Identification

Summary

Tilactase is a beta-D-galactosidase use to treat lactose intolerance.

Generic Name
Tilactase
DrugBank Accession Number
DB13761
Background

Tilactase is a beta-D-galactosidase obtained from Aspergillus oryzae. It is produced as a chewable tablet that has to be taken before the consumption of a lactose-containing meal.1 The beta-D-galactosidase us a large monomeric multi-domain enzyme of 985 residues that presents a catalytic (alpha/beta)8-barrel domain.3 It is considered by the WHO as part of the International Nonpropietary Names for Pharmaceutical Substances.6

Type
Biotech
Groups
Approved, Experimental
Biologic Classification
Protein Based Therapies
Other protein based therapies
Protein Structure
Db13761
Protein Chemical Formula
Not Available
Protein Average Weight
102000.0 Da
Sequences
>tr|B7VU80|B7VU80_ASPOZ Beta-galactosidase OS=Aspergillus oryzae OX=5062 GN=lacA PE=2 SV=1<<
MKLLSVAAVALLAAQAAGASIKHRLNGFTILEHPDPAKRDLLQDIVTWDDKSLFINGERI
MLFSGEVHPFRLPVPSLWLDIFHKIRALGFNCVSFYIDWALLEGKPGDYRAEGIFALEPF
FDAAKEAGIYLIARPGSYINAEVSGGGFPGWLQRVNGTLRSSDEPFLKATDNYIANAAAA
VAKAQITNGGPVILYQPENEYSGGCCGVKYPDADYMQYVMDQARKADIVVPFISNDASPS
GHNAPGSGTSAVDIYGHDSYPLGFDCANPSVWPEGKLPDNFRTLHLEQSPSTPYSLLEFQ
AGAFDPWGGPGFEKCYALVNHEFSRVFYRNDLSFGVSTFNLYMTFGGTNWGNLGHPGGYT
SYDYGSPITETRNVTREKYSDIKLLANFVKASPSYLTATPRNLTTGVYTDTSDLAVTPLI
GDSPGSFFVVRHTDYSSQESTSYKLKLPTSAGNLTIPQLEGTLSLNGRDSKIHVVDYNVS
GTNIIYSTAEVFTWKKFDGNKVLVLYGGPKEHHELAIASKSNVTIIEGSDSGIVSTRKGS
SVIIGWDVSSTRRIVQVGDLRVFLLDRNSAYNYWVPELPTEGTSPGFSTSKTTASSIIVK
AGYLLRGAHLDGADLHLTADFNATTPIEVIGAPTGAKNLFVNGEKASHTVDKNGIWSSEV
KYAAPEIKLPGLKDLDWKYLDTLPEIKSSYDDSAWVSADLPKTKNTHRPLDTPTSLYSSD
YGFHTGYLIYRGHFVANGKESEFFIRTQGGSAFGSSVWLNETYLGSWTGADYAMDGNSTY
KLSQLESGKNYVITVVIDNLGLDENWTVGEETMKNPRGILSYKLSGQDASAITWKLTGNL
GGEDYQDKVRGPLNEGGLYAERQGFHQPQPPSESWESGSPLEGLSKPGIGFYTAQFDLDL
PKGWDVPLYFNFGNNTQAARAQLYVNGYQYGKFTGNVGPQTSFPVPEGILNYRGTNYVAL
SLWALESDGAKLGSFELSYTTPVLTGYGNVESPEQPKYEQRKGAY
Download FASTA Format
Synonyms
  • beta-D-Galactosidase
  • beta-Galactosidase
  • Lactase
  • Tilactasa
  • Tilactase
  • Tilactasum
External IDs
  • S 2107
  • SL 396

Pharmacology

Indication

Tilactase is indicated for the symptomatic treatment of lactose intolerance in infants and older patients requiring a parenteral nutrition or fluid diet.6

Lactose intolerance occurs when there is an existence of an inability to break down lactose which is commonly found in dairy products. This inability occurs when the lactase levels are reduced and thus there is no via to digest and break down the lactose. The undigested lactose moves into the large intestine where normal flora bacteria can interact with it and cause bloating, gas and diarrhea.4

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

The use of a single oral administration of tilactase has been shown to be highly effective in decreasing the symptoms and hydrogen excretion of hypolactasia in tests of lactose H(2)-breath. The analysis has shown a decrease of approximately 80% in both malabsorbers and intolerants.1The administration of tilacatase also decreases the presence of bloating and flatus.2

Mechanism of action

Lactose is the primary disaccharide found in dairy products. Tilactase is a type of lactase which is the enzyme that is in charge of the breakdown of lactose to glucose and galactose which can be used by the body.7 Basically, tilactase acts by replacing the missing lactase in the body and allows avoidance of the reach of lactose to the small intestine and the normal bacteria and thus, preventing the symptoms of the lactose intolerance. Once tilactase has metabolized the lactose, the metabolism products are reabsorbed by the normal process of digestion.8

TargetActionsOrganism
ALactose
cleavage
Humans
Absorption

Tilactase is not absorbed in the GI tract and thus the pharmacokinetic parameters related to absorption are not relevant.8

Volume of distribution

Tilactase is not absorbed and thus the volume of distribution is not relevant.

