eptifibatide
Trade name: integrilin
Approved
May 18, 1998
Eptifibatide is a platelet aggregation inhibitor - an anti-coagulant that selectively blocks the platelet glycoprotein IIb/IIIa receptor. It is a cyclic heptapeptide derived from a protein found in the venom of the southeastern pygmy rattlesnake. It belongs to the class of the so called arginin-glycin-aspartat-mimetics and reversibly binds to platelets. Eptifibatide inhibits platelet aggregation by reversibly binding to the platelet receptor glycoprotein (GP) IIb/IIIa of human platelets, thus preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands. Inhibition of platelet aggregation occurs in a dose- and concentration-dependent manner. It is used for treatment of myocardial infarction and acute coronary syndrome. — NCATS
Clinical trial activity
29 trials · 32 clinical orgs · 21 marketing orgs
Earliest trial started May 1, 2003 (NCT00061373)
Timeline
1990s
2000s
2010s
- Jun 5, 2015
Teva — Marketing Organization
- Dec 8, 2015
Aurobindo Pharma — Marketing Organization
- Dec 8, 2015
Eugia Pharma — Marketing Organization
- Dec 8, 2016
Amneal Pharmaceuticals — Marketing Organization
- Apr 18, 2017
Akorn, Inc. — Marketing Organization
- Apr 18, 2017
Rising Pharmaceuticals — Marketing Organization
- Nov 6, 2017
Accord Research — Marketing Organization
- Mar 7, 2018
Sagent Pharmaceuticals, Inc. — Marketing Organization
- Mar 7, 2018
Nichi-Iko Pharmaceutical Co., Ltd. — Marketing Organization
- Jul 20, 2018
Mylan — Marketing Organization
- Nov 23, 2018
Baxalta — Marketing Organization
- Nov 23, 2018
Shire — Marketing Organization
- Jan 25, 2019
Hainan Poly Pharm — Marketing Organization
- Jan 25, 2019
SLATE RUN PHARMA — Marketing Organization
- Mar 11, 2019
USV — Marketing Organization
2020s
- Mar 20, 2020
Hybio — Marketing Organization
- Sep 7, 2021
Shuangcheng — Marketing Organization
- May 9, 2024
Eu Yan Sang — Marketing Organization
- May 9, 2024
Meitheal — Marketing Organization
Indications
Approved for
Studied for
- Acute Coronary Syndrome · Phase 3
- Anemia, Sickle Cell · Phase 1/Phase 2
- Angina, Unstable · Phase 2
- Angioplasty · Phase 4
- Brain Diseases · Phase 2
- Brain Infarction · Phase 2
- Cardiovascular Diseases · Phase 3
- Cerebral Infarction · Phase 2
- Coronary Artery Disease · Phase 4
- Coronary Disease · Phase 2
- Ischemic Stroke · Phase 3
- Myocardial Infarction · Phase 4
- Myocardial Ischemia · Phase 3
- Non-ST Elevated Myocardial Infarction · Phase 4
- Pneumonia · Phase 2
- Shock, Septic · Phase 2
- ST Elevation Myocardial Infarction · Phase 2
- Stroke · Phase 2
Mechanism of action
Integrin alpha-V/beta-3/alpha-V/beta-5 inhibitor
- Integrin alpha-IIb/beta-3INHIBITOR
Integrin alpha-IIb/beta-3 inhibitor
Approval history
- approvedPriority reviewMay 18, 1998
Chemistry & pharmacology
SMILES
NC(=N)NCCCC[C@@H]1NC(=O)CCSSC[C@H](NC(=O)[C@@H]2CCCN2C(=O)[C@H](CC3=CNC4=C3C=CC=C4)NC(=O)[C@H](CC(O)=O)NC(=O)CNC1=O)C(N)=O- Mol. weight
- 831.962 g/mol
- Lipinski Ro5
- 3 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Parenteral
- Availability
- Prescription Only
- Multi-specific
- No
Oral
No
Parenteral
Yes
Topical
No
Sources
- WikipediaEptifibatide ↗
- NCATSNA8320J834 ↗
- ChEMBLCHEMBL1174 ↗
Also known as
- eftifibatide
- epifibatide
- epifibratide
- eptifibatide
- eptifibatide
- eptifibatide
- eptifibatide
- eptifibatide
- eptifibatide
- eptifibatide
- eptifibatide
- eptifibatide
- eptifibatide
- eptifibatide
- eptifibatide
- integrelin
- integrelin
- integrelin
- integrelin
- integrilin
- integrilin
- integrilin
- integrilin
- integrilin
- intrifiban
- intrifiban
- intrifiban
- intrifiban
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06712004 | Phase 2 | Dec 15, 2024 | Southern Medical University |
| NCT05415150 | Phase 1/Phase 2 (Phase 2) | Feb 18, 2022 | Baylor University |
| NCT03735979 | Phase 3 | Jun 30, 2019 | National Institute of Neurological Disorders and Stroke (NINDS), University of Cincinnati |
| NCT03844594 | Phase 3 | Apr 6, 2019 | Capital Medical University, Government of China |
