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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
Alfa1 antitrypsin
Alpha 1-antitrypsin
Alpha 1-Proteinase Inhibitor
Alpha 1-proteinase inhibitor (human)
Alpha 1-proteinase inhibitor, human
Alpha-1 protease inhibitor
Alpha-1 proteinase inhibitor (human)
Alpha-1-antiproteinase
Alpha-1-antitrypsin
Alpha-1-proteinase Inhibitor (human)
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
Alpha1-proteinase Inhibitor (human)Powder, for solution500 mgIntravenousGrifols Therapeutics IncNot applicableNot applicableCanada
Alpha1-proteinase Inhibitor (human)Powder, for solution1 gIntravenousGrifols Therapeutics IncNot applicableNot applicableCanada
Aralast NpKitBaxalta Us Inc.2002-12-23Not applicableUs
Aralast NpKitBaxalta Us Inc.2002-12-23Not applicableUs
GlassiaInjection, solution1 g/50mLIntravenousBaxalta Us Inc.2011-05-31Not applicableUs
Prolastin Inj 25.0mg/mlPowder, for solution25 mgIntravenousCutter Biological, Division Of Miles Lab Inc.1988-12-311998-09-25Canada
Prolastin-CKitGRIFOLS USA, LLC1987-12-02Not applicableUs
Prolastin-CKitGRIFOLS USA, LLC1987-12-02Not applicableUs
Prolastin-CPowder, for solution1000 mgIntravenousGrifols Therapeutics Inc1996-11-11Not applicableCanada
Prolastin-CKitGRIFOLS USA, LLC1987-12-02Not applicableUs
RespreezaInjection, powder, for solution1000 mgIntravenousCsl Behring Gmb H2015-08-20Not applicableEu
ZemairaKitCSL Behring LLC2003-07-08Not applicableUs
ZemairaKit; Powder, for solution1000 mgIntravenousCsl Behring Canada IncNot applicableNot applicableCanada
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
Pharmacology
IndicationFor chronic augmentation and maintenance therapy in individuals with alpha1-proteinase inhibitor (A1-PI) deficiency and clinical evidence of emphysema.
Structured Indications
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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Neutrophil elastaseProteinyes
inhibitor
HumanP08246 details
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
Interactions
Drug Interactions
DrugInteractionDrug group
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved, Investigational
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved, Investigational
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved, Illicit, Investigational
Ambroxol acefyllinateThe serum concentration of Ambroxol acefyllinate can be decreased when it is combined with Alpha-1-proteinase inhibitor.Experimental
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Alpha-1-proteinase inhibitor.Illicit, Withdrawn
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
BoceprevirThe serum concentration of Alpha-1-proteinase inhibitor can be decreased when it is combined with Boceprevir.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved, Investigational
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
CarbamazepineThe metabolism of Alpha-1-proteinase inhibitor can be increased when combined with Carbamazepine.Approved, Investigational
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Alpha-1-proteinase inhibitor.Withdrawn
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved, Investigational, Withdrawn
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Alpha-1-proteinase inhibitor.Approved
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved, Vet Approved
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
CyclophosphamideThe risk or severity of adverse effects can be increased when Alpha-1-proteinase inhibitor is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved, Investigational, Vet Approved
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
DienestrolThe serum concentration of Dienestrol can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Alpha-1-proteinase inhibitor.Approved
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved, Investigational
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Alpha-1-proteinase inhibitor.Investigational
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Estramustine can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
Estrogens, esterifiedThe serum concentration of Estrogens, esterified can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
GarlicThe serum concentration of Alpha-1-proteinase inhibitor can be decreased when it is combined with Garlic.Approved
HexestrolThe serum concentration of Hexestrol can be decreased when it is combined with Alpha-1-proteinase inhibitor.Withdrawn
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved, Investigational
MestranolThe serum concentration of Mestranol can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
MethallenestrilThe serum concentration of Methallenestril can be decreased when it is combined with Alpha-1-proteinase inhibitor.Experimental
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved, Illicit
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved, Withdrawn
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
OpipramolThe serum concentration of Opipramol can be increased when it is combined with Alpha-1-proteinase inhibitor.Investigational
PethidineThe risk or severity of adverse effects can be increased when Alpha-1-proteinase inhibitor is combined with Pethidine.Approved
PimozideThe serum concentration of Pimozide can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved, Investigational
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
St. John's WortThe metabolism of Alpha-1-proteinase inhibitor can be increased when combined with St. John's Wort.Nutraceutical
Synthetic Conjugated Estrogens, AThe serum concentration of Synthetic Conjugated Estrogens, A can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Alpha-1-proteinase inhibitor.Approved, Investigational
TemsirolimusThe risk or severity of adverse effects can be increased when Alpha-1-proteinase inhibitor is combined with Temsirolimus.Approved
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
TipranavirThe serum concentration of Alpha-1-proteinase inhibitor can be decreased when it is combined with Tipranavir.Approved, Investigational
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
Valproic AcidThe serum concentration of Valproic Acid can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved, Investigational
VerapamilThe metabolism of Verapamil can be decreased when combined with Alpha-1-proteinase inhibitor.Approved
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
Food InteractionsNot 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
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Powder, for solutionIntravenous1 g
Powder, for solutionIntravenous500 mg
Injection, solutionIntravenous1 g/50mL
Powder, for solutionIntravenous25 mg
Kit
Powder, for solutionIntravenous1000 mg
Injection, powder, for solutionIntravenous1000 mg
Kit
Kit; powder, for solutionIntravenous1000 mg
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
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

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 November 18, 2016 13:38