Olsalazine

Identification

Summary

Olsalazine is an anti-inflammatory aminosalicylate used in the treatment of inflammatory bowel disease and ulcerative colitis.

Brand Names
Dipentum
Generic Name
Olsalazine
DrugBank Accession Number
DB01250
Background

Olsalazine is an aminosalicylate and a prodrug of mesalamine (5-aminosalicylic acid, 5-ASA).1 It was first developed for delivering mesalamine to the colon without the use of sulfapyridine.2 Olsalazine comprises two mesalamine molecules joined by an azo bridge, which is cleaved in the colon.2 Olsalazine is an anti-inflammatory agent that works by inhibiting cyclooxygenase and lipoxygenase, subsequently reducing the production of pro-inflammatory factors like prostaglandin and leukotriene.1 Olsalazine is used in the treatment of ulcerative colitis.5,6

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 302.239
Monoisotopic: 302.053886062
Chemical Formula
C14H10N2O6
Synonyms
  • Olsalazine

Pharmacology

Indication

In the US, olsalazine is indicated for the maintenance of remission of ulcerative colitis in adult patients who are intolerant to sulfasalazine.5

In Canada, it is used in the treatment of acute ulcerative colitis of mild to moderate severity, with or without the concomitant use of steroids. It is also indicated for the long-term maintenance of patients with ulcerative colitis in remission.6

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Management ofUlcerative colitis•••••••••••••••••••••••••••••••••
Management ofUlcerative colitis••••••••••••••••••••••••
Adjunct therapy in management ofMild acute ulcerative colitis••••••••••••••••••••••••
Management ofMild acute ulcerative colitis••••••••••••••••••••••••
Management ofModerate acute ulcerative colitis••••••••••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Olsalazine is an anti-inflammatory agent that blocks the production of cyclooxygenase (COX)-derived products of arachidonic acid metabolism.5 It works to alleviate inflammation in ulcerative colitis.1

Olsalazine was shown to decrease water and sodium absorption. While olsalazine is not expected to affect the motility and transit time of small intestines, it decreased small bowel transit time at high doses ranging from 60 to 120 mg/kg. In about 40% of the patients with ulcerative colitis, administration of olsalazine 1g daily was associated with a decrease in whole gut transit time.1

Mechanism of action

Upon administration, the azo bond connecting two molecules of mesalamine (also known as 5-aminosalicylic acid or 5-ASA) is cleaved by azoreductase-containing bacteria in the colon. The two molecules of mesalamine are released to mediate therapeutic effects.1 The exact mechanism of action of olsalazine and its active moiety mesalamine in ulcerative colitis has not been elucidated; however, it is understood that mesalamine mediates an anti-inflammatory action on epithelial cells of the colon.5 The COX-derived (i.e., prostanoids such as prostaglandin E2) and lipoxygenase-derived products (i.e., leukotrienes [LTs] and hydroxyeicosatetraenoic acids [HETEs]) of arachidonic acid metabolism have been implicated in the pathogenesis and maintenance of inflammatory disorders, including ulcerative colitis and inflammatory bowel disease.1,5 Mesalamine may attenuate inflammation by blocking the COX enzyme and inhibiting prostaglandin production in the colon.3,4,5 Olsalazine was also shown to inhibit xanthine oxidase, an enzyme that generates oxygen-derived free radicals.2

Olsalazine may attenuate intestinal inflammation by limiting macrophage migration to inflamed intestinal mucosa: it was shown to inhibit in vitro migration of intestinal macrophages in response to leukotriene B4. Olsalazine may also act as a free radical scavenger, and mesalazine may suppress fatty acid peroxidation.1

TargetActionsOrganism
AHuman Cyclooxygenases
inhibitor
Humans
AThiopurine S-methyltransferase
inhibitor
Humans
AInterferon gammaNot AvailableHumans
UXanthine dehydrogenase/oxidase
inhibitor
Humans
Absorption

After oral administration, olsalazine has limited systemic bioavailability, with less than 5% of the oral dose being absorbed.1 Based on oral and intravenous dosing studies, approximately 2.4% of a single 1 g oral dose is absorbed. Maximum serum concentrations of olsalazine appear after approximately one hour and, even after a 1 g single dose, are low (e.g., 1.6 to 6.2 µmol/L).5

