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

Accord Healthcare SLU

Hainan Poly Pharm. Co., Ltd.GlaxoSmithKline (Ireland) Ltd.

+ [1]

Inactive Organization

Merck Sharp & Dohme Corp.

GSK PlcSchering-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: *****

Fungal and mycotoxin contamination threaten poultry health, feed safety, and global food security. Mycotoxins result in reduced poultry growth, nutrient absorption, and a compromised immune system, causing severe financial losses. The rise of antibiotic resistance due to excessive antibiotic use in poultry also necessitates alternative strategies.

METHODS AND RESULTS:

Total 28 strains were isolated from the gut of indigenous Aseel and broiler chickens. Strains SB1, SB2, and SD2 completely inhibited Aspergillus flavus, Aspergillus ochraceus, and Fusarium proliferatum and were assessed via spore germination and mycotoxin reduction assays. The strains significantly inhibited fungal spore germination (up to 91.7 ± 0.3%;P ≤ 0.001) and reduced aflatoxin, ochratoxin, and fumonisin production by 91.6 ± 1.2%, 93.6 ± 0.6%, and 93.0 ± 0.5%, respectively. FTIR analysis of bacterial metabolites revealed shifts in peaks at 1467-3240 cm^- 1, indicating the presence of various functional groups. LC-MS/MS metabolomics, supported by multivariate analysis, revealed that metabolites were enriched with antifungal and mycotoxin-reducing compounds, including phenylacetic acid. Metabolites showed zones of inhibition up to 38.0 ± 1.1 mm against A. flavus, up to 36.0 ± 0.5 mm against A. ochraceus, and up to 34.0 ± 0.5 mm ZOI against F. proliferatum (P ≤ 0.0001). They also showed the lowest minimum inhibitory concentrations and fungicidal concentrations between 3 and 5 µLmL^- 1 (P ≤ 0.001). 16 S rRNA sequencing identified SB1 as Bacillus subtilis (PV569530), SB2 as Bacillus clausii (PV569531), and SD2 as Bacillus sp. (PV569532).

CONCLUSION:

Thus, this study highlights the microflora of indigenous Aseel chickens as a potential source of antifungal and mycotoxin-reducing compounds, offering a sustainable approach to control fungal and mycotoxin contamination in poultry feed.

CLINICAL TRIAL NUMBER:

As this study did not involve higher animals, no clinical trial number was required.

01 Oct 2025·INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS

Human serum lipids affect Staphylococcus aureus sensitivity to phage infection

Article

Author: Tavanti, Arianna ; Rindi, Laura ; Turchi, Barbara ; Di Luca, Mariagrazia ; Fausti, Elisa ; Freer, Giulia ; Bottai, Daria ; Cesta, Novella ; Campobasso, Claudia

OBJECTIVES:

To explore phage therapy as an alternative for targeting multidrug-resistant bacterial strains, it is crucial to study phage-bacteria interaction under conditions that mimic in vivo environments. Recent studies have demonstrated that staphylococcal phage activity can be significantly hindered by human blood components, including plasma and serum. This study aimed to identify serum components responsible for phage inhibition and assess whether this effect occurred across multiple Staphylococcus aureus strains.

METHODS:

Phage Sb-1 activity against S. aureus ATCC 43300 was tested by pre-incubating or co-incubating bacteria and phages with 30% (v/v) heat-inactivated (56 °C and 80 °C) human, bovine, or foetal calf serum, IgG-depleted or delipidated serum, and BSA. Bacteria were incubated with serum before phage exposure, followed by washing with 0.1% Triton X-100. Additionally, growth kinetics of ten S. aureus strains incubated with or without Sb-1 were assessed over 24 hours in the presence of human serum.

RESULTS:

We found that adult human serum completely impairs phage infectivity due to interactions between serum components and bacterial cells rather than direct phage neutralisation. Albumin, IgG, and thermolabile components were demonstrated not to significantly contribute to the inhibitory effect, whereas lipids were identified as playing a key role. Furthermore, the sensitivity of different bacterial strains to phages was shown to be differentially affected by the presence of serum, as two of the strains tested remained susceptible to lysis despite serum exposure.

CONCLUSIONS:

Taken together, our findings suggest that serum lipid fraction impacts phage infectivity in a strain-specific manner, highlighting the need for tailored approaches for phage therapy.

01 Jul 2025·MOLECULAR THERAPY

Selective inhibition of ERO1α with M6766, a novel small-molecule inhibitor, prevents arterial thrombosis and ischemic stroke in mice

Article

Author: Jha, Vishwanath ; Castelblanco, Esmeralda ; Lee, Jingu ; Bokorova, Radka ; Ahmed, Muteen ; Cho, Jaehyung ; Prinsen, Michael ; Brown, Gavriel ; Ilagan, Ma Xenia G ; Remedi, Maria S ; Kim, Jae-Sung ; Johnson, Daniel ; Jin, Bo-Ram ; Razani, Babak ; Dolle, Roland E ; Wang, Jinzhi

