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Identification
NameMirabegron
Accession NumberDB08893
TypeSmall Molecule
GroupsApproved
Description

Mirabegron is a beta-3 adrenergic receptor agonist for the management of overactive bladder. It is an alternative to antimuscarinic drugs for this indication. FDA approved on June 28, 2012.

Structure
Thumb
Synonyms
Myrbetriq
External Identifiers
  • YM-178
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Myrbetriqtablet, film coated, extended release25 mg/1oralAstellas Pharma US, Inc.2012-06-28Not applicableUs
Myrbetriqtablet, film coated, extended release25 mg/1oralAvera Mc Kennan Hospital2015-03-23Not applicableUs
Myrbetriqtablet (extended-release)50 mgoralAstellas Pharma Canada Inc2013-03-28Not applicableCanada
Myrbetriqtablet (extended-release)25 mgoralAstellas Pharma Canada Inc2013-03-28Not applicableCanada
Myrbetriqtablet, film coated, extended release50 mg/1oralAstellas Pharma US, Inc.2012-06-28Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
BetanisNot Available
Metmiga Not Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIMVR3JL3B2V
CAS number223673-61-8
WeightAverage: 396.506
Monoisotopic: 396.161996722
Chemical FormulaC21H24N4O2S
InChI KeyInChIKey=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[[email protected]](O)C3=CC=CC=C3)C=C2)=CS1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as n-arylamides. These are organic compounds that contain a carboxamide group that is N-linked to a aryl group. They have the generic structure RC(=O)N(R')H, R = organyl group and R'= aryl group.
KingdomOrganic compounds
Super ClassOrganonitrogen compounds
ClassN-arylamides
Sub ClassNot Available
Direct ParentN-arylamides
Alternative Parents
Substituents
  • N-arylamide
  • Phenethylamine
  • Aralkylamine
  • 2,4-disubstituted 1,3-thiazole
  • Benzenoid
  • Primary aromatic amine
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Thiazole
  • Azole
  • Secondary carboxylic acid amide
  • Secondary alcohol
  • Carboxamide group
  • 1,2-aminoalcohol
  • Azacycle
  • Organoheterocyclic compound
  • Secondary amine
  • Secondary aliphatic amine
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Aromatic alcohol
  • Primary amine
  • Organooxygen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationMirabegron is a beta-3 adrenergic agonist indicated for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency.
PharmacodynamicsMirabegron has little effect on the mean maximum flow rate or mean detrusor pressure at maximum flow rate in patients with lower urinary tract symptoms and bladder outlet obstruction. Furthermore, mirabegron increases blood pressure in a dose dependent manner. However, this effect is reversible when mirabegron is discontinued. Mirabegron also increases heart rate in a dose dependent manner. The dose in which half-maximal efficacy is demonstrated is 25 mg. Comparatively, the dose in which maximal efficacy is demonstrated is 100 mg.
Mechanism of actionMirabegron is a potent and selective agonist for beta-3 adrenergic receptors. Once beta-3 receptors are activated, the detrusor smooth muscle relaxes to allow for a larger bladder capacity. At higher doses (200 mg), there is a potential for mirabegron to activate beta-1 and beta-2 adrenergic receptors.
Related Articles
AbsorptionThe absolute bioavailability increases from 29% at a dose of 25 mg to 35% at a dose of 50 mg. Mean Cmax and AUC increase more than dose proportionally. This relationship is more apparent at doses above 50 mg. Females generally have a lower magnitude of increase of Cmax and AUCtau compared to males when doses of mirabegron doubles or quadruples. Steady state concentrations are achieved within 7 days of once daily dosing with mirabegron. After once daily administration, plasma exposure of mirabegron at steady state is approximately double that seen after a single dose. Tmax, oral dose, healthy subjects= 3.5 hours;
Volume of distribution

Vd, steady state, IV dose = 1670 L. This high value suggests that mirabegron is extensively distributed in the body.

Protein binding71% bound to plasma proteins. It binds to albumin and alpha-1-acid glycoprotein with moderate affinity.
Metabolism

Mirabegron is metabolized via multiple pathways involving dealkylation, oxidation, (direct) glucuronidation, and amide hydrolysis. The major circulating entity is mirabegron. Two major and inactive metabolites (phase 2 glucuronides) are produced. Although mirabegron is a substrate for CYP2D6 and CYP3A4, its role in the elimination of the drug is limited. Studies also suggest that CYP3A4 is the main enzyme that facilitates the oxidative metabolism of the drug. Furthermore, butylcholinesterase, uridine diphospho-glucuronosyltransferases (UGT), and possibly alcohol dehydrogenase may be involved with the metabolism of mirabegron.

