrhagic transformation of cerebral ischemia–reperfusion injury.

Conclusions:

Unlike eptifibatide, glenzocimab is safe in the setting of ICH. These results suggest that glenzocimab could be administered upon suspicion of ischemic stroke, before assessment of its ischemic nature, thus opening the way to hastening of treatment initiation.

16 Dec 2024·EUROPEAN HEART JOURNAL

Glycoprotein IIb/IIIa inhibitors in acute myocardial infarction and angiographic microvascular obstruction: the REVERSE-FLOW trial

Article

Author: Stiermaier, Thomas ; Eitel, Ingo ; Thiele, Holger ; Jurczyk, Dominik ; Mueller, Christian ; Desch, Steffen ; Fach, Andreas ; Hambrecht, Rainer ; Frerker, Christian ; Haaf, Philip ; Saraei, Roza ; Kurz, Thomas ; Joost, Alexander ; Wienbergen, Harm ; Marquetand, Christoph ; Schmidt, Tobias ; Fahrni, Gregor ; Allali, Abdelhakim

Abstract:

Background and Aims:

Glycoprotein (GP) IIb/IIIa inhibitors are recommended in acute myocardial infarction (AMI) for bailout treatment in case of angiographic microvascular obstruction (MVO), also termed no-reflow phenomenon, after percutaneous coronary intervention (PCI) with, however, lacking evidence (class IIa, level C).

Methods:

The investigator-initiated, international, multicentre REVERSE-FLOW trial randomized 120 patients with AMI and thrombolysis in myocardial infarction flow grade ≤ 2 after primary PCI to optimal medical therapy with or without GP IIb/IIIa inhibitor. The primary endpoint was infarct size [percentage of left ventricular (LV) mass assessed by cardiac magnetic resonance (CMR). Secondary endpoints included CMR-derived MVO and 30-day adverse clinical events. The trial is registered with ClinicalTrials.gov: NCT02739711.

Results:

The population was predominantly male (76.7%) with a median age of 66 years and ST-elevation myocardial infarction in 73.3% of patients. Clinical and angiographic characteristics were well balanced between the cohorts. Patients in the treatment group (n = 62) received eptifibatide (n = 41) or tirofiban (n = 21). Infarct size assessed by CMR imaging was similar in both study groups [25.4% of LV mass (%LV) vs. 25.2%LV; P = .386]. However, the number of patients with evidence of CMR-derived MVO (74.5% vs. 92.2%; P = .017) and the extent of MVO (2.1%LV vs. 3.4%LV; P = .025) were significantly reduced in the GP IIb/IIIa inhibitor group compared with controls. Thirty-day outcome showed an increased bleeding risk after GP IIb/IIIa inhibitor administration restricted to non–life-threatening bleedings (22.6% vs. 6.9%; P = .016) without differences in all-cause mortality (4.8% vs. 3.4%; P = .703).

Conclusions:

Bailout GP IIb/IIIa inhibition in AMI patients with angiographic MVO failed to reduce the primary endpoint infarct size but decreased CMR-derived MVO and led to an increase in non-fatal bleeding events.

