Identification
- Summary
Papain is a proteolytic enzyme derived from papaya used for its anti-inflammatory properties.
- Generic Name
- Papain
- DrugBank Accession Number
- DB11193
- Background
Papain, also known as papaya proteinase I, is a cysteine protease (EC 3.4.22.2) enzyme that is found in species of papaya, Carica papaya and Vasconcellea cundinamarcensis. The enzyme is found to be localized in the skin of papaya, and is collected from slashed unripe papayas as a crude latex. Papain is used in food, pharmaceutical, textile, and cosmetic industries. While it has been used for the treatment of inflammation and pain via topical administration, papain has also shown to have anthelmintic and tooth-whitening properties. Present in over-the-counter mixture products consisting of different digestive enzymes, its active site contains a catalytic diad that plays a role in breaking peptide bonds. Papain is also used as an ingredient in various enzymatic debriding preparations.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Peptides - Protein Chemical Formula
- Not Available
- Protein Average Weight
- Not Available
- Sequences
>PAPA1_CARPA, Papain, Carica papaya MAMIPSISKLLFVAICLFVYMGLSFGDFSIVGYSQNDLTSTERLIQLFESWMLKHNKIYK NIDEKIYRFEIFKDNLKYIDETNKKNNSYWLGLNVFADMSNDEFKEKYTGSIAGNYTTTE LSYEEVLNDGDVNIPEYVDWRQKGAVTPVKNQGSCGSCWAFSAVVTIEGIIKIRTGNLNE YSEQELLDCDRRSYGCNGGYPWSALQLVAQYGIHYRNTYPYEGVQRYCRSREKGPYAAKT DGVRQVQPYNEGALLYSIANQPVSVVLEAAGKDFQLYRGGIFVGPCGNKVDHAVAAVGYG PNYILIKNSWGTGWGENGYIRIKRGTGNSYGVCGLYTSSFYPVKN
Download FASTA FormatReferences:
- UniProt: P00784, PAPA1_CARPA [Link]
- Synonyms
- Papain
- Papaína
Pharmacology
- Indication
No FDA-approved therapeutic indications.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Prevention of Inflammatory reaction ••• ••• ••••• •••••••• •••••• Treatment of Inflammatory reaction ••• ••• ••••• •••••••• •••••• - Contraindications & Blackbox Warnings
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Papain is a digestive enzyme and often acts as a skin allergen.
- Mechanism of action
When topically applied, papain induces an allergen-like inflammatory response via recruiting neutrophils, mast cells, and CD3-positive cells and by induction of a TH2-biased antibody response 1. In vitro, treatment of papain resulted in the breakdown of tight junctions of primary human keratinocytes that maintain the epithelial barrier integrity. These tight junction proteins include zonula occludens-1, claudin-4, and occludin 1. It is proposed that papain induces allergic responses via activation of TLR4, leading to an increase in neutrophils, CD3+ cells, mast cells, and CCL8-positive cells 1.
Target Actions Organism UToll-like receptor 4 activatorHumans - Absorption
No pharmacokinetic data available.
- Volume of distribution
No pharmacokinetic data available.
- Protein binding
No pharmacokinetic data available.
- Metabolism
No pharmacokinetic data available.
- Route of elimination
No pharmacokinetic data available.
- Half-life
No pharmacokinetic data available.
- Clearance
No pharmacokinetic data available.
- Adverse Effects
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Acute oral LD50 of 200 mcu papain is 4000 mg/kg in rat and 12500 mg/kg in mouse MSDS. It acts as an irritant in case of inhalation or contact with eyes.
