Mirabegron
Identification
- Summary
Mirabegron is a beta-3 adrenergic agonist used to treat overactive bladder and neurogenic detrusor overactivity.
- Brand Names
- Myrbetriq
- Generic Name
- Mirabegron
- DrugBank Accession Number
- DB08893
- Background
Mirabegron is a sympathomimetic beta-3 adrenergic receptor agonist used to relax the smooth muscle of the bladder in the treatment of urinary frequency and incontinence. It is unique amongst overactive bladder treatment options in that, unlike other treatments such as solifenacin and darifenacin, it lacks significant antimuscarinic activity,3 which is responsible both for the therapeutic effects of these medications and their broad range of adverse effects. Mirabegron has a comparatively favorable adverse effect profile as compared to other available treatment options, and its complementary mechanism to the antimuscarinics that came before it allows for its use alongside solifenacin in refractory cases.6
Mirabegron first received FDA approval in 2012, under the brand name Myrbetriq, for the treatment of adults with overactive bladder.6 An extended-release granule formulation was subsequently granted approval in March 2021 for the treatment of pediatric patients with neurogenic detrusor overactivity.6 Mirabegron is also used in other jurisdictions across the globe, including Canada,7 the EU,8 and Japan.2
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Mirabegron (DB08893)
- Weight
- Average: 396.506
Monoisotopic: 396.161996722 - Chemical Formula
- C21H24N4O2S
- Synonyms
- Mirabegron
- External IDs
- YM-178
- YM178
Pharmacology
- Indication
Mirabegron is indicated for the treatment of overactive bladder (OAB) - with symptoms of urge urinary incontinence, urgency, and urinary frequency - either alone or in combination with solifenacin.6 It is also indicated for the treatment of neurogenic detrusor overactivity (NDO) in pediatric patients 3 years of age and older and weighing 35kg or more.6
Accelerate your drug discovery research with the industry’s only fully connected ADMET dataset, ideal for:Accelerate your drug discovery research with our fully connected ADMET dataset- Associated Conditions
- Contraindications & Blackbox Warnings
Contraindications & Blackbox WarningsWith our commercial data, access important information on dangerous risks, contraindications, and adverse effects.Our Blackbox Warnings cover Risks, Contraindications, and Adverse Effects- Pharmacodynamics
Mirabegron exerts its pharmacologic effects by forcing bladder smooth muscle to relax, thereby expanding its capacity and relieving urgency. Mirabegron does not appear to adversely affect the mean maximum flow rate or mean detrusor pressure at maximum flow rate in patients with lower urinary tract symptoms and bladder outlet obstruction (BOO), but should be used with in patients with BOO due to reports of significant urinary retention. Furthermore, mirabegron increases both blood pressure and heart rate in a dose-dependent manner and should therefore be used with caution in patients with severely uncontrolled hypertension or others for whom these increases may prove dangerous.6
- Mechanism of action
Mirabegron is a potent and selective agonist of beta-3 adrenergic receptors. The activation of beta-3 receptors relaxes detrusor smooth muscle during the storage phase of the urinary bladder fill-void cycle, which increases the bladder's storage capacity thereby alleviating feelings of urgency and frequency.6
Target Actions Organism ABeta-3 adrenergic receptor agonistHumans UBeta-1 adrenergic receptor agonistHumans - Absorption
The absolute bioavailability of orally administered mirabegron ranges from 29% at a dose of 25 mg to 35% at a dose of 50 mg.6 The Tmax for the extended-release tablet and suspension formulations are approximately 3.5 hours, while the Tmax for the granule formulation is 4-5 hours.6 Both Cmax and AUC increase more than dose proportionally - an increase in dose from 50mg to 100mg results in a 2.9- and 2.6-fold increase in Cmax and AUC, respectively, whereas an increase from 50mg to 200mg results in a 8.4- and 6.5-fold increase in Cmax and AUC, respectively.6
Steady-state concentrations of mirabegron are achieved after approximately 7 days of once-daily administration.6
- Volume of distribution
