mirabegron Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
beta3-adrenoreceptor agonists 4382 223673-61-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • YM178
  • myrbetriq
  • mirabegron
a beta-3 adrenergic agonist, relaxes the detrusor smooth muscle during the storage phase of the urinary bladder fill-void cycle by activation of beta-3 AR which increases bladder capacity
  • Molecular weight: 396.51
  • Formula: C21H24N4O2S
  • CLOGP: 1.32
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 4
  • TPSA: 100.27
  • ALOGS: -4.98
  • ROTB: 9

Drug dosage:

DoseUnitRoute
50 mg O

Approvals:

DateAgencyCompanyOrphan
June 28, 2012 FDA APGDI

FDA Adverse Event Reporting System

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Intentional product misuse 316.45 33.24 78 855 12623 3372303
Drug ineffective 186.29 33.24 91 842 115999 3268927
Intentional product use issue 173.15 33.24 34 899 1876 3383050
Blood pressure increased 164.67 33.24 53 880 22177 3362749
Urinary retention 155.46 33.24 40 893 7532 3377394
Hypertension 104.96 33.24 44 889 38422 3346504
Off label use 84.64 33.24 42 891 53935 3330991
Headache 81.49 33.24 49 884 91931 3292995
Nocturia 77.32 33.24 17 916 1617 3383309
Dry mouth 74.77 33.24 24 909 9798 3375128
Constipation 69.91 33.24 31 902 30781 3354145
Inappropriate schedule of drug administration 59.39 33.24 22 911 13731 3371195
Drug effect incomplete 58.97 33.24 19 914 7831 3377095
Atrial fibrillation 47.60 33.24 22 911 23919 3361007
Dizziness 45.87 33.24 32 901 76480 3308446
Palpitations 39.36 33.24 18 915 19065 3365861
Urinary tract infection 36.36 33.24 20 913 31308 3353618
Wrong technique in product usage process 35.17 33.24 16 917 16735 3368191

Pharmacologic Action:

SourceCodeDescription
ATC G04BD12 GENITO URINARY SYSTEM AND SEX HORMONES
UROLOGICALS
UROLOGICALS
Drugs for urinary frequency and incontinence
FDA EPC N0000185008 beta3-Adrenergic Agonist
FDA MoA N0000185007 Adrenergic beta3-Agonists
FDA MoA N0000182137 Cytochrome P450 2D6 Inhibitors
MeSH PA D018663 Adrenergic Agents
MeSH PA D000322 Adrenergic Agonists
MeSH PA D058667 Adrenergic beta-3 Receptor Agonists
MeSH PA D000318 Adrenergic beta-Agonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D064804 Urological Agents
CHEBI has role CHEBI:35522 beta-adrenergic agonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Bladder muscle dysfunction - overactive indication 236633002
Hypertensive disorder contraindication 38341003 DOID:10763

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.32 acidic
pKa2 8.7 Basic
pKa3 4.93 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
25MG MYRBETRIQ APGDI N202611 June 28, 2012 RX TABLET, EXTENDED RELEASE ORAL 8835474 Nov. 4, 2023 FOR THE TREATMENT OF OVERACTIVE BLADDER (OAB) WITH SYMPTOMS OF URGE URINARY INCONTINENCE, URGENCY, AND URINARY FREQUENCY
25MG MYRBETRIQ APGDI N202611 June 28, 2012 RX TABLET, EXTENDED RELEASE ORAL RE44872 Nov. 4, 2023 FOR THE TREATMENT OF OVERACTIVE BLADDER (OAB) WITH SYMPTOMS OF URGE URINARY INCONTINENCE, URGENCY, AND URINARY FREQUENCY
50MG MYRBETRIQ APGDI N202611 June 28, 2012 RX TABLET, EXTENDED RELEASE ORAL 8835474 Nov. 4, 2023 FOR THE TREATMENT OF OVERACTIVE BLADDER (OAB) WITH SYMPTOMS OF URGE URINARY INCONTINENCE, URGENCY, AND URINARY FREQUENCY
50MG MYRBETRIQ APGDI N202611 June 28, 2012 RX TABLET, EXTENDED RELEASE ORAL RE44872 Nov. 4, 2023 FOR THE TREATMENT OF OVERACTIVE BLADDER (OAB) WITH SYMPTOMS OF URGE URINARY INCONTINENCE, URGENCY, AND URINARY FREQUENCY

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Beta-3 adrenergic receptor GPCR AGONIST EC50 7.65 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
7445 IUPHAR_LIGAND_ID
D09535 KEGG_DRUG
C3485428 UMLSCUI
DB08893 DRUGBANK_ID
CHEMBL2095212 ChEMBL_ID
1300786 RXNORM
28616 MMSL
d07876 MMSL
014540 NDDF
4031804 VANDF
N0000186060 NDFRT
703803006 SNOMEDCT_US
703804000 SNOMEDCT_US
9865528 PUBCHEM_CID
MVR3JL3B2V UNII
8907 INN_ID
C520025 MESH_SUPPLEMENTAL_RECORD_UI
CHEBI:65349 CHEBI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Myrbetriq HUMAN PRESCRIPTION DRUG LABEL 1 0469-2601 TABLET, FILM COATED, EXTENDED RELEASE 25 mg ORAL NDA 17 sections
Myrbetriq HUMAN PRESCRIPTION DRUG LABEL 1 0469-2602 TABLET, FILM COATED, EXTENDED RELEASE 50 mg ORAL NDA 17 sections
Myrbetriq HUMAN PRESCRIPTION DRUG LABEL 1 55154-8712 TABLET, FILM COATED, EXTENDED RELEASE 25 mg ORAL NDA 17 sections
Myrbetriq HUMAN PRESCRIPTION DRUG LABEL 1 55154-8713 TABLET, FILM COATED, EXTENDED RELEASE 50 mg ORAL NDA 17 sections
Myrbetriq HUMAN PRESCRIPTION DRUG LABEL 1 69189-2601 TABLET, FILM COATED, EXTENDED RELEASE 25 mg ORAL NDA 18 sections