- 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.Not Available
- Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image AXCEL PAPAIN TABLET Tablet 10000 U Oral KOTRA PHARMA (M) SDN. BHD. 2017-10-06 2019-05-09 Malaysia 
Axcel Papain Tablet 10,000 USP Units Tablet Oral KOTRA PHARMA (M) SDN. BHD. 2020-09-08 Not applicable Malaysia AXCEL PAPAIN TABLETS 10,000 units Tablet 10000 units Oral KOTRA PHARMA MARKETING 1999-12-03 Not applicable Singapore 
BEAUTIFUL CONTRACT - Deep V Breast contract -Hui Ju Sheng Enterprise Corporation Ltd. Capsule, gelatin coated 35 mg/500mg Oral Phytopia Co., Ltd. 2016-04-01 2017-02-01 US 
BEAZYME TABLET Tablet Oral DUOPHARMA MANUFACTURING (BANGI) SDN BHD 2020-09-08 Not applicable Malaysia - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Bromelain and Papain Tab Papain (35 mg) + Bromelains (75 mg) Tablet Oral Vita Health Products Inc 1978-12-31 2002-07-31 Canada 
Chewable Enzymes Tablets Papain (100 mg) + Bromelains (15 mg) + Pancrelipase amylase (5 mg) Tablet Oral Gahler Enterprises Ltd. 1988-12-31 2002-07-17 Canada Dygest Papain (100 mg) + Betaine hydrochloride (90 mg) + Ox bile extract (75 mg) + Pancrelipase (200 mg) + Peppermint (50 mg) + Pepsin (125 mg) Tablet Oral Creative Nutrition Canada Corp. 1987-12-31 2007-07-11 Canada Enzyme Tablets Papain (65 mg) + Betaine hydrochloride (65 mg) + Ox bile extract (8.125 mg) + Pancrelipase (100 mg) + Pancrelipase amylase (130 mg) + Pepsin (65 mg) Tablet Oral General Nutrition Canada Inc. 2001-10-20 2007-08-01 Canada Herbalax Forte No 70 Tab Papain (129.6 mg) + Capsicum oleoresin (1.62 mg) + Frangula purshiana bark (97.2 mg) + Phenolphthalein (97.2 mg) + Sodium taurocholate (64.8 mg) Tablet Oral SantÉ Naturelle (Ag) LtÉe 1981-12-31 1997-09-09 Canada - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image BEAUTIFUL CONTRACT - Deep V Breast contract -Hui Ju Sheng Enterprise Corporation Ltd. Papain (35 mg/500mg) Capsule, gelatin coated Oral Phytopia Co., Ltd. 2016-04-01 2017-02-01 US Puralor Papain (20 mg/1) + 1-(c14-c18 esteroyl)-2-docosahexanoyl-sn-glycero-3-phosphocholine (5 mg/1) + 1-(c14-c18 esteroyl)-2-docosahexanoyl-sn-glycero-3-phosphoethanolamine (2.5 mg/1) + Acetylcysteine amide (5 mg/1) + Ascorbic acid (25 mg/1) + Cholecalciferol (100 [iU]/1) + Citric acid (1.6 mg/1) + Cobamamide (2 mg/1) + Egg phospholipids (42.5 mg/1) + Folic acid (42.5 mg/1) + Gastric intrinsic factor (2.5 mg/1) + Magnesium L-threonate (2.5 mg/1) + Leucovorin (3 mg/1) + Levomefolic acid (0.4 mg/1) + Magnesium glycinate (1 mg/1) + Niacin (0.5 mg/1) + Pantethine (2.5 mg/1) + Riboflavin (0.5 mg/1) + Sodium citrate (0.8 mg/1) + Thiamine chloride (0.5 mg/1) Tablet, chewable Oral Centurion Labs 2014-01-01 2017-09-20 US
Categories
- Drug Categories
- 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
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- A236A06Y32
- CAS number
- 9001-73-4
References
- General References
- Stremnitzer C, Manzano-Szalai K, Willensdorfer A, Starkl P, Pieper M, Konig P, Mildner M, Tschachler E, Reichart U, Jensen-Jarolim E: Papain Degrades Tight Junction Proteins of Human Keratinocytes In Vitro and Sensitizes C57BL/6 Mice via the Skin Independent of its Enzymatic Activity or TLR4 Activation. J Invest Dermatol. 2015 Jul;135(7):1790-1800. doi: 10.1038/jid.2015.58. Epub 2015 Feb 23. [Article]
- External Links
- MSDS
- Download (47.7 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count Not Available Completed Basic Science Papain / Pruritus / Skin Prick Test (SPT) 1 Not Available Completed Basic Science Pruritus 1 Not Available Unknown Status Treatment Microbial Colonization 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 10000 U Tablet Oral 10000 units Capsule, gelatin coated Oral 35 mg/500mg Tablet Oral Tablet Oral 29.5 mg Tablet Oral 200 mg Tablet Oral 30 mg Capsule Oral Gel Topical 0.5 g Cream Topical 0.5 g Tablet Oral Tablet, chewable Oral Tablet, delayed release Oral - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Soluble in cold water MSDS
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Activator
- Curator comments
- Activation is indicated in vitro.
- General Function
- Transmembrane signaling receptor activity
- Specific Function
- Cooperates with LY96 and CD14 to mediate the innate immune response to bacterial lipopolysaccharide (LPS). Acts via MYD88, TIRAP and TRAF6, leading to NF-kappa-B activation, cytokine secretion and ...
- Gene Name
- TLR4
- Uniprot ID
- O00206
- Uniprot Name
- Toll-like receptor 4
- Molecular Weight
- 95679.19 Da
References
- Stremnitzer C, Manzano-Szalai K, Willensdorfer A, Starkl P, Pieper M, Konig P, Mildner M, Tschachler E, Reichart U, Jensen-Jarolim E: Papain Degrades Tight Junction Proteins of Human Keratinocytes In Vitro and Sensitizes C57BL/6 Mice via the Skin Independent of its Enzymatic Activity or TLR4 Activation. J Invest Dermatol. 2015 Jul;135(7):1790-1800. doi: 10.1038/jid.2015.58. Epub 2015 Feb 23. [Article]
Drug created at December 03, 2015 16:51 / Updated at April 18, 2024 09:15