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1659 details
Primary information
ThPP IDTh1152
Therapeutic Peptide/Protein NameDrotrecogin alfa
SequenceHeavy Chain: LIDGKMTRRGDSPWQVVLLDSKKKLACGAVLIHPSWV view full sequnce in fasta
Functional ClassificationIb
Molecular Weight55000
Chemical FormulaC1786H2779N509O519S29
Isoelectric Point6.78
Hydrophobicity-0.291
Melting Point (℃)N.A.
Half Life5.5 Hrs (Mammalian reticulocytes,in vitro
DescriptionDrotrecogin alfa is activated human protein C that is synthesized by recombinant DNA technology. It is a glycoprotein of approximately 55 kilodalton molecular weight, consisting of a heavy chain and a light chain linked by a disulfide bond. Drotrecogin alfa was withdrawn from the market after a major study indicated that it was not effective in improving outcomes in patients with sepsis.
Indication/DiseaseFor reduction of mortality in patients with severe sepsis.
PharmacodynamicsDrotrecogin alfa is activated human protein C that is synthesized by recombinant DNA technology. It is a glycoprotein of approximately 55 kilodalton molecular weight, consisting of a heavy chain and a light chain linked by a disulfide bond. Drotrecogin alfa inhibits factor Va and VIIIa, thereby reducing the coagulability of blood.
Mechanism of ActionActivated protein C combines with protein S on platelet surfaces and then degrades factor Va and factor VIIIa, thereby reducing blood coagulability.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
Clearance40 L/hr- Severe sepsis adults, 30±8L/hr patients without sepsis undergoing haemodialysis, 28±9L/hr for healthy patients
CategoriesAntisepsis
Patents NumberCA2036894
Date of Issue15/01/02
Date of Expiry22/02/11
Drug InteractionClopidogrel, Enoxaprin, Dalteparin, Fondaparinux, Tinzaparin, enhance the adverse or toxic effect of drotrecogin alfa
TargetCoagulation factor VIII, V, Plasminogen activator inhibitor 1, Thrombomodulin, Vitamin K-dependent protein S, Ceruloplasmin, Prothrombin, Platelet factor 4, Plasma serine protease inhibitor, Serpin B6, Vitamin K-dependent gamma-carboxylase, Endothelial protein C receptor
Information of corresponding available drug in the market
Brand NameXigris
CompanyEli Lilly and Company
Brand DiscriptionXigris (drotrecogin alfa (activated)) is a recombinant form of human activated protein C. An established human cell line possessing the complementary DNA for the inactive human protein C zymogen secretes the protein into the fermentation medium. Fermentation is carried out in a nutrient medium containing the antibiotic geneticin sulfate. Geneticin sulfate is not detectable in the final product.
Prescribed forXigris (drotrecogin alfa) is indicated for the reduction of mortality in adult patients with severe sepsis (sepsis associated with acute organ dysfunction) who have a high risk of death
Chemical NameN.A.
FormulationThe 5 and 20 mg vials of Xigris contain 5.3 mg and 20.8 mg of drotrecogin alfa (activated), respectively. The 5 and 20 mg vials of Xigris (drotrecogin alfa) also contain 40.3 and 158.1 mg of sodium chloride, 10.9 and 42.9 mg of sodium citrate, and 31.8 and 124.9 mg of sucrose, respectively.
Physcial AppearnceXigris (drotrecogin alfa) is supplied as a sterile, lyophilized, white to off-white powder
Route of AdministrationIntravenous Infusion
Recommended DosageXigris (drotrecogin alfa) should be administered intravenously at an infusion rate of 24 mcg/kg/hr (based on actual body weight) for a total duration of infusion of 96 hours. Dose adjustment based on clinical or laboratory
ContraindicationXigris (drotrecogin alfa) increases the risk of bleeding. Xigris (drotrecogin alfa) is contraindicated in the active internal bleeding, hemorraghic stroke, intracranial surgery, Trauma, Intracranial neospasm
Side EffectsBleeding is the most commonly reported adverse reaction in patients receiving Xigris therapy
Useful Linkhttp://www.rxlist.com/xigris-drug.htm
PubMed ID22616830, 16333441
3-D StructureTh1152 (View) or (Download)