Explore a selection of our essential drug information below, or:
Identification
- Summary
Olopatadine is a histamine H1 antagonist used to treat allergic conjunctivitis and rhinitis.
- Brand Names
- Pataday, Patanase, Patanol, Pazeo, Ryaltris
- Generic Name
- Olopatadine
- DrugBank Accession Number
- DB00768
- Background
Olopatadine is a selective histamine H1 antagonist and mast cell stabilizer that works by attenuating inflammatory and allergic reactions. It is a structural analog of doxepin, which has a minimal anti-allergic activity.10 Olopatadine works by blocking the effects of histamine, which is a primary inflammatory mediator that causes inflammatory and allergic reactions. An ophthalmic solution of olopatadine was approved by the FDA and European Union for the treatment of seasonal and perennial allergic conjunctivitis in 1996 and 2002, respectively.2 In comparison to other anti-allergenic ophthalmic medications, olopatadine displays a good comfort and tolerability profile since it does not cause perturbation of cell membranes.6 Olopatadine is used for the symptomatic treatment of ocular itching associated with allergic conjunctivitis in ophthalmic formulations and seasonal allergic rhinitis in intranasal formulations. It is currently marketed under several brand names, including Pazeo, Patanase, and Opatanol.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Olopatadine (DB00768)
- Weight
- Average: 337.4122
Monoisotopic: 337.167793607 - Chemical Formula
- C21H23NO3
- Synonyms
- Olopatadin
- Olopatadina
- Olopatadine
- Olopatadinum
- External IDs
- AL-4943A
- ALO 4943 A
- KW 4679
Pharmacology
- Indication
Olopatadine is indicated for the symptomatic treatment of ocular itching associated with allergic conjunctivitis as ophthalmic solution.7
As a nasal spray, as a monotherapy or in combination with mometasone furoate, olopatadine is indicated for the symptomatic relief of seasonal allergic rhinitis in patients 12 years of age and older.8,12
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 Symptomatic treatment of Allergic conjunctivitis •••••••••••• ••••••••• •••••••••• Symptomatic treatment of Allergic rhinitis (ar) •••••••••••• •••••••• Used in combination for symptomatic treatment of Seasonal allergic rhinitis Combination Product in combination with: Mometasone furoate (DB14512) •••••••••••• •••••• ••••••••• ••••• Symptomatic treatment of Seasonal allergic rhinitis •••••••••••• ••••• Used in combination for symptomatic treatment of Moderate, severe seasonal allergic rhinitis Combination Product in combination with: Mometasone furoate (DB14512) •••••••••••• •••••• ••••••••• ••••• - 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
Inflammatory reactions in response to various stimuli are mediated by endogenous mediators and other pro-inflammatory factors. Histamine receptor activation and mast cell degranulation are primary mechanisms that cause inflammatory reactions such as ocular itching, hyperemia, chemosis, eyelid swelling, and tearing of seasonal allergic conjunctivitis.3 Olopatadine is an anti-allergenic molecule and mast cell stabilizer that inhibits the in vivo type 1 immediate hypersensitivity reaction.10 By blocking the effects of histamine, olopatadine works to reduce the symptoms of allergies and inflammation at various sites of administration, including the eyes and nose. It has shown to exert antihistaminic effects in isolated tissues, animal models, and humans.8 Olopatadine also demonstrated dose-dependent inhibition of immunologically-stimulated release of histamine from rat basophilic leukemia cells and human conjunctival mast cells in vitro.3 Olopatadine has a relatively rapid onset of action and prolonged duration, where it was shown to mediate anti-histaminic effects at 5 minutes to 24 hours post-administration.3
While olopatadine is a non-sedating antihistamine agent, there have been reports of somnolence in some patients taking nasal olopatadine during clinical trials.8 Temporary blurred vision or other visual disturbances were observed following ophthalmic administration. Olopatadine has negligible effects on alpha-adrenergic, dopamine, muscarinic type 1 and 2, and serotonin receptors.10 In clinical trials, there was no evidence of any effect of olopatadine on QT prolongation was observed following intranasal administration.8
- Mechanism of action
Histamine is a biogenic vasoactive amine that binds to its receptors, which are G-protein coupled receptors. Signaling through the histamine H1 receptor is thought to primarily promote the activation of inflammatory reactions, such as allergy, asthma, and autoimmune diseases.4 H1 receptor signaling activates the intracellular transcription factors, such as IP3, PLC, PKC, DAG, and intracellular calcium ions, which all work to activate further downstream cascades. Activated downstream cascades lead to the production of cytokines, the release of mast cell inflammatory mediators, synthesis of prostacyclins, activation of platelet factor, as well as the synthesis of nitric oxide, arachidonic acid, and thromboxane, which all contribute to inflammatory reactions.4
