mirabegron 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
beta3-adrenoreceptor agonists	4382	223673-61-8

Description:

Molecule	Description
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 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

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

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
50	mg	O

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	50 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	23.80 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	13.60 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.29 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
June 28, 2012	FDA	APGDI

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Blepharospasm	196.87	12.50	75	21715	5921	63461311
Taste disorder	160.34	12.50	83	21707	13579	63453653
Urinary retention	160.09	12.50	110	21680	30191	63437041
Urinary tract infection	141.91	12.50	293	21497	264391	63202841
Blood pressure increased	123.83	12.50	209	21581	161853	63305379
Intentional product misuse	114.34	12.50	122	21668	60795	63406437
Memory impairment	112.78	12.50	158	21632	104100	63363132
Epilepsy	110.38	12.50	84	21706	26981	63440251
Urinary incontinence	89.92	12.50	80	21710	31934	63435298
Fall	78.87	12.50	304	21486	392030	63075202

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Urinary retention	180.79	16.41	115	9131	36173	34911512
Hallucination	117.41	16.41	102	9144	51396	34896289
Fall	81.60	16.41	171	9075	202714	34744971
Confusional state	56.07	16.41	120	9126	144040	34803645
Intentional product misuse	50.05	16.41	61	9185	45550	34902135
Urinary tract infection	46.13	16.41	81	9165	84000	34863685
Platypnoea	45.04	16.41	8	9238	32	34947653
Nocturia	44.97	16.41	30	9216	10180	34937505
Urinary incontinence	42.16	16.41	37	9209	18837	34928848
Micturition urgency	40.93	16.41	24	9222	6501	34941184

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Urinary retention	196.73	12.25	155	25260	56475	79662498
Urinary tract infection	144.62	12.25	289	25126	274223	79444750
Fall	136.67	12.25	402	25013	487227	79231746
Blepharospasm	129.68	12.25	54	25361	5797	79713176
Taste disorder	108.85	12.25	66	25349	15757	79703216
Urinary incontinence	102.88	12.25	93	25322	40816	79678157
Memory impairment	84.76	12.25	138	25277	111596	79607377
Toxicity to various agents	84.58	12.25	16	25399	421524	79297449
Hallucination	70.65	12.25	110	25305	85635	79633338
Blood pressure increased	69.54	12.25	185	25230	211175	79507798

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	G04BD12	GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS UROLOGICALS Drugs for urinary frequency and incontinence
CHEBI has role	CHEBI:35522	beta-adrenergic agonists
FDA EPC	N0000185008	beta3-Adrenergic Agonist
FDA MoA	N0000182137	Cytochrome P450 2D6 Inhibitors
FDA MoA	N0000185007	Adrenergic beta3-Agonists
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000190114	Cytochrome P450 3A Inhibitors
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D000322	Adrenergic Agonists
MeSH PA	D058667	Adrenergic beta-3 Receptor Agonists

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Bladder muscle dysfunction - overactive	indication	236633002
Hypertensive disorder	contraindication	38341003	DOID:10763

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.32	acidic
pKa2	8.7	Basic
pKa3	4.93	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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
25MG	MYRBETRIQ	APGDI	N202611	June 28, 2012	RX	TABLET, EXTENDED RELEASE	ORAL	8772315	Oct. 30, 2028	USE IN COMBINATION WITH THE MUSCARINIC ANTAGONIST SOLIFENACIN SUCCINATE 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	10842780	Sept. 28, 2029	ADMINISTRATION OF AN EXTENDED RELEASE TABLET 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
50MG	MYRBETRIQ	APGDI	N202611	June 28, 2012	RX	TABLET, EXTENDED RELEASE	ORAL	8772315	Oct. 30, 2028	USE IN COMBINATION WITH THE MUSCARINIC ANTAGONIST SOLIFENACIN SUCCINATE 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	10842780	Sept. 28, 2029	ADMINISTRATION OF AN EXTENDED RELEASE TABLET FOR THE TREATMENT OF OVERACTIVE BLADDER (OAB) WITH SYMPTOMS OF URGE URINARY INCONTINENCE, URGENCY, AND URINARY FREQUENCY
8MG/ML	MYRBETRIQ GRANULES	APGDI	N213801	March 25, 2021	RX	FOR SUSPENSION, EXTENDED RELEASE	ORAL	10058536	March 31, 2036	TREATMENT OF NEUROGENIC DETRUSOR OVERACTIVITY (NDO) IN PEDIATRIC PATIENTS AGED 3 YEARS AND OLDER BY ADMINISTRATION OF AN EXTENDED-RELEASE SUSPENSION FORMULATION OF MIRABEGRON

