| Primary information |
|---|
| ThPP ID | Th1172 |
| Therapeutic Peptide/Protein Name | Coagulation Factor XIII A-Subunit (Recombinant) |
| Sequence | NA view full sequnce in fasta |
| Functional Classification | Ia |
| Molecular Weight | NA |
| Chemical Formula | NA |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting Point (℃) | NA |
| Half Life | 5.1 (2.6) days |
| Description | Coagulation Factor XIII A-Subunit (Recombinant) is a recombinant human factor XIII-A2 homodimer composed of two factor XIII (FXIII) A-subunits. The FXIII A-subunit is a 731 amino acid chain with an acetylated N- terminal serine. When FXIII is activated by thrombin, a 37 amino acid peptide is cleaved from the N-terminus of the A-subunit. Coagulation Factor XIII A-Subunit (Recombinant) is manufactured as an intracellular, soluble protein in yeast (Saccharomyces cerevisiae) production strain containing the episomal expression vector, pD16. It is subsequently isolated by homogenization of cells and purification by several chromatography steps, including hydrophobic interaction and ion exchange chromatography. No human or animal derived products are used in the manufacturing process. |
| Indication/Disease | For routine prophylaxis of bleeding in patients with congenital factor XIII A-Subunit deficiency. |
| Pharmacodynamics | A qualitative assay of clot solubility is widely used as an indicator of FXIII deficiency; when performed correctly the test is positive only when the FXIII activity in the sample is close to zero. The results of standard coagulation tests are normal as it is the quality of the clot that is affected. In addition, at present there are no markers that can quantitatively assess the in vivo pharmacodynamics of FXIII. |
| Mechanism of Action | Coagulation Factor XIII A-Subunit (Recombinant) is a protransglutaminase (rFXIII [rA2] homodimer) and binds to free human FXIII B-subunit resulting in a heterotetramer [rA2B2] with a similar half-life to [A2B2]. rFXIII has been shown to be activated by thrombin in the presence of Ca2+. Activated rFXIII has been shown in dose-dependent manner to increase mechanical strength of fibrin clots, retard fibrinolysis, and rFXIII has been shown to enhance platelet adhesion to the site of injury. After combining with available plasma B-subunits, Coagulation Factor XIII A-subunit (Recombinant) has been shown to have the same pharmacodynamic properties in plasma as endogenous FXIII. |
| Toxicity | NA |
| Metabolism | NA |
| Absorption | AUC (0-inf): 128.3 (40.5) (IU*h/mL) |
| Volume of Distribution | NA |
| Clearance | 0.33 (0.11) (mL/h/kg) |
| Categories | NA |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | NA |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Tretten |
| Company | Novo Nordisk Canada Inc |
| Brand Discription | TRETTEN, Coagulation Factor XIII A-Subunit (Recombinant), is a recombinant human factor XIII-A2 homodimer composed of two factor XIII (FXIII) A-subunits. The FXIII A-subunit is a 731 amino acid chain with an acetylated N-terminal serine. When FXIII is activated by thrombin, a 37 amino acid peptide is cleaved from the N-terminus of the A-subunit. |
| Prescribed for | TRETTEN, Coagulation Factor XIII A-Subunit (Recombinant), is indicated for routine prophylaxis for bleeding in patients with congenital factor XIII A-subunit deficiency. |
| Chemical Name | NA |
| Formulation | 15mg |
| Physcial Appearnce | powder for solution |
| Route of Administration | IV |
| Recommended Dosage | Treatment should be initiated under the supervision of a physician experienced in the treatment of rare bleeding disorders. The dose for routine prophylaxis for bleeding in patients with congenital factor XIII (FXIII) A-subunit deficiency is 35 international units (IU) per kilogram body weight once monthly to achieve a target trough level of FXIII activity at or above 10% using a validated assay. Consider dose adjustment if adequate coverage is not achieved with the recommended 35 IU/kg dose. |
| Contraindication | TRETTEN is contraindicated in patients who have known hypersensitivity to the active substance or to any of the excipients |
| Side Effects | The most common adverse reactions reported in clinical trials ( ≥ 1%), were headache, pain in the extremities, injection site pain, and increase in fibrin D dimer levels. |
| Useful Link | http://www.rxlist.com/tretten-drug.htm |
| PubMed ID | 25031548, 27019464, 22451423 |
| 3-D Structure | N.A. |