Patients on daily doses of 1 g olsalazine for two to four years show a stable plasma concentration of olsalazine-S (3.3 to 12.4 µmol/L). Olsalazine-S accumulates to a steady state within two to three weeks. Serum concentrations of mesalamine are detected after four to eight hours. The peak levels of mesalamine after an oral dose of 1 g olsalazine are low (i.e., 0 to 4.3 µmol/L).5

Volume of distribution

The steady-state volume of distribution determined in healthy volunteers is approximately 5L.1

Protein binding

Olsalazine and its metabolite olsalazine-S, are more than 99% bound to plasma proteins. Less than 1% of both olsalazine and olsalazine-S appears undissociated in plasma. It does not interfere with the protein binding of warfarin.5

Mesalamine (5-aminosalicylic acid, 5-ASA) and its metabolite, N-acetyl-5-ASA, are 74 and 81%, respectively, bound to plasma proteins.5

Metabolism

Olsalazine is cleaved by colonic bacteria to release its active ingredient, mesalamine. Mesalamine can undergo acetylation to form N-acetyl-5-aminosalicylic acid (N-acetyl-5-ASA, Ac-5-ASA) by the colonic epithelium; however, the extent of acetylation depends on transit time.1 Approximately 0.1% of an oral dose of olsalazine is metabolized in the liver to olsalazine-O-sulfate (olsalazine-S).5

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Route of elimination

Olsalazine and its metabolites are excreted in the urine.1 Total recovery of oral 14C-labeled olsalazine in animals and humans ranges from 90 to 97%. Approximately 20% of the total mesalamine is recovered in the urine. Of the total mesalamine found in the urine, more than 90% is N-acetyl-5-ASA. Only small amounts of mesalamine are detected in the urine. The remaining mesalamine is partially acetylated and excreted in the feces. From fecal dialysis, the concentration of mesalamine in the colon following olsalazine has been calculated to be 18 to 49 mmol/L.5

The urinary recovery of olsalazine is below 1%.5 Less than 5% of an oral dose (0.25 to 2g) was recovered unchanged in the feces; however, more than 50% of the oral dose was excreted in feces as unchanged olsalazine when the whole gut transit time was decreased by approximately 50%.1

Half-life

Olsalazine has a very short serum half-life, approximately 0.9 hours. Olsalazine-S has a half-life of seven days due to slow dissociation from the protein binding site.1,5

Clearance

Not Available

Adverse Effects
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Toxicity

There is no information available regarding acute toxicity (LD50) of olsalazine. Symptoms of salicylate toxicity include nausea, vomiting and abdominal pain, tachypnea, hyperpnea, tinnitus, and neurologic symptoms (headache, dizziness, confusion, seizures). Severe intoxication may lead to electrolyte and blood pH imbalance and potentially to organ damage. There is no antidote for olsalazine overdose; however, conventional therapy for salicylate toxicity, such as gastrointestinal tract decontamination, may be beneficial in acute overdosage. Overdose should be managed with proper medical care and appropriate supportive care, including the possible use of emesis, cathartics, and activated charcoal to prevent further absorption. Fluid and electrolyte imbalance may be managed with appropriate intravenous therapy and maintenance of adequate renal function.5

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.
DrugInteraction
AbacavirOlsalazine may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbciximabThe risk or severity of bleeding can be increased when Olsalazine is combined with Abciximab.
AcarboseOlsalazine may increase the hypoglycemic activities of Acarbose.
AceclofenacThe risk or severity of nephrotoxicity can be increased when Aceclofenac is combined with Olsalazine.
AcemetacinThe risk or severity of nephrotoxicity can be increased when Acemetacin is combined with Olsalazine.
Food Interactions
  • Take with food. Food does not affect drug absorption or exposure, but may mitigate the risk for drug-related adverse effects.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Olsalazine sodiumY7JEW0XG7I6054-98-4QQWFSVYVHLECFP-XBPUGJBTSA-L
Active Moieties
NameKindUNIICASInChI Key
Mesalazineprodrug4Q81I59GXC89-57-6KBOPZPXVLCULAV-UHFFFAOYSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
DipentumCapsule250 mgOralAtnahs Pharma Uk Limited1995-12-31Not applicableCanada flag
DipentumCapsule, gelatin coated250 mg/1OralCarilion Materials Management2015-05-15Not applicableUS flag
DipentumCapsule250 mg/1OralUnither Manufacturing, LLC1990-07-312010-07-31US flag
DipentumCapsule, gelatin coated250 mg/1OralCarilion Materials Management1990-07-31Not applicableUS flag
DipentumCapsule, gelatin coated250 mg/1OralAlaven Pharmaceutical1990-07-312017-05-11US flag

