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Identification
NameAlpha-1-proteinase inhibitor
Accession NumberDB00058  (BTD00002, BIOD00002)
TypeBiotech
GroupsApproved
Description

Human alpha-1 proteinase inhibitor or alpha-1-antitrypsin, prepared from human plasma via Cohn alcohol fractionation followed by PEG and zinc chloride fractionation.

Protein structureDb00058
Related Articles
Protein chemical formulaC2001H3130N514O601S10
Protein average weight44324.5 Da
Sequences
>DB00058 sequence
EDPQGDAAQKTDTSHHDQDHPTFNKITPNLAEFAFSLYRQLAHQSNSTNIFFSPVSIATA
FAMLSLGTKADTHDEILEGLNFNLTEIPEAQIHEGFQELLRTLNQPDSQLQLTTGNGLFL
SEGLKLVDKFLEDVKKLYHSEAFTVNFGDTEEAKKQINDYVEKGTQGKIVDLVKELDRDT
VFALVNYIFFKGKWERPFEVKDTEEEDFHVDQVTTVKVPMMKRLGMFNIQHCKKLSSWVL
LMKYLGNATAIFFLPDEGKLQHLENELTHDIITKFLENEDRRSASLHLPKLSITGTYDLK
SVLGQLGITKVFSNGADLSGVTEEAPLKLSKAVHKAVLTIDEKGTEAAGAMFLEAIPMSI
PPEVKFNKPFVFLMIEQNTKSPLFMGKVVNPTQK
Download FASTA Format
Synonyms
Alpha 1-antitrypsin
Alpha 1-Proteinase Inhibitor
Alpha-1 protease inhibitor
Alpha-1-antiproteinase
Alpha-1-antitrypsin
Alpha-1-proteinase Inhibitor (human)
Alpha-1-proteinase inhibitor human
Alpha-1-proteinase Inhibitor, Human
Alpha1-proteinase Inhibitor
Alpha1-proteinase inhibitor (human)
alpha1-proteinase inhibitor human
API
External Identifiers
  • 232-924-7
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alpha1-proteinase Inhibitor (human)powder for solution1 gintravenousGrifols Therapeutics IncNot applicableNot applicableCanada
Alpha1-proteinase Inhibitor (human)powder for solution500 mgintravenousGrifols Therapeutics IncNot applicableNot applicableCanada
Aralast NpkitBaxter Healthcare Corporation2002-12-232016-04-05Us
Aralast NpkitBaxter Healthcare Corporation2002-12-232016-04-05Us
Glassiainjection, solution1 g/50mLintravenousBaxter Healthcare Corporation2011-05-312016-04-05Us
Prolastin Inj 25.0mg/mlpowder for solution25 mgintravenousCutter Biological, Division Of Miles Lab Inc.1988-12-311998-09-25Canada
Prolastin-CkitGRIFOLS USA, LLC1987-12-022016-04-05Us
Prolastin-Cpowder for solution1000 mgintravenousGrifols Therapeutics Inc1996-11-11Not applicableCanada
Prolastin-CkitGRIFOLS USA, LLC1987-12-022016-04-05Us
ZemairakitCSL Behring LLC2003-07-082016-04-23Us
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International Brands
NameCompany
AralastBaxter
GlassiaNot Available
ProlastinTalecris Biotherapeutics C formerly Bayer
Prolastin-CNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIF43I396OIS
CAS number9041-92-3
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationFor chronic augmentation and maintenance therapy in individuals with alpha1-proteinase inhibitor (A1-PI) deficiency and clinical evidence of 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.
Related Articles
AbsorptionNot Available
Volume of distribution
  • 5632 ± 2006 mL [ARALAST NP]
  • 5618 ± 1618 mL [Aralast]
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
Clearance
  • 940 +/- 275 mL/day [Patients with congenital α1-PI deficiency with single IV infusion of 60 mg/kg]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Powder for solutionintravenous1 g
Powder for solutionintravenous500 mg
Injection, solutionintravenous1 g/50mL
Powder for solutionintravenous25 mg
Powder for solutionintravenous1000 mg
Kit
Prices
Unit descriptionCostUnit
Aralast 1000 mg vial0.52USD vial
Aralast np 1000 mg vial0.52USD vial
Aralast np 500 mg vial0.52USD vial
Aralast 500 mg vial0.5USD vial
Zemaira 1000 mg vial0.5USD vial
Prolastin 1000 mg vial0.46USD vial
Prolastin 500 mg vial0.46USD vial
Prolastin c 1000 mg vial0.46USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point59 °C at pH 7.8Tew D.J., Bottomley, S.P. J. Mol. Biol. 313:1161-1169 (2001)
hydrophobicity-0.302Not Available
isoelectric point5.37Not Available
References
Synthesis Reference

Michael H. Coan, William J. Brockway, “Method of preparing alpha-1-proteinase inhibitor.” U.S. Patent US4379087, issued December, 1968.

US4379087
General References
  1. Karnaukhova E, Ophir Y, Golding B: Recombinant human alpha-1 proteinase inhibitor: towards therapeutic use. Amino Acids. 2006 Jun;30(4):317-32. Epub 2006 May 26. [PubMed:16773239 ]
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB Entries
FDA labelDownload (101 KB)
MSDSNot Available
Interactions
Drug InteractionsNot Available
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Serine-type endopeptidase activity
Specific Function:
Modifies the functions of natural killer cells, monocytes and granulocytes. Inhibits C5a-dependent neutrophil enzyme release and chemotaxis.
Gene Name:
ELANE
Uniprot ID:
P08246
Molecular Weight:
28517.81 Da
References
  1. Topic A, Ljujic M, Nikolic A, Petrovic-Stanojevic N, Dopudja-Pantic V, Mitic-Milikic M, Radojkovic D: Alpha-1-antitrypsin phenotypes and neutrophil elastase gene promoter polymorphisms in lung cancer. Pathol Oncol Res. 2011 Mar;17(1):75-80. doi: 10.1007/s12253-010-9283-5. Epub 2010 Jun 3. [PubMed:20521180 ]
  2. Karnaukhova E, Ophir Y, Golding B: Recombinant human alpha-1 proteinase inhibitor: towards therapeutic use. Amino Acids. 2006 Jun;30(4):317-32. Epub 2006 May 26. [PubMed:16773239 ]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
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Drug created on June 13, 2005 07:24 / Updated on April 25, 2016 12:51