Following intravenous administration, mirabegron has an apparent steady-state volume of distribution (Vd) of 1670 L indicating extensive distribution.6
- Protein binding
Mirabegron is approximately 71% protein-bound in plasma, primarily to albumin and alpha-1-acid glycoprotein.6
- Metabolism
Mirabegron is extensively metabolized via a number of mechanisms, although unchanged parent drug is still the major circulating component following oral administration.6 Presumed metabolic pathways and their resultant metabolites include amide hydrolysis (M5, M16, M17), glucuronidation (mirabegron O-glucuronide, N-glucuronide, N-carbamoylglucuronide, M12), and secondary amine oxidation or dealkylation (M8, M9, M15), amongst others.4 The enzymes responsible for the oxidative metabolism of mirabegron are thought to be CYP3A4 and CYP2D6,6 while the UDP-glucuronosyltransferases responsible for conjugation reactions have been identified as UGT2B7, UGT1A3, and UGT1A8.5 Other enzymes that may be involved in the metabolism of mirabegron include butylcholinesterase and possibly alcohol dehydrogenase.6
Hover over products below to view reaction partners
- Route of elimination
Of a 160mg radiolabeled dose administered to healthy volunteers, approximately 55% of the radioactivity was recovered in the urine and 34% in the feces. Approximately 25% of unchanged mirabegron was recovered in the urine while 0% was recovered in the feces.6
Renal elimination is achieved primarily via active tubular secretion with some contribution by glomerular filtration.6
- Half-life
The mean terminal elimination half-life of mirabegron in adults being treated for overactive bladder is approximately 50 hours.6 In pediatric patients receiving the granule formulation for the treatment of neurogenic detrusor overactivity, the mean terminal elimination half-life is approximately 26-31 hours.6
- Clearance
Total plasma clearance following intravenous administration is approximately 57 L/h, with renal clearance accounting for roughly 25% at approximately 13 L/h.6
- Adverse Effects
Reduce medical errorsand improve treatment outcomes with our comprehensive & structured data on drug adverse effects.Reduce medical errors & improve treatment outcomes with our adverse effects data- Toxicity
At doses of up to 400mg in healthy volunteers (~8x the recommended maximum), reported symptoms of overdose included palpitations and increased heart rate. Symptoms of chronic overdosage are similar in presentation and may also include a rise in systolic blood pressure. In cases of overdosage, employ standard symptomatic and supportive measures in addition to ECG monitoring.6
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Mirabegron which could result in a higher serum level. Abametapir The serum concentration of Mirabegron can be increased when it is combined with Abametapir. Abatacept The metabolism of Mirabegron can be increased when combined with Abatacept. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Mirabegron. Abiraterone The metabolism of Mirabegron can be decreased when combined with Abiraterone. Acebutolol The serum concentration of Mirabegron can be increased when it is combined with Acebutolol. Aceclofenac Aceclofenac may decrease the excretion rate of Mirabegron which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Mirabegron which could result in a higher serum level. Acetaminophen The serum concentration of Mirabegron can be increased when it is combined with Acetaminophen. Acetazolamide Acetazolamide may increase the excretion rate of Mirabegron which could result in a lower serum level and potentially a reduction in efficacy. 
Improve patient outcomesBuild effective decision support tools with the industry’s most comprehensive drug-drug interaction checker.Learn more - Food Interactions
- Take with food. While adults may take mirabegron with or without food, prescribing information recommends that children always co-administer mirabegron with food.
Products
Comprehensive & structured drug product infoFrom application numbers to product codes, connect different identifiers through our commercial datasets.Easily connect various identifiers back to our datasets- Product Images
- International/Other Brands
- Betanis / Metmiga
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Betmiga Tablet, extended release 25 mg Oral Astellas Pharma Europe Bv 2016-09-08 Not applicable EU 
