eptifibatide Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| peptides and glycopeptides | 1040 | 188627-80-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Cyclic peptide that acts as a platelet glycoprotein IIB-IIIA antagonist, reversibly inhibiting the binding of FIBRINOGEN; VON WILLEBRAND FACTOR; and other adhesive molecules to the GPIIB-IIIA RECEPTORS of platelets. It is used in the management of UNSTABLE ANGINA and in patients undergoing coronary ANGIOPLASTY and stenting procedures.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 65 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 3.68 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 0 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.17 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.20 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.75 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 4.20 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 18, 1998 | FDA | SCHERING |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Retroperitoneal haemorrhage | 207.55 | 57.25 | 38 | 1077 | 2856 | 53345095 |
| Thrombocytopenia | 99.19 | 57.25 | 51 | 1064 | 138676 | 53209275 |
| Thrombosis in device | 89.38 | 57.25 | 19 | 1096 | 3046 | 53344905 |
| Haemorrhage | 61.46 | 57.25 | 28 | 1087 | 57959 | 53289992 |
| Haematoma | 58.01 | 57.25 | 23 | 1092 | 33821 | 53314130 |
| Haemorrhage intracranial | 57.42 | 57.25 | 18 | 1097 | 13334 | 53334617 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Thrombocytopenia | 252.66 | 41.20 | 150 | 2336 | 148149 | 32362891 |
| Haemorrhage intracranial | 126.45 | 41.20 | 47 | 2439 | 15840 | 32495200 |
| Post procedural complication | 120.18 | 41.20 | 42 | 2444 | 11865 | 32499175 |
| Thrombosis in device | 102.37 | 41.20 | 28 | 2458 | 3506 | 32507534 |
| Coronary artery thrombosis | 84.89 | 41.20 | 22 | 2464 | 2239 | 32508801 |
| Vascular stent thrombosis | 82.29 | 41.20 | 22 | 2464 | 2525 | 32508515 |
| Pulmonary alveolar haemorrhage | 75.16 | 41.20 | 26 | 2460 | 7103 | 32503937 |
| Haemorrhage | 65.64 | 41.20 | 43 | 2443 | 49405 | 32461635 |
| Blood creatine phosphokinase MB increased | 54.16 | 41.20 | 15 | 2471 | 1962 | 32509078 |
| Post procedural haemorrhage | 53.20 | 41.20 | 21 | 2465 | 8279 | 32502761 |
| Myocardial infarction | 49.23 | 41.20 | 54 | 2432 | 125622 | 32385418 |
| Procedural complication | 45.15 | 41.20 | 16 | 2470 | 4684 | 32506356 |
| Vascular pseudoaneurysm | 43.99 | 41.20 | 13 | 2473 | 2141 | 32508899 |
| Arterial thrombosis | 43.51 | 41.20 | 12 | 2474 | 1544 | 32509496 |
| Post procedural haematoma | 43.15 | 41.20 | 12 | 2474 | 1592 | 32509448 |
| Pulmonary haemorrhage | 43.14 | 41.20 | 19 | 2467 | 9838 | 32501202 |
| Heparin-induced thrombocytopenia | 42.10 | 41.20 | 16 | 2470 | 5698 | 32505342 |
| Acute myocardial infarction | 41.36 | 41.20 | 34 | 2452 | 55115 | 32455925 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | B01AC16 | BLOOD AND BLOOD FORMING ORGANS ANTITHROMBOTIC AGENTS ANTITHROMBOTIC AGENTS Platelet aggregation inhibitors excl. heparin |
| FDA PE | N0000008832 | Decreased Platelet Aggregation |
| FDA EPC | N0000175578 | Platelet Aggregation Inhibitor |
| MeSH PA | D006401 | Hematologic Agents |
| MeSH PA | D010975 | Platelet Aggregation Inhibitors |
| CHEBI has role | CHEBI:50249 | anticoagulante |
| CHEBI has role | CHEBI:50427 | platelet aggregation inhibitors |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Acute coronary syndrome | indication | 394659003 | |
| Percutaneous coronary intervention | indication | 415070008 | |
| Acute hemorrhage | contraindication | 8573003 | |
| Blood coagulation disorder | contraindication | 64779008 | DOID:1247 |
| Impaired renal function disorder | contraindication | 197663003 | |
| Hemorrhagic cerebral infarction | contraindication | 230706003 | |
| Renal dialysis | contraindication | 265764009 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Surgical procedure | contraindication | 387713003 | |
| Hypertensive urgency | contraindication | 443482000 | |
| Acute Thromboembolic Stroke | contraindication | ||
| Puncture of Noncompressible Artery | contraindication |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.75 | acidic |
| pKa2 | 12.86 | acidic |
| pKa3 | 13.39 | acidic |
| pKa4 | 13.57 | acidic |
