==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

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1423 details
Primary information
ThPP IDTh1071
Therapeutic Peptide/Protein NamePancrelipase
SequencePancreatic alpha amylase: QYSPNTQQGRTSIVHLFEWRWVDI view full sequnce in fasta
Functional ClassificationIa
Molecular Weight131125.6
Chemical FormulaC5850H8902N1606O1739S49
Isoelectric Point7.44
HydrophobicityN.A.
Melting Point (℃)48-51
Half LifePancrelipase is not significantly absorbed from the gastrointestinal tract and acts locally, so ther
DescriptionPancrelipase is an enzyme mixture isolated from porcine or bovine pancreas, sometimes called pancreatin. It contains 3 enzymes: amylase, lipase, and a protease (chymotrypsin). Pancrelipase is marketed under several brand names such as Ultresa and Viokace.
Indication/DiseaseFor treatment of exocrine pancreatic insufficiency in cystic fibrosis (Ultresa), chronic pancreatitis (Viokace in combination with a proton pump inhibitor), and pancreatectomy (Viokace in combination with a proton pump inhibitor)
PharmacodynamicsUsed in the treatment of cystic fibrosis or pancreatic dysfunction, pancrelipase helps improve fat digestion in the small intestine. Specifically, the lipase, protease and amylase components break down fat, protein, and starches, respectively, in the small intestine. Lipase hydrolyzes fats into glycerol and fatty acids. Protease converts proteins into proteoses and derived substances, while amylase converts starches into dextrins and sugars. Pancreatic enzymes are used to correct maldigestion, malabsorption and pain associated with pancreatic insufficiency. The major maldigestion/malabsorption problems arise from incomplete fat digestion. Exogenous pancrelipase reduces the amount of nitrogen and fat excreted in the stool.
Mechanism of ActionThe lipase, protease and amylase components of pancrelipase break down fat, protein, and starches, respectively, in the small intestine. Lipase hydrolyzes fats into glycerol and fatty acids. Protease converts proteins into proteoses and derived substances, while amylase converts starches into dextrins and sugars.
ToxicityOverdose symptoms may include diarrhea or stomach upset. The most common adverse reactions seen are ear, neck, and abdominal pain; headache, nasal congestion, and beta-hemolytic streptococcal infection.
MetabolismPancrelipase acts locally, so there is minimal metabolism.
AbsorptionPancrelipase is not significantly absorbed from the gastrointestinal tract.
Volume of DistributionN.A.
ClearancePancrelipase is not significantly absorbed, so there is minimal clearance from the body.
CategoriesGastrointestinal Agents and Enzyme Replacement Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameViokace
CompanyAptalis Pharma US, Inc.
Brand DiscriptionVIOKACE is a pancreatic enzyme preparation for oral administration consisting of pancrelipase, an extract derived from porcine pancreatic glands. Pancrelipase contains multiple enzyme classes, including porcine-derived lipases, amylases, and proteases.
Prescribed forVIOKACE (pancrelipase) tablets, in combination with a proton pump inhibitor, is indicated in adults for the treatment of exocrine paencratic insufficiencydue to chronic pancreatitis or pancreatectomy.
Chemical NameN.A.
Formulation10,440 USP units of lipase; 39,150 USP units of protease; 39,150 USP units of amylase tablets are tan, round biconvex and have VIO9111 engraved on one side and 9111 on the other side.Inactive ingredients in VIOKACE include: colloidal silicon dioxide, crosscarmellose sodium, lactose monohydrate, microcrystalline cellulose, stearic acid and talc.
Physcial AppearncePancrelipase is a beige-white amorphous powder. It is miscible in water and practically insoluble in alcohol and converted to tablet form
Route of AdministrationOral route
Recommended DosageEnzyme dosing should begin with 500 lipase units/kg of body weight per meal to a maximum of 2,500 lipase units/kg of body weight per meal (or less than or equal to 10,000 lipase units/kg of body weight per day), or less than 4,000 lipase units/g fat ingested per day.
ContraindicationNone
Side EffectsThe most serious adverse reactions reported with different pancreatic enzyme products of the same active ingredient (pancrelipase) that are described elsewhere in the label include fibrosing colonopathy, hyperuricemia and allergic reactions.
Useful Linkhttp://www.rxlist.com/viokace-drug.htm
PubMed ID28099252, 27560634, 26748629, 26726093, 26709820, 26495784, 26495776, 26150571, 26036459
3-D StructureTh1071 (View) or (Download)