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Identification
NameAlpha-1-proteinase inhibitor
Accession NumberDB00058  (BTD00002, BIOD00002)
TypeBiotech
GroupsApproved
DescriptionHuman 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
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Aralast NpkitBaxter Healthcare Corporation2002-12-23Not applicableUs
Aralast NpkitBaxter Healthcare Corporation2002-12-23Not applicableUs
Glassiainjection, solution1 g/50mLintravenousBaxter Healthcare Corporation2011-05-31Not applicableUs
Prolastin-CkitGRIFOLS USA, LLC1987-12-02Not applicableUs
Prolastin-CkitGRIFOLS USA, LLC1987-12-02Not applicableUs
ZemairakitCSL Behring LLC2003-07-08Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not 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
Injection, solutionintravenous1 g/50mL
Kit
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 Interactions
Drug
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Alpha-1-proteinase inhibitor.
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Alpha-1-proteinase inhibitor.
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Alpha-1-proteinase inhibitor.
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Alpha-1-proteinase inhibitor.
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Alpha-1-proteinase inhibitor.
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Alpha-1-proteinase inhibitor.
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Alpha-1-proteinase inhibitor.
BoceprevirThe serum concentration of Alpha-1-proteinase inhibitor can be decreased when it is combined with Boceprevir.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Alpha-1-proteinase inhibitor.
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Alpha-1-proteinase inhibitor.
CarbamazepineThe metabolism of Alpha-1-proteinase inhibitor can be increased when combined with Carbamazepine.
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Alpha-1-proteinase inhibitor.
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Alpha-1-proteinase inhibitor.
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Alpha-1-proteinase inhibitor.
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Alpha-1-proteinase inhibitor.
CyclophosphamideThe risk or severity of adverse effects can be increased when Alpha-1-proteinase inhibitor is combined with Cyclophosphamide.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Alpha-1-proteinase inhibitor.
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Alpha-1-proteinase inhibitor.
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Alpha-1-proteinase inhibitor.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Alpha-1-proteinase inhibitor.
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Alpha-1-proteinase inhibitor.
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Alpha-1-proteinase inhibitor.
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Alpha-1-proteinase inhibitor.
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Alpha-1-proteinase inhibitor.
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Alpha-1-proteinase inhibitor.
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Alpha-1-proteinase inhibitor.
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Alpha-1-proteinase inhibitor.
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Alpha-1-proteinase inhibitor.
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Alpha-1-proteinase inhibitor.
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Alpha-1-proteinase inhibitor.
GarlicThe serum concentration of Alpha-1-proteinase inhibitor can be decreased when it is combined with Garlic.
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Alpha-1-proteinase inhibitor.
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Alpha-1-proteinase inhibitor.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Alpha-1-proteinase inhibitor.
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Alpha-1-proteinase inhibitor.
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Alpha-1-proteinase inhibitor.
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Alpha-1-proteinase inhibitor.
PethidineThe risk or severity of adverse effects can be increased when Alpha-1-proteinase inhibitor is combined with Pethidine.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Alpha-1-proteinase inhibitor.
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Alpha-1-proteinase inhibitor.
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Alpha-1-proteinase inhibitor.
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Alpha-1-proteinase inhibitor.
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Alpha-1-proteinase inhibitor.
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Alpha-1-proteinase inhibitor.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Alpha-1-proteinase inhibitor.
St. John's WortThe metabolism of Alpha-1-proteinase inhibitor can be increased when combined with St. John's Wort.
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Alpha-1-proteinase inhibitor.
TemsirolimusThe risk or severity of adverse effects can be increased when Alpha-1-proteinase inhibitor is combined with Temsirolimus.
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Alpha-1-proteinase inhibitor.
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Alpha-1-proteinase inhibitor.
TipranavirThe serum concentration of Alpha-1-proteinase inhibitor can be decreased when it is combined with Tipranavir.
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Alpha-1-proteinase inhibitor.
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Alpha-1-proteinase inhibitor.
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Alpha-1-proteinase inhibitor.
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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23