Betmiga Tablet, extended release 50 mg Oral Astellas Pharma Europe Bv 2016-09-08 Not applicable EU Betmiga Tablet, extended release 25 mg Oral Astellas Pharma Europe Bv 2016-09-08 Not applicable EU Betmiga Tablet, extended release 50 mg Oral Astellas Pharma Europe Bv 2016-09-08 Not applicable EU Betmiga Tablet, extended release 25 mg Oral Astellas Pharma Europe Bv 2016-09-08 Not applicable EU Betmiga Tablet, extended release 50 mg Oral Astellas Pharma Europe Bv 2016-09-08 Not applicable EU Betmiga Tablet, extended release 25 mg Oral Astellas Pharma Europe Bv 2016-09-08 Not applicable EU Betmiga Tablet, extended release 50 mg Oral Astellas Pharma Europe Bv 2016-09-08 Not applicable EU Betmiga Tablet, extended release 25 mg Oral Astellas Pharma Europe Bv 2016-09-08 Not applicable EU Betmiga Tablet, extended release 50 mg Oral Astellas Pharma Europe Bv 2016-09-08 Not applicable EU
Categories
- ATC Codes
- G04BD12 — Mirabegron
- Drug Categories
- Adrenergic Agents
- Adrenergic Agonists
- Adrenergic beta-3 Receptor Agonists
- Adrenergic beta-Agonists
- Agents producing tachycardia
- Agents that produce hypertension
- Amides
- Amines
- Anilides
- Aniline Compounds
- Cholinesterase substrates
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (moderate)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Drugs for Urinary Frequency and Incontinence
- Drugs that are Mainly Renally Excreted
- Genito Urinary System and Sex Hormones
- OCT1 substrates
- OCT2 Substrates
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Potential QTc-Prolonging Agents
- QTc Prolonging Agents
- Selective Beta 3-adrenergic Agonists
- Sulfur Compounds
- UGT1A3 substrates
- UGT2B7 substrates
- Urological Agents
- Urologicals
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as anilides. These are organic heterocyclic compounds derived from oxoacids RkE(=O)l(OH)m (l not 0) by replacing an OH group by the NHPh group or derivative formed by ring substitution.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Anilides
- Direct Parent
- Anilides
- Alternative Parents
- Phenethylamines / N-arylamides / 2,4-disubstituted thiazoles / Aralkylamines / 2-amino-1,3-thiazoles / Heteroaromatic compounds / 1,2-aminoalcohols / Amino acids and derivatives / Secondary alcohols / Secondary carboxylic acid amides show 8 more
- Substituents
- 1,2-aminoalcohol / 1,3-thiazol-2-amine / 2,4-disubstituted 1,3-thiazole / Alcohol / Amine / Amino acid or derivatives / Anilide / Aralkylamine / Aromatic alcohol / Aromatic heteromonocyclic compound show 22 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- monocarboxylic acid amide, 1,3-thiazole, aromatic amide, ethanolamines (CHEBI:65349)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- MVR3JL3B2V
- CAS number
- 223673-61-8
- InChI Key
- PBAPPPCECJKMCM-IBGZPJMESA-N
- InChI
- InChI=1S/C21H24N4O2S/c22-21-25-18(14-28-21)12-20(27)24-17-8-6-15(7-9-17)10-11-23-13-19(26)16-4-2-1-3-5-16/h1-9,14,19,23,26H,10-13H2,(H2,22,25)(H,24,27)/t19-/m0/s1
- IUPAC Name
- 2-(2-amino-1,3-thiazol-4-yl)-N-[4-(2-{[(2R)-2-hydroxy-2-phenylethyl]amino}ethyl)phenyl]acetamide
- SMILES
- NC1=NC(CC(=O)NC2=CC=C(CCNC[C@H](O)C3=CC=CC=C3)C=C2)=CS1
References
- General References
- Takasu T, Ukai M, Sato S, Matsui T, Nagase I, Maruyama T, Sasamata M, Miyata K, Uchida H, Yamaguchi O: Effect of (R)-2-(2-aminothiazol-4-yl)-4'-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl} acetanilide (YM178), a novel selective beta3-adrenoceptor agonist, on bladder function. J Pharmacol Exp Ther. 2007 May;321(2):642-7. Epub 2007 Feb 9. [Article]
- Kashyap M, Tyagi P: The pharmacokinetic evaluation of mirabegron as an overactive bladder therapy option. Expert Opin Drug Metab Toxicol. 2013 May;9(5):617-27. doi: 10.1517/17425255.2013.786700. Epub 2013 Apr 4. [Article]
- Dawood O, El-Zawahry A: Mirabegron . [Article]
- Takusagawa S, van Lier JJ, Suzuki K, Nagata M, Meijer J, Krauwinkel W, Schaddelee M, Sekiguchi M, Miyashita A, Iwatsubo T, van Gelderen M, Usui T: Absorption, metabolism and excretion of [(14)C]mirabegron (YM178), a potent and selective beta(3)-adrenoceptor agonist, after oral administration to healthy male volunteers. Drug Metab Dispos. 2012 Apr;40(4):815-24. doi: 10.1124/dmd.111.043588. Epub 2012 Jan 23. [Article]
