Alpha-1-proteinase inhibitor
Identification
- Name
- Alpha-1-proteinase inhibitor
- Accession Number
- DB00058
- 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.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Other protein based therapies - Protein Structure
- Protein Chemical Formula
- C2001H3130N514O601S10
- Protein Average Weight
- 44324.5 Da
- Sequences
>DB00058 sequence EDPQGDAAQKTDTSHHDQDHPTFNKITPNLAEFAFSLYRQLAHQSNSTNIFFSPVSIATA FAMLSLGTKADTHDEILEGLNFNLTEIPEAQIHEGFQELLRTLNQPDSQLQLTTGNGLFL SEGLKLVDKFLEDVKKLYHSEAFTVNFGDTEEAKKQINDYVEKGTQGKIVDLVKELDRDT VFALVNYIFFKGKWERPFEVKDTEEEDFHVDQVTTVKVPMMKRLGMFNIQHCKKLSSWVL LMKYLGNATAIFFLPDEGKLQHLENELTHDIITKFLENEDRRSASLHLPKLSITGTYDLK SVLGQLGITKVFSNGADLSGVTEEAPLKLSKAVHKAVLTIDEKGTEAAGAMFLEAIPMSI PPEVKFNKPFVFLMIEQNTKSPLFMGKVVNPTQK
Download FASTA Format- Synonyms
- Alfa 1-proteinase inhibitor (human)
- Alfa-1-antitripsina
- 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 IDs
- 232-924-7
Pharmacology
- Indication
For chronic augmentation and maintenance therapy in individuals with alpha1-proteinase inhibitor (A1-PI) deficiency and clinical evidence of emphysema.
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- Pharmacodynamics
Prevents excessive accumulation of active neutrophil elastase and consequent proteolysis of elastin tissues in alveolar lung structures. This prevents the development of emphysema.
- Mechanism of action
Alpha-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.
Target Actions Organism ANeutrophil elastase inhibitorHumans - Absorption
- Not Available
- Volume of distribution
- 5632 ± 2006 mL [ARALAST NP]
- 5618 ± 1618 mL [Aralast]
- Protein binding
- Not Available
- Metabolism
- Not Available
- Route of elimination
- Not Available
- Half-life
- Not Available
- Clearance
- 940 +/- 275 mL/day [Patients with congenital α1-PI deficiency with single IV infusion of 60 mg/kg]
- Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More- Toxicity
- Not Available
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Unlock Additional DataAlbutrepenonacog alfa Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Albutrepenonacog alfa. Aminocaproic acid Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Aminocaproic acid. Andexanet alfa Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Andexanet alfa. Anti-inhibitor coagulant complex Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Anti-inhibitor coagulant complex. Antihemophilic Factor (Recombinant), PEGylated Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Antihemophilic Factor (Recombinant), PEGylated. Antihemophilic factor human Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Antihemophilic factor human. Antihemophilic factor, human recombinant Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Antihemophilic factor, human recombinant. Aprotinin Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Aprotinin. Beroctocog alfa Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Beroctocog alfa. Calcium acetate Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Calcium acetate. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- Not Available
Products
- International/Other Brands
- Aralast (Baxter) / Prolastin (Talecris Biotherapeutics C formerly Bayer)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataAlpha1-proteinase Inhibitor (human) Powder, for solution Intravenous Grifols Therapeutics Llc Not applicable Not applicable Canada 
Alpha1-proteinase Inhibitor (human) Powder, for solution Intravenous Grifols Therapeutics Llc Not applicable Not applicable Canada Aralast NP Kit 16 mg/1mL Intravenous Baxalta u.s. Inc. 2002-12-23 Not applicable US 
