==== 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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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 Point10.44
HydrophobicityN.A.
Melting Point (℃)48-54
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 NameULTRASE
CompanyAxcan Pharma
Brand DiscriptionULTRASE (pancrelipase) Capsules are orally administered and contain 250 mg of enteric-coated microspheres of porcine pancreatic enzymeconcentrate, predominantly pancreatic lipase, amylase, and protease.
Prescribed forULTRASE (pancrelipase) Capsules are indicated for patients with partial or complete exocrine pancreatic insufficiency caused by cystic fibrosis, Chronic pancreatitis due to alcohol, Obstruction, Other pancreatic disease, Poor mixing
Chemical NameN.A.
FormulationEach ULTRASE (pancrelipase) Capsule contains 4500 USP units of lipase; 25000 USP units of protease; 20000 USP units of amylase. It contains povidone, talc, sugar, methacrylic acid copolymer (Type C), triethyl citrate, simethicone emulsion.
Physcial AppearnceCapsules Enteric-Coated Microspheres
Route of AdministrationOral route
Recommended DosageInitial dosing of pancreatic enzyme supplements should begin with 500 lipase U/kg/meal using enteric-coated microsphere products.
ContraindicationPancrelipase capsules are contraindicated in patients known to be hypersensitive to pork protein. Pancrelipase capsules are contraindicated in patients with acute pancreatitis or with acute exacerbations of chronicpancreatic diseases.
Side Effects Extremely high doses of exogenouspancreatic enzymes have been associated with hyperuricosuria andhyperuricemia,
Useful Linkhttp://www.rxlist.com/ultrase-drug.htm
PubMed ID28099252, 27560634, 26748629, 26726093, 26709820, 26495784, 26495776, 26150571, 26036459
3-D StructureTh1071 (View) or (Download)