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:

Property	Value	Reference
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
t_half (Half-life)	50 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
June 28, 2012	FDA	APGDI

FDA Adverse Event Reporting System (Female)

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
Toxicity to various agents	71.99	12.50	3	21787	247247	63219985
Migraine	68.11	12.50	125	21665	103221	63364011
Drug dispensed to wrong patient	53.90	12.50	14	21776	308	63466924
Hypertension	53.24	12.50	213	21577	279090	63188142
Off label use	53.17	12.50	404	21386	674058	62793174
Residual urine volume increased	52.39	12.50	10	21780	47	63467185
Multiple sclerosis relapse	51.66	12.50	73	21717	48405	63418827
Multiple sclerosis	51.42	12.50	52	21738	24320	63442912
Contraindicated product administered	51.23	12.50	7	21783	217641	63249591
Gastrooesophageal reflux disease	51.21	12.50	106	21684	95533	63371699
Cystitis	50.22	12.50	77	21713	54914	63412318
Hypoaesthesia	49.15	12.50	148	21642	168245	63298987
Dry mouth	46.10	12.50	90	21700	77773	63389459
Paraesthesia	43.97	12.50	136	21654	156830	63310402
Bladder pain	42.17	12.50	19	21771	2289	63464943
Kidney infection	40.97	12.50	45	21745	23131	63444101
Pemphigus	40.74	12.50	7	21783	183719	63283513
Abdominal pain upper	39.74	12.50	158	21632	206286	63260946
Pollakiuria	38.93	12.50	48	21742	27889	63439343
Maternal exposure during pregnancy	38.02	12.50	14	21776	220048	63247184
Antineutrophil cytoplasmic antibody increased	36.73	12.50	9	21781	155	63467077
Sinonasal obstruction	36.62	12.50	10	21780	268	63466964
Scleral discolouration	36.25	12.50	11	21779	432	63466800
Therapeutic product effect decreased	35.61	12.50	11	21779	193176	63274056
Exposure during pregnancy	34.32	12.50	6	21784	155541	63311691
Micturition urgency	33.08	12.50	27	21763	9584	63457648
Muscular weakness	31.49	12.50	103	21687	122250	63344982
Treatment failure	30.64	12.50	15	21775	199028	63268204
Anal incontinence	30.54	12.50	30	21760	13546	63453686
Gait disturbance	30.40	12.50	134	21656	183044	63284188
On and off phenomenon	30.05	12.50	14	21776	1821	63465411
Anxiety disorder	29.50	12.50	18	21772	4032	63463200
Pericarditis	29.19	12.50	5	21785	131574	63335658
Sputum retention	29.00	12.50	10	21780	592	63466640
Systemic lupus erythematosus	28.89	12.50	18	21772	208900	63258332
Intercepted medication error	28.68	12.50	10	21780	612	63466620
Bladder disorder	28.43	12.50	24	21766	8922	63458310
Swelling	27.95	12.50	32	21758	275346	63191886
Synovitis	27.41	12.50	15	21775	186903	63280329
Glossodynia	26.75	12.50	14	21776	178862	63288370
Dermatitis atopic	26.70	12.50	24	21766	9700	63457532
Lip disorder	26.51	12.50	12	21778	1462	63465770
Urinary tract disorder	26.50	12.50	15	21775	2926	63464306
Vitamin D deficiency	26.35	12.50	28	21762	13864	63453368
Vascular stenosis	25.49	12.50	8	21782	352	63466880
Palpitations	24.71	12.50	90	21700	112680	63354552
Hand deformity	24.56	12.50	12	21778	159445	63307787
Rheumatoid arthritis	24.16	12.50	31	21759	253788	63213444
Dementia	24.13	12.50	31	21759	18763	63448469
Discomfort	23.72	12.50	14	21776	167360	63299872
Balance disorder	23.47	12.50	73	21717	84349	63382883
Lymphocyte count decreased	23.01	12.50	39	21751	30218	63437014
Disease progression	22.60	12.50	7	21783	122751	63344481
Dysuria	22.44	12.50	41	21749	33697	63433535
Schizophrenia	22.40	12.50	22	21768	9930	63457302
Infusion related reaction	22.33	12.50	31	21759	245490	63221742
Nocturia	22.17	12.50	20	21770	8121	63459111
Drug hypersensitivity	22.04	12.50	46	21744	310641	63156591
Arthropathy	22.01	12.50	29	21761	234763	63232469
Feeling drunk	21.77	12.50	15	21775	4127	63463105
Arrhythmia	21.25	12.50	43	21747	38097	63429135
Lip swelling	20.98	12.50	38	21752	31025	63436207
Idiopathic orbital inflammation	20.83	12.50	6	21784	196	63467036
Haemorrhoids	20.19	12.50	31	21759	22119	63445113
Product blister packaging issue	20.17	12.50	6	21784	220	63467012
Tender joint count	20.04	12.50	6	21784	225	63467007
Clubbing	19.91	12.50	7	21783	439	63466793
Dizziness	19.81	12.50	230	21560	429695	63037537
Rheumatoid factor positive	19.18	12.50	3	21787	84403	63382829
Anti-cyclic citrullinated peptide antibody positive	19.06	12.50	8	21782	116204	63351028
Metastatic neoplasm	18.99	12.50	14	21776	4281	63462951
Wound	18.79	12.50	17	21773	163246	63303986
Lung neoplasm malignant	18.63	12.50	28	21762	19605	63447627
Pharyngeal mass	18.40	12.50	6	21784	299	63466933
Thrombocytopenia	18.30	12.50	15	21775	151142	63316090
Loefgren syndrome	18.20	12.50	5	21785	137	63467095
Neutropenia	18.11	12.50	20	21770	174985	63292247
Product packaging quantity issue	18.11	12.50	9	21781	1350	63465882
Hypertensive crisis	17.75	12.50	24	21766	15262	63451970
Dyskinesia	17.74	12.50	36	21754	31966	63435266
Constipation	17.72	12.50	135	21655	224808	63242424
Pyrexia	16.72	12.50	94	21696	470384	62996848
Duodenal ulcer perforation	16.00	12.50	5	21785	87204	63380028
Hypothyroidism	15.89	12.50	41	21749	42591	63424641
Mouth swelling	15.65	12.50	13	21777	4727	63462505
Hypersensitivity	15.63	12.50	50	21740	292635	63174597
Steroid diabetes	15.49	12.50	8	21782	1300	63465932
Product use in unapproved indication	14.96	12.50	109	21681	178971	63288261
Urine albumin/creatinine ratio decreased	14.95	12.50	4	21786	99	63467133
Diabetic ketosis	14.93	12.50	5	21785	271	63466961
Dyspepsia	14.89	12.50	72	21718	102124	63365108
Magnetic resonance imaging head abnormal	14.80	12.50	9	21781	2004	63465228
Persistent genital arousal disorder	14.75	12.50	5	21785	281	63466951
Conjunctival discolouration	14.69	12.50	4	21786	106	63467126
Hyperventilation	14.67	12.50	14	21776	6102	63461130
Angina pectoris	14.54	12.50	32	21758	30046	63437186
Allergy to arthropod bite	14.31	12.50	5	21785	308	63466924
VIIth nerve injury	14.25	12.50	4	21786	119	63467113
Sleep apnoea syndrome	14.09	12.50	31	21759	29102	63438130
Wrong patient received product	14.03	12.50	9	21781	2198	63465034
Febrile neutropenia	14.03	12.50	12	21778	118437	63348795
Cystitis interstitial	13.94	12.50	8	21782	1600	63465632
Pancreatitis necrotising	13.48	12.50	8	21782	1704	63465528
Hyperlipidaemia	13.29	12.50	24	21766	19547	63447685
Blister	13.24	12.50	15	21775	129799	63337433
COVID-19	13.24	12.50	75	21715	113028	63354204
Concussion	13.07	12.50	16	21774	9228	63458004
Muscle atrophy	13.03	12.50	14	21776	7019	63460213
Neurogenic bladder	12.96	12.50	10	21780	3275	63463957
Breast disorder	12.92	12.50	9	21781	2521	63464711
Muscle tightness	12.79	12.50	18	21772	11882	63455350

