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

GSK Plc

Merck Sharp & Dohme Corp.Schering-Plough Corp.

License Organization

Schering-Plough Corp.Guangzhou Qianxi Pharmaceutical Co., Ltd.

Millennium Pharmaceuticals, Inc.

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: *****

The modified Rankin Scale (mRS) is a key measure of functional outcomes in stroke trials. To minimize variability, structured tools like the Rankin Focused Assessment and central adjudication are recommended. This study compares local versus centrally adjudicated mRS scores in the MOST trial (Multi-Arm Optimization of Stroke Thrombolysis).

METHODS::

MOST was a phase 3, single-blind, randomized trial evaluating argatroban, eptifibatide, or placebo in addition to intravenous thrombolysis. The primary outcome, 90-day mRS score, was gathered through in-person video recordings by blinded local personnel. Recordings were sent to central adjudicators for final scoring. As in-person visits became limited due to SARS-CoV-2, remote interviews were allowed. We hypothesized that local mRS scores would be moderately associated with central scores. Fleiss-Cohen quadratic weighted κ statistics were used to determine the strength of agreement.

RESULTS::

Out of 514 participants, 378 had recorded visits available (121 in-person video, 157 remote video, 100 remote audio). Local assessors were blinded 96.8% of the time and 85.4% of visits used the Rankin Focused Assessment. Overall agreement between local and central mRS scores was excellent (weighted κ, 0.87 [95% CI, 0.83–0.90]). A nonsignificant decrease in strength of agreement was noted for those with a nonzero baseline mRS (mRS score=0, 0.87 [95% CI, 0.84–0.91] versus mRS score >0, 0.80 [95% CI, 0.68–0.91]). Trial conclusions were unchanged when utilizing the local mRS versus central adjudication.

CONCLUSIONS::

Local mRS scores demonstrated strong agreement with central scores across all assessment modes. With blinded end point assessments, central mRS adjudication in acute stroke trials may not be necessary.

REGISTRATION::

URL: https://www.clinicaltrials.gov ; Unique identifier: NCT03735979.

01 May 2025·Journal of NeuroInterventional Surgery

Safety and efficacy of cangrelor in endovascular thrombectomy compared with glycoprotein IIb/IIIa Inhibitors

Article

Author: Goldman, Daryl ; Rao, Naina ; Oxley, Thomas ; Wu, Katty ; Ouf, Aya ; Zhang, Jack ; Dangayach, Neha ; Caton, Michael T ; Kellner, Christopher Paul ; De Leacy, Reade Andrew ; Shoirah, Hazem ; Majidi, Shahram ; Fara, Michael G ; Davy, Connor ; Mocco, J ; Musallam, Nadine ; Fifi, Johanna T ; Devarajan, Alex ; Shigematsu, Tomoyoshi ; Gottiparthi, Shouri ; Davis, Nicole

Background:

Cangrelor, an intravenous P2Y12-receptor inhibitor, is a reversible and short-acting antithrombotic medication non-inferior to irreversible glycoprotein IIb/IIIa inhibitors (GPIs) like eptifibatide. There are insufficient data to compare the medications in endovascular thrombectomies (EVTs) requiring emergent platelet inhibition.

Objective:

To review our institution’s experience with cangrelor in EVT and compares its safety and efficacy against GPIs.

Methods:

A large healthcare system retrospective review identified all patients who had received cangrelor or eptifibatide intraoperatively during EVT between December 2018 and March 2023 for this cohort study. Clinical data were reviewed. Functional status was defined by the modified Rankin Scale (mRS) and National Institutes of Health Stroke Scale (NIHSS) at multiple time points. Multivariate regression was performed.

Results:

Of 1010 EVT patients, 36 cangrelor and 104 eptifibatide patients were selected. There were no differences in baseline function or presentations. Cangrelor was frequently administered for stenting tandem occlusions (n=16, 44.4%), and successful reperfusion occurred in 30 (83.3%) patients. On multivariate analysis, cangrelor was associated with decreased odds of hemorrhagic conversion (adjusted OR (aOR)=0.76, P=0.004) and symptomatic hemorrhage (aOR=0.86, P=0.021). There were no differences in thrombotic re-occlusion. Cangrelor was associated with a lower 24-hour NIHSS score (7.0 vs 12.0, P=0.013) and discharge NIHSS score (3.0 vs 9.0, P=0.004). There were no differences in in-hospital mortality or length of stay. Cangrelor was associated with improved odds of favorable outcome, defined as mRS score 0–2, at discharge (aOR=2.69, P=0.001) and on 90-day follow-up (aOR=2.23, P=0.031).

