Identification

Name
Mirabegron
Accession Number
DB08893  (DB05702)
Type
Small Molecule
Groups
Approved
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
Not Available
External IDs
YM-178 / YM178
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BetmigaTablet, extended release25 mgOralAstellas Pharma Europe Bv2012-12-20Not applicableEu
BetmigaTablet, extended release25 mgOralAstellas Pharma Europe Bv2012-12-20Not applicableEu
BetmigaTablet, extended release50 mgOralAstellas Pharma Europe Bv2012-12-20Not applicableEu
BetmigaTablet, extended release50 mgOralAstellas Pharma Europe Bv2012-12-20Not applicableEu
BetmigaTablet, extended release25 mgOralAstellas Pharma Europe Bv2012-12-20Not applicableEu
BetmigaTablet, extended release50 mgOralAstellas Pharma Europe Bv2012-12-20Not applicableEu
BetmigaTablet, extended release25 mgOralAstellas Pharma Europe Bv2012-12-20Not applicableEu
BetmigaTablet, extended release25 mgOralAstellas Pharma Europe Bv2012-12-20Not applicableEu
BetmigaTablet, extended release50 mgOralAstellas Pharma Europe Bv2012-12-20Not applicableEu
BetmigaTablet, extended release50 mgOralAstellas Pharma Europe Bv2012-12-20Not applicableEu
International/Other Brands
Betanis / Metmiga / Myrbetriq
Categories
UNII
MVR3JL3B2V
CAS number
223673-61-8
Weight
Average: 396.506
Monoisotopic: 396.161996722
Chemical Formula
C21H24N4O2S
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

Pharmacology

Indication

Mirabegron is a beta-3 adrenergic agonist indicated for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency.

Associated Conditions
Pharmacodynamics

Mirabegron 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 action

Mirabegron 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.

TargetActionsOrganism
ABeta-3 adrenergic receptor
agonist
Human
Absorption

The 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 binding

71% 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 elimination

Mirabegron 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 life

Terminal elimination half-life = 50 hours

Clearance

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

Toxicity

Most commonly reported adverse reactions (> 2% and > placebo) were hypertension, nasopharyngitis, urinary tract infection and headache

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of Mirabegron can be decreased when combined with (R)-warfarin.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Mirabegron.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Mirabegron.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Mirabegron.
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be decreased when combined with Mirabegron.
5-androstenedioneThe metabolism of Mirabegron can be decreased when combined with 5-androstenedione.
6-Deoxyerythronolide BThe metabolism of Mirabegron can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Mirabegron.
AbacavirAbacavir may decrease the excretion rate of Mirabegron which could result in a higher serum level.
AbemaciclibThe serum concentration of Mirabegron can be increased when it is combined with Abemaciclib.
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.

