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11874 details
Primary information
ID11874
Therapeutic IDTh1264
Protein NamePexelizumab
Sequence>Th1264_Pexelizumab MADIQMTQSPSSLSASVGDRVTITCGASENIYGALNWYQRKPGKAPKLLIYGATNLADGVPSRFSGSGSGTDYTLTISSLQPEDFATYYCQNVLNTPLTFGQGTKVEIKRTGGGGSGGGGSGGGGSQVQLVQSGAEVEKPGASVKKVSCKASGYIFSNYWIQWVRQAPGQGLEWMGEILPGSGSTEYAQKFQGRVTMTADTSTSTAYMELSSLRSEDTAVYYCARYFFGSSPNYWYFDVWGQGTLVTVSS
Molecular WeightNA
Chemical FormulaNA
Isoelectric PointNA
HydrophobicityNA
Melting pointNA
Half-life7.0 hours to 14.5 hours.
DescriptionPexelizumab is a humanized monoclonal antibody used as an immunosuppressive drug. It is being investigated by Alexion Pharmaceuticals.
Indication/DiseaseFor the treatment of inflammation during cardiac surgery.
PharmacodynamicsMyocardial injury and dysfunction in acute infarction and during cardiac surgery with cardiopulmonary bypass (CPB) are associated with an undesirable systemic inflammatory response, in which the complement cascade plays a major role. In animal models C5 inhibition has been found to significantly reduce myocardial infarct size and decrease cellular necrosis and apoptosis. Pexelizumab is a humanized, monoclonal, single-chain antibody fragment that inhibits C5, thereby blocking its cleavage into active forms.
Mechanism of ActionAlthough inflammation is a normal response, continued exposure to foreign surfaces, toxic antigens, and tissue injury results in pathologic local and systemic inflammation (SIRS). This response involves multiple humoral and cellular components, including the coagulation (Factor XII, thrombin, Proteins C and S, platelets) and complement systems, cytokines (TNF-alpha, interleukins), leukocytes, monocytes, adhesion molecules (ICAM-1), and endothelial cells, among others. The complement system is a group of glycoproteins, which, when activated, results in the formation of C3-convertase, which converts C3 to C3a and C3b. C3a cleaves C5 to C5a and C5b. C5b, in conjunction with C6, C7, C8, and C9, forms the membrane attack or terminal complement complex (TCC) C5b-9. Both C5a and C5b-9 activate, promote, and amplify inflammatory components, and likely play central roles in the development of SIRS, tissue injury, reperfusion injury, and apoptosis. Pexelizumab, a recombinant humanized single chain monoclonal antibody to C5, blocks the conversion of C5 to C5a and C5b-9.
ToxicityNA
MetabolismNA
AbsorptionNA
NA
ClearanceNA
CategoriesBiochemical Phenomena
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetNA
Brand NameNA
CompanyNA
Brand DescriptionNA
Prescribed ForNA
Chemical NameNA
FormulationNA
Physical Appearance NA
Route of AdministrationNA
Recommended DosageNA
ContraindicationNA
Side EffectsNA
Useful Link 1Link
Useful Link 2NA
RemarksNA