FDA Adverse Event Reporting System (Male)

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
Phaeochromocytoma malignant	39.51	16.41	8	9238	72	34947613
Delusion	39.22	16.41	30	9216	12605	34935080
Blood pressure increased	32.65	16.41	72	9174	88030	34859655
Arrhythmia	31.59	16.41	43	9203	35765	34911920
Dementia	30.80	16.41	27	9219	13721	34933964
Gait disturbance	29.78	16.41	68	9178	85072	34862613
Bone marrow oedema	26.50	16.41	9	9237	663	34947022
Pollakiuria	24.35	16.41	28	9218	19646	34928039
Constipation	23.84	16.41	85	9161	136897	34810788
Spinal cord haemorrhage	23.72	16.41	7	9239	326	34947359
Prescribed underdose	22.99	16.41	19	9227	8914	34938771
Blood pressure systolic increased	22.45	16.41	29	9217	22923	34924762
Drug ineffective	21.98	16.41	200	9046	456551	34491134
Oesophageal dilatation	21.85	16.41	6	9240	215	34947470
Dysuria	21.55	16.41	31	9215	27121	34920564
Extradural haematoma	21.51	16.41	9	9237	1180	34946505
Hypertensive crisis	21.25	16.41	18	9228	8733	34938952
On and off phenomenon	20.61	16.41	11	9235	2486	34945199
Toxicity to various agents	20.44	16.41	14	9232	200348	34747337
Cerebral infarction	19.85	16.41	30	9216	27425	34920260
Hallucination, visual	19.83	16.41	24	9222	17767	34929918
Device dislocation	19.75	16.41	15	9231	6234	34941451
Embedded device	19.45	16.41	6	9240	325	34947360
Head injury	19.43	16.41	24	9222	18136	34929549
Dropped head syndrome	19.13	16.41	5	9241	148	34947537
Cystitis interstitial	18.46	16.41	5	9241	170	34947515
Dyskinesia oesophageal	18.34	16.41	4	9242	53	34947632
Blood pressure abnormal	18.31	16.41	16	9230	8090	34939595
Orthostatic hypotension	18.28	16.41	28	9218	25891	34921794
Heart rate abnormal	17.79	16.41	9	9237	1822	34945863
Vasoplegia syndrome	17.67	16.41	9	9237	1847	34945838
Hypertonic bladder	17.64	16.41	9	9237	1855	34945830
Perineal pain	17.43	16.41	7	9239	826	34946859
Oesophageal obstruction	16.93	16.41	6	9240	502	34947183
Product use complaint	16.78	16.41	8	9238	1424	34946261
Blood prolactin decreased	16.48	16.41	5	9241	256	34947429

FDA Adverse Event Reporting System (Geriatric)