Aralast NP Kit 16 mg/1mL Intravenous Baxter Laboratories 2010-09-01 2014-11-09 US Aralast NP Kit 16 mg/1mL Intravenous Baxalta u.s. Inc. 2002-12-23 Not applicable US Aralast NP Kit 16 mg/1mL Intravenous Baxter Laboratories 2010-09-01 2014-11-09 US Aralast NP Kit 16 mg/1mL Intravenous Baxter Laboratories 2010-04-19 2014-11-09 US Glassia Injection, solution 1 g/50mL Intravenous Baxalta Usa Inc. 2010-07-01 Not applicable US Prolastin Inj 25.0mg/ml Powder, for solution Intravenous Cutter Biological, Division Of Miles Lab Inc. 1988-12-31 1998-09-25 Canada Prolastin-C 1000 mg/20mL Intravenous GRIFOLS USA, LLC 1987-12-02 Not applicable US Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
Categories
- ATC Codes
- B02AB02 — Alfa1 antitrypsin
- Drug Categories
- Acute-Phase Proteins
- Alpha-Globulins
- Amino Acids, Peptides, and Proteins
- Antifibrinolytic Agents
- Blood and Blood Forming Organs
- Blood Proteins
- Carbohydrates
- Enzyme Inhibitors
- Enzymes
- Globulins
- Glycoconjugates
- Glycoproteins
- Hemostatics
- Human alpha-1 Proteinase Inhibitor
- Peptides
- Protease Inhibitors
- Proteinase Inhibitors
- Proteins
- Serine Protease Inhibitors
- Serpins
- Serum Globulins
- Trypsin Inhibitors
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
Chemical Identifiers
- UNII
- F43I396OIS
- CAS number
- 9041-92-3
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
- 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
- UniProt
- P01009
- Genbank
- K01396
- PubChem Substance
- 46506364
- 535
- Therapeutic Targets Database
- DAP001102
- PharmGKB
- PA10308
- RxList
- RxList Drug Page
- Wikipedia
- Alpha-1_antitrypsin
- AHFS Codes
- 44:00.00 — Enzymes
- FDA label
- Download (101 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Alpha 1-Antitrypsin Deficiency 1 4 Completed Treatment Alpha 1-proteinase Inhibitor Deficiency / Emphysema 1 4 Completed Treatment Alpha-1 Anti-trypsin Deficiency / Healthy Volunteers 1 4 Completed Treatment Alpha1-proteinase Inhibitor Deficiency / Emphysema 1 4 Recruiting Treatment Pancreatitis, Chronic; Diabetes; Transplant 1 4 Terminated Treatment Alpha-1 Anti-trypsin Deficiency 1 4 Withdrawn Treatment Alpha-1 Anti-trypsin Deficiency / Chronic Obstructive Pulmonary Disease (COPD) 1 3 Completed Treatment Alpha 1-Antitrypsin Deficiency 2 3 Completed Treatment Alpha-1 Anti-trypsin Deficiency 1 3 Enrolling by Invitation Treatment Pulmonary Emphysema in Alpha-1 Antitrypsin Deficiency 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Baxter International Inc.
- CSL Behring LLC
- Talecris Biotherapeutics
- Dosage Forms
Form Route Strength Kit Intravenous 16 mg/1mL Injection, solution Intravenous 1 g/50mL Injection, powder, for solution Parenteral 1000 mg Injection Intravenous 1000 mg Powder, for solution Intravenous Powder, for solution Intravenous 1000 mg Injection, solution Intravenous 1000 mg/20mL Solution Intravenous 1000 mg Injection, powder, lyophilized, for solution Intravenous 1000 mg Injection, powder, for solution Intravenous 1000 mg Kit Intravenous 1000 mg/20mL Kit Intravenous 4000 mg/76mL Kit Intravenous 5000 mg/95mL Kit; powder, for solution Intravenous 1000 mg Kit; powder, for solution Intravenous 4000 mg Kit; powder, for solution Intravenous 5000 mg - Prices
Unit description Cost Unit Aralast 1000 mg vial 0.52USD vial Aralast np 1000 mg vial 0.52USD vial Aralast np 500 mg vial 0.52USD vial Aralast 500 mg vial 0.5USD vial Zemaira 1000 mg vial 0.5USD vial Prolastin 1000 mg vial 0.46USD vial Prolastin 500 mg vial 0.46USD vial Prolastin c 1000 mg vial 0.46USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 59 °C at pH 7.8 Tew D.J., Bottomley, S.P. J. Mol. Biol. 313:1161-1169 (2001) hydrophobicity -0.302 Not Available isoelectric point 5.37 Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- 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
- Uniprot Name
- Neutrophil elastase
- Molecular Weight
- 28517.81 Da
References
- 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]
- 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]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Drug created on June 13, 2005 07:24 / Updated on October 21, 2020 01:55
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