Detailed description page of ThPDB2
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Th1164 details |
| Primary information | |
|---|---|
| ID | 10711 |
| Therapeutic ID | Th1164 |
| Protein Name | Antithrombin Alfa |
| Sequence | NA |
| Molecular Weight | 57,215 |
| Chemical Formula | C2191H3451N583O656S18 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | NA |
| Half-life | 11.6 (84.7) for 50 IU/KG to17.7 (60.9) for 100IU/KG |
| Description | Antithrombin (Recombinant) and plasma-derived antithrombin both contain six cysteine residues forming three disulphide bridges and 3-4 N-linked carbohydrate moieties. The glycosylation profile of antithrombin (Recombinant) is different from plasma-derived antithrombin, which results in an increased heparin affinity. When assayed in the presence of excess of heparin the potency of the recombinant product is not different from that of plasma-derived product. |
| Indication/Disease | Indicated for the prevention of peri-operative and peri-partum thromboembolic events in hereditary antithrombin deficient patients |
| Pharmacodynamics | Hereditary AT deficiency causes an increased risk of venous thromboembolism (VTE). During high-risk situations such as surgery or trauma or for pregnant women, during the peripartum period, the risk of development of VTEs as compared to the normal population in these situations is increased by a factor 10 to 506,7. In hereditary antithrombin deficient patients ATryn restores (normalizes) plasma AT activity levels during peri-operative and peri-partum periods. |
| Mechanism of Action | Antithrombin (AT) plays a central role in the regulation of hemostasis. AT is the principal inhibitor of thrombin and Factor Xa5, the serine proteases that play pivotal roles in blood coagulation. AT neutralizes the activity of thrombin and Factor Xa by forming a complex which is rapidly removed from the circulation. The ability of antithrombin to inhibit thrombin and Factor Xa can be enhanced by greater than 300 to 1000 fold when AT is bound to heparin. |
| Toxicity | Highest dose tested was 360mg/kg/day in rats resulted in transient limb swelling. |
| Metabolism | Not metabolized. |
| Absorption | Given IV so not absorbed. |
| Dose of: 50IU/kg: 126.2 ml/kg 100IU/kg: 156.1 ml/kg Vd in hereditary deficient pregnant women in high risk situations had increased Vd of 14.3L. | |
| Clearance | Dose of: 50IU/kg: 9.6 ml/hr/kg 100IU/kg: 7.2 ml/hr/kg Cl in hereditary deficient pregnant women in high risk situations had increased Cl of 1.38L/h. |
| Categories | Anticoagulants,Decreased Coagulation Factor Activity,Factor Xa Inhibitors,Recombinant Antithrombin,Thrombin Inhibitors |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | Prothrombin,Coagulation factor X |
| Brand Name | NA |
| Company | NA |
| Brand Description | NA |
| Prescribed For | NA |
| Chemical Name | NA |
| Formulation | NA |
| Physical Appearance | NA |
| Route of Administration | NA |
| Recommended Dosage | The dosage is to be individualized based on the patient's pre-treatment functional AT activity level (expressed in percent of normal) and body weight (expressed in kilograms) and using therapeutic drug monitoring |
| Contraindication | NA |
| Side Effects | Hemorrhage (intra-abdominal, hemarthrosis and post procedural) |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |
| Primary information | |
|---|---|
| ID | 10712 |
| Therapeutic ID | Th1164 |
| Protein Name | Antithrombin Alfa |
| Sequence | NA |
| Molecular Weight | 57,215 |
| Chemical Formula | C2191H3451N583O656S19 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | NA |
| Half-life | 11.6 (84.7) for 50 IU/KG to17.7 (60.9) for 100IU/KG |
| Description | Antithrombin (Recombinant) and plasma-derived antithrombin both contain six cysteine residues forming three disulphide bridges and 3-4 N-linked carbohydrate moieties. The glycosylation profile of antithrombin (Recombinant) is different from plasma-derived antithrombin, which results in an increased heparin affinity. When assayed in the presence of excess of heparin the potency of the recombinant product is not different from that of plasma-derived product. |
| Indication/Disease | Indicated for the prevention of peri-operative and peri-partum thromboembolic events in hereditary antithrombin deficient patients |
| Pharmacodynamics | Hereditary AT deficiency causes an increased risk of venous thromboembolism (VTE). During high-risk situations such as surgery or trauma or for pregnant women, during the peripartum period, the risk of development of VTEs as compared to the normal population in these situations is increased by a factor 10 to 506,7. In hereditary antithrombin deficient patients ATryn restores (normalizes) plasma AT activity levels during peri-operative and peri-partum periods. |
| Mechanism of Action | Antithrombin (AT) plays a central role in the regulation of hemostasis. AT is the principal inhibitor of thrombin and Factor Xa5, the serine proteases that play pivotal roles in blood coagulation. AT neutralizes the activity of thrombin and Factor Xa by forming a complex which is rapidly removed from the circulation. The ability of antithrombin to inhibit thrombin and Factor Xa can be enhanced by greater than 300 to 1000 fold when AT is bound to heparin. |
