Pancrelipase

Identification

Name
Pancrelipase
Accession Number
DB00085  (BTD00067, BIOD00067, DB05356)
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Other protein based therapies
Description

Pancrelipase, in general, is composed of a mixture of pancreatic enzymes which include amylases, lipases, and proteases. These enzymes are extracted from porcine pancreatic glands.[5] The pancrelipase mixture was developed by Ortho-McNeil-Janssen Pharmaceuticals, Inc and FDA approved on April 12, 2010.[6] For further information on the components of this mixture please visit Pancrelipase amylase, Pancrelipase protease and Pancrelipase lipase.

Protein chemical formula
Not Available
Protein average weight
131000.0 Da
Sequences
Not Available
Synonyms
  • Pancrealipase
  • Pancreatic extract pancrelipase
  • Pancreatic protease
  • Pancreatin
  • Pancreatinum
  • Pancrelipase (amylase;lipase;protease)
External IDs
EUR-1008 / EUR-1066 / SA-001
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Bio-zyme Tab 50mgTablet50 mgOralMetagenics, Inc.1997-01-272012-08-07Canada
Pancreatin Tab 400mgTablet400 mgOralJamieson Laboratories Ltd1979-12-312000-09-08Canada
Pancrex Granules1 gOralPaines and Byrne Ltd.1953-12-311996-08-21Canada
Pancrex V CapsulesCapsule340 mgOralPaines and Byrne Ltd.1962-12-311996-08-21Canada
Pancrex V Forte Tablets 1gm/tabTablet, delayed release1 gOralPaines and Byrne Ltd.1955-12-311996-08-21Canada
Pancrex V PowderPowderOralPaines and Byrne Ltd.1955-12-311996-08-21Canada
Pancrex V Tab 0.33gmTablet, delayed release330 mgOralPaines and Byrne Ltd.1955-12-311996-08-21Canada
Phytozyme Tab 150mgTablet150 mgOralPhyto Health Corporation1976-12-312008-07-21Canada
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Alka-pan TabletsPancrelipase (135 mg) + Bromelains (50 mg) + Betaine hydrochloride (20 mg) + Ox bile extract (35 mg) + Papaya (125 mg)TabletOralMorter HealthsystemNot applicableNot applicableCanada
DygestPancrelipase (200 mg) + Betaine hydrochloride (90 mg) + Ox bile extract (75 mg) + Papain (100 mg) + Peppermint (50 mg) + Pepsin (125 mg)TabletOralCreative Nutrition Canada Corp.1987-12-312007-07-11Canada
Neo Life Enzyme TabPancrelipase (200 mg) + Papain (50 mg) + Pepsin (125 mg)TabletOralGolden Neo Life International Ltd.1979-12-311997-08-01Canada
ZypanaxPancrelipase (90 mg) + Ammonium chloride (9 mg) + Betaine hydrochloride (165 mg) + Pepsin (.03 mg)TabletOralTherapeutic Foods Co.1980-04-021996-09-09Canada
International/Other Brands
Cotazym (Organon) / Ku-Zyme (Koichi) / Pancrease (Ortho-McNeil) / Ultrase (Axcan Scandipharm) / Ultresa (delayed-release enteric coated capsules) (APTALIS PHARMA US) / Viokace (tablets) (APTALIS PHARMA US) / Zymase (Organon)
Categories
UNII
FQ3DRG0N5K
CAS number
53608-75-6

Pharmacology

Indication

The use of pancrelipase amylase is part of the pancreatic enzyme replacement therapy. This therapy is indicated for the treatment of pancreatic insufficiency attributed to cystic fibrosis, chronic pancreatitis or any other medically defined pancreatic disease that might require it.[2, 1] Pancreatic diseases are associated with the deterioration of pancreatic parenchyma and of the dual physiological functions of the pancreas. Once established, pancreatic insufficiency results in malnutrition, weight loss, and steatorrhea.[3]

Associated Conditions
Pharmacodynamics

The major maldigestion/malabsorption problems arise from incomplete fat digestion. In clinical trials, the administration of pancrelipase as a mixture of amylase, lipase, and protease demonstrated a significant improvement in the coefficient of fat absorption and nitrogen absorption. These effects are accompanied by increased in body weight and body mass index.[2]

Mechanism of action

Pancrelipase is used to replace the deficiency of pancreatic enzymes. As abovementioned, pancrelipase is formed by a mixture of lipase, protease, and amylase which are able to break down fat, protein, and starches, respectively, in the small intestine.[4] For a more specific description of each mechanism of action, please visit Pancrelipase amylase, Pancrelipase protease and Pancrelipase lipase.