10

News (Medical) associated with Eptifibatide

23 Sep 2024

·www.businesswire.com

Avenacy to Share Company’s Year One Progress at CPHI Milan 2024

SCHAUMBURG, Ill.--( BUSINESS WIRE )--Avenacy, a specialty pharmaceutical company focused on supplying critical medications, looks forward to celebrating its first year of growth and success since launching in October 2023. Backed by a robust global network of development and FDA-inspected contract manufacturing partners, Avenacy has already brought 13 injectable products to the U.S. market to address key gaps in the drug supply chain. “We are incredibly proud of the achievements and progress we have made at Avenacy since launching nearly a year ago as a trusted partner and provider of critical injectable medicines for the U.S. healthcare system,” said Jeff Yordon, Co-Founder and CEO of Avenacy. “We have acted swiftly and decisively to bring over a dozen medications to the U.S. market to help meet the needs of patients, strengthened our financial position with the addition of esteemed pharmaceutical investor and businessman, Dr. Patrick Soon-Shiong, and built out our infrastructure and leadership to support scaling up our business. As we look to usher in the next phase of growth for Avenacy, we will remain steadfast in our goal of enhancing patient care and enabling access to safe, high-quality essential medications.” Through a rigorous and optimized selection process, Avenacy has launched thirteen products in the U.S. market, including: Melphalan Hydrochloride for Injection Bivalirudin for Injection Fosaprepitant for Injection Fulvestrant Injection Furosemide for Injection Desmopressin Acetate for Injection Eptifibatide for Injection Magnesium Sulfate in Water for Injection Isoproterenol Hydrochloride Injection, USP Tranexamic Acid Injection, USP Prochlorperazine Edisylate Injection, USP Palonosetron Hydrochloride Injection, USP Metoclopramide Injection, USP The Company is well-positioned to continue expanding its differentiated portfolio to meet the needs of today’s dynamic drug supply chain while ensuring quality of care to patients. All of Avenacy’s products feature unique packaging and labeling designed to assist healthcare providers with accurate medication selection, thereby supporting a reduction in administration errors and improper dosing. The Company also utilizes ready-to-use formulations of essential medications to help address dosing inaccuracies, enhance patient safety, and streamline efficiency – all with the ultimate goal of improving patient care. Avenacy will be sharing its first year progress, differentiated business model, and diverse partner network at this year’s CPHI 2024 Conference, taking place in Milan from October 8-10. During this time, the Company will be hosting meetings with potential partners, customers, and investors, as it seeks to expand its global presence and portfolio of critical injectable medicines. About Avenacy Avenacy is a U.S.-based specialty pharmaceutical company focused on supplying critical injectable medications used to treat patients in various medically supervised settings, from acute care hospitals to outpatient clinics and physician offices. Through a rigorous and optimized selection process, the Company is building out a pipeline of high-quality FDA approved injectable products in order to ensure a resilient portfolio that can meet the needs of today’s dynamic drug supply chain. With an experienced team, commitment to quality and reliability, and product offerings intended to facilitate safe and efficient patient care, Avenacy strives to be a trusted partner for essential medications. Avenacy was launched in 2023 and is headquartered in Schaumburg, IL. For more information, please visit http://www.avenacy.com/ .

Executive Change

06 Sep 2024

·www.drugs.com

Adjunctive IV Argatroban, Eptifibatide Do Not Cut Disability After Stroke

FRIDAY, Sept. 6, 2024 -- Adjunctive treatment with intravenous argatroban or eptifibatide does not reduce poststroke disability among patients with acute ischemic stroke treated with intravenous thrombolysis within three hours after symptom onset, according to a study published in the Sept. 5 issue of the New England Journal of Medicine . Opeolu Adeoye, M.D., from Washington University in St. Louis, and colleagues conducted a phase 3, randomized, controlled clinical trial at 57 U.S. sites involving patients with acute ischemic stroke who had received intravenous thrombolysis within three hours after symptom onset. Participants received intravenous argatroban (59 patients), eptifibatide (227 patients), or placebo (228 patients) within 75 minutes after initiation of thrombolysis. The researchers found that at 90 days, the mean utility-weighted modified Rankin scale scores were 5.2 ± 3.7, 6.3 ± 3.2, and 6.8 ± 3.0 with argatroban, eptifibatide, and placebo, respectively. The posterior probabilities that argatroban was better than placebo and that eptifibatide was better than placebo were 0.002 and 0.041, respectively (posterior mean difference in utility-weighted modified Rankin scale score, −1.51 ± 0.51 and −0.50 ± 0.29, respectively). The three groups had a similar incidence of symptomatic intracranial hemorrhage (4, 3, and 2 percent, respectively). Mortality at 90 days was higher in the argatroban and eptifibatide groups versus the placebo group (24 and 12 percent, respectively, versus 8 percent). "We found no benefit of adjunctive intravenous argatroban or eptifibatide in patients with acute ischemic stroke treated with intravenous thrombolysis within three hours after symptom onset," the authors write. Several authors disclosed ties to the biopharmaceutical industry.

