==== 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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1331 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 Distribution5632 ± 2006 mL [ARALAST NP]
Clearance940 ± 275 mL/day [Patients with congenital deficiency with single IV infusion of 60mg/kg]
CategoriesSerine Proteinase Inhibitors
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetNeutrophil elastase
Information of corresponding available drug in the market
Brand NameAralast
CompanyBaxter
Brand DiscriptionARALAST is an Alpha-1 proteinase inhibitor. ARALAST contains approximately 67% Alpha-PI with the C-T-terminal lysine truncation.
Prescribed forIts used to treat lung problems (emphysema) caused by a certain inherited disease (alpha-1-proteinase inhibitor deficiency). In people with this condition, lung damage is caused by elastase, a natural substance that the body needs to kill bacteria in the
Chemical NameN.A.
FormulationARALAST NP is available as a lyophilized powder in single dose vials containing 0.5 gram or 1 gram of functional Alpha 1 -Protenase inhibitor
Physcial AppearnceLyophilized powder
Route of AdministrationIntravenous infusion
Recommended DosageRecommended dose is 60 mg/kg of body weight, administered once in a week.
ContraindicationARALAST NP is contraindicated in immunoglobulin A deficient patients with antibodies against IgA, due to the risk of severe hypersensitivity.
Side EffectsFever, chills, body aches, flu symptoms, sores in your mouth and throat; pain or burning when you urinate; wheezing, chest pain or tightness, trouble breathing; or vision changes.
Useful Linkhttp://www.baxter.com/downloads/healthcare_professionals/products/Aralast_NP_PI.pdf
PubMed ID16773239
3-D StructureTh1047 (View) or (Download)