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
Gait disturbance	58.76	12.25	172	25243	207334	79511639
Migraine	54.42	12.25	99	25316	87394	79631579
Cystitis	54.05	12.25	75	25340	52657	79666316
Micturition urgency	51.33	12.25	38	25377	12603	79706370
Epilepsy	50.98	12.25	64	25351	40796	79678177
Bladder pain	49.88	12.25	21	25394	2316	79716657
Pollakiuria	49.04	12.25	60	25355	37257	79681716
Residual urine volume increased	48.41	12.25	9	25406	39	79718934
Multiple sclerosis relapse	45.93	12.25	65	25350	46468	79672505
Drug dispensed to wrong patient	44.06	12.25	14	25401	692	79718281
Hypoaesthesia	43.61	12.25	141	25274	179211	79539762
Platypnoea	43.55	12.25	8	25407	32	79718941
On and off phenomenon	43.30	12.25	21	25394	3219	79715754
Hypertension	43.10	12.25	214	25201	330778	79388195
Kidney infection	40.46	12.25	42	25373	21809	79697164
Confusional state	38.87	12.25	202	25213	317795	79401178
Phaeochromocytoma malignant	38.02	12.25	8	25407	72	79718901
Dysuria	37.35	12.25	62	25353	50889	79668084
Muscular weakness	36.95	12.25	124	25291	160605	79558368
Multiple sclerosis	34.55	12.25	39	25376	22243	79696730
Intentional product misuse	34.02	12.25	86	25329	95079	79623894
Arrhythmia	33.95	12.25	66	25349	61206	79657767
Dry mouth	33.00	12.25	81	25334	87938	79631035
Nocturia	32.23	12.25	30	25385	13651	79705322
Dementia	31.35	12.25	39	25376	24620	79694353
Sinonasal obstruction	31.10	12.25	9	25406	323	79718650
Paraesthesia	29.64	12.25	123	25292	176200	79542773
Scleral discolouration	29.55	12.25	10	25405	603	79718370
Gastrooesophageal reflux disease	29.07	12.25	86	25329	104160	79614813
Thrombocytopenia	27.95	12.25	26	25389	265233	79453740
Delusion	27.09	12.25	33	25382	20390	79698583
Anal incontinence	25.15	12.25	30	25385	18138	79700835
Hypertonic bladder	25.04	12.25	16	25399	4185	79714788
Antineutrophil cytoplasmic antibody increased	24.84	12.25	7	25408	228	79718745
Abdominal pain upper	24.49	12.25	138	25277	223681	79495292
Constipation	24.35	12.25	164	25251	282886	79436087
Balance disorder	24.26	12.25	78	25337	98779	79620194
Lip disorder	23.74	12.25	11	25404	1523	79717450
Dizziness	23.18	12.25	263	25152	526178	79192795
Head injury	22.86	12.25	42	25373	37327	79681646
Therapeutic product effect decreased	22.61	12.25	12	25403	163851	79555122
Dyskinesia oesophageal	22.53	12.25	5	25410	59	79718914
Exposure during pregnancy	22.13	12.25	3	25412	101129	79617844
Vascular stenosis	21.99	12.25	8	25407	598	79718375
Hypertensive crisis	21.97	12.25	30	25385	20740	79698233
Palpitations	21.80	12.25	89	25326	126521	79592452
Urinary tract disorder	21.68	12.25	14	25401	3728	79715245
Cystitis interstitial	21.66	12.25	10	25405	1373	79717600
Tender joint count	21.07	12.25	6	25409	203	79718770
Contraindicated product administered	21.06	12.25	12	25403	157526	79561447
Feeling drunk	21.01	12.25	15	25400	4704	79714269
Sputum retention	20.58	12.25	9	25406	1088	79717885
Product blister packaging issue	20.50	12.25	6	25409	224	79718749
Coma	19.77	12.25	4	25411	100645	79618328
Idiopathic orbital inflammation	19.76	12.25	6	25409	255	79718718
Hallucination, visual	19.04	12.25	36	25379	32693	79686280
Product use complaint	18.74	12.25	11	25404	2472	79716501
Spinal cord haemorrhage	18.70	12.25	7	25408	567	79718406
Intercepted medication error	18.67	12.25	8	25407	921	79718052
Feeling abnormal	18.64	12.25	100	25315	159099	79559874