TargetActionsOrganism
ADietary fat
cleavage
Human
ADietary protein
cleavage
Human
ADietary starch
cleavage
Human
Absorption

Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount.[7]

Volume of distribution

Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount thus, the volume of distribution is not relevant.[7]

Protein binding

Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount thus, the protein binding is not relevant.[7]

Metabolism

Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount thus, the metabolism is not relevant.[7]

Route of elimination

Pancrelipase is entirely eliminated in the feces.[7]

Half life

Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount thus, the elimination half-life is not relevant.[7]

Clearance

Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount thus, the clearance rate is not relevant.[7]

Toxicity

The studies of the toxicology of pancrelipase are not needed as this drug has been used clinically for a long time.[8] Clinical overdose studies proved no effect on lungs, pancreas, liver and kidneys but it can produce symptoms such as diarrhea or stomach upset. Carcinogenicity studies have not shown any increased incidence with the use of pancrelipase. As pancrelipase is not absorbed, the effect on fetal development or reproduction is not expected.[9]

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
Ferric ammonium citratePancrelipase can cause a decrease in the absorption of Ferric ammonium citrate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric cationPancrelipase can cause a decrease in the absorption of Ferric cation resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric hydroxidePancrelipase can cause a decrease in the absorption of Ferric hydroxide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric oxidePancrelipase can cause a decrease in the absorption of Ferric oxide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric oxyhydroxidePancrelipase can cause a decrease in the absorption of Ferric oxyhydroxide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric sulfatePancrelipase can cause a decrease in the absorption of Ferric sulfate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous bisglycinatePancrelipase can cause a decrease in the absorption of Ferrous bisglycinate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous chloridePancrelipase can cause a decrease in the absorption of Ferrous chloride resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous fumaratePancrelipase can cause a decrease in the absorption of Ferrous fumarate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous gluconatePancrelipase can cause a decrease in the absorption of Ferrous gluconate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Food Interactions
  • Delayed release capsules should not be broken or crushed, but for those patients who cannot swallow the capsules, sprinkle the contents of the capsule onto soft acidic foods (pH of ≤4.5). Alkaline foods with a higher pH will promote early release of pancrelipase followed by enzyme inactivation in the stomach.
  • Multivitamins/minerals which have vitamins ADEK, folate, or iron: If pancrelipase is used in combination with multivitamins/minerals that have vitamins ADEK, folate, or iron then monitor therapy because pancrelipase may decrease absorption of iron in these multivitamin/mineral products.
  • Take pancrelipase with meals and a sufficient amount of water.