Categories

ATC Codes
A07EC03 — Olsalazine
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as azobenzenes. These are organonitrogen aromatic compounds that contain a central azo group, where each nitrogen atom is conjugated to a benzene ring.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Azobenzenes
Sub Class
Not Available
Direct Parent
Azobenzenes
Alternative Parents
Salicylic acids / Benzoic acids / Benzoyl derivatives / 1-hydroxy-2-unsubstituted benzenoids / Dicarboxylic acids and derivatives / Vinylogous acids / Azo compounds / Propargyl-type 1,3-dipolar organic compounds / Carboxylic acids / Organopnictogen compounds
show 3 more
Substituents
1-hydroxy-2-unsubstituted benzenoid / Aromatic homomonocyclic compound / Azo compound / Azobenzene / Benzenoid / Benzoic acid / Benzoic acid or derivatives / Benzoyl / Carboxylic acid / Carboxylic acid derivative
show 16 more
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
ULS5I8J03O
CAS number
15722-48-2
InChI Key
QQBDLJCYGRGAKP-FOCLMDBBSA-N
InChI
InChI=1S/C14H10N2O6/c17-11-3-1-7(5-9(11)13(19)20)15-16-8-2-4-12(18)10(6-8)14(21)22/h1-6,17-18H,(H,19,20)(H,21,22)/b16-15+
IUPAC Name
5-[(1E)-2-(3-carboxy-4-hydroxyphenyl)diazen-1-yl]-2-hydroxybenzoic acid
SMILES
OC(=O)C1=CC(=CC=C1O)\N=N\C1=CC=C(O)C(=C1)C(O)=O

References

General References
  1. Wadworth AN, Fitton A: Olsalazine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in inflammatory bowel disease. Drugs. 1991 Apr;41(4):647-64. doi: 10.2165/00003495-199141040-00009. [Article]
  2. Campbell DE, Berglindh T: Pharmacology of olsalazine. Scand J Gastroenterol Suppl. 1988;148:7-12. doi: 10.3109/00365528809101539. [Article]
  3. Horn H, Preclik G, Stange EF, Ditschuneit H: Modulation of arachidonic acid metabolism by olsalazine and other aminosalicylates in leukocytes. Scand J Gastroenterol. 1991 Aug;26(8):867-79. doi: 10.3109/00365529109037024. [Article]
  4. Allgayer H: Review article: mechanisms of action of mesalazine in preventing colorectal carcinoma in inflammatory bowel disease. Aliment Pharmacol Ther. 2003 Sep;18 Suppl 2:10-4. [Article]
  5. FDA Approved Drug Products: DIPENTUM (olsalazine) Oral Capsules (November 2022) [Link]
  6. Health Canada Approved Drug Products: DIPENTUM (olsalazine sodium) Oral Capsules [Link]
  7. FDA Approved Drug Products: Dipentum (olsalazine) oral capsules (October 2023) [Link]
Human Metabolome Database
HMDB0015380
KEGG Drug
D00727
KEGG Compound
C07323
PubChem Compound
6003770
PubChem Substance
46506356
ChemSpider
10642377
RxNav
32385
ChEMBL
CHEMBL425
ZINC
ZINC000003812865
PharmGKB
PA450700
PDBe Ligand
JBC
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Olsalazine
PDB Entries
7era