References

General References
  1. 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. [PubMed:17293563]
  2. 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
KEGG Drug
D09535
PubChem Compound
9865528
PubChem Substance
175427137
ChemSpider
8041219
ChEBI
65349
ChEMBL
CHEMBL2095212
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Mirabegron
ATC Codes
G04BD12 — Mirabegron
AHFS Codes
  • 86:12.08.12 — Selective Beta 3-adrenergic Agonists
FDA label
Download (510 KB)
MSDS
Download (481 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Enrolling by InvitationTreatmentCognitive Change / Neurogenic Bladder Dysfunction / Spinal Cord Injuries (SCI)1
0RecruitingBasic ScienceMetabolic Syndromes / Obese1
0RecruitingTreatmentAchalasia1
1CompletedNot AvailableBioavailability / Healthy Volunteers / Pharmacokinetics of Mirabegron1
1CompletedNot AvailableCardiovascular / Healthy Volunteers / Pharmacokinetics1
1CompletedNot AvailableHealthy Chinese Volunteers1
1CompletedNot AvailableHealthy Volunteers1
1CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of Mirabegron3
1CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of YM1783
1CompletedNot AvailableHealthy Volunteers / Plasma Concentration of Mirabegron1
1CompletedNot AvailableImpaired Renal Function1
1CompletedNot AvailableIntraocular Pressure1
1CompletedNot AvailablePharmacokinetics of YM1781
1CompletedBasic ScienceBioavailability / Healthy Volunteers / Phase 11
1CompletedBasic ScienceDrug Drug Interaction (DDI) / Healthy Volunteers / Pharmacokinetics2
1CompletedBasic ScienceHealthy Volunteers1
1CompletedBasic ScienceHealthy Volunteers / Mild and Moderate Hepatic Impairment / Pharmacokinetics1
1CompletedBasic ScienceHealthy Volunteers / Pharmacodynamics of Mirabegron1
1CompletedBasic ScienceHealthy Volunteers / Pharmacokinetics of Mirabegron3
1CompletedBasic ScienceHealthy Volunteers / Pharmacokinetics of YM1781
1CompletedBasic ScienceMetabolic Processes1
1CompletedBasic ScienceNeurogenic Detrusor Overactivity / Pharmacokinetics of Mirabegron / Urinary Bladder, Overactive1
1CompletedBasic ScienceNeurogenic Detrusor Overactivity / Urinary Bladder, Overactive1
1CompletedBasic SciencePharmacokinetics / Urinary Bladder, Overactive1
1CompletedOtherHealthy Volunteers / Pharmacokinetics of Mirabegron1
1RecruitingBasic ScienceHealthy Volunteers1
1, 2RecruitingTreatmentErectile Dysfunction (ED) / Urinary Bladder, Overactive / Urinary Incontinence (UI)1
2Active Not RecruitingTreatmentLower Urinary Tract Symptoms (LUTS) / Pain NOS / Urinary Bladder, Overactive1
2CompletedTreatmentBladder Outlet Obstruction / Lower Urinary Tract Symptoms (LUTS)1
2CompletedTreatmentEssential Thrombocythemia (ET) / Myeloproliferative Neoplasms / Polycythemia Vera (PV) / Primary Myelofibrosis1
2CompletedTreatmentSigns and Symptoms / Urinary Bladder Diseases / Urinary Bladder, Overactive / Urologic Diseases / Urological Manifestations1
2CompletedTreatmentUrinary Bladder, Overactive3
2Enrolling by InvitationTreatmentLeft Ventricular Hypertrophy1
2Not Yet RecruitingTreatmentHeart Failure, Unspecified / Mirabegron / Pulmonary Hypertension (PH) / Pulmonary vascular resistance abnormality1
2Not Yet RecruitingTreatmentSpinal Cord Injuries (SCI) / Urinary Bladder, Neurogenic1
2RecruitingBasic ScienceBrown Fat1
2RecruitingTreatmentAutonomic Dysreflexia / Autonomic Integrity / Baroreceptor Integrity / Blood Pressures / Cerebral Blood Flow / Cognitive Function / Hypotensive / Spinal Cord Injuries (SCI) / Sympathetic Integrity / Vagal Integrity1
2RecruitingTreatmentChronic Heart Failure With Reduced Ejection Fraction (HFrEF)1
2RecruitingTreatmentFlank Pain / Ureteral Obstruction1
2RecruitingTreatmentUrinary Bladder, Overactive1
2, 3TerminatedTreatmentUrinary Bladder, Neurogenic1
3Active Not RecruitingTreatmentNeurogenic Detrusor Overactivity1
3CompletedTreatmentUrgency Incontinence / Urinary Bladder Diseases\Urologic Diseases / Urinary Bladder, Overactive2
3CompletedTreatmentUrinary Bladder Diseases / Urinary Bladder, Overactive / Urologic Diseases2
3CompletedTreatmentUrinary Bladder, Overactive7
3CompletedTreatmentUrinary Bladder, Overactive / Urinary Incontinence (UI)3
3RecruitingTreatmentInterstitial Cystitis1
