Pepsin

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Identification

Summary

Pepsin is a protease indicated in the treatment of digestive disorders.

Generic Name

Pepsin

DrugBank Accession Number

DB13198

Background

Pepsin is a potent enzyme in gastric juice that digests proteins such as those in meat, eggs, seeds, and dairy products ¹².

Studies on gastric digestion from 1820-1840 led to the discovery of pepsin as the substance which, in the presence of stomach acid, causes nutrients including meat or coagulated egg whites to dissolve. Soon afterward, it was shown that these protein nutrients were cleaved by pepsin to products called peptones ².

Pepsin is often used as a replacement enzyme for those with pancreatic insufficiency ¹¹. Stimulation of the pancreas and therefore enzymatic digestion of food is a tightly controlled and is a hormonally mediated process. Any changes or conditions affecting metabolic steps for successful digestion and absorption negatively affect pancreatic enzymatic secretion, entry into the intestine, functionality once inside the intestine, and appropriate mixing with foods/nutrients. Many causes of pancreatic insufficiency require that enzyme replacement therapy is started, including cystic fibrosis, pancreatic cancer, acute and chronic pancreatitis, as well as pancreatic surgery ¹¹.

Pepsin is approved by the FDA and is used in food at levels not to exceed current good manufacturing practice ¹⁷. Interestingly, it has been used as a marker for laryngopharyngeal reflux (LPR), which is a common illness of otolaryngology (ear, nose and throat specialist) visits ³.

Interestingly, recent research has suggested that pepsin participates in the digestion of nucleic acids ²².

Type

Biotech

Groups

Approved, Experimental, Investigational

Biologic Classification

Protein Based Therapies
Other protein based therapies

Protein Chemical Formula

Not Available

Protein Average Weight

Not Available

Sequences

> Pepsin A Sus Scrofa (Pig)
MKWLLLLSLVVLSECLVKVPLVRKKSLRQNLIKNGKLKDFLKTHKHNPASKYFPEAAALI
GDEPLENYLDTEYFGTIGIGTPAQDFTVIFDTGSSNLWVPSVYCSSLACSDHNQFNPDDS
STFEATSQELSITYGTGSMTGILGYDTVQVGGISDTNQIFGLSETEPGSFLYYAPFDGIL
GLAYPSISASGATPVFDNLWDQGLVSQDLFSVYLSSNDDSGSVVLLGGIDSSYYTGSLNW
VPVSVEGYWQITLDSITMDGETIACSGGCQAIVDTGTSLLTGPTSAIANIQSDIGASENS
DGEMVISCSSIDSLPDIVFTINGVQYPLSPSAYILQDDDSCTSGFEGMDVPTSSGELWIL
GDVFIRQYYTVFDRANNKVGLAPVA

Download FASTA Format

Synonyms

Lactated pepsin
Pepsin A
Pepsin porcine
Pepsin, bovine
Pepsina
Saccharated pepsin

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Pharmacology

Indication

Used as a pancreatic enzyme replacement in pancreatic insufficiency ¹¹. It is intended to mimic naturally produced human pepsin ¹⁴.

Pepsin powder is prepared from the gastric mucosa of pigs, cattle or sheep ¹⁹. In the laboratory, it is primarily used for the unspecific hydrolysis of proteins and peptides in acidic media. In addition, it provides limited hydrolysis of native immunoglobulins, yielding biologically active fragments ⁷.

In certain supplements, pepsin may be combined with betaine and HCl (hydrochloric acid) to aid in digestion in various gastrointestinal conditions ¹⁴, ⁶.

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Dose Form
Used in combination to treat	Diarrhea	Combination Product in combination with: Glutamic acid (DB00142)	••••••••••••	••••••• •••• ••••••
Used in combination to treat	Gastritis chronic	Combination Product in combination with: Glutamic acid (DB00142)	••••••••••••	••••••• •••• ••••••
Used in combination to treat	Hypochlorhydria	Combination Product in combination with: Glutamic acid (DB00142)	••••••••••••	••••••• •••• ••••••
Used in combination to treat	Postoperative digestive insufficiency	Combination Product in combination with: Glutamic acid (DB00142)	••••••••••••	••••••• •••• ••••••

Contraindications & Blackbox Warnings

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Pharmacodynamics

Pepsin digests protein ¹². It classified by the FDA that is characterizing enzyme activity is that of a peptide hydrolase ¹⁷.

Mechanism of action

Glands present in the mucous membrane lining of the stomach produce and store an inactive protein named pepsinogen. Impulses from the vagus nerve and the hormonal secretions of the hormones gastrin and secretin promote the release of pepsinogen into the stomach, where it is mixed with hydrochloric acid and quickly converted to the active enzyme pepsin. The digestive potency of pepsin is highest at the acidic pH of normal gastric juice. In the intestine, the gastric acids are then neutralized, and pepsin is no longer effective ¹².

Pepsin, the proteolytic enzyme of the stomach is normally responsible for less than 20% of the protein digestion occuring the gastrointestinal tract. It is an endopeptidase enzyme that metabolizes proteins to peptides. It preferentially hydrolyzes peptide linkages where one of the amino acids is aromatic. Pepsin, like other protease enzymes, is produced from an inactive precursor, pepsinogen, which is stored in granule form in the chief cells of the stomach and are released by a process called exocytosis ¹⁶.

In the digestive tract, pepsin activity only contributes to the partial breakdown of proteins into smaller units called peptides, which then either are absorbed from the intestine into the bloodstream or are broken down further by pancreatic enzymes ¹².

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Pepsin is the first of several enzymes that digest proteins. In the stomach, polypeptide chains bind in the deep active site groove of pepsin, and are then digested into smaller pieces. Following this, a variety of proteases and peptidases in the intestine complete the process. The small fragments, which are amino acids and dipeptides, are then absorbed by cells for use as metabolic energy or construction of new proteins ¹⁵.

Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects

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Toxicity

Oral LD50 Rat 90000 mg/kg ^MSDS

Chronic backflow of pepsin, acid, and other substances from the stomach into the esophagus, is the basis of reflux conditions, particularly gastroesophageal reflux disease (GERD) and laryngopharyngeal reflux. In the latter, pepsin and acid travel all the way up to the larynx, where they can lead to damage of the laryngeal mucosa and lead to symptoms ranging from hoarseness of the voice and chronic cough to laryngospasm (involuntary contraction of the vocal cords) as well as laryngeal cancer ¹².

Though limited data is available on the toxicity of exogenous pepsin (not naturally produced in one's gastrointestinal tract), it can be extrapolated from the above-mentioned information that pepsin overdose may lead to mucosal tissue damage of the gastrointestinal tract.

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

Drink plenty of fluids.
Take before a meal.

Products

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Over the Counter Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Digestex	Liquid	100 mg / 30 mL	Oral	Theralab Inc.	1981-04-25	2000-08-01

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
Bemosin Tab	Pepsin (130 mg) + Ammonium chloride (97.2 mg) + Betaine hydrochloride (130 mg)	Tablet	Oral	Therapeutic Foods Co.	1988-12-31	2003-07-16
Betaine HCl and Pepsin	Pepsin (135 mg) + Betaine hydrochloride (324 mg)	Tablet	Oral	Rheingold Food International Ltd.	1985-12-31	2007-07-26
Betasin Tab	Pepsin (130 mg / tab) + Ammonium chloride (97.2 mg / tab) + Betaine hydrochloride (130 mg / tab)	Tablet	Oral	Bio Vita	1987-12-31	1996-09-09
Debiline	Pepsin (50 mg) + Deoxycholic acid (100 mg)	Tablet	Oral	Lab Nadeau LtÉe, Division Of Technilab Inc.	1951-12-31	1999-09-28
Debiline H	Pepsin (50 mg / tab) + Deoxycholic acid (100 mg / tab) + Homatropine methylbromide (2.5 mg / tab)	Tablet	Oral	Lab Nadeau LtÉe, Division Of Technilab Inc.	1951-12-31	1999-09-28

Chemical Identifiers

UNII: GID333S43J
CAS number: 9001-75-6

References

General References

Iannella G, Di Nardo G, Plateroti R, Rossi P, Plateroti AM, Mariani P, Magliulo G: Investigation of pepsin in tears of children with laryngopharyngeal reflux disease. Int J Pediatr Otorhinolaryngol. 2015 Dec;79(12):2312-5. doi: 10.1016/j.ijporl.2015.10.034. Epub 2015 Oct 30. [Article]
Fruton JS: A history of pepsin and related enzymes. Q Rev Biol. 2002 Jun;77(2):127-47. [Article]
Calvo-Henriquez C, Ruano-Ravina A, Vaamonde P, Martinez-Capoccioni G, Martin-Martin C: Is Pepsin a Reliable Marker of Laryngopharyngeal Reflux? A Systematic Review. Otolaryngol Head Neck Surg. 2017 Sep;157(3):385-391. doi: 10.1177/0194599817709430. Epub 2017 Jun 6. [Article]
Petersen KU: Pepsin and Its Importance for Functional Dyspepsia: Relic, Regulator or Remedy? Dig Dis. 2018;36(2):98-105. doi: 10.1159/000481399. Epub 2017 Oct 5. [Article]
Hedemann MS, Jensen BB: Variations in enzyme activity in stomach and pancreatic tissue and digesta in piglets around weaning. Arch Anim Nutr. 2004 Feb;58(1):47-59. [Article]
Nutritional Interventions for Gastroesophageal Reflux, Irritable Bowel Syndrome, and Hypochlorhydria: A Case Report [Link]
Pepsin, Sigma Aaldrich [Link]
Effect of Pepsin on the Absorption of Food Vitamin B12 and Iron [Link]
Pepsin [Link]
Pepsin: science.gov topics [Link]
Pancreatic Enzyme Replacement Therapy During Pancreatic Insufficiency [Link]
Pepsin [Link]
Gastritis [Link]
Zypan [Link]
PDB-pepsin [Link]
NIH Dictionary- Pepsin [Link]
Code of Federal Regulations, Pepsin [Link]
Pepsin Drug Monograph [Link]
Pepsin, Drugs.com [Link]
Determining the Safety of Enzymes Used in Food Processing [Link]
PEPSIN, SIGMA AALDRICH [Link]
Digestion of Nucleic Acids Starts in the Stomach [Link]

External Links

PubChem Substance: 347911445
RxNav: 8016
Wikipedia: Pepsin

MSDS

Download (282 KB)

Clinical Trials

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Phase	Status	Purpose	Conditions	Count	Start Date	Why Stopped	100+ additional columns
Unlock 175K+ rows when you subscribe.View sample data
Not Available	Completed	Not Available	Abdominal Pain / Dyspepsia / Flatulence / Functional Gastrointestinal Disorders (FGID) / Nausea / Vomiting	1	somestatus	stop reason	just information to hide

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Liquid	Oral	100 mg / 30 mL
Tablet, delayed release	Oral
Tablet	Oral
Tablet, film coated	Oral
Tablet

Prices

Not Available

Patents

Not Available

Properties

State

Solid

Experimental Properties

Property	Value	Source
water solubility	very soluble	MSDS

Drug created at June 23, 2017 20:37 / Updated at June 05, 2021 09:12

Pepsin

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Clinical Trial & Rare Diseases Add-on Data Package

Pharmacoeconomics

Properties