Protein binding

Tilactase is not absorbed and thus the plasma protein binding is not possible.

Metabolism

Tilactase is degraded by the stomach acid and by the normal flora bacterial metabolism.8

Route of elimination

Tilactase is completely eliminated in the feces either unchanged or as metabolites.8

Half-life

Tilactase half-life at 35ÂșC is registered to be 123.77 min. This half-life can be affected by temperature in an inversely proportional manner.5

Clearance

Tilactase is not absorbed and thus the clearance rate is not relevant.

Adverse Effects
Adverseeffects
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Toxicity

Tilactase is known to present a low acute oral toxicity in preclinical trials. The lowest toxic dose for subcutaneous exposure is of 26 g/kg administered over 30 days.7 There have not been performed enough studies regarding the use of pregnancy or related to the fetal development. There are no reports of overdose with tilactase.8

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
  • Take before a meal. Take tilactase before eating food containing lactose.

Products

Products2
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International/Other Brands
Dairyaid (Major Pharmaceuticals) / Lacdigest / Oryzatym
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Dairy Digestive Aid Tab 3000fcc Lactase UnitTablet3000 unitOralPharmavite1995-12-312000-08-24Canada flag
Extra Strength Lactaid Tablets - 4500fccluTablet4500 unit / tabOralLactaid Inc.1996-12-312000-05-01Canada flag
Lactace Cap 3400unitCapsule3400 unit / capOralNature's Way Products Inc.1990-12-312004-07-26Canada flag
Lactaid Tab 3000unitTablet3000 unitOralLactaid Inc.1985-12-312000-05-01Canada flag
Lactaid Tab 3300unitTablet3300 unitOralMcneil Consumer Healthcare Division Of Johnson & Johnson Inc1992-12-311998-08-10Canada flag
Lactase 3400 Fcc Units CapCapsule3400 unit / capOralAttogram Corp1994-12-311996-08-16Canada flag
Lactase EnzymeCapsule3300 unit / capOralHolista Health (Canada) Inc.1998-04-132002-08-06Canada flag
Lactase EnzymeCapsule3000 unitOralHolista Health (Canada) Inc.2001-05-082001-08-01Canada flag
Lactase Enzyme Tablets 3300 Lac UnitsTablet3300 unitOralPharmetics (2011) Inc.1999-11-232009-07-30Canada flag
Milk AidTablet3000 unitOralSwiss Herbal Remedies Ltd.2001-02-282001-08-02Canada flag

Categories

ATC Codes
A09AA04 — Tilactase
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
  • Humans and other mammals

Chemical Identifiers

UNII
37515NWH9U
CAS number
9031-11-2

References

General References
  1. Portincasa P, Di Ciaula A, Vacca M, Montelli R, Wang DQ, Palasciano G: Beneficial effects of oral tilactase on patients with hypolactasia. Eur J Clin Invest. 2008 Nov;38(11):835-44. doi: 10.1111/j.1365-2362.2008.02035.x. [Article]
  2. DiPalma JA, Collins MS: Enzyme replacement for lactose malabsorption using a beta-D-galactosidase. J Clin Gastroenterol. 1989 Jun;11(3):290-3. [Article]
  3. Maksimainen MM, Lampio A, Mertanen M, Turunen O, Rouvinen J: The crystal structure of acidic beta-galactosidase from Aspergillus oryzae. Int J Biol Macromol. 2013 Sep;60:109-15. doi: 10.1016/j.ijbiomac.2013.05.003. Epub 2013 May 17. [Article]
  4. Vandenplas Y: Lactose intolerance. Asia Pac J Clin Nutr. 2015;24 Suppl 1:S9-13. [Article]
  5. Selvarajan E, Mohanasrinivasan V: Kinetic studies on exploring lactose hydrolysis potential of beta galactosidase extracted from Lactobacillus plantarum HF571129. J Food Sci Technol. 2015 Oct;52(10):6206-17. doi: 10.1007/s13197-015-1729-z. Epub 2015 Jan 16. [Article]
  6. WHO [Link]
  7. Australian Complementary Medicines Evaluation [Link]
  8. Lacdigest monograph [Link]
  9. AIFA: Lacdigest (Tilactase) Oral Tablet [Link]
PubChem Substance
347911450
RxNav
41397
MSDS
Download (269 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentHypolactasia1
3CompletedTreatmentLactose Intolerance1
Not AvailableCompletedBasic ScienceLactose Intolerance1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
TabletOral3000 unit
TabletOral4500 unit / tab
Tablet, chewableOral2250 U
Tablet, chewableOral
CapsuleOral3400 unit / cap
TabletOral3300 unit
CapsuleOral3000 unit
CapsuleOral3300 unit / cap
TabletOral500 mg / tab
Solution / dropsOral
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilitySlightly soluble Official monographs
isoelectric point4.5 Tanaka Y., et al. J biochem. 1975.

Drug created at June 23, 2017 20:48 / Updated at October 26, 2021 21:40