Using endoplasmic reticulum oxidoreductase 1α (ERO1α) conditional knockout (CKO) mice, a recent study underscores the crucial role of ERO1α in platelet activation under thrombotic conditions. Through a high-throughput screen of 39,901 compounds, we identify M6766 as a selective inhibitor of ERO1α with an IC₅₀ of 1.4 μM and a K_D of 1.1 μM. A docking model and biochemical studies reveal that M6766 binds to the flavin adenine dinucleotide-binding pocket in ERO1α and exhibits >70-fold selectivity over other tested enzymes, except ERO1β, which it inhibits with an IC₅₀ of 7.2 μM. M6766 concentration-dependently inhibits granule secretion, αIIbβ3 integrin activation, Ca²⁺ mobilization, and platelet aggregation induced by various agonists, but it does not affect agonist-induced production of reactive oxygen species. Pretreatment of ERO1α with M6766 reduces its binding to the Ca²⁺ sensor stromal interaction molecule 1. To validate whether these inhibitory effects result from the inhibition of ERO1α and ERO1β, we generate megakaryocyte-specific Ero1β or Ero1α/β CKO mice. Deletion of platelet Ero1α/β impairs platelet activation and aggregation, whereas deletion of Ero1β has no effect. While EN460 markedly inhibits the function of Ero1α/β-null platelets, M6766 does not, highlighting its specificity. M6766 treatment diminishes platelet accumulation on collagen-coated surfaces under arterial shear conditions. Moreover, intravenous injection of M6766 into mice decreases arterial thrombosis and infarct volume during ischemic stroke without prolonging tail bleeding times. 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.

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	Acute Ischemic Stroke	60	Eptifibatide	rskcgduzaz(rjjkhcgftc) = oxmxcfmdqv rgajguekxu (aqhymuqrjz )	Positive	30 Jan 2025
				No Eptifibatide	rskcgduzaz(rjjkhcgftc) = jascelvoye rgajguekxu (aqhymuqrjz )
NCT03735979 (phase 3 \| MOST, CTgov)	Phase 3	Acute Ischemic Stroke	514	Argatroban (Argatroban)	jypwmvkmkd(khjqaqrfyx) = wfnzmrigan umirumxuqb (tlebxpkmvy, 3.7) View more	-	19 Nov 2024
				Eptifibatide (Eptifibatide)	jypwmvkmkd(khjqaqrfyx) = psovzrivis umirumxuqb (tlebxpkmvy, 3.2) View more
NCT03735979 (MOST, Literature \| Pubmed \| N Engl J Med) Manual	Phase 3	Ischemic stroke Adjuvant	514	Argatroban	ipnwuzibuc(dctapxaotl) = kibocvyhro vpojxcgjxo (fpmyxvllwy ) View more	Negative	04 Sep 2024
				Eptifibatide	ipnwuzibuc(dctapxaotl) = dhuxfcqlux vpojxcgjxo (fpmyxvllwy ) View more
EHA2024	Not Applicable	Acute Coronary Syndrome	26	Eptifibatide	kgmrfakztz(zonssrocnn) = 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. zqizzsfpao (noevixdkoc )	-	14 May 2024
ISC2024	Not Applicable	-	-	IA Eptifibatide	jdiqwtzddz(mbfawuuccx): 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	ailpcsjgrw(yloolxhdbk) = hbnbseagxy yioijitoqo (kjiybykhvh ) View more	Positive	02 Feb 2022
				mechanical thrombectomy	ailpcsjgrw(yloolxhdbk) = ocdplknpzo yioijitoqo (kjiybykhvh ) View more
ISC2022	Not Applicable	Ischemic stroke	236	Eptifibatide	ycoamzhfdz(oprflxmwev) = EPT during EVT was associated with a higher rate of PH-2 grade hemorrhages zmdsjgnlvd (gowtggsrjs )	-	01 Feb 2022
				Eptifibatide (Control groups)
NCT02925923 (CTgov)	Phase 2	Acute Coronary Syndrome \| Angina, Unstable \| Acrocallosal Syndrome	100	Ticagrelor (Ticagrelor)	ebazqjlxxq = vazrbitmyq wiazllduvh (oqecsegazr, vtxxzbkkly - gcwcgluvqd) View more	-	04 May 2020
				Clopidogrel+Eptifibatide (Eptifibatide Bolus+Clopidogrel)	ebazqjlxxq = yfvkcyotbh wiazllduvh (oqecsegazr, jwifdrnyde - ctxaldlbnf) View more
NCT01977456 (CLEAR-FDR, ISC2016)	Phase 2	Ischemic stroke	-	Full dose rt-PA plus eptifibatide	smpthijgpr(opvzdcxfwb) = hsmttpvsbe wuqfrijifb (qvpklftzvy ) View more	-	01 Feb 2016
				rt-PA alone	smpthijgpr(opvzdcxfwb) = igijxlpbla wuqfrijifb (qvpklftzvy ) View more
NCT01977456 (CLEAR-FDR, CTgov)	Phase 2	Brain Infarction \| Acute Ischemic Stroke	27	Eptifibatide	lldbybqqoi = madczzbsri aeppqgzblk (ytraiqfuat, sbzpzabafc - swvmskgorc) View more	-	25 Nov 2015