Loefgren syndrome	18.57	12.25	5	25410	137	79718836
Orthostatic hypotension	18.26	12.25	49	25366	56115	79662858
Pharyngeal mass	18.23	12.25	6	25409	332	79718641
Prescribed underdose	17.84	12.25	33	25382	29481	79689492
Multiple organ dysfunction syndrome	17.81	12.25	8	25407	120238	79598735
Bladder disorder	17.66	12.25	18	25397	9147	79709826
Treatment failure	17.61	12.25	17	25398	170469	79548504
Intentional medical device removal by patient	17.43	12.25	6	25409	381	79718592
Maternal exposure during pregnancy	17.41	12.25	11	25404	136527	79582446
Clubbing	17.20	12.25	7	25408	708	79718265
Lymphocyte count decreased	17.17	12.25	43	25372	47246	79671727
Pericarditis	16.97	12.25	6	25409	104230	79614743
Neutropenia	16.95	12.25	42	25373	287668	79431305
Bone marrow oedema	16.78	12.25	9	25406	1702	79717271
Dysstasia	16.74	12.25	31	25384	27715	79691258
Amnesia	16.61	12.25	51	25364	63006	79655967
Oesophageal dilatation	16.48	12.25	6	25409	449	79718524
COVID-19	16.43	12.25	96	25319	157578	79561395
Cardio-respiratory arrest	16.42	12.25	7	25408	108503	79610470
Hyperventilation	16.11	12.25	16	25399	7883	79711090
Pemphigus	15.76	12.25	6	25409	99576	79619397
Hip fracture	15.67	12.25	32	25383	30729	79688244
Leukopenia	15.39	12.25	9	25406	116504	79602469
Allergy to arthropod bite	15.29	12.25	5	25410	271	79718702
Persistent genital arousal disorder	15.20	12.25	5	25410	276	79718697
Disease progression	15.17	12.25	22	25393	184340	79534633
Breast disorder	15.14	12.25	9	25406	2072	79716901
Pyrexia	15.08	12.25	141	25274	678568	79040405
Febrile neutropenia	14.99	12.25	32	25383	230967	79488006
Infusion related reaction	14.86	12.25	32	25383	230205	79488768
Discomfort	14.84	12.25	11	25404	125606	79593367
Extradural haematoma	14.82	12.25	10	25405	2866	79716107
Urine albumin/creatinine ratio decreased	14.67	12.25	4	25411	115	79718858
Lip swelling	14.64	12.25	37	25378	40874	79678099
Dyskinesia	14.49	12.25	39	25376	44734	79674239
Synovitis	14.47	12.25	16	25399	150718	79568255
Somatic dysfunction	14.46	12.25	3	25412	25	79718948
Perineal pain	14.42	12.25	7	25408	1075	79717898
Drug hypersensitivity	14.41	12.25	48	25367	298868	79420105
Dropped head syndrome	14.24	12.25	5	25410	337	79718636
Blood pressure abnormal	14.09	12.25	22	25393	17147	79701826
Insomnia	13.86	12.25	129	25286	245041	79473932
Product use in unapproved indication	13.79	12.25	131	25284	250228	79468745
Concussion	13.66	12.25	16	25399	9487	79709486
Product dose omission issue	13.38	12.25	129	25286	247408	79471565
Freezing phenomenon	13.20	12.25	8	25407	1906	79717067
Muscle spasticity	12.96	12.25	24	25391	21451	79697522
Urine analysis abnormal	12.92	12.25	13	25402	6507	79712466
Magnetic resonance imaging head abnormal	12.91	12.25	9	25406	2717	79716256
Dementia with Lewy bodies	12.89	12.25	6	25409	840	79718133
VIIth nerve injury	12.80	12.25	4	25411	187	79718786
Rheumatoid arthritis	12.61	12.25	30	25385	208440	79510533
Impaired quality of life	12.60	12.25	19	25396	14367	79704606
Sensory loss	12.60	12.25	18	25397	12973	79706000
Lower urinary tract symptoms	12.41	12.25	4	25411	207	79718766
Diabetic ketosis	12.39	12.25	5	25410	495	79718478
Overdose	12.39	12.25	25	25390	184181	79534792
Acute kidney injury	12.36	12.25	106	25309	519298	79199675
Open fracture	12.34	12.25	5	25410	500	79718473
Blood bilirubin increased	12.26	12.25	3	25412	66229	79652744