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentAnkylosing Spondylitis (AS)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Alaven Pharmaceutical
  • Pfizer Inc.
  • Pharmacia Inc.
  • UCB Pharma
Dosage Forms
FormRouteStrength
CapsuleOral
CapsuleOral250 mg/1
CapsuleOral250 mg
Capsule, gelatin coatedOral250 mg/1
Tablet
Prices
Unit descriptionCostUnit
Dipentum 250 mg capsule1.8USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP2.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0781 mg/mLALOGPS
logP2.77ALOGPS
logP4.39Chemaxon
logS-3.6ALOGPS
pKa (Strongest Acidic)2.93Chemaxon
pKa (Strongest Basic)-0.019Chemaxon
Physiological Charge-2Chemaxon
Hydrogen Acceptor Count8Chemaxon
Hydrogen Donor Count4Chemaxon
Polar Surface Area139.78 Å2Chemaxon
Rotatable Bond Count4Chemaxon
Refractivity78.85 m3·mol-1Chemaxon
Polarizability28.61 Å3Chemaxon
Number of Rings2Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.8502
Blood Brain Barrier+0.6279
Caco-2 permeable-0.6449
P-glycoprotein substrateNon-substrate0.7433
P-glycoprotein inhibitor INon-inhibitor0.8628
P-glycoprotein inhibitor IINon-inhibitor0.9525
Renal organic cation transporterNon-inhibitor0.8844
CYP450 2C9 substrateNon-substrate0.7774
CYP450 2D6 substrateNon-substrate0.8748
CYP450 3A4 substrateNon-substrate0.6636
CYP450 1A2 substrateNon-inhibitor0.8006
CYP450 2C9 inhibitorNon-inhibitor0.7804
CYP450 2D6 inhibitorNon-inhibitor0.9047
CYP450 2C19 inhibitorNon-inhibitor0.8638
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8912
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.5546
BiodegradationNot ready biodegradable0.8701
Rat acute toxicity1.4882 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9506
hERG inhibition (predictor II)Non-inhibitor0.9453
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-0udi-1941000000-280432522076c6c2ecde
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0f79-0095000000-7bb7db19b1af6177042d
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0udi-0049000000-7c76ad0d3a0538fee9aa
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-000i-0291000000-6edd53b6191e1d5f90e1
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0bt9-0191000000-3db29b271b8637083453
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-03di-0090000000-c3ec7be9279852083204
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-06tf-0190000000-17f0e51857b98451430f
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-178.3518076
predicted
DarkChem Lite v0.1.0
[M-H]-165.00941
predicted
DeepCCS 1.0 (2019)
[M+H]+175.2893076
predicted
DarkChem Lite v0.1.0
[M+H]+167.36742
predicted
DeepCCS 1.0 (2019)
[M+Na]+175.3766076
predicted
DarkChem Lite v0.1.0
[M+Na]+173.70184
predicted
DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.
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Kind
Protein group
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Prostaglandin-endoperoxide synthase activity
Specific Function
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gas...

