==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

Detailed description page of THPdb

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1332 details
Primary information
ThPP IDTh1047
Therapeutic Peptide/Protein NameAlpha-1-proteinase inhibitor
SequenceEDPQGDAAQKTDTSHHDQDHPTFNKITPNLAEFAFSLYRQLAHQSNSTNI view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight44324.5
Chemical FormulaC2001H3130N514O601S10
Isoelectric Point5.37
Hydrophobicity-0.302
Melting Point (℃)59
Half LifeN.A.
DescriptionHuman alpha-1 proteinase inhibitor or alpha-1-antitrypsin, prepared from human plasma via Cohn alcohol fractionation followed by PEG and zinc chloride fractionation.
Indication/DiseaseFor treatment of panacinar emphysema.
PharmacodynamicsPrevents excessive accumulation of active neutrophil elastase and consequent proteolysis of elastin tissues in alveolar lung structures. This prevents the development of emphysema.
Mechanism of ActionAlpha-1 proteinase inhibitor is a serine protease inhibitor (Serpin). Its primary mechanism is inhibiting the action of the serine protease called elastase (also plasmin and thrombin) in the lungs. The reactive center loop (RCL) of alpha-1 proteinase inhibitor extends out from the body of the protein and directs binding to the target protease. The protease cleaves the serpin at the reactive site, establishing a covalent linkage between the carboxyl group of the serpin reactive site and the serine hydroxyl of the protease. The resulting inactive serpin-protease complex is highly stable.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of Distribution5618 ± 1618 mL [Aralast]
Clearance940 ± 275 mL/day [Patients with congenital deficiency with single IV infusion of 60mg/kg]
CategoriesTrypsin Inhibitors
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameN.A.
CompanyN.A.
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearnceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsNausea, bloating; headache, dizziness, drowsiness; feeling tired; back pain, joint or muscle pain; swelling in your hands or feet; flushing (warmth, redness, or tingly feeling); cold symptoms such as stuffy nose, sneezing, sore throat, cough; or mild itch
Useful Linkhttp://www.drugs.com/mtm/aralast.html
PubMed ID16773239
3-D StructureTh1047 (View) or (Download)