Conclusion:

Cangrelor was associated with a decreased risk of hemorrhagic conversion and might lead to favorable functional outcomes for patients during hospitalization in comparison with GPIs. Prospective studies are warranted to investigate its use in EVT.

01 Apr 2025·Pharmacological Reports

Red cell microparticles produced using high-pressure extrusion enhance both primary and secondary hemostasis

Article

Author: Cho, Sunjoo ; Rehni, Ashish K ; Dave, Kunjan R ; Jy, Wenche ; Sama, Snigdha

Abstract:

Background:

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.

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	jfhdgzatqu(ixiajrsvqp) = uimhtrfsdh jprqygyapa (uwtwcwjxbu )	Positive	30 Jan 2025
				No Eptifibatide	jfhdgzatqu(ixiajrsvqp) = cqhnyzlooq jprqygyapa (uwtwcwjxbu )
NCT03735979 (phase 3 \| MOST, CTgov)	Phase 3	Acute Ischemic Stroke	514	Argatroban (Argatroban)	pvscjkoqmq(itruerxvhm) = oxtvcghdcx zpnreyhxgi (cfqpaukygd, 3.7) View more	-	19 Nov 2024
				Eptifibatide (Eptifibatide)	pvscjkoqmq(itruerxvhm) = pbfwwabdnr zpnreyhxgi (cfqpaukygd, 3.2) View more
NCT03735979 (MOST, Literature \| Pubmed \| N Engl J Med) Manual	Phase 3	Ischemic stroke Adjuvant	514	Argatroban	vaesaynmce(mqrmouziko) = xxlevwlqln rwpkmjrxpx (umnchxahla ) View more	Negative	04 Sep 2024
				Eptifibatide	vaesaynmce(mqrmouziko) = tbwwvpjzhh rwpkmjrxpx (umnchxahla ) View more
EHA2024	Not Applicable	Acute Coronary Syndrome	26	Eptifibatide	czxpsuggaf(tjgsjihysd) = 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. rdnohhlzzl (qkugmgjfzy )	-	14 May 2024
ISC2024	Not Applicable	-	-	IA Eptifibatide	fefxubtqlt(nslfaklsgl): 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	gfvvnophtt(ljtspvhvpe) = gbnuaouydc kwrrrxstat (gxiraeqvyd ) View more	Positive	02 Feb 2022
				mechanical thrombectomy	gfvvnophtt(ljtspvhvpe) = yorbuxhvyk kwrrrxstat (gxiraeqvyd ) View more
ISC2022	Not Applicable	Ischemic stroke	236	Eptifibatide	cbraesasxp(bzzregowbh) = EPT during EVT was associated with a higher rate of PH-2 grade hemorrhages zzenymerle (xshvevopxx )	-	01 Feb 2022
				Eptifibatide (Control groups)
NCT02925923 (CTgov)	Phase 2	Acute Coronary Syndrome \| Angina, Unstable \| Acrocallosal Syndrome	100	Ticagrelor (Ticagrelor)	jhatufzgod = grberylrun hnuuvqpybx (wavmtrtekz, dbqjsgflcj - wcwaviwork) View more	-	04 May 2020
				Clopidogrel+Eptifibatide (Eptifibatide Bolus+Clopidogrel)	jhatufzgod = lihjypzfbi hnuuvqpybx (wavmtrtekz, voknnzmuds - qeiqqojauz) View more
NCT01977456 (CLEAR-FDR, ISC2016)	Phase 2	Ischemic stroke	-	Full dose rt-PA plus eptifibatide	rjofphvorj(cdkqcgwwix) = xnecmitxyi qdqdjqjnuw (vasdqkhrrt ) View more	-	01 Feb 2016
				rt-PA alone	rjofphvorj(cdkqcgwwix) = itlvroamfw qdqdjqjnuw (vasdqkhrrt ) View more
NCT01977456 (CLEAR-FDR, CTgov)	Phase 2	Brain Infarction \| Acute Ischemic Stroke	27	Eptifibatide	jydpnvoser = ukzqtojwwg dzfvzbtlas (hmtzyntdpu, lfinlxkkpr - xtkkzqefwt) View more	-	25 Nov 2015