Components:
References
  1. Allgayer H: Review article: mechanisms of action of mesalazine in preventing colorectal carcinoma in inflammatory bowel disease. Aliment Pharmacol Ther. 2003 Sep;18 Suppl 2:10-4. [Article]
  2. FDA Approved Drug Products: DIPENTUM (olsalazine) Oral Capsules (November 2022) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Thiopurine s-methyltransferase activity
Specific Function
Catalyzes the S-methylation of thiopurine drugs such as 6-mercaptopurine.
Gene Name
TPMT
Uniprot ID
P51580
Uniprot Name
Thiopurine S-methyltransferase
Molecular Weight
28180.09 Da
References
  1. Lewis LD, Benin A, Szumlanski CL, Otterness DM, Lennard L, Weinshilboum RM, Nierenberg DW: Olsalazine and 6-mercaptopurine-related bone marrow suppression: a possible drug-drug interaction. Clin Pharmacol Ther. 1997 Oct;62(4):464-75. [Article]
  2. Lennard L: TPMT in the treatment of Crohn's disease with azathioprine. Gut. 2002 Aug;51(2):143-6. [Article]
  3. Lennard L: Clinical implications of thiopurine methyltransferase--optimization of drug dosage and potential drug interactions. Ther Drug Monit. 1998 Oct;20(5):527-31. [Article]
  4. Shipkova M, Niedmann PD, Armstrong VW, Oellerich M, Wieland E: Determination of thiopurine methyltransferase activity in isolated human erythrocytes does not reflect putative in vivo enzyme inhibition by sulfasalazine. Clin Chem. 2004 Feb;50(2):438-41. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
General Function
Interferon-gamma receptor binding
Specific Function
Produced by lymphocytes activated by specific antigens or mitogens. IFN-gamma, in addition to having antiviral activity, has important immunoregulatory functions. It is a potent activator of macrop...
Gene Name
IFNG
Uniprot ID
P01579
Uniprot Name
Interferon gamma
Molecular Weight
19348.165 Da
References
  1. Egan LJ, Sandborn WJ: Inhibition of nuclear factor kappaB by sulfasalazine: a new target for inflammatory bowel disease therapy? Gastroenterology. 1998 Nov;115(5):1295-6. [Article]
  2. Ito R, Shin-Ya M, Kishida T, Urano A, Takada R, Sakagami J, Imanishi J, Kita M, Ueda Y, Iwakura Y, Kataoka K, Okanoue T, Mazda O: Interferon-gamma is causatively involved in experimental inflammatory bowel disease in mice. Clin Exp Immunol. 2006 Nov;146(2):330-8. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xanthine oxidase activity
Specific Function
Key enzyme in purine degradation. Catalyzes the oxidation of hypoxanthine to xanthine. Catalyzes the oxidation of xanthine to uric acid. Contributes to the generation of reactive oxygen species. Ha...
Gene Name
XDH
Uniprot ID
P47989
Uniprot Name
Xanthine dehydrogenase/oxidase
Molecular Weight
146422.99 Da
References
  1. Campbell DE, Berglindh T: Pharmacology of olsalazine. Scand J Gastroenterol Suppl. 1988;148:7-12. doi: 10.3109/00365528809101539. [Article]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Downregulator
Curator comments
Olsalazine reduced the mRNA expression of this transporter in hyperuricemic mice.
General Function
Sugar:proton symporter activity
Specific Function
Transport urate and fructose. May have a role in the urate reabsorption by proximal tubules. Also transports glucose at low rate.
Gene Name
SLC2A9
Uniprot ID
Q9NRM0
Uniprot Name
Solute carrier family 2, facilitated glucose transporter member 9
Molecular Weight
58701.205 Da
References
  1. Niu Y, Yang P, Li H, Li Q, Lin H, Gao L, Li L: Olsalazine Sodium Increases Renal Urate Excretion by Modulating Urate Transporters in Hyperuricemic Animals. Biol Pharm Bull. 2020 Nov 1;43(11):1653-1659. doi: 10.1248/bpb.b20-00362. Epub 2020 Aug 28. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Upregulator
Curator comments
Olsalazine increased the mRNA expression of this transporter in hyperuricemic mice.
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one ...
Gene Name
SLC22A6
Uniprot ID
Q4U2R8
Uniprot Name
Solute carrier family 22 member 6
Molecular Weight
61815.78 Da
References
  1. Niu Y, Yang P, Li H, Li Q, Lin H, Gao L, Li L: Olsalazine Sodium Increases Renal Urate Excretion by Modulating Urate Transporters in Hyperuricemic Animals. Biol Pharm Bull. 2020 Nov 1;43(11):1653-1659. doi: 10.1248/bpb.b20-00362. Epub 2020 Aug 28. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Upregulator
Curator comments
Olsalazine increased the mRNA expression of this transporter in hyperuricemic mice.
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name
SLC22A8
Uniprot ID
Q8TCC7
Uniprot Name
Solute carrier family 22 member 8
Molecular Weight
59855.585 Da
References
  1. Niu Y, Yang P, Li H, Li Q, Lin H, Gao L, Li L: Olsalazine Sodium Increases Renal Urate Excretion by Modulating Urate Transporters in Hyperuricemic Animals. Biol Pharm Bull. 2020 Nov 1;43(11):1653-1659. doi: 10.1248/bpb.b20-00362. Epub 2020 Aug 28. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Upregulator
Curator comments
Olsalazine increased the mRNA expression of this transporter in hyperuricemic mice.
General Function
Not Available
Specific Function
Not Available
Gene Name
SLC20A1
Uniprot ID
Q8WUM9
Uniprot Name
Sodium-dependent phosphate transporter 1
Molecular Weight
73699.01 Da
References
  1. Niu Y, Yang P, Li H, Li Q, Lin H, Gao L, Li L: Olsalazine Sodium Increases Renal Urate Excretion by Modulating Urate Transporters in Hyperuricemic Animals. Biol Pharm Bull. 2020 Nov 1;43(11):1653-1659. doi: 10.1248/bpb.b20-00362. Epub 2020 Aug 28. [Article]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Olsalazine and its active ingredient mesalazine inhibited ileal and colonic NA+/K+-ATPase in a concentration-dependent manner with an IC50 of 4.1 mM and 4.8 mM, respectively.
General Function
Steroid hormone binding
Specific Function
This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates th...

Components:
References
  1. Scheurlen C, Allgayer H, Kruis W, Erdmann E, Sauerbruch T: Effect of olsalazine and mesalazine on human ileal and colonic (Na+ + K+)-ATPase. A possible diarrhogenic factor? Clin Investig. 1993 Apr;71(4):286-9. doi: 10.1007/BF00184728. [Article]
  2. Wadworth AN, Fitton A: Olsalazine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in inflammatory bowel disease. Drugs. 1991 Apr;41(4):647-64. doi: 10.2165/00003495-199141040-00009. [Article]

Drug created at March 30, 2007 12:25 / Updated at February 26, 2024 01:19