Route of eliminationMirabegron is eliminated via urine (radiolabeled drug: 55%; unchanged drug: ~25%) and feces (radiolabeled drug: 34%; unchanged drug: 0%). Renal elimination of mirabegron is primarily through active tubular secretion and glomerular filtration. Extent of elimination via urine is dose-dependent.
Half lifeTerminal elimination half-life = 50 hours
Clearance

Total body clearance (CLtot), IV dose = 57 L/h;
Renal clearance (CLR) = 13 L/h

ToxicityMost commonly reported adverse reactions (> 2% and > placebo) were hypertension, nasopharyngitis, urinary tract infection and headache
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9398
Blood Brain Barrier+0.8115
Caco-2 permeable-0.6462
P-glycoprotein substrateSubstrate0.5567
P-glycoprotein inhibitor INon-inhibitor0.8492
P-glycoprotein inhibitor IINon-inhibitor0.8487
Renal organic cation transporterNon-inhibitor0.7223
CYP450 2C9 substrateNon-substrate0.7656
CYP450 2D6 substrateNon-substrate0.7786
CYP450 3A4 substrateNon-substrate0.641
CYP450 1A2 substrateNon-inhibitor0.5904
CYP450 2C9 inhibitorInhibitor0.6156
CYP450 2D6 inhibitorNon-inhibitor0.8873
CYP450 2C19 inhibitorNon-inhibitor0.574
CYP450 3A4 inhibitorInhibitor0.5223
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5711
Ames testNon AMES toxic0.6422
CarcinogenicityNon-carcinogens0.8972
BiodegradationNot ready biodegradable0.5977
Rat acute toxicity2.4527 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9094
hERG inhibition (predictor II)Inhibitor0.567
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tablet (extended-release)oral25 mg
Tablet (extended-release)oral50 mg
Tablet, film coated, extended releaseoral25 mg/1
Tablet, film coated, extended releaseoral50 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2305802 No2008-11-182018-10-15Canada
CA2464068 No2007-10-162022-10-29Canada
CA2503570 No2023-11-042011-04-19Canada
US6346532 No1998-10-152018-10-15Us
US6562375 No2000-08-012020-08-01Us
US7342117 No2003-11-042023-11-04Us
US7750029 No2003-12-182023-12-18Us
US7982049 No2003-11-042023-11-04Us
US8835474 No2003-11-042023-11-04Us
USRE44872 No2003-12-182023-12-18Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityInsoluble FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.00412 mg/mLALOGPS
logP2.2ALOGPS
logP2.89ChemAxon
logS-5ALOGPS
pKa (Strongest Acidic)13.84ChemAxon
pKa (Strongest Basic)9.62ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area100.27 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity113.23 m3·mol-1ChemAxon
Polarizability44.2 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General References
  1. 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. [PubMed:23550899 ]
External Links
ATC CodesG04BD12
AHFS Codes
  • 86:12
PDB EntriesNot Available
FDA labelDownload (510 KB)
MSDSDownload (481 KB)
Interactions
Drug Interactions
Drug
AclidiniumThe risk or severity of adverse effects can be increased when Aclidinium is combined with Mirabegron.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Mirabegron.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Mirabegron.
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Mirabegron.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Mirabegron.
AtropineThe risk or severity of adverse effects can be increased when Atropine is combined with Mirabegron.
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with Mirabegron.
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Mirabegron.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Mirabegron.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Mirabegron.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Mirabegron.
BrompheniramineThe risk or severity of adverse effects can be increased when Brompheniramine is combined with Mirabegron.
CarbinoxamineThe risk or severity of adverse effects can be increased when Carbinoxamine is combined with Mirabegron.
CetirizineThe risk or severity of adverse effects can be increased when Cetirizine is combined with Mirabegron.
ChlorphenamineThe risk or severity of adverse effects can be increased when Chlorphenamine is combined with Mirabegron.
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Mirabegron.
CitalopramMirabegron may increase the QTc-prolonging activities of Citalopram.
ClemastineThe risk or severity of adverse effects can be increased when Clemastine is combined with Mirabegron.
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Mirabegron.
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Mirabegron.
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Mirabegron.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Mirabegron.
CyclizineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Mirabegron.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Mirabegron.
CyclopentolateThe risk or severity of adverse effects can be increased when Cyclopentolate is combined with Mirabegron.
CyproheptadineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Mirabegron.
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Mirabegron.
DarifenacinThe risk or severity of adverse effects can be increased when Darifenacin is combined with Mirabegron.
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Mirabegron.
DesloratadineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Mirabegron.
Dexchlorpheniramine maleateThe risk or severity of adverse effects can be increased when Dexchlorpheniramine maleate is combined with Mirabegron.
DicyclomineThe risk or severity of adverse effects can be increased when Dicyclomine is combined with Mirabegron.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Mirabegron.
DimenhydrinateThe risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Mirabegron.
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Mirabegron.
DofetilideMirabegron may increase the QTc-prolonging activities of Dofetilide.
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Mirabegron.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Mirabegron.
DoxylamineThe risk or severity of adverse effects can be increased when Doxylamine is combined with Mirabegron.
DroperidolThe risk or severity of adverse effects can be increased when Droperidol is combined with Mirabegron.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Mirabegron.
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Mirabegron.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Mirabegron.
FesoterodineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Mirabegron.
FexofenadineThe risk or severity of adverse effects can be increased when Fexofenadine is combined with Mirabegron.
FlavoxateThe risk or severity of adverse effects can be increased when Flavoxate is combined with Mirabegron.
FlecainideThe serum concentration of Flecainide can be increased when it is combined with Mirabegron.
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Mirabegron.
FluvoxamineThe metabolism of Fluvoxamine can be decreased when combined with Mirabegron.
GlycopyrroniumThe risk or severity of adverse effects can be increased when Glycopyrrolate is combined with Mirabegron.
GoserelinMirabegron may increase the QTc-prolonging activities of Goserelin.
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Mirabegron.
HomatropineThe risk or severity of adverse effects can be increased when Homatropine is combined with Mirabegron.
HydroxyzineThe risk or severity of adverse effects can be increased when Hydroxyzine is combined with Mirabegron.
HyoscyamineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Mirabegron.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Mirabegron.
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Mirabegron.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Mirabegron.
KetoconazoleThe serum concentration of Mirabegron can be increased when it is combined with Ketoconazole.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Mirabegron.
LeuprolideMirabegron may increase the QTc-prolonging activities of Leuprolide.
LevocabastineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Mirabegron.
LevocetirizineThe risk or severity of adverse effects can be increased when Levocetirizine is combined with Mirabegron.
LoratadineThe risk or severity of adverse effects can be increased when Loratadine is combined with Mirabegron.
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Mirabegron.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Mirabegron.
MeclizineThe risk or severity of adverse effects can be increased when Meclizine is combined with Mirabegron.
MepenzolateThe risk or severity of adverse effects can be increased when Mepenzolate is combined with Mirabegron.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Mirabegron.
MethscopolamineThe risk or severity of adverse effects can be increased when Methscopolamine is combined with Mirabegron.
MetoprololMirabegron may decrease the antihypertensive activities of Metoprolol.
MifepristoneMifepristone may increase the QTc-prolonging activities of Mirabegron.
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Mirabegron.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Mirabegron.
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Mirabegron.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Mirabegron.
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Mirabegron.
OlopatadineThe risk or severity of adverse effects can be increased when Olopatadine is combined with Mirabegron.
OrphenadrineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Mirabegron.
OxybutyninThe risk or severity of adverse effects can be increased when Oxybutynin is combined with Mirabegron.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Mirabegron.
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Mirabegron.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Mirabegron.
PizotifenThe risk or severity of adverse effects can be increased when Pizotifen is combined with Mirabegron.
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Mirabegron.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Mirabegron.
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Mirabegron.
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Mirabegron.
PropafenoneThe serum concentration of Propafenone can be increased when it is combined with Mirabegron.
PropanthelineThe risk or severity of adverse effects can be increased when Propantheline is combined with Mirabegron.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Mirabegron.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Mirabegron.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Mirabegron.
RifampicinThe serum concentration of Mirabegron can be decreased when it is combined with Rifampicin.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Mirabegron.
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Mirabegron.
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Mirabegron.
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Mirabegron.
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Scopolamine butylbromide is combined with Mirabegron.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Mirabegron.
SolifenacinThe risk or severity of adverse effects can be increased when Mirabegron is combined with Solifenacin.
TamoxifenThe serum concentration of the active metabolites of Tamoxifen can be reduced when Tamoxifen is used in combination with Mirabegron resulting in a loss in efficacy.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Mirabegron.
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Mirabegron.
TiotropiumThe risk or severity of adverse effects can be increased when Tiotropium is combined with Mirabegron.
TolterodineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Mirabegron.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Mirabegron.
TramadolThe therapeutic efficacy of Tramadol can be decreased when used in combination with Mirabegron.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Mirabegron.
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Mirabegron.
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Mirabegron.
TrimethobenzamideThe risk or severity of adverse effects can be increased when Trimethobenzamide is combined with Mirabegron.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Mirabegron.
TriprolidineThe risk or severity of adverse effects can be increased when Triprolidine is combined with Mirabegron.
TrospiumThe risk or severity of adverse effects can be increased when Trospium is combined with Mirabegron.
UmeclidiniumThe risk or severity of adverse effects can be increased when Umeclidinium is combined with Mirabegron.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Mirabegron.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Mirabegron.
Food Interactions
  • When taken with meals, levels of mirabegron decreased. Furthermore, the magnitude of this effect was greater if taken with a low fat meal, rather than a high fat meal. Despite these findings, dose adjustment is not required.

Targets

Kind
Protein
Organism
Human
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
Molecular Weight:
43518.615 Da
References
  1. 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. [PubMed:23550899 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. 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. [PubMed:23625188 ]
  2. 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. [PubMed:22509825 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. 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. [PubMed:23625188 ]
  2. 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. [PubMed:22509825 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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
Molecular Weight:
68417.575 Da
References
  1. 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. [PubMed:22509825 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
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 colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
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 the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
Gene Name:
ORM1
Uniprot ID:
P02763
Molecular Weight:
23511.38 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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
Molecular Weight:
141477.255 Da
References
  1. 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. [PubMed:23560393 ]
Kind
Protein
Organism
Human
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 inhibited by the grapefruit juice component naringin.
Gene Name:
SLCO1A2
Uniprot ID:
P46721
Molecular Weight:
74144.105 Da
References
  1. 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. [PubMed:23560393 ]
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Drug created on May 30, 2013 23:44 / Updated on July 01, 2016 01:52