| NCT02925923 | Phase 2 | Sep 1, 2016 | University of Alabama, Birmingham |
| NCT02204852 | Phase 2 | Sep 1, 2014 | University of Copenhagen |
| NCT01919723 | Phase 2 | Feb 1, 2014 | AstraZeneca, University of Alabama, Birmingham |
| NCT01977456 | Phase 2 | Sep 1, 2013 | National Institute of Neurological Disorders and Stroke (NINDS), University of Cincinnati |
| NCT01532544 | Phase 2 | Jun 1, 2012 | Thrombologic ApS, University of Copenhagen |
| NCT01522417 | Phase 2 | Apr 1, 2012 | Medicure, SCRI Development Innovations |
| NCT01076764 | Phase 3 | Apr 1, 2010 | Sanofi |
| NCT00945308 | Phase 2 | Aug 1, 2009 | Tel Aviv University |
| NCT00894803 | Phase 2 | Jul 1, 2009 | National Institute of Neurological Disorders and Stroke (NINDS), University of Cincinnati |
| NCT00834899 | Phase 1/Phase 2 (Phase 2) | Jan 1, 2009 | University of North Carolina at Chapel Hill |
| NCT00638976 | Phase 3 | Nov 1, 2007 | Fondazione Mediolanum per Attività e Ricerche Cardiovascolari Onlus |
| NCT00719914 | Phase 2 | Nov 1, 2007 | Harvard University, Schering-Plough, TIMI Study Group, Boston, MA |
| NCT01454440 | Phase 4 | Oct 1, 2007 | University of Turin |
| NCT00812435 | Phase 3 | Aug 1, 2007 | Georgetown University |
| NCT01103440 | N/A | Apr 1, 2007 | Icahn School of Medicine at Mount Sinai |
| NCT00426751 | Phase 3 | Oct 1, 2006 | GlaxoSmithKline |
Organizations
Research & Development (32)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| National Institute of Neurological Disorders and Stroke (NINDS) | Government | 5 | 1 | 2 | 2003 |
| University of Cincinnati | Academic/Hospital | 4 | 4 | 2 | 2003 |
| Schering-Plough | For profit | 3 | 0 | 3 | 2005 |
| Harvard University | Academic/Hospital | 2 | 2 | 2 | 2006 |
| Sanofi | For profit | 2 | 2 | 2 | 2006 |
| University of Alabama, Birmingham | Academic/Hospital | 2 | 2 | 1 | 2014 |
| University of Copenhagen | Academic/Hospital | 2 | 1 | 1 | 2012 |
| AstraZeneca | For profit | 1 | 0 | 1 | 2014 |
| Baylor University | Academic/Hospital | 1 | 1 | 1 | 2022 |
| Capital Medical University | Academic/Hospital | 1 | 0 | 1 | 2019 |
| Case Western Reserve University | Academic/Hospital | 1 | 0 | 1 | 2006 |
| Duke University | Academic/Hospital | 1 | 0 | 1 | 2004 |
| Fondazione Mediolanum per Attività e Ricerche Cardiovascolari Onlus | Academic/Hospital | 1 | 1 | 1 | 2007 |
| Georgetown University | Academic/Hospital | 1 | 1 | 1 | 2007 |
| GlaxoSmithKline | For profit | 1 | 1 | 1 | 2006 |
| Government of China | Government | 1 | 1 | 1 | 2019 |
| Icahn School of Medicine at Mount Sinai | Academic/Hospital | 1 | 1 | 1 | 2007 |
| LifeBridge Health | Academic/Hospital | 1 | 1 | 1 | 2006 |
| Medicure | For profit | 1 | 1 | 1 | 2012 |
| Medtronic | For profit | 1 | 0 | 1 | 2005 |
Marketing (24)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Accord Research | For profit | MKTG | Nov 6, 2017 |
| Akorn, Inc. | For profit | MKTG | Apr 18, 2017 |
| Amneal Pharmaceuticals | For profit | MKTG | Dec 8, 2016 |
| Aurobindo Pharma | For profit | MKTG | Dec 8, 2015 |
| Baxalta | For profit | MKTG | Nov 23, 2018 |
| Eu Yan Sang | For profit | MKTG | May 9, 2024 |
| Eugia Pharma | For profit | MKTG | Dec 8, 2015 |
| Hainan Poly Pharm | For profit | MKTG | Jan 25, 2019 |
| Hybio | For profit | MKTG | Mar 20, 2020 |
| Meitheal | For profit | MKTG | May 9, 2024 |
| Merck | For profit | MKTG | May 18, 1998 |
| Merck | For profit | NDA2 | May 18, 1998 |
| Mylan | For profit | MKTG | Jul 20, 2018 |
| Nichi-Iko Pharmaceutical Co., Ltd. | For profit | MKTG | Mar 7, 2018 |
| Rising Pharmaceuticals | For profit | MKTG | Apr 18, 2017 |
| SLATE RUN PHARMA | For profit | MKTG | Jan 25, 2019 |
| Sagent Pharmaceuticals, Inc. | For profit | SYN | Mar 7, 2018 |
| Sagent Pharmaceuticals, Inc. | For profit | MKTG | Mar 7, 2018 |
| Schering | For profit | NDA | May 18, 1998 |
| Schering | For profit | NDA2 | May 18, 1998 |
| Shire | For profit | MKTG | Nov 23, 2018 |
| Shuangcheng | For profit | MKTG | Sep 7, 2021 |
| Teva | For profit | MKTG | Jun 5, 2015 |
| USV | For profit | MKTG | Mar 11, 2019 |