Olopatadine is an anti-allergic molecule that works via several mechanisms. As a mast cell stabilizer, it stabilizes rodent basophils and human conjunctival mast cells and inhibits the immunologically-stimulated release of histamine.3 Olopatadine acts as an antagonist at the histamine H1 receptors with high selectivity, which is explained by a unique receptor binding pocket that consists of the aspartate residue in the third transmembrane helix and other sites in the H1 receptor.1 Upon binding, olopatadine blocks the H1 receptor signaling pathway, inhibiting the release of inflammatory mediators, such as tryptase, prostaglandin D2, TNF-alpha, as well as pro-inflammatory cytokines.10 It also decreases chemotaxis and inhibits eosinophil activation.7 In vitro, olopatadine was shown to inhibit epithelial cell intercellular adhesion molecule-1 (ICAM-1), which promotes the recruitment of migrating pro-inflammatory mediators.3
Target Actions Organism AHistamine H1 receptor antagonistHumans UHistamine H2 receptor antagonistHumans UHistamine H3 receptor antagonistHumans UProtein S100-A1 antagonistHumans UProtein S100-A12 antagonistHumans UProtein S100-B other/unknownHumans UProtein S100-A13 other/unknownHumans UProtein S100-A2 antagonistHumans - Absorption
Ocular administration of olopatadine in healthy subjects resulted in the Cmax of 1.6 ± 0.9 ng/mL, which was reached after about 2.0 hours. The AUC was 9.7 ± 4.4 ngxh/mL.7
The average absolute bioavaiability of intranasal olopatadine is about 57%. Following intranasal administration in healthy subjects, the Cmax of 6.0 ± 8.99 ng/mL at steady-state was reached between 30 minutes to 1 hour after twice daily intranasal administration. The average AUC was 66.0 ± 26.8 ng·h/mL. In patients with seasonal allergic rhinitis, the Cmax of 23.3 ± 6.2 ng/mL at steady-state was reached between 15 minutes and 2 hours post-dosing and the average AUC was 78.0 ± 13.9 ng·h/mL.8
- Volume of distribution
In an open-label study consisting of healthy Chinese subjects receiving oral administration of olopatadine, the mean apparent volume of distribution was 133.83 L.5
- Protein binding
About 55% of total olopatadine is bound to human serum proteins, with serum albumin being the primary protein of binding.8
- Metabolism
Olopatadine undergoes hepatic metabolism in a non-extensive manner.8,9 Based on oral pharmacokinetic studies, there are at least 6 circulating metabolites in human plasma.8 Following topical ocular application of olopatadine, olopatadine N-oxide is formed by metabolism catalyzed by flavin-containing monooxygenase (FMO) 1 and 3 8 and was detected in the plasma after 4 hours post-dosing in less than 10% of the total plasma in half of the patients.7 Mono-desmethyl olopatadine, or N-desmethyl olopatadine, is formed by CYP3A4 8 and may be detected in minimal levels.7
Hover over products below to view reaction partners
- Route of elimination
Olopatadine is mainly eliminated through urinary excretion. Following oral administration, about 70% and 17% of the total dose was recovered in the urine and feces, respectively.8
- Half-life
Following ocular administration, the elimination half-life of olopatadine was 3.4 ± 1.2 hours. In oral pharmacokinetics study, the elimination half-life was reported to be 8 to 12 hours.9
- Clearance
In an open-label study consisting of healthy Chinese subjects receiving oral administration of olopatadine, the mean apparent oral clearance (CL/F) was 23.45 L/h.5
- 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
Based on the findings of an acute toxicity study in animals, the oral LD50 of olopatadine was >1150 mg/kg in mice and >3870 mg/kg in rats.10 The Lowest published toxic dose via the oral route was 20 mg/kg in rat and 0.1 mg/kg in mouse.MSDS
There are no known reports on overdosage following oral, ophthalmic, or intranasal administration of olopatadine. Likely symptoms of antihistamine overdose may include drowsiness in adults and, initially, agitation and restlessness, followed by drowsiness in children. In case of suspected overdose, supportive and symptomatic treatment is recommended.8
- Pathways
Pathway Category Olopatadine H1-Antihistamine Action Drug action - 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.
Drug Interaction Integrate drug-drug
interactions in your softwareOxymetazoline The absorption of Olopatadine can be decreased when combined with Oxymetazoline. - Food Interactions
- No interactions found.