- Konishi K, Tenmizu D, Takusagawa S: Identification of Uridine 5'-Diphosphate-Glucuronosyltransferases Responsible for the Glucuronidation of Mirabegron, a Potent and Selective beta3-Adrenoceptor Agonist, in Human Liver Microsomes. Eur J Drug Metab Pharmacokinet. 2018 Jun;43(3):301-309. doi: 10.1007/s13318-017-0450-x. [Article]
- FDA Approved Drug Products: Myrbetriq (mirabegron) extended-release tablets/granules for oral use [Link]
- Health Canada Product Monograph: Myrbetriq (mirabegron) extended-release tablets [Link]
- EMA Summary of Product Characteristics: Betmiga (mirabegron) prolonged-release tablets [Link]
- External Links
- KEGG Drug
- D09535
- PubChem Compound
- 9865528
- PubChem Substance
- 175427137
- ChemSpider
- 8041219
- 1300786
- ChEBI
- 65349
- ChEMBL
- CHEMBL2095212
- ZINC
- ZINC000001996784
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Mirabegron
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Not Available Healthy Volunteers / Pharmacokinetics of Mirabegron and Tolterodine 1 4 Completed Basic Science Food Effect / Healthy Chinese Subjects / Pharmacokinetics of Mirabegron 1 4 Completed Treatment Benign Prostatic Hyperplasia (BPH) / Urinary Bladder, Overactive 1 4 Completed Treatment Disseminated Sclerosis 1 4 Completed Treatment Impaired Cognition / Parkinson's Disease (PD) / Urinary Bladder, Overactive 1 4 Completed Treatment Parkinson's Disease (PD) 1 4 Completed Treatment Urinary Bladder, Overactive 8 4 Completed Treatment Urinary Urge Incontinence 1 4 Not Yet Recruiting Treatment Benign Prostatic Hyperplasia (BPH) / Urinary Bladder, Overactive 1 4 Not Yet Recruiting Treatment Sjögren's Syndrome / Urinary Bladder, Overactive 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, extended release Oral Tablet, extended release Oral 25 mg Tablet, film coated Oral Tablet, extended release Oral 50 mg Granule, for suspension, extended release Oral 8 mg/1mL Tablet, film coated, extended release Oral 25 mg/1 Tablet, film coated, extended release Oral 50 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2305802 No 2008-11-18 2018-10-15 Canada 
CA2464068 No 2007-10-16 2022-10-29 Canada CA2503570 No 2023-11-04 2011-04-19 Canada USRE44872 Yes 2014-04-29 2024-05-04 US 
US7750029 No 2010-07-06 2023-12-18 US US6346532 Yes 2002-02-12 2022-09-27 US US8835474 Yes 2014-09-16 2024-05-04 US US6562375 No 2003-05-13 2020-08-01 US US7982049 Yes 2011-07-19 2024-05-04 US US7342117 Yes 2008-03-11 2024-05-04 US US8772315 Yes 2014-07-08 2029-04-30 US US10842780 Yes 2010-03-28 2030-03-28 US US10058536 No 2016-03-31 2036-03-31 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility 0.082 mg/mL https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/202611s017lbl.pdf - Predicted Properties
Property Value Source Water Solubility 0.00412 mg/mL ALOGPS logP 2.2 ALOGPS logP 2.89 ChemAxon logS -5 ALOGPS pKa (Strongest Acidic) 13.84 ChemAxon pKa (Strongest Basic) 9.62 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 5 ChemAxon Hydrogen Donor Count 4 ChemAxon Polar Surface Area 100.27 Å2 ChemAxon Rotatable Bond Count 9 ChemAxon Refractivity 113.23 m3·mol-1 ChemAxon Polarizability 44.2 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 Yes ChemAxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9398 Blood Brain Barrier + 0.8115 Caco-2 permeable - 0.6462 P-glycoprotein substrate Substrate 0.5567 P-glycoprotein inhibitor I Non-inhibitor 0.8492 P-glycoprotein inhibitor II Non-inhibitor 0.8487 Renal organic cation transporter Non-inhibitor 0.7223 CYP450 2C9 substrate Non-substrate 0.7656 CYP450 2D6 substrate Non-substrate 0.7786 CYP450 3A4 substrate Non-substrate 0.641 CYP450 1A2 substrate Non-inhibitor 0.5904 CYP450 2C9 inhibitor Inhibitor 0.6156 CYP450 2D6 inhibitor Non-inhibitor 0.8873 CYP450 2C19 inhibitor Non-inhibitor 0.574 CYP450 3A4 inhibitor Inhibitor 0.5223 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.5711 Ames test Non AMES toxic 0.6422 Carcinogenicity Non-carcinogens 0.8972 Biodegradation Not ready biodegradable 0.5977 Rat acute toxicity 2.4527 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9094 hERG inhibition (predictor II) Inhibitor 0.567
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS Not Available MS/MS Spectrum - , positive LC-MS/MS splash10-004j-0429000000-a1fa6e47b60253c53578
Targets
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with our fully connected ADMET & drug target dataset.