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

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

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

🐶 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)

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
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
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
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
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	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

Orange Book exclusivity data (new drug applications)

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
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
8MG/ML	MYRBETRIQ GRANULES	APGDI	N213801	March 25, 2021	RX	FOR SUSPENSION, EXTENDED RELEASE	ORAL	March 25, 2024	NEW PRODUCT
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	Sept. 25, 2024	PEDIATRIC EXCLUSIVITY
8MG/ML	MYRBETRIQ GRANULES	APGDI	N213801	March 25, 2021	RX	FOR SUSPENSION, EXTENDED RELEASE	ORAL	Sept. 25, 2024	PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

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

External reference:

ID	Source
D09535	KEGG_DRUG
4031804	VANDF
CHEBI:65349	CHEBI
H6U	PDB_CHEM_ID
CHEMBL2095212	ChEMBL_ID
C520025	MESH_SUPPLEMENTAL_RECORD_UI
7445	IUPHAR_LIGAND_ID
8907	INN_ID
DB08893	DRUGBANK_ID
MVR3JL3B2V	UNII
1300786	RXNORM
191568	MMSL
28616	MMSL
d07876	MMSL
014540	NDDF
703803006	SNOMEDCT_US
703804000	SNOMEDCT_US
C2983812	UMLSCUI
9865528	PUBCHEM_CID

Pharmaceutical products:

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
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	55154-8712	TABLET, FILM COATED, EXTENDED RELEASE	25 mg	ORAL	NDA	27 sections
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	55154-8713	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	NDA	27 sections
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	55154-8713	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	NDA	27 sections
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	70518-2435	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	NDA	27 sections
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	70518-2435	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	NDA	27 sections
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	70518-2435	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	NDA	27 sections
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	70518-3158	TABLET, FILM COATED, EXTENDED RELEASE	25 mg	ORAL	NDA	27 sections
Myrbetriq	HUMAN PRESCRIPTION DRUG LABEL	1	70518-3158	TABLET, FILM COATED, EXTENDED RELEASE	25 mg	ORAL	NDA	27 sections