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 Olopatadine hydrochloride 2XG66W44KF 140462-76-6 HVRLZEKDTUEKQH-NOILCQHBSA-N - International/Other Brands
- Alchek (Apex) / Alerchek (Indoco) / Allelock (Dae Woong) / Patanol S (Alcon)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Act Olopatadine 0.1% Solution 0.1 % w/v Ophthalmic Teva Italia S.R.L. 2013-12-06 2021-07-30 Canada 
Act Olopatadine 0.2% Solution 0.2 % w/v Ophthalmic Teva Italia S.R.L. 2014-02-20 2021-07-30 Canada Olopatadine Solution 0.1 % w/v Ophthalmic Sanis Health Inc 2022-07-13 Not applicable Canada Olopatadine 0.2% Solution 0.2 % w/v Ophthalmic Sanis Health Inc 2024-04-08 Not applicable Canada Olopatadine Hydrochloride Nasal Spray 665 ug/1 Nasal Perrigo New York Inc. 2015-04-01 2018-02-01 US 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-olopatadine Solution 0.2 % w/v Ophthalmic Apotex Corporation 2014-04-10 Not applicable Canada Apo-olopatadine Solution 0.1 % Ophthalmic Apotex Corporation 2013-07-26 Not applicable Canada Jamp-olopatadine Solution 0.1 % w/v Ophthalmic Jamp Pharma Corporation 2017-10-06 Not applicable Canada Mint-olopatadine Solution 0.1 % w/v Ophthalmic Mint Pharmaceuticals Inc 2014-07-29 Not applicable Canada Mint-olopatadine 0.2% Solution 0.2 % w/v Ophthalmic Mint Pharmaceuticals Inc 2021-12-17 Not applicable Canada - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Clear Eyes Once Daily Eye Allergy Itch Relief Solution / drops 2 mg/1mL Ophthalmic Prestige Brands Holdings, Inc. 2021-09-15 Not applicable US CVS Eye Allergy Itch Relief Once Daily Solution 2 mg/1mL Ophthalmic CVS Health 2020-09-20 Not applicable US CVS Eye Allergy Itch Relief Twice Daily Solution / drops 1 mg/1mL Ophthalmic CVS Health 2020-09-20 Not applicable US Eye Allergy Itch and Redness Relief Solution / drops 1 mg/1mL Ophthalmic Strategic Sourcing Specialists, LLC 2021-03-15 Not applicable US Eye Allergy Itch and Redness Relief Solution / drops 1 mg/1mL Ophthalmic LEADER/ Cardinal Health 110, Inc. 2021-01-15 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image OFNOL FRESH % 0.1 + %0.15 STERİL OFTALMİK ÇÖZELTİ, 1 ADET Olopatadine hydrochloride (1.11 mg/mL) + Sodium hyaluronate (1.5 mg/mL) Solution Ophthalmic ABDİ İBRAHİM İLAÇ SAN. VE TİC. A.Ş. 2017-07-06 Not applicable Turkey 
Ryaltris Olopatadine hydrochloride (665 mcg / act) + Mometasone furoate monohydrate (25 mcg / act) Spray, metered Nasal Glenmark Specialty Sa 2023-03-17 Not applicable Canada Ryaltris Olopatadine hydrochloride (665 ug/1) + Mometasone furoate monohydrate (25 ug/1) Spray, metered Nasal Hikma Specialty USA Inc. 2022-08-15 Not applicable US
Categories
- ATC Codes
- S01GX09 — Olopatadine
- S01GX — Other antiallergics
- S01G — DECONGESTANTS AND ANTIALLERGICS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- Drug Categories
- Anti-Allergic Agents
- Anti-Inflammatory Agents
- Antiallergic Agents, Excl. Corticosteroids
- Antihistamine Drugs
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Decongestants and Antiallergics
- Decreased Histamine Release
- Dibenzoxepins
- Heterocyclic Compounds, Fused-Ring
- Histamine Agents
- Histamine Antagonists
- Histamine H1 Antagonists
- Histamine H1 Antagonists, Non-Sedating
- Histamine H1 Inhibitors
- Mast Cell Stabilizers
- Nasal Preparations
- Neurotransmitter Agents
- Ophthalmologicals
- P-glycoprotein substrates
- Peripheral Nervous System Agents
- Sensory Organs
- Sensory System Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as dibenzoxepines. These are compounds containing a dibenzoxepine moiety, which consists of two benzene connected by an oxazepine ring.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Benzoxepines
- Sub Class
- Dibenzoxepines
- Direct Parent
- Dibenzoxepines
- Alternative Parents
- Alkyl aryl ethers / Benzenoids / Trialkylamines / Amino acids / Oxacyclic compounds / Monocarboxylic acids and derivatives / Carboxylic acids / Organopnictogen compounds / Organic oxides / Hydrocarbon derivatives show 1 more
- Substituents
- Alkyl aryl ether / Amine / Amino acid / Amino acid or derivatives / Aromatic heteropolycyclic compound / Benzenoid / Carbonyl group / Carboxylic acid / Carboxylic acid derivative / Dibenzoxepine show 12 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- D27V6190PM
- CAS number
- 113806-05-6
- InChI Key
- JBIMVDZLSHOPLA-LSCVHKIXSA-N
- InChI
- InChI=1S/C21H23NO3/c1-22(2)11-5-8-18-17-7-4-3-6-16(17)14-25-20-10-9-15(12-19(18)20)13-21(23)24/h3-4,6-10,12H,5,11,13-14H2,1-2H3,(H,23,24)/b18-8-
- IUPAC Name
- 2-[(2Z)-2-[3-(dimethylamino)propylidene]-9-oxatricyclo[9.4.0.0^{3,8}]pentadeca-1(15),3(8),4,6,11,13-hexaen-5-yl]acetic acid
- SMILES
- CN(C)CC\C=C1\C2=CC=CC=C2COC2=C1C=C(CC(O)=O)C=C2
References
- Synthesis Reference
Thomas Bader, Hans-Ulrich Bichsel, Bruno Gilomen, Imelda Meyer-Wilmes, Mark Sundermeier, "Polymorphic forms of olopatadine hydrochloride and methods for producing olopatadine and salts thereof." U.S. Patent US20070232814, issued October 04, 2007.