Accelerate your drug discovery research with our ADMET & drug target dataset
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Protein homodimerization activity
- Specific Function
- Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. Beta-3 is involved in the regulation of lipolysis and thermogenesis.
- Gene Name
- ADRB3
- Uniprot ID
- P13945
- Uniprot Name
- Beta-3 adrenergic receptor
- Molecular Weight
- 43518.615 Da
References
- Kashyap M, Tyagi P: The pharmacokinetic evaluation of mirabegron as an overactive bladder therapy option. Expert Opin Drug Metab Toxicol. 2013 May;9(5):617-27. doi: 10.1517/17425255.2013.786700. Epub 2013 Apr 4. [Article]
- FDA Approved Drug Products: Myrbetriq (mirabegron) extended-release tablets/granules for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Receptor signaling protein activity
- Specific Function
- Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately e...
- Gene Name
- ADRB1
- Uniprot ID
- P08588
- Uniprot Name
- Beta-1 adrenergic receptor
- Molecular Weight
- 51322.1 Da
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Lee J, Moy S, Meijer J, Krauwinkel W, Sawamoto T, Kerbusch V, Kowalski D, Roy M, Marion A, Takusagawa S, van Gelderen M, Keirns J: Role of cytochrome p450 isoenzymes 3A and 2D6 in the in vivo metabolism of mirabegron, a beta3-adrenoceptor agonist. Clin Drug Investig. 2013 Jun;33(6):429-40. doi: 10.1007/s40261-013-0084-y. [Article]
- Takusagawa S, Yajima K, Miyashita A, Uehara S, Iwatsubo T, Usui T: Identification of human cytochrome P450 isoforms and esterases involved in the metabolism of mirabegron, a potent and selective beta3-adrenoceptor agonist. Xenobiotica. 2012 Oct;42(10):957-67. doi: 10.3109/00498254.2012.675095. Epub 2012 Apr 18. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Lee J, Moy S, Meijer J, Krauwinkel W, Sawamoto T, Kerbusch V, Kowalski D, Roy M, Marion A, Takusagawa S, van Gelderen M, Keirns J: Role of cytochrome p450 isoenzymes 3A and 2D6 in the in vivo metabolism of mirabegron, a beta3-adrenoceptor agonist. Clin Drug Investig. 2013 Jun;33(6):429-40. doi: 10.1007/s40261-013-0084-y. [Article]
- Takusagawa S, Yajima K, Miyashita A, Uehara S, Iwatsubo T, Usui T: Identification of human cytochrome P450 isoforms and esterases involved in the metabolism of mirabegron, a potent and selective beta3-adrenoceptor agonist. Xenobiotica. 2012 Oct;42(10):957-67. doi: 10.3109/00498254.2012.675095. Epub 2012 Apr 18. [Article]
- FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Identical protein binding
- Specific Function
- Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
- Gene Name
- BCHE
- Uniprot ID
- P06276
- Uniprot Name
- Cholinesterase
- Molecular Weight
- 68417.575 Da
References
- Takusagawa S, Yajima K, Miyashita A, Uehara S, Iwatsubo T, Usui T: Identification of human cytochrome P450 isoforms and esterases involved in the metabolism of mirabegron, a potent and selective beta3-adrenoceptor agonist. Xenobiotica. 2012 Oct;42(10):957-67. doi: 10.3109/00498254.2012.675095. Epub 2012 Apr 18. [Article]
- FDA Approved Drug Products: Myrbetriq (mirabegron) extended-release tablets/granules for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Glucuronosyltransferase activity
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol su...