Clinical ResultPhase 3

29 Apr 2024

·www.biospace.com

Avenacy Announces Launch of Eptifibatide for Injection in the U.S. Market

SCHAUMBURG, Ill.--(BUSINESS WIRE)-- Avenacy, a specialty pharmaceutical company focused on supplying critical injectable medications, today announced it has launched Eptifibatide for Injection in the United States as a therapeutic equivalent generic for Integrilin® for Injection (Eptifibatide) approved by the U.S. Food and Drug Administration. Eptifibatide for Injection is indicated for use in acute coronary syndrome (ACS) and percutaneous coronary intervention (PCI). This press release features multimedia. View the full release here: (Photo: Business Wire) Avenacy’s Eptifibatide for Injection is available as a 75 mg/100 mL single-dose vial. In line with Avenacy’s mission to champion patient safety and streamline patient care, Eptifibatide for Injection will feature the Company’s highly differentiated packaging and labeling to support accurate medication selection. Avenacy will begin shipping Eptifibatide for Injection to wholesale partners this week. The Company is supported by a global network of development and FDA-approved cGMP-certified contract manufacturing partners. Eptifibatide for Injection had U.S. sales of approximately $8.3 million for the twelve months ending in June 2023.1 Approved Indications: Acute Coronary Syndrome (ACS) Eptifibatide injection is indicated to decrease the rate of a combined endpoint of death or new myocardial infarction in patients with ACS (unstable angina/non-ST-elevation myocardial infarction), including patients who are to be managed medically and those undergoing percutaneous coronary intervention. Percutaneous Coronary Intervention (PCI) Eptifibatide injection is indicated to decrease the rate of a combined endpoint of death, new MI, or need for urgent intervention in patients undergoing PCI, including those undergoing intracoronary stenting. Please see link for Full Prescribing Information. Integrilin® is a registered trademark of Merck. 1Source: IQVIA About Avenacy Avenacy is a U.S.-based specialty pharmaceutical company focused on supplying critical injectable medications used to treat patients in various medically supervised settings, from acute care hospitals to outpatient clinics and physician offices. Through a rigorous and optimized selection process, the Company is building out a pipeline of high-quality FDA approved injectable products in order to ensure a resilient portfolio that can meet the needs of today’s dynamic drug supply chain. With an experienced team, commitment to quality and reliability, and product offerings intended to facilitate safe and efficient patient care, Avenacy strives to be a trusted partner for essential medications. Avenacy was launched in 2023 and is headquartered in Schaumburg, IL. For more information, please visit .

Drug Approval

100 Deals associated with Eptifibatide

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External Link

KEGG	Wiki	ATC	Drug Bank
D06888	Eptifibatide	B01AC16	DB00063

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Angina, Unstable	United States	Merck Sharp & Dohme Corp.	16 Jun 2003
Non-St Elevated Myocardial Infarction	United States	Merck Sharp & Dohme Corp.	16 Jun 2003
Acute Coronary Syndrome	United States	Merck Sharp & Dohme Corp.	18 May 1998
Myocardial Infarction	United States	Merck Sharp & Dohme Corp.	18 May 1998

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
ST Elevation Myocardial Infarction	Phase 3	France	GSK Plc	01 Oct 2006
ST Elevation Myocardial Infarction	Phase 3	Germany	GSK Plc	01 Oct 2006