US20070232814- General References
- Ohmori K, Hayashi K, Kaise T, Ohshima E, Kobayashi S, Yamazaki T, Mukouyama A: Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride, a new antiallergic drug. Jpn J Pharmacol. 2002 Apr;88(4):379-97. [Article]
- Ohmori K, Hasegawa K, Tamura T, Miyake K, Matsubara M, Masaki S, Karasawa A, Urayama N, Horikoshi K, Kajita J, Hasegawa M, Taniguchi K, Komada T, Kawamoto Y: Properties of olopatadine hydrochloride, a new antiallergic/antihistaminic drug. Arzneimittelforschung. 2004;54(12):809-29. [Article]
- Rosenwasser LJ, O'Brien T, Weyne J: Mast cell stabilization and anti-histamine effects of olopatadine ophthalmic solution: a review of pre-clinical and clinical research. Curr Med Res Opin. 2005 Sep;21(9):1377-87. doi: 10.1185/030079905X56547. [Article]
- Branco ACCC, Yoshikawa FSY, Pietrobon AJ, Sato MN: Role of Histamine in Modulating the Immune Response and Inflammation. Mediators Inflamm. 2018 Aug 27;2018:9524075. doi: 10.1155/2018/9524075. eCollection 2018. [Article]
- Chu NN, Chen WL, Xu HR, Li XN: Pharmacokinetics of orally administered single- and multiple-dose olopatadine in healthy Chinese subjects: an open-label study. Clin Drug Investig. 2009;29(7):451-457. doi: 10.2165/00044011-200929070-00003. [Article]
- Lichtenstein SJ, Abelson MB: Pharmacology, clinical efficacy and safety of olopatadine hydrochloride. Expert Rev Clin Immunol. 2006 May;2(3):341-51. doi: 10.1586/1744666X.2.3.341. [Article]
- FDA Approved Drug Products: PAZEO (olopatadine hydrochloride) ophthalmic solution [Link]
- FDA Approved Drug Products: PATANASE (olopatadine hydrochloride) Nasal Spray [Link]
- Opatanol, INN-olopatadine - European Medicines Agency - Europa EU [Link]
- OLOPATADINE - Product Monograph - Sandoz Canada Inc. [Link]
- Patanol (olopatadine hydrochloride ophthalmic solution) 0.1% - FDA Label [Link]
- FDA Approved Drug Products: Ryaltris (olopatadine hydrochloride/mometasone furoate monohydrate) nasal spray [Link]
- Health Canada Approved Drug Proucts: Ryaltris (olopatadine hydrochloride/mometasone furoate monohydrate) nasal spray [Link]
- External Links
- Human Metabolome Database
- HMDB0014906
- KEGG Compound
- C07789
- PubChem Compound
- 5281071
- PubChem Substance
- 46506025
- ChemSpider
- 4444528
- BindingDB
- 50002096
- 135391
- ChEMBL
- CHEMBL1189432
- ZINC
- ZINC000000001850
- Therapeutic Targets Database
- DAP001062
- PharmGKB
- PA450698
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Olopatadine
- MSDS
- Download (26.4 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Basic Science Allergic Conjunctivitis (AC) 1 somestatus stop reason just information to hide Not Available Completed Diagnostic Allergic Conjunctivitis (AC) / Allergic Rhinitis (AR) 1 somestatus stop reason just information to hide Not Available Completed Treatment Eye allergy 1 somestatus stop reason just information to hide 4 Completed Not Available Allergic Conjunctivitis (AC) 1 somestatus stop reason just information to hide 4 Completed Not Available Seasonal Allergic Rhinitis 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Alcon inc
- Alcon laboratories inc
- Alcon Laboratories, Inc.
- Packagers
- Alcon Laboratories
- A-S Medication Solutions LLC
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Lake Erie Medical and Surgical Supply
- Physicians Total Care Inc.
- Redpharm Drug
- Dosage Forms
Form Route Strength Solution Conjunctival; Ophthalmic 2 mg Solution Ophthalmic 7 mg Solution Ophthalmic 700000 mg Solution Ophthalmic 1.00 mg/ml Solution Ophthalmic 2.00 mg/ml Solution Ophthalmic 0.1 % Solution Conjunctival; Ophthalmic 1 mg Solution Ophthalmic 2.216 mg Solution Ophthalmic 2.000 mg Solution / drops Ophthalmic 1.11 mg Solution Ophthalmic Solution / drops Ophthalmic 0.2 % Solution Ophthalmic 2 mg Spray Nasal 6.65 mg/ml Tablet Oral 5.000 mg Solution / drops Ophthalmic 0.1 % w/v Solution Ophthalmic 1.000 mg Solution Intrasinal; Nasal 600 mg Solution / drops Ophthalmic 1 mg/ml Solution Ophthalmic 100000 mg Solution Intraocular; Ophthalmic 2 mg Solution / drops Ophthalmic 1.0 mg/1mL Solution / drops Ophthalmic 2.0 mg/1mL Solution / drops Ophthalmic 1.11 mg/5ml Powder Not applicable 1 kg/1kg Solution Ophthalmic 2 mg/1mL Solution / drops Ophthalmic 1.11 mg/1mL Spray, metered Nasal 665 ug/100uL Spray Nasal 665 ug/1 Solution Not applicable 2 mg/1mL Tablet, coated Oral 2.5 mg Tablet, coated Oral 5 mg Solution Ophthalmic 1 mg Solution Conjunctival; Ophthalmic 200000 mg Spray Nasal 6.65 % Solution / drops Ophthalmic 1.15 mg Solution / drops Ophthalmic 2 mg/1mL Solution / drops Ophthalmic 0.2 %w/v Solution Ophthalmic 1 mg/1mL Solution Ophthalmic 0.2 % w/v Spray, metered Nasal 600 ug/1 Spray, metered Nasal 665 ug/1 Solution Ophthalmic 1.000 mg Solution / drops Ophthalmic Solution / drops Ophthalmic 1 mg/1mL Solution / drops Ophthalmic 0.1 % Solution Ophthalmic 0.2 % Solution Ophthalmic 1 mg/ml Solution Ophthalmic; Topical 2 mg Solution / drops Ophthalmic 0.2 % w/v Solution Ophthalmic 0.7 % w/v Solution Ophthalmic 7 mg/1mL Solution / drops Ophthalmic 0.7 % Solution / drops Ophthalmic 7 mg/1ml Solution Ophthalmic 0.7 % Solution Ophthalmic; Topical 7.76 mg Solution Ophthalmic 1.108 mg Solution / drops Ophthalmic 5 mg/2.5mL Spray, metered Nasal Solution Ophthalmic 0.1 % w/v Solution Ophthalmic 2.220 mg Solution Conjunctival; Ophthalmic 0.2 g - Prices
