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eptifibatide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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) | 5 mg/mL | Bocci G, Oprea TI, Benet LZ |
| 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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,CDK5,EIF2AK3,GRK2,ITK,PDK1,PDK2,PDK4,PRKDC | 9 | |||
| kinase-selectivity-class | GRK2 | 1 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 18, 1998 | FDA | SCHERING | |
| July 1, 1999 | EMA | GLAXOSMITHKLINE (IRELAND) LIMITED |
FDA Adverse Event Reporting System (Female)
None
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 |
|---|---|---|---|---|---|---|
| Vascular stent thrombosis | 113.03 | 54.11 | 24 | 1037 | 3218 | 42617056 |
| Thrombocytopenia | 90.85 | 54.11 | 57 | 1004 | 190222 | 42430052 |
| Arterial thrombosis | 61.01 | 54.11 | 13 | 1048 | 1763 | 42618511 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Vascular stent thrombosis | 143.09 | 61.45 | 27 | 1307 | 4134 | 110583831 |
| Thrombocytopenia | 126.97 | 61.45 | 68 | 1266 | 348817 | 110239148 |
| Thrombosis in device | 106.64 | 61.45 | 22 | 1312 | 5305 | 110582660 |
| Acute myocardial infarction | 83.44 | 61.45 | 33 | 1301 | 83744 | 110504221 |
| Arterial thrombosis | 68.98 | 61.45 | 14 | 1320 | 3105 | 110584860 |
FDA Adverse Event Reporting System (Pediatric)
None
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 | anticoagulant |
| CHEBI has role | CHEBI:50427 | platelet aggregation inhibitor |
Related Drugs by ATC class:
B01AC Platelet aggregation inhibitors excl. heparin 24 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Unstable angina | indication | 4557003 | |
| NonQ wave myocardial infarction | indication | 314207007 | |
| 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 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
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 | 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 | 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 | 52958-040 | INJECTION, SOLUTION | 0.75 mg | INTRAVENOUS | ANDA | 25 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52958-402 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 25 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 | 62147-0601 | 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 | 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 | 71288-412 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 26 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71288-413 | INJECTION, SOLUTION | 0.75 mg | INTRAVENOUS | ANDA | 26 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 |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 83634-300 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | ANDA | 27 sections |
| Eptifibatide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 83634-301 | INJECTION, SOLUTION | 0.75 mg | INTRAVENOUS | ANDA | 27 sections |