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ISC2025	Not Applicable	-	60	Eptifibatide	jwltumkjfb(obyksbuqnl) = sumkwlnukq cmoidpamhe (dqqvawqxuc )	Positive	30 Jan 2025
				No Eptifibatide	jwltumkjfb(obyksbuqnl) = qwcwpjsqkz cmoidpamhe (dqqvawqxuc )
NCT03735979 (phase 3 \| MOST, CTgov)	Phase 3	Acute Ischemic Stroke	514	Argatroban (Argatroban)	kxwghyyofe(jyjqazwibv) = imfnxyrtxy ulqmelswnw (tsfesglhmi, 3.7) View more	-	19 Nov 2024
				Eptifibatide (Eptifibatide)	kxwghyyofe(jyjqazwibv) = ksbljdynzb ulqmelswnw (tsfesglhmi, 3.2) View more
NCT03735979 (MOST, Literature \| Pubmed \| N Engl J Med) Manual	Phase 3	Ischemic stroke Adjuvant	514	Argatroban	qtqgubqktc(brwqmotsqv) = gavmidvuqt wpaaitzhgs (ehxcaswbfn ) View more	Negative	04 Sep 2024
				Eptifibatide	qtqgubqktc(brwqmotsqv) = vkcmkdzspp wpaaitzhgs (ehxcaswbfn ) View more
EHA2024	Not Applicable	Acute Coronary Syndrome	26	Eptifibatide	zexpagxvwd(mxrcsfctio) = 54% of patients experienced a platelet drop exceeding 50%, with a median post-exposure count of 76 × 10^9/L after a median duration of 36 hours. Ten percent of patients necessitated permanent eptifibatide cessation due to severe thrombocytopenia (lowest platelet count: 2 × 10^9). Treatment primarily involved a temporary hold of eptifibatide infusion in 90% of cases, with a minority receiving platelet transfusions; no patients received steroids or immunoglobulins. akkwmadphe (fkmyjlybvq )	-	14 May 2024
ISC2024	Not Applicable	-	-	IA Eptifibatide	gaihmqafcp(gsgjwxzkko): OR = 0.592 (95% CI, 0.228 - 1.539), P-Value = 0.28	-	01 Feb 2024
				No IA Eptifibatide
NCT03370939 \| NCT03844594 (ANGEL-ACT, Pubmed \| Stroke)	Phase 3	Acute Ischemic Stroke	162	mechanical thrombectomy+Eptifibatide	vfoutvtqxd(ghduvyyebz) = forbppjodo mympmotemy (lgyrrnwhto ) View more	Positive	02 Feb 2022
				mechanical thrombectomy	vfoutvtqxd(ghduvyyebz) = uqasrvxdhj mympmotemy (lgyrrnwhto ) View more
ISC2022	Not Applicable	Ischemic stroke	236	Eptifibatide	lbstudvpho(tyyvqshokd) = EPT during EVT was associated with a higher rate of PH-2 grade hemorrhages miajzukmfe (wbnpcmucnc )	-	01 Feb 2022
				Eptifibatide (Control groups)
NCT02925923 (CTgov)	Phase 2	Angina, Unstable \| Acute Coronary Syndrome \| Acrocallosal Syndrome	100	Ticagrelor (Ticagrelor)	rmbyimlpto = nxshehsywx udnwinphof (bkmowkslvh, kkyfonganv - evqitnvauy) View more	-	04 May 2020
				clopidogrel+Eptifibatide (Eptifibatide Bolus+Clopidogrel)	rmbyimlpto = nibufcwfpm udnwinphof (bkmowkslvh, lxdkeycpjw - frvvzezlxe) View more
NCT01977456 (CLEAR-FDR, ISC2016)	Phase 2	Ischemic stroke	-	Full dose rt-PA plus eptifibatide	nbdmsvgppv(tpaslvkzoe) = rxvjssmnxz dsbpusiwvt (mejcwjhxay ) View more	-	01 Feb 2016
				rt-PA alone	nbdmsvgppv(tpaslvkzoe) = qsnkqiawke dsbpusiwvt (mejcwjhxay ) View more
NCT01977456 (CLEAR-FDR, CTgov)	Phase 2	Brain Infarction \| Acute Ischemic Stroke	27	Eptifibatide	gdkmpsgeek = lajtqhcsln lcpxiqltyp (gksqwnytis, gwkangcmrc - krndrruuyc) View more	-	25 Nov 2015