Unit description Cost Unit Patanol 0.1% Solution 5ml Bottle 111.2USD bottle Pataday 0.2% eye drops 52.98USD ml Patanol 0.1% eye drops 21.38USD ml Patanase 0.6% nasal spray 3.83USD g DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5116863 No 1992-05-26 2010-12-18 US CA2195094 No 2002-02-26 2016-05-03 Canada CA1337603 No 1995-11-21 2012-11-21 Canada US6995186 Yes 2006-02-07 2024-05-12 US US7402609 Yes 2008-07-22 2022-12-19 US US8399508 Yes 2013-03-19 2023-03-17 US US7977376 Yes 2011-07-12 2023-08-02 US US8791154 No 2014-07-29 2032-05-19 US US5641805 Yes 1997-06-24 2015-12-06 US US9533053 No 2017-01-03 2032-05-19 US US10765686 No 2020-09-08 2034-09-04 US US10758550 No 2020-09-01 2034-09-04 US US10646500 No 2020-05-12 2034-09-04 US US10548907 No 2020-02-04 2034-09-04 US US10016443 No 2018-07-10 2034-09-04 US US10517880 No 2019-12-31 2034-09-04 US US9750754 No 2017-09-05 2034-09-04 US US9078923 No 2015-07-14 2034-09-04 US US9937189 No 2018-04-10 2034-09-04 US US10376526 No 2019-08-13 2034-09-04 US US9370483 No 2016-06-21 2034-09-04 US US10561672 No 2020-02-18 2034-09-04 US US11400101 No 2014-09-04 2034-09-04 US US11679210 No 2018-09-03 2038-09-03 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.0313 mg/mL ALOGPS logP 3.99 ALOGPS logP 0.75 Chemaxon logS -4 ALOGPS pKa (Strongest Acidic) 3.78 Chemaxon pKa (Strongest Basic) 9.76 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 49.77 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 109.55 m3·mol-1 Chemaxon Polarizability 37.44 Å3 Chemaxon Number of Rings 3 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 + 0.9747 Blood Brain Barrier + 0.6925 Caco-2 permeable + 0.7249 P-glycoprotein substrate Substrate 0.8607 P-glycoprotein inhibitor I Inhibitor 0.5948 P-glycoprotein inhibitor II Non-inhibitor 0.8196 Renal organic cation transporter Inhibitor 0.5413 CYP450 2C9 substrate Non-substrate 0.7691 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Substrate 0.7242 CYP450 1A2 substrate Inhibitor 0.7906 CYP450 2C9 inhibitor Non-inhibitor 0.8316 CYP450 2D6 inhibitor Inhibitor 0.6567 CYP450 2C19 inhibitor Non-inhibitor 0.8466 CYP450 3A4 inhibitor Non-inhibitor 0.8222 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8676 Ames test Non AMES toxic 0.8032 Carcinogenicity Non-carcinogens 0.8499 Biodegradation Not ready biodegradable 0.6088 Rat acute toxicity 2.7626 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8082 hERG inhibition (predictor II) Inhibitor 0.5
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 197.8976199 predictedDarkChem Lite v0.1.0 [M-H]- 180.20973 predictedDeepCCS 1.0 (2019) [M+H]+ 198.3578199 predictedDarkChem Lite v0.1.0 [M+H]+ 182.56772 predictedDeepCCS 1.0 (2019) [M+Na]+ 197.8179199 predictedDarkChem Lite v0.1.0 [M+Na]+ 189.47931 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- G-protein-coupled receptor for histamine, a biogenic amine that functions as an immune modulator and a neurotransmitter (PubMed:33828102, PubMed:8280179). Through the H1 receptor, histamine mediates the contraction of smooth muscles and increases capillary permeability due to contraction of terminal venules. Also mediates neurotransmission in the central nervous system and thereby regulates circadian rhythms, emotional and locomotor activities as well as cognitive functions (By similarity)
- Specific Function
- G protein-coupled serotonin receptor activity
- Gene Name
- HRH1
- Uniprot ID
- P35367
- Uniprot Name
- Histamine H1 receptor
- Molecular Weight
- 55783.61 Da
References
- Tamura T, Masaki S, Ohmori K, Karasawa A: Effect of olopatadine and other histamine H1 receptor antagonists on the skin inflammation induced by repeated topical application of oxazolone in mice. Pharmacology. 2005 Dec;75(1):45-52. Epub 2005 Jun 7. [Article]
- Ohmori K, Hayashi K, Kaise T, Ohshima E, Kobayashi S, Yamazaki T, Mukouyama A: Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride, a new antiallergic drug. Jpn J Pharmacol. 2002 Apr;88(4):379-97. [Article]
- Yanni JM, Stephens DJ, Miller ST, Weimer LK, Graff G, Parnell D, Lang LS, Spellman JM, Brady MT, Gamache DA: The in vitro and in vivo ocular pharmacology of olopatadine (AL-4943A), an effective anti-allergic/antihistaminic agent. J Ocul Pharmacol Ther. 1996 Winter;12(4):389-400. [Article]
- Ohmori K, Hasegawa K, Tamura T, Miyake K, Matsubara M, Masaki S, Karasawa A, Urayama N, Horikoshi K, Kajita J, Hasegawa M, Taniguchi K, Komada T, Kawamoto Y: Properties of olopatadine hydrochloride, a new antiallergic/antihistaminic drug. Arzneimittelforschung. 2004;54(12):809-29. [Article]