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
25MG	MYRBETRIQ	APGDI	N202611	June 28, 2012	RX	TABLET, EXTENDED RELEASE	ORAL	March 25, 2024	TREATMENT OF NEUROGENIC DETRUSOR OVERACTIVITY (NDO) IN PEDIATRIC PATIENTS 3 YEARS AND OLDER AND WEIGHING 35 KILOGRAMS OR MORE
25MG	MYRBETRIQ	APGDI	N202611	June 28, 2012	RX	TABLET, EXTENDED RELEASE	ORAL	Sept. 25, 2024	PEDIATRIC EXCLUSIVITY
50MG	MYRBETRIQ	APGDI	N202611	June 28, 2012	RX	TABLET, EXTENDED RELEASE	ORAL	March 25, 2024	TREATMENT OF NEUROGENIC DETRUSOR OVERACTIVITY (NDO) IN PEDIATRIC PATIENTS 3 YEARS AND OLDER AND WEIGHING 35 KILOGRAMS OR MORE
50MG	MYRBETRIQ	APGDI	N202611	June 28, 2012	RX	TABLET, EXTENDED RELEASE	ORAL	Sept. 25, 2024	PEDIATRIC EXCLUSIVITY
8MG/ML	MYRBETRIQ GRANULES	APGDI	N213801	March 25, 2021	RX	FOR SUSPENSION, EXTENDED RELEASE	ORAL	March 25, 2024	NEW PRODUCT
8MG/ML	MYRBETRIQ GRANULES	APGDI	N213801	March 25, 2021	RX	FOR SUSPENSION, EXTENDED RELEASE	ORAL	Sept. 25, 2024	PEDIATRIC EXCLUSIVITY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Beta-3 adrenergic receptor	GPCR	P13945	ADRB3_HUMAN	AGONIST	EC50	7.65		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE

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External reference:

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ID	Source
014540	NDDF
1300786	RXNORM
191568	MMSL
28616	MMSL
4031804	VANDF
703803006	SNOMEDCT_US
703804000	SNOMEDCT_US
7445	IUPHAR_LIGAND_ID
8907	INN_ID
9865528	PUBCHEM_CID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	0469-2601	TABLET, FILM COATED, EXTENDED RELEASE	25 mg	ORAL	NDA	27 sections
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	0469-2601	TABLET, FILM COATED, EXTENDED RELEASE	25 mg	ORAL	NDA	27 sections
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	0469-2601	TABLET, FILM COATED, EXTENDED RELEASE	25 mg	ORAL	NDA	27 sections
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	0469-2602	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	NDA	27 sections
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	0469-2602	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	NDA	27 sections
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	0469-2602	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	NDA	27 sections
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	0469-5020	GRANULE, FOR SUSPENSION, EXTENDED RELEASE	8 mg	ORAL	NDA	27 sections
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	0469-5020	GRANULE, FOR SUSPENSION, EXTENDED RELEASE	8 mg	ORAL	NDA	27 sections
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	0469-5020	GRANULE, FOR SUSPENSION, EXTENDED RELEASE	8 mg	ORAL	NDA	27 sections
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	55154-8712	TABLET, FILM COATED, EXTENDED RELEASE	25 mg	ORAL	NDA	27 sections

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