- Gene Name
- UGT2B7
- Uniprot ID
- P16662
- Uniprot Name
- UDP-glucuronosyltransferase 2B7
- Molecular Weight
- 60694.12 Da
References
- Konishi K, Tenmizu D, Takusagawa S: Identification of Uridine 5'-Diphosphate-Glucuronosyltransferases Responsible for the Glucuronidation of Mirabegron, a Potent and Selective beta3-Adrenoceptor Agonist, in Human Liver Microsomes. Eur J Drug Metab Pharmacokinet. 2018 Jun;43(3):301-309. doi: 10.1007/s13318-017-0450-x. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Retinoic acid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
- Gene Name
- UGT1A3
- Uniprot ID
- P35503
- Uniprot Name
- UDP-glucuronosyltransferase 1-3
- Molecular Weight
- 60337.835 Da
References
- Konishi K, Tenmizu D, Takusagawa S: Identification of Uridine 5'-Diphosphate-Glucuronosyltransferases Responsible for the Glucuronidation of Mirabegron, a Potent and Selective beta3-Adrenoceptor Agonist, in Human Liver Microsomes. Eur J Drug Metab Pharmacokinet. 2018 Jun;43(3):301-309. doi: 10.1007/s13318-017-0450-x. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
- Gene Name
- UGT1A8
- Uniprot ID
- Q9HAW9
- Uniprot Name
- UDP-glucuronosyltransferase 1-8
- Molecular Weight
- 59741.035 Da
References
- Konishi K, Tenmizu D, Takusagawa S: Identification of Uridine 5'-Diphosphate-Glucuronosyltransferases Responsible for the Glucuronidation of Mirabegron, a Potent and Selective beta3-Adrenoceptor Agonist, in Human Liver Microsomes. Eur J Drug Metab Pharmacokinet. 2018 Jun;43(3):301-309. doi: 10.1007/s13318-017-0450-x. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- FDA Approved Drug Products: Myrbetriq (mirabegron) extended-release tablets/granules for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Binder
- General Function
- Not Available
- Specific Function
- Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
- Gene Name
- ORM1
- Uniprot ID
- P02763
- Uniprot Name
- Alpha-1-acid glycoprotein 1
- Molecular Weight
- 23511.38 Da
References
- FDA Approved Drug Products: Myrbetriq (mirabegron) extended-release tablets/granules for oral use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- Curator comments
- Mirabegron inhibited P-gp-mediated drug transport at high concentrations, according to the FDA Label.
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Takusagawa S, Ushigome F, Nemoto H, Takahashi Y, Li Q, Kerbusch V, Miyashita A, Iwatsubo T, Usui T: Intestinal absorption mechanism of mirabegron, a potent and selective beta(3)-adrenoceptor agonist: involvement of human efflux and/or influx transport systems. Mol Pharm. 2013 May 6;10(5):1783-94. doi: 10.1021/mp300582s. Epub 2013 Apr 24. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
- Gene Name
- SLCO1A2
- Uniprot ID
- P46721
- Uniprot Name
- Solute carrier organic anion transporter family member 1A2
- Molecular Weight
- 74144.105 Da
References
- Takusagawa S, Ushigome F, Nemoto H, Takahashi Y, Li Q, Kerbusch V, Miyashita A, Iwatsubo T, Usui T: Intestinal absorption mechanism of mirabegron, a potent and selective beta(3)-adrenoceptor agonist: involvement of human efflux and/or influx transport systems. Mol Pharm. 2013 May 6;10(5):1783-94. doi: 10.1021/mp300582s. Epub 2013 Apr 24. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Secondary active organic cation transmembrane transporter activity
- Specific Function
- Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
- Gene Name
- SLC22A1
- Uniprot ID
- O15245
- Uniprot Name
- Solute carrier family 22 member 1
- Molecular Weight
- 61153.345 Da
References
- FDA Approved Drug Products: Myrbetriq (mirabegron) extended-release tablets/granules for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Quaternary ammonium group transmembrane transporter activity
- Specific Function
- Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
- Gene Name
- SLC22A2
- Uniprot ID
- O15244
- Uniprot Name
- Solute carrier family 22 member 2
- Molecular Weight
- 62579.99 Da
References
- FDA Approved Drug Products: Myrbetriq (mirabegron) extended-release tablets/granules for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Toxin transporter activity
- Specific Function
- Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
- Gene Name
- SLC22A3
- Uniprot ID
- O75751
- Uniprot Name
- Solute carrier family 22 member 3
- Molecular Weight
- 61279.485 Da
References
- FDA Approved Drug Products: Myrbetriq (mirabegron) extended-release tablets/granules for oral use [Link]
Drug created on May 31, 2013 05:44 / Updated on August 05, 2021 19:41