- Ohmori K, Ikemura T, Kobayashi H, Mukouyama A: [Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride' (olopatadine), an antiallergic drug]. Nihon Yakurigaku Zasshi. 2001 Jul;118(1):51-8. [Article]
- Roland PS, Ryan MW, Wall GM: Olopatadine nasal spray for the treatment of seasonal allergic rhinitis in patients aged 6 years and older. Expert Opin Pharmacother. 2010 Jun;11(9):1559-67. doi: 10.1517/14656566.2010.485609. [Article]
- Kaliner MA, Oppenheimer J, Farrar JR: Comprehensive review of olopatadine: the molecule and its clinical entities. Allergy Asthma Proc. 2010 Mar-Apr;31(2):112-9. doi: 10.2500/aap.2010.31.3317. [Article]
- Roland PS, Marple BF, Wall GM: Olopatadine nasal spray for the treatment of allergic rhinitis. Expert Rev Clin Immunol. 2010 Mar;6(2):197-204. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and differentiation. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase and, through a separate G protein-dependent mechanism, the phosphoinositide/protein kinase (PKC) signaling pathway (By similarity)
- Specific Function
- G protein-coupled serotonin receptor activity
- Gene Name
- HRH2
- Uniprot ID
- P25021
- Uniprot Name
- Histamine H2 receptor
- Molecular Weight
- 40097.65 Da
References
- Rosenwasser LJ, O'Brien T, Weyne J: Mast cell stabilization and anti-histamine effects of olopatadine ophthalmic solution: a review of pre-clinical and clinical research. Curr Med Res Opin. 2005 Sep;21(9):1377-87. doi: 10.1185/030079905X56547. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- The H3 subclass of histamine receptors could mediate the histamine signals in CNS and peripheral nervous system. Signals through the inhibition of adenylate cyclase and displays high constitutive activity (spontaneous activity in the absence of agonist). Agonist stimulation of isoform 3 neither modified adenylate cyclase activity nor induced intracellular calcium mobilization
- Specific Function
- G protein-coupled acetylcholine receptor activity
- Gene Name
- HRH3
- Uniprot ID
- Q9Y5N1
- Uniprot Name
- Histamine H3 receptor
- Molecular Weight
- 48670.81 Da
References
- Rosenwasser LJ, O'Brien T, Weyne J: Mast cell stabilization and anti-histamine effects of olopatadine ophthalmic solution: a review of pre-clinical and clinical research. Curr Med Res Opin. 2005 Sep;21(9):1377-87. doi: 10.1185/030079905X56547. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Small calcium binding protein that plays important roles in several biological processes such as Ca(2+) homeostasis, chondrocyte biology and cardiomyocyte regulation (PubMed:12804600). In response to an increase in intracellular Ca(2+) levels, binds calcium which triggers conformational changes (PubMed:23351007). These changes allow interactions with specific target proteins and modulate their activity (PubMed:22399290). Regulates a network in cardiomyocytes controlling sarcoplasmic reticulum Ca(2+) cycling and mitochondrial function through interaction with the ryanodine receptors RYR1 and RYR2, sarcoplasmic reticulum Ca(2+)-ATPase/ATP2A2 and mitochondrial F1-ATPase (PubMed:12804600). Facilitates diastolic Ca(2+) dissociation and myofilament mechanics in order to improve relaxation during diastole (PubMed:11717446)
- Specific Function
- ATPase binding
- Gene Name
- S100A1
- Uniprot ID
- P23297
- Uniprot Name
- Protein S100-A1
- Molecular Weight
- 10545.755 Da
References
- Okada M, Tokumitsu H, Kubota Y, Kobayashi R: Interaction of S100 proteins with the antiallergic drugs, olopatadine, amlexanox, and cromolyn: identification of putative drug binding sites on S100A1 protein. Biochem Biophys Res Commun. 2002 Apr 12;292(4):1023-30. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- S100A12 is a calcium-, zinc- and copper-binding protein which plays a prominent role in the regulation of inflammatory processes and immune response. Its pro-inflammatory activity involves recruitment of leukocytes, promotion of cytokine and chemokine production, and regulation of leukocyte adhesion and migration. Acts as an alarmin or a danger associated molecular pattern (DAMP) molecule and stimulates innate immune cells via binding to receptor for advanced glycation endproducts (AGER). Binding to AGER activates the MAP-kinase and NF-kappa-B signaling pathways leading to production of pro-inflammatory cytokines and up-regulation of cell adhesion molecules ICAM1 and VCAM1. Acts as a monocyte and mast cell chemoattractant. Can stimulate mast cell degranulation and activation which generates chemokines, histamine and cytokines inducing further leukocyte recruitment to the sites of inflammation. Can inhibit the activity of matrix metalloproteinases; MMP2, MMP3 and MMP9 by chelating Zn(2+) from their active sites. Possesses filariacidal and filariastatic activity. Calcitermin possesses antifungal activity against C.albicans and is also active against E.coli and P.aeruginosa but not L.monocytogenes and S.aureus
- Specific Function
