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
Structure for Olsalazine (DB01250)
- 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
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Ulcerative colitis •••••••••••• ••••• ••••••••• ••••••• Management of Ulcerative colitis •••••••••••• ••••• ••••••• Adjunct therapy in management of Mild acute ulcerative colitis •••••••••••• ••••• ••••••• Management of Mild acute ulcerative colitis •••••••••••• ••••• ••••••• Management of Moderate acute ulcerative colitis •••••••••••• ••••• ••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- 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
Target Actions Organism AHuman Cyclooxygenases inhibitorHumans AThiopurine S-methyltransferase inhibitorHumans AInterferon gamma Not Available Humans UXanthine dehydrogenase/oxidase inhibitorHumans - 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
Hover over products below to view reaction partners
- 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- 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 Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Olsalazine may decrease the excretion rate of Abacavir which could result in a higher serum level. Abciximab The risk or severity of bleeding can be increased when Olsalazine is combined with Abciximab. Acarbose Olsalazine may increase the hypoglycemic activities of Acarbose. Aceclofenac The risk or severity of nephrotoxicity can be increased when Aceclofenac is combined with Olsalazine. Acemetacin The 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
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Olsalazine sodium Y7JEW0XG7I 6054-98-4 QQWFSVYVHLECFP-XBPUGJBTSA-L - Active Moieties
Name Kind UNII CAS InChI Key Mesalazine prodrug 4Q81I59GXC 89-57-6 KBOPZPXVLCULAV-UHFFFAOYSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Dipentum Capsule, gelatin coated 250 mg/1 Oral Carilion Materials Management 2015-05-15 Not applicable US 
Dipentum Capsule, gelatin coated 250 mg/1 Oral Meda Pharmaceuticals Inc. 2015-05-15 Not applicable US Dipentum Capsule, gelatin coated 250 mg/1 Oral Carilion Materials Management 1990-07-31 Not applicable US Dipentum Capsule 250 mg Oral Atnahs Pharma Uk Limited 1995-12-31 Not applicable Canada 
Dipentum Capsule, gelatin coated 250 mg/1 Oral Alaven Pharmaceutical 1990-07-31 2017-05-11 US
Categories
- ATC Codes
- A07EC03 — Olsalazine
- Drug Categories
- Acids, Carbocyclic
- Agents causing hyperkalemia
- Agents that produce hypertension
- Alimentary Tract and Metabolism
- Aminosalicylate
- Analgesics
- Analgesics, Non-Narcotic
- Anti-Inflammatory Agents
- Antidiarrheals, Intestinal Antiinflammatory/antiinfective Agents
- Benzene Derivatives
- Benzoates
- Gastrointestinal Agents
- Hydroxy Acids
- Hydroxybenzoates
- Intestinal Antiinflammatory Agents
- Nephrotoxic agents
- Non COX-2 selective NSAIDS
- Peripheral Nervous System Agents
- Phenols
- Salicylates
- Sensory System Agents
- 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
- 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]
- Campbell DE, Berglindh T: Pharmacology of olsalazine. Scand J Gastroenterol Suppl. 1988;148:7-12. doi: 10.3109/00365528809101539. [Article]
- 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]
- 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]
- FDA Approved Drug Products: DIPENTUM (olsalazine) Oral Capsules (November 2022) [Link]
- Health Canada Approved Drug Products: DIPENTUM (olsalazine sodium) Oral Capsules [Link]
- FDA Approved Drug Products: Dipentum (olsalazine) oral capsules (October 2023) [Link]
- External Links
- Human Metabolome Database
- HMDB0015380
- KEGG Drug
- D00727
- KEGG Compound
- C07323
- PubChem Compound
- 6003770
- PubChem Substance
- 46506356
- ChemSpider
- 10642377
- 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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 2 Completed Treatment Ankylosing Spondylitis (AS) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Alaven Pharmaceutical
- Pfizer Inc.
- Pharmacia Inc.
- UCB Pharma
- Dosage Forms
Form Route Strength Capsule Oral Capsule Oral 250 mg/1 Capsule Oral 250 mg Capsule, gelatin coated Oral 250 mg/1 Tablet - Prices
Unit description Cost Unit Dipentum 250 mg capsule 1.8USD capsule DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 2.3 Not Available - Predicted Properties
Property Value Source Water Solubility 0.0781 mg/mL ALOGPS logP 2.77 ALOGPS logP 4.39 Chemaxon logS -3.6 ALOGPS pKa (Strongest Acidic) 2.93 Chemaxon pKa (Strongest Basic) -0.019 Chemaxon Physiological Charge -2 Chemaxon Hydrogen Acceptor Count 8 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 139.78 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 78.85 m3·mol-1 Chemaxon Polarizability 28.61 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.8502 Blood Brain Barrier + 0.6279 Caco-2 permeable - 0.6449 P-glycoprotein substrate Non-substrate 0.7433 P-glycoprotein inhibitor I Non-inhibitor 0.8628 P-glycoprotein inhibitor II Non-inhibitor 0.9525 Renal organic cation transporter Non-inhibitor 0.8844 CYP450 2C9 substrate Non-substrate 0.7774 CYP450 2D6 substrate Non-substrate 0.8748 CYP450 3A4 substrate Non-substrate 0.6636 CYP450 1A2 substrate Non-inhibitor 0.8006 CYP450 2C9 inhibitor Non-inhibitor 0.7804 CYP450 2D6 inhibitor Non-inhibitor 0.9047 CYP450 2C19 inhibitor Non-inhibitor 0.8638 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8912 Ames test Non AMES toxic 0.9132 Carcinogenicity Non-carcinogens 0.5546 Biodegradation Not ready biodegradable 0.8701 Rat acute toxicity 1.4882 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9506 hERG inhibition (predictor II) Non-inhibitor 0.9453
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-0udi-1941000000-280432522076c6c2ecde Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0f79-0095000000-7bb7db19b1af6177042d Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0udi-0049000000-7c76ad0d3a0538fee9aa Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-000i-0291000000-6edd53b6191e1d5f90e1 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0bt9-0191000000-3db29b271b8637083453 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-03di-0090000000-c3ec7be9279852083204 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-06tf-0190000000-17f0e51857b98451430f Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 178.3518076 predictedDarkChem Lite v0.1.0 [M-H]- 165.00941 predictedDeepCCS 1.0 (2019) [M+H]+ 175.2893076 predictedDarkChem Lite v0.1.0 [M+H]+ 167.36742 predictedDeepCCS 1.0 (2019) [M+Na]+ 175.3766076 predictedDarkChem Lite v0.1.0 [M+Na]+ 173.70184 predictedDeepCCS 1.0 (2019)
Targets
- 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
- 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
- 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]
- Lennard L: TPMT in the treatment of Crohn's disease with azathioprine. Gut. 2002 Aug;51(2):143-6. [Article]
- 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]
- 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
- 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]
- 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
- 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
- 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
- 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
- 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
- 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
- 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]
- 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 21, 2024 02:38