3RecruitingTreatmentUrinary Bladder, Overactive1
4CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of Mirabegron and Tolterodine1
4CompletedNot AvailableUrinary Bladder, Overactive1
4CompletedTreatmentBenign Prostatic Hyperplasia (BPH) / Urinary Bladder, Overactive1
4CompletedTreatmentImpaired Cognition / Parkinson's Disease (PD) / Urinary Bladder, Overactive1
4CompletedTreatmentUrinary Bladder, Overactive7
4Not Yet RecruitingTreatmentBenign Prostatic Hyperplasia (BPH) / Urinary Bladder, Overactive1
4Not Yet RecruitingTreatmentUrinary Bladder, Overactive1
4RecruitingTreatmentBMI >30 kg/m21
4RecruitingTreatmentCalcium Nephrolithiasis1
4RecruitingTreatmentDisseminated Sclerosis1
4RecruitingTreatmentParkinson's Disease (PD) / Urinary Bladder, Overactive1
4RecruitingTreatmentParkinsons's Disease1
4RecruitingTreatmentUrge Incontinence / Urinary Incontinence, Urge1
4RecruitingTreatmentUrinary Bladder, Overactive2
4Unknown StatusTreatmentUrinary Bladder, Overactive1
4WithdrawnTreatmentBladder Irritable / Bladder Pain Syndrome / Urinary Frequency/Urgency1
Not AvailableActive Not RecruitingNot AvailableLower Urinary Tract Symptoms (LUTS) / Nocturia1
Not AvailableActive Not RecruitingNot AvailableUrinary Bladder, Overactive1
Not AvailableCompletedNot AvailableCardiovascular Disease (CVD) / Urinary Bladder, Overactive1
Not AvailableCompletedNot AvailableUrgency Incontinence / Urinary Bladder Diseases / Urinary Bladder, Overactive / Urologic Diseases1
Not AvailableCompletedNot AvailableUrinary Bladder Diseases / Urinary Bladder, Overactive / Urologic Diseases1
Not AvailableCompletedNot AvailableUrinary Bladder, Overactive3
Not AvailableCompletedOtherType 2 Diabetes Mellitus1
Not AvailableNot Yet RecruitingTreatmentUrinary Bladder, Overactive1
Not AvailableRecruitingNot AvailableUrinary Bladder, Overactive1
Not AvailableRecruitingTreatmentBenign Prostatic Hypertrophy (BPH) / Erectile Abnormalities / Erectile Dysfunction (ED) / Prostate Hyperplasia / Prostatic Neoplasms1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Tablet, extended releaseOral25 mg
Tablet, extended releaseOral50 mg
Tablet, film coated, extended releaseOral25 mg/1
Tablet, film coated, extended releaseOral50 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2305802No2008-11-182018-10-15Canada
CA2464068No2007-10-162022-10-29Canada
CA2503570No2023-11-042011-04-19Canada
USRE44872No2014-04-292023-12-18Us
US7750029No2010-07-062023-12-18Us
US6346532No2002-02-122018-10-15Us
US8835474No2014-09-162023-11-04Us
US6562375No2003-05-132020-08-01Us
US7982049No2011-07-192023-11-04Us
US7342117No2008-03-112023-11-04Us
US8772315No2014-07-082028-10-30Us

Properties

State
Solid
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 RuleNoChemAxon
MDDR-like RuleYesChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-004j-0429000000-a1fa6e47b60253c53578

Taxonomy

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
Phenethylamine / Anilide / N-arylamide / 2,4-disubstituted 1,3-thiazole / Aralkylamine / 1,3-thiazol-2-amine / Azole / Thiazole / Heteroaromatic compound / 1,2-aminoalcohol
show 22 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
monocarboxylic acid amide, 1,3-thiazole, aromatic amide, ethanolamines (CHEBI:65349)

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
Uniprot Name
Beta-3 adrenergic receptor
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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
Substrate
Inhibitor
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
  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
Uniprot Name
Cholinesterase
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 colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
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...
Gene Name
ORM1
Uniprot ID
P02763
Uniprot Name
Alpha-1-acid glycoprotein 1
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
Uniprot Name
Multidrug resistance protein 1
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 inhibit...
Gene Name
SLCO1A2
Uniprot ID
P46721
Uniprot Name
Solute carrier organic anion transporter family member 1A2
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]

Drug created on May 30, 2013 23:44 / Updated on November 18, 2018 13:32