- calcium ion binding
- Gene Name
- S100A12
- Uniprot ID
- P80511
- Uniprot Name
- Protein S100-A12
- Molecular Weight
- 10574.975 Da
References
- Kishimoto K, Kaneko S, Ohmori K, Tamura T, Hasegawa K: Olopatadine suppresses the migration of THP-1 monocytes induced by S100A12 protein. Mediators Inflamm. 2006;2006(1):42726. [Article]
- Okada M, Tokumitsu H, Kubota Y, Kobayashi R: Interaction of S100 proteins with the antiallergic drugs, olopatadine, amlexanox, and cromolyn: identification of putative drug binding sites on S100A1 protein. Biochem Biophys Res Commun. 2002 Apr 12;292(4):1023-30. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Other/unknown
- General Function
- Small zinc- and- and calcium-binding protein that is highly expressed in astrocytes and constitutes one of the most abundant soluble proteins in brain (PubMed:20950652, PubMed:6487634). Weakly binds calcium but binds zinc very tightly-distinct binding sites with different affinities exist for both ions on each monomer (PubMed:20950652, PubMed:6487634). Physiological concentrations of potassium ion antagonize the binding of both divalent cations, especially affecting high-affinity calcium-binding sites (By similarity). Acts as a neurotrophic factor that promotes astrocytosis and axonal proliferation (By similarity). Involved in innervation of thermogenic adipose tissue by acting as an adipocyte-derived neurotrophic factor that promotes sympathetic innervation of adipose tissue (By similarity). Binds to and initiates the activation of STK38 by releasing autoinhibitory intramolecular interactions within the kinase (By similarity). Interaction with AGER after myocardial infarction may play a role in myocyte apoptosis by activating ERK1/2 and p53/TP53 signaling (By similarity). Could assist ATAD3A cytoplasmic processing, preventing aggregation and favoring mitochondrial localization (PubMed:20351179). May mediate calcium-dependent regulation on many physiological processes by interacting with other proteins, such as TPR-containing proteins, and modulating their activity (PubMed:22399290)
- Specific Function
- calcium ion binding
- Gene Name
- S100B
- Uniprot ID
- P04271
- Uniprot Name
- Protein S100-B
- Molecular Weight
- 10712.985 Da
References
- Okada M, Tokumitsu H, Kubota Y, Kobayashi R: Interaction of S100 proteins with the antiallergic drugs, olopatadine, amlexanox, and cromolyn: identification of putative drug binding sites on S100A1 protein. Biochem Biophys Res Commun. 2002 Apr 12;292(4):1023-30. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Other/unknown
- General Function
- Plays a role in the export of proteins that lack a signal peptide and are secreted by an alternative pathway. Binds two calcium ions per subunit. Binds one copper ion. Binding of one copper ion does not interfere with calcium binding. Required for the copper-dependent stress-induced export of IL1A and FGF1. The calcium-free protein binds to lipid vesicles containing phosphatidylserine, but not to vesicles containing phosphatidylcholine (By similarity)
- Specific Function
- calcium ion binding
- Gene Name
- S100A13
- Uniprot ID
- Q99584
- Uniprot Name
- Protein S100-A13
- Molecular Weight
- 11471.095 Da
References
- Okada M, Tokumitsu H, Kubota Y, Kobayashi R: Interaction of S100 proteins with the antiallergic drugs, olopatadine, amlexanox, and cromolyn: identification of putative drug binding sites on S100A1 protein. Biochem Biophys Res Commun. 2002 Apr 12;292(4):1023-30. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- May function as calcium sensor and modulator, contributing to cellular calcium signaling. May function by interacting with other proteins, such as TPR-containing proteins, and indirectly play a role in many physiological processes. May also play a role in suppressing tumor cell growth
- Specific Function
- calcium ion binding
- Gene Name
- S100A2
- Uniprot ID
- P29034
- Uniprot Name
- Protein S100-A2
- Molecular Weight
- 11116.695 Da
References
- Okada M, Tokumitsu H, Kubota Y, Kobayashi R: Interaction of S100 proteins with the antiallergic drugs, olopatadine, amlexanox, and cromolyn: identification of putative drug binding sites on S100A1 protein. Biochem Biophys Res Commun. 2002 Apr 12;292(4):1023-30. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of sterols, steroid hormones, retinoids and fatty acids (PubMed:10681376, PubMed:11093772, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:19965576, PubMed:20702771, PubMed:21490593, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:21490593, PubMed:21576599, PubMed:2732228). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C-16 position (PubMed:11555828, PubMed:12865317, PubMed:14559847). Plays a role in the metabolism of androgens, particularly in oxidative deactivation of testosterone (PubMed:15373842, PubMed:15764715, PubMed:22773874, PubMed:2732228). Metabolizes testosterone to less biologically active 2beta- and 6beta-hydroxytestosterones (PubMed:15373842, PubMed:15764715, PubMed:2732228). Contributes to the formation of hydroxycholesterols (oxysterols), particularly A-ring hydroxylated cholesterol at the C-4beta position, and side chain hydroxylated cholesterol at the C-25 position, likely contributing to cholesterol degradation and bile acid biosynthesis (PubMed:21576599). Catalyzes bisallylic hydroxylation of polyunsaturated fatty acids (PUFA) (PubMed:9435160). Catalyzes the epoxidation of double bonds of PUFA with a preference for the last double bond (PubMed:19965576). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:20702771). Plays a role in the metabolism of retinoids. Displays high catalytic activity for oxidation of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes atRA toward 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Responsible for oxidative metabolism of xenobiotics. Acts as a 2-exo-monooxygenase for plant lipid 1,8-cineole (eucalyptol) (PubMed:11159812). Metabolizes the majority of the administered drugs. Catalyzes sulfoxidation of the anthelmintics albendazole and fenbendazole (PubMed:10759686). Hydroxylates antimalarial drug quinine (PubMed:8968357). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850). Also involved in vitamin D catabolism and calcium homeostasis. Catalyzes the inactivation of the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:29461981)
- Specific Function
- 1,8-cineole 2-exo-monooxygenase activity
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Kajita J, Inano K, Fuse E, Kuwabara T, Kobayashi H: Effects of olopatadine, a new antiallergic agent, on human liver microsomal cytochrome P450 activities. Drug Metab Dispos. 2002 Dec;30(12):1504-11. doi: 10.1124/dmd.30.12.1504. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Broad spectrum monooxygenase that catalyzes the oxygenation of a wide variety of nitrogen- and sulfur-containing compounds including xenobiotics (PubMed:32156684). Catalyzes the S-oxygenation of hypotaurine to produce taurine, an organic osmolyte involved in cell volume regulation as well as a variety of cytoprotective and developmental processes (PubMed:32156684). In vitro, catalyzes the N-oxygenation of trimethylamine (TMA) to produce trimethylamine N-oxide (TMAO) and could therefore participate to the detoxification of this compound that is generated by the action of gut microbiota from dietary precursors such as choline, choline containing compounds, betaine or L-carnitine (By similarity)
- Specific Function
- flavin adenine dinucleotide binding
- Gene Name
- FMO1
- Uniprot ID
- Q01740
- Uniprot Name
- Flavin-containing monooxygenase 1
- Molecular Weight
- 60310.285 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Essential hepatic enzyme that catalyzes the oxygenation of a wide variety of nitrogen- and sulfur-containing compounds including drugs as well as dietary compounds (PubMed:10759686, PubMed:30381441, PubMed:32156684). Plays an important role in the metabolism of trimethylamine (TMA), via the production of trimethylamine N-oxide (TMAO) metabolite (PubMed:9776311). TMA is generated by the action of gut microbiota using dietary precursors such as choline, choline containing compounds, betaine or L-carnitine. By regulating TMAO concentration, FMO3 directly impacts both platelet responsiveness and rate of thrombus formation (PubMed:29981269)
- Specific Function
- albendazole monooxygenase activity
- Gene Name
- FMO3
- Uniprot ID
- P31513
- Uniprot Name
- Flavin-containing monooxygenase 3
- Molecular Weight
- 60032.975 Da
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Binder
- General Function
- Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc (PubMed:19021548). Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity). Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity). Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli (PubMed:6234017). Does not prevent iron uptake by the bacterial siderophore aerobactin (PubMed:6234017)
- Specific Function
- antioxidant activity
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Albumin
- Molecular Weight
- 69365.94 Da
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Translocates drugs and phospholipids across the membrane (PubMed:2897240, PubMed:35970996, PubMed:8898203, PubMed:9038218). Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins (PubMed:8898203). Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells (PubMed:2897240, PubMed:35970996, PubMed:9038218)
- Specific Function
- ABC-type xenobiotic transporter activity
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- ATP-dependent translocase ABCB1
- Molecular Weight
- 141477.255 Da
References
- Mimura N, Nagata Y, Kuwabara T, Kubo N, Fuse E: P-glycoprotein limits the brain penetration of olopatadine hydrochloride, H1-receptor antagonist. Drug Metab Pharmacokinet. 2008;23(2):106-14. [Article]
Drug created at June 13, 2005 13:24 / Updated at October 14, 2024 10:01