| pKa5 | 13.79 | acidic |
| pKa6 | 9.79 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Integrin alpha-IIb/beta-3 | Adhesion | INHIBITOR | IC50 | 6.24 | SCIENTIFIC LITERATURE | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| 4021114 | VUID |
| N0000148569 | NUI |
| D06888 | KEGG_DRUG |
| 4021114 | VANDF |
| C0253563 | UMLSCUI |
| CHEBI:291902 | CHEBI |
| CHEMBL1174 | ChEMBL_ID |
| D000077542 | MESH_DESCRIPTOR_UI |
| DB00063 | DRUGBANK_ID |
| 6585 | IUPHAR_LIGAND_ID |
| 7717 | INN_ID |
| NA8320J834 | UNII |
| 448812 | PUBCHEM_CID |
| 288688 | RXNORM |
| 11710 | MMSL |
| 213655 | MMSL |
| 4670 | MMSL |
| d04316 | MMSL |
| 007557 | NDDF |
| 116065005 | SNOMEDCT_US |
| 386998009 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0338-9558 | INJECTION | 75 mg | INTRAVENOUS | ANDA | 25 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0338-9559 | INJECTION | 200 mg | INTRAVENOUS | ANDA | 25 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 14335-070 | INJECTION | 2 mg | INTRAVENOUS | ANDA | 25 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 14335-071 | INJECTION | 0.75 mg | INTRAVENOUS | ANDA | 25 sections |
| EPTIFIBATIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16729-259 | INJECTION, SOLUTION | 0.75 mg | INTRAVENOUS | ANDA | 27 sections |
| EPTIFIBATIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16729-260 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 27 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-902 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 26 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-903 | INJECTION, SOLUTION | 0.75 mg | INTRAVENOUS | ANDA | 26 sections |
| eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25021-408 | INJECTION, SOLUTION | 0.75 mg | INTRAVENOUS | ANDA | 26 sections |
| eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25021-409 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 26 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52958-402 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 26 sections |
| Eptifibatide | Human Prescription Drug Label | 1 | 55150-218 | INJECTION | 75 mg | INTRAVENOUS | ANDA | 25 sections |
| Eptifibatide | Human Prescription Drug Label | 1 | 55150-219 | INJECTION | 20 mg | INTRAVENOUS | ANDA | 25 sections |
| Eptifibatide | Human Prescription Drug Label | 1 | 55150-220 | INJECTION | 200 mg | INTRAVENOUS | ANDA | 25 sections |
| Eptifibatide | Human Prescription Drug Label | 1 | 62147-0600 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 25 sections |
| Eptifibatide | Human Prescription Drug Label | 1 | 62147-0601 | INJECTION, SOLUTION | 0.75 mg | INTRAVENOUS | ANDA | 25 sections |
| Eptifibatide | Human Prescription Drug Label | 1 | 62147-0602 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 25 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67457-629 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 24 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67457-630 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 24 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67457-631 | INJECTION, SOLUTION | 0.75 mg | INTRAVENOUS | ANDA | 24 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70121-1002 | INJECTION | 2 mg | INTRAVENOUS | ANDA | 25 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70121-1003 | INJECTION | 0.75 mg | INTRAVENOUS | ANDA | 25 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70436-026 | INJECTION | 2 mg | INTRAVENOUS | ANDA | 25 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70436-027 | INJECTION | 0.75 mg | INTRAVENOUS | ANDA | 25 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70436-162 | INJECTION | 2 mg | INTRAVENOUS | ANDA | 25 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70436-163 | INJECTION | 0.75 mg | INTRAVENOUS | ANDA | 25 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70860-303 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 27 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72078-025 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 24 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72078-026 | INJECTION, SOLUTION | 0.75 mg | INTRAVENOUS | ANDA | 24 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72078-027 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 24 sections |