References

General References
  1. Kuhn RJ, Gelrud A, Munck A, Caras S: CREON (Pancrelipase Delayed-Release Capsules) for the treatment of exocrine pancreatic insufficiency. Adv Ther. 2010 Dec;27(12):895-916. doi: 10.1007/s12325-010-0085-7. Epub 2010 Nov 15. [PubMed:21086085]
  2. Nakajima K, Oshida H, Muneyuki T, Kakei M: Pancrelipase: an evidence-based review of its use for treating pancreatic exocrine insufficiency. Core Evid. 2012;7:77-91. doi: 10.2147/CE.S26705. Epub 2012 Jul 19. [PubMed:22936895]
  3. Dominguez Munoz JE: Diagnosis of chronic pancreatitis: Functional testing. Best Pract Res Clin Gastroenterol. 2010 Jun;24(3):233-41. doi: 10.1016/j.bpg.2010.03.008. [PubMed:20510825]
  4. Shorr R., Hoth A. and Rawls N. (2007). Drugs for the Geriatric Patient. Elsevier. [ISBN:978-1-4160-0208-6]
  5. Creon monograph [Link]
  6. FDA approval [Link]
  7. FDA reports [Link]
  8. CENTER FOR DRUG EVALUATION AND RESEARCH- 20755 [Link]
  9. EMA reports [Link]
External Links
UniProt
P04746
Genbank
M18785
KEGG Drug
D05349
PubChem Substance
46504728
ChEMBL
CHEMBL2108074
PharmGKB
PA448428
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Pancrelipase
ATC Codes
A09AA02 — Multienzymes (lipase, protease etc.)
AHFS Codes
  • 56:16.00 — Digestants
FDA label
Download (79.5 KB)
MSDS
Download (42.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Unknown StatusTreatmentPancreatitis, Chronic1
1, 2RecruitingTreatmentMalignant Neoplasm of Pancreas / Pancreatic enzyme abnormality / Pancreatic Insufficiency1
2CompletedTreatmentConjunctivitis, Seasonal Allergic1
2CompletedTreatmentPoisoning by BCG Vaccine1
2CompletedTreatmentPulmonary Tuberculosis (TB)1
2Not Yet RecruitingSupportive CareMalignant Neoplasm of Pancreas1
2RecruitingDiagnosticPancreatitis, Chronic1
2WithdrawnTreatmentPancreatitis1
3Active Not RecruitingTreatmentPulmonary Tuberculosis (TB)1
3CompletedTreatmentCystic Fibrosis (CF) / Exocrine Pancreatic Insufficiency2
3CompletedTreatmentCystic Fibrosis (CF) / Pancreatic Insufficiency1
3CompletedTreatmentExocrine Pancreatic Insufficiency, Chronic Pancreatitis1
3CompletedTreatmentExocrine Pancreatic Insufficiency / Pancreatitis, Chronic1
3CompletedTreatmentPancreatic Exocrine Insufficiency1
3CompletedTreatmentPancreatic Exocrine Insufficiency, Chronic Pancreatitis, Pancreatectomy1
3CompletedTreatmentPancreatic Insufficiency1
4CompletedTreatmentCrohn's Disease (CD) / Ulcerative Colitis (UC)1
4CompletedTreatmentCystic Fibrosis (CF) / Exocrine Pancreatic Insufficiency2
4CompletedTreatmentGastric Resection1
4CompletedTreatmentIrritable Bowel Syndrome (IBS)1
4Enrolling by InvitationTreatmentGluten Enteropathy1
4TerminatedSupportive CareCystic Fibrosis (CF) / Exocrine Pancreatic Insufficiency / Pancreatitis, Chronic1
Not AvailableCompletedTreatmentCystic Fibrosis (CF)1
Not AvailableRecruitingNot AvailableFibrosing colonopathy / Fibrosing Colonopathy in Patients With Cystic Fibrosis1
Not AvailableTerminatedNot AvailableExocrine Pancreatic Insufficiency1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Axcan Pharma Inc.
  • Confab Laboratories Inc.
  • Eurand Pharmaceuticals Inc.
  • Global Pharmaceuticals
  • Kaiser Foundation Hospital
  • Ortho Mcneil Janssen Pharmaceutical Inc.
  • Ortho-McNeil-Janssen Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Schwarz Pharma Inc.
  • Solvay Pharmaceuticals
  • X-Gen Pharmaceuticals
  • Yung Shin Pharmaceutical Industry Ltd.
Dosage forms
FormRouteStrength
TabletOral50 mg
TabletOral
TabletOral400 mg
CapsuleOral340 mg
Tablet, delayed releaseOral1 g
PowderOral
Tablet, delayed releaseOral330 mg
TabletOral150 mg
Prices
Unit descriptionCostUnit
Creon 24000 unit Enteric Coated Capsule3.32USD capsule
Ultrase MT 20 65-20-65mu Enteric Coated Capsule3.06USD capsule
Pancrease MT 20 56-20-44mu Enteric Coated Capsule2.99USD capsule
Creon 20 66.4-20-75mu Enteric Coated Capsule2.83USD capsule
Ultrase MT 18 58.5-18-58.5mu Enteric Coated Capsule2.65USD capsule
Pancrease MT 16 48-16-48mu Enteric Coated Capsule2.4USD capsule
Pancrelipase 16000 48-16-48mu Enteric Coated Capsule2.02USD capsule
Ultrase MT 12 39-12-39mu Enteric Coated Capsule1.65USD capsule
Creon 10 33.2-10-37.5mu Enteric Coated Capsule1.54USD capsule
Pancrease MT 10 30-10-30mu Enteric Coated Capsule1.49USD capsule
Pancrelipase 10000 30-10-30mu Enteric Coated Capsule1.38USD capsule
Pancrelipase MST-16 48-16-48mu Enteric Coated Capsule1.03USD capsule
Pancrease 4500 unit Enteric Coated Capsule0.87USD capsule
Creon 5 16.6-5-18.75mu Enteric Coated Capsule0.86USD capsule
Ultrase 4500 unit Enteric Coated Capsule0.8USD capsule
Pancrease ec capsule0.76USD capsule
Pancrelipase ec 4500 capsule0.64USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US9198871No2015-12-012030-02-07Us
US8562979No2013-10-222028-02-20Us
US8562980No2013-10-222028-02-20Us
US8562981No2013-10-222028-02-20Us
US8221747No2012-07-172028-02-20Us
US8562978No2013-10-222028-02-20Us
US8246950No2012-08-212028-02-20Us
US7658918No2010-02-092028-02-20Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)48-50 °CVinogradov, A.A. et al., Protein Eng. 14:683-689 (2001)
water solubility1 mg/mlMonograph

Taxonomy

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

Targets

1. Dietary fat
Kind
Group
Organism
Human
Pharmacological action
Yes
Actions
Cleavage
References
  1. Svendsen A: Lipase protein engineering. Biochim Biophys Acta. 2000 Dec 29;1543(2):223-238. [PubMed:11150608]
2. Dietary protein
Kind
Group
Organism
Human
Pharmacological action
Yes
Actions
Cleavage
References
  1. Rawlings ND, Barrett AJ: Families of serine peptidases. Methods Enzymol. 1994;244:19-61. [PubMed:7845208]
3. Dietary starch
Kind
Group
Organism
Human
Pharmacological action
Yes
Actions
Cleavage
References
  1. Udani J, Hardy M, Madsen DC: Blocking carbohydrate absorption and weight loss: a clinical trial using Phase 2 brand proprietary fractionated white bean extract. Altern Med Rev. 2004 Mar;9(1):63-9. [PubMed:15005645]

Drug created on June 13, 2005 07:24 / Updated on November 20, 2018 00:38