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

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Indication

For chronic augmentation and maintenance therapy in individuals with alpha1-proteinase inhibitor (A1-PI) deficiency and clinical evidence of emphysema.

Associated Conditions

• Emphysema

Contraindications & Blackbox Warnings

Contraindications & Blackbox Warnings

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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	inhibitor	Humans

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

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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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Albutrepenonacog alfa	Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Albutrepenonacog alfa.
Alteplase	The therapeutic efficacy of Alpha-1-proteinase inhibitor can be decreased when used in combination with Alteplase.
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.
Anistreplase	The therapeutic efficacy of Alpha-1-proteinase inhibitor can be decreased when used in combination with Anistreplase.
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.

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Food Interactions

No interactions found.

Products

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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
Alpha1-proteinase Inhibitor (human)	Powder, for solution		Intravenous	Grifols Therapeutics Llc	Not applicable	Not applicable
Alpha1-proteinase Inhibitor (human)	Powder, for solution		Intravenous	Grifols Therapeutics Llc	Not applicable	Not applicable
Aralast NP	Kit	16 mg/1mL	Intravenous	Baxalta u.s. Inc.	2002-12-23	Not applicable
Aralast NP	Kit	16 mg/1mL	Intravenous	Baxter Laboratories	2010-09-01	2014-11-09
Aralast NP	Kit	16 mg/1mL	Intravenous	Baxter Laboratories	2010-04-19	2014-11-09
Aralast NP	Kit	16 mg/1mL	Intravenous	Baxalta u.s. Inc.	2002-12-23	Not applicable
Aralast NP	Kit	16 mg/1mL	Intravenous	Baxter Laboratories	2010-09-01	2014-11-09
Glassia	Injection, solution	1 g/50mL	Intravenous	Baxalta Usa Inc.	2010-07-01	Not applicable
Prolastin Inj 25.0mg/ml	Powder, for solution		Intravenous	Cutter Biological, Division Of Miles Lab Inc.	1988-12-31	1998-09-25
Prolastin-C		1000 mg/20mL	Intravenous	GRIFOLS USA, LLC	1987-12-02	Not applicable

Categories

ATC Codes

B02AB02 — Alfa1 antitrypsin

• B02AB — Proteinase inhibitors
• B02A — ANTIFIBRINOLYTICS
• B02 — ANTIHEMORRHAGICS
• B — BLOOD AND BLOOD FORMING ORGANS

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
• Enzymes and Coenzymes
• 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

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

UniProt

P01009

Genbank

K01396

PubChem Substance

46506364

RxNav

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	Active Not Recruiting	Treatment	Pancreatitis, Chronic; Diabetes; Transplant	1
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	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
Injection	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
Injection, powder, for solution	Intravenous	4000 mg
Injection, powder, for solution	Intravenous	5000 mg
Powder, for solution	Intravenous
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
Injection, powder, for solution	Intravenous

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

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Details1. Neutrophil elastase

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

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 13:24 / Updated on April 11, 2021 00:58