| Toxicity | Highest dose tested was 360mg/kg/day in rats resulted in transient limb swelling. |
| Metabolism | Not metabolized. |
| Absorption | Given IV so not absorbed. |
| Dose of: 50IU/kg: 126.2 ml/kg 100IU/kg: 156.1 ml/kg Vd in hereditary deficient pregnant women in high risk situations had increased Vd of 14.3L. | |
| Clearance | Dose of: 50IU/kg: 9.6 ml/hr/kg 100IU/kg: 7.2 ml/hr/kg Cl in hereditary deficient pregnant women in high risk situations had increased Cl of 1.38L/h. |
| Categories | Anticoagulants,Decreased Coagulation Factor Activity,Factor Xa Inhibitors,Recombinant Antithrombin,Thrombin Inhibitors |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | Prothrombin,Coagulation factor X |
| Brand Name | Atryn |
| Company | Gtc Biotherapeutics, Inc. |
| Brand Description | Gtc Biotherapeutics, Inc. |
| Prescribed For | It is indicated for the prevention of peri-operative and peri-partum thromboembolic events in hereditary antithrombin deficient patients |
| Chemical Name | NA |
| Formulation | 1750 [iU]/1 |
| Physical Appearance | injection, powder, lyophilized, for solution |
| Route of Administration | IV |
| Recommended Dosage | The dosage is to be individualized based on the patient's pre-treatment functional AT activity level (expressed in percent of normal) and body weight (expressed in kilograms) and using therapeutic drug monitoring |
| Contraindication | NA |
| Side Effects | Hemorrhage (intra-abdominal, hemarthrosis and post procedural) |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |
| Primary information | |
|---|---|
| ID | 10713 |
| Therapeutic ID | Th1164 |
| Protein Name | Antithrombin Alfa |
| Sequence | NA |
| Molecular Weight | 57,215 |
| Chemical Formula | C2191H3451N583O656S20 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | NA |
| Half-life | 11.6 (84.7) for 50 IU/KG to17.7 (60.9) for 100IU/KG |
| Description | Antithrombin (Recombinant) and plasma-derived antithrombin both contain six cysteine residues forming three disulphide bridges and 3-4 N-linked carbohydrate moieties. The glycosylation profile of antithrombin (Recombinant) is different from plasma-derived antithrombin, which results in an increased heparin affinity. When assayed in the presence of excess of heparin the potency of the recombinant product is not different from that of plasma-derived product. |
| Indication/Disease | Indicated for the prevention of peri-operative and peri-partum thromboembolic events in hereditary antithrombin deficient patients |
| Pharmacodynamics | Hereditary AT deficiency causes an increased risk of venous thromboembolism (VTE). During high-risk situations such as surgery or trauma or for pregnant women, during the peripartum period, the risk of development of VTEs as compared to the normal population in these situations is increased by a factor 10 to 506,7. In hereditary antithrombin deficient patients ATryn restores (normalizes) plasma AT activity levels during peri-operative and peri-partum periods. |
| Mechanism of Action | Antithrombin (AT) plays a central role in the regulation of hemostasis. AT is the principal inhibitor of thrombin and Factor Xa5, the serine proteases that play pivotal roles in blood coagulation. AT neutralizes the activity of thrombin and Factor Xa by forming a complex which is rapidly removed from the circulation. The ability of antithrombin to inhibit thrombin and Factor Xa can be enhanced by greater than 300 to 1000 fold when AT is bound to heparin. |
| Toxicity | Highest dose tested was 360mg/kg/day in rats resulted in transient limb swelling. |
| Metabolism | Not metabolized. |
| Absorption | Given IV so not absorbed. |
| Dose of: 50IU/kg: 126.2 ml/kg 100IU/kg: 156.1 ml/kg Vd in hereditary deficient pregnant women in high risk situations had increased Vd of 14.3L. | |
| Clearance | Dose of: 50IU/kg: 9.6 ml/hr/kg 100IU/kg: 7.2 ml/hr/kg Cl in hereditary deficient pregnant women in high risk situations had increased Cl of 1.38L/h. |
| Categories | Anticoagulants,Decreased Coagulation Factor Activity,Factor Xa Inhibitors,Recombinant Antithrombin,Thrombin Inhibitors |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | Prothrombin,Coagulation factor X |
| Brand Name | Atryn |
| Company | R Evo Bioloigics, Inc. |
| Brand Description | R Evo Bioloigics, Inc. |
| Prescribed For | It is indicated for the prevention of peri-operative and peri-partum thromboembolic events in hereditary antithrombin deficient patients |
| Chemical Name | NA |
| Formulation | 525 [iU]/mL |
| Physical Appearance | injection, powder, lyophilized, for solution |
| Route of Administration | IV |
| Recommended Dosage | The dosage is to be individualized based on the patient's pre-treatment functional AT activity level (expressed in percent of normal) and body weight (expressed in kilograms) and using therapeutic drug monitoring |
| Contraindication | NA |
| Side Effects | Hemorrhage (intra-abdominal, hemarthrosis and post procedural) |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |