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

Stem definition	Drug id	CAS RN
muscarinic receptors antagonists	2457	242478-37-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: YM-67905 YM-905 solifenacin solifenacin succinate vesicare	A quinuclidine and tetrahydroisoquinoline derivative and selective M3 MUSCARINIC ANTAGONIST. It is used as a UROLOGIC AGENT in the treatment of URINARY INCONTINENCE. Molecular weight: 362.47 Formula: C23H26N2O2 CLOGP: 4.68 LIPINSKI: 0 HAC: 4 HDO: 0 TPSA: 32.78 ALOGS: -3.70 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

YM-67905
YM-905
solifenacin
solifenacin succinate
vesicare

A quinuclidine and tetrahydroisoquinoline derivative and selective M3 MUSCARINIC ANTAGONIST. It is used as a UROLOGIC AGENT in the treatment of URINARY INCONTINENCE.

Molecular weight: 362.47
Formula: C23H26N2O2
CLOGP: 4.68
LIPINSKI: 0
HAC: 4
HDO: 0
TPSA: 32.78
ALOGS: -3.70
ROTB: 3

Status: OFP

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

Drug dosage:

Dose	Unit	Route
5	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	90 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	8.20 L/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	52 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2.10 mL/min/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	12.50 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.30 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Nov. 19, 2004	FDA	ASTELLAS

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
Dry mouth	172.48	11.55	183	25243	77680	63385916
Multiple sclerosis relapse	136.85	11.55	130	25296	48348	63415248
Fall	118.20	11.55	385	25041	391949	63071647
Urinary retention	116.90	11.55	97	25329	30204	63433392
Urinary tract infection	85.24	11.55	266	25160	264418	63199178
Urinary incontinence	84.94	11.55	83	25343	31931	63431665
Vision blurred	71.00	11.55	130	25296	91794	63371802
Dementia	70.07	11.55	59	25367	18735	63444861
Residual urine volume increased	63.20	11.55	12	25414	45	63463551
Multiple sclerosis	62.44	11.55	62	25364	24310	63439286

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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	106.94	14.32	90	10990	36198	34909653
Confusional state	79.34	14.32	154	10926	144006	34801845
Dry mouth	79.08	14.32	70	11010	30095	34915756
Hallucination	62.07	14.32	79	11001	51419	34894432
Fall	59.10	14.32	169	10911	202716	34743135
Constipation	54.13	14.32	128	10952	136854	34808997
Duplicate therapy error	41.67	14.32	10	11070	171	34945680
Urinary incontinence	40.15	14.32	39	11041	18835	34927016
Urinary tract infection	38.09	14.32	83	10997	83998	34861853
Gastrointestinal hypomotility	34.71	14.32	13	11067	1060	34944791

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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
Fall	141.99	11.28	454	29556	487175	79227203
Urinary retention	139.46	11.28	137	29873	56493	79657885
Dry mouth	125.38	11.28	160	29850	87859	79626519
Multiple sclerosis relapse	107.96	11.28	109	29901	46424	79667954
Urinary tract infection	91.24	11.28	268	29742	274244	79440134
Urinary incontinence	89.76	11.28	93	29917	40816	79673562
Confusional state	76.41	11.28	278	29732	317719	79396659
Hallucination	66.10	11.28	117	29893	85628	79628750
Multiple sclerosis	64.54	11.28	59	29951	22223	79692155
Constipation	61.77	11.28	240	29770	282810	79431568

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	G04BD08	GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS UROLOGICALS Drugs for urinary frequency and incontinence
ATC	G04CA53	GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS DRUGS USED IN BENIGN PROSTATIC HYPERTROPHY Alpha-adrenoreceptor antagonists
FDA EPC	N0000175700	Cholinergic Muscarinic Antagonist
FDA MoA	N0000000125	Cholinergic Muscarinic Antagonists
MeSH PA	D018678	Cholinergic Agents
MeSH PA	D018680	Cholinergic Antagonists
MeSH PA	D018727	Muscarinic Antagonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D064804	Urological Agents

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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
Urgent desire to urinate	indication	75088002
Urge incontinence of urine	indication	87557004
Bladder muscle dysfunction - overactive	indication	236633002
Increased Urinary Frequency	indication
Torsades de pointes	contraindication	31722008
Acute nephropathy	contraindication	58574008
Hepatic failure	contraindication	59927004
Prolonged QT interval	contraindication	111975006
Gastrointestinal obstruction	contraindication	126765001
Disease of liver	contraindication	235856003	DOID:409

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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	8.21	Basic

Orange Book patent data (new drug applications)

None

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
1MG/ML	VESICARE LS	ASTELLAS	N209529	May 26, 2020	RX	SUSPENSION	ORAL	May 26, 2023	NEW PRODUCT
1MG/ML	VESICARE LS	ASTELLAS	N209529	May 26, 2020	RX	SUSPENSION	ORAL	Nov. 26, 2023	PEDIATRIC EXCLUSIVITY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN	ANTAGONIST	IC50	6.88	CHEMBL	CHEMBL
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN	ANTAGONIST	IC50	6.24	CHEMBL	CHEMBL
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN	ANTAGONIST	Ki	7.20	IUPHAR
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		IC50	7.20	CHEMBL
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN	ANTAGONIST	Ki	6.80	IUPHAR
Muscarinic acetylcholine receptor M2	GPCR		ACM2_RAT		Ki	6.92	CHEMBL
Muscarinic acetylcholine receptor M1	GPCR		ACM1_RAT		Ki	8	CHEMBL
Muscarinic acetylcholine receptor M3	GPCR		ACM3_RAT		Ki	8	CHEMBL

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External reference:

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ID	Source
008712	NDDF
008713	NDDF
154059	PUBCHEM_CID
19082	MMSL
242478-38-2	SECONDARY_CAS_RN
256920	MMSL
322167	RXNORM
4021510	VANDF
4024390	VUID
4024390	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Solifenacin Succinate	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1933	TABLET, FILM COATED	5 mg	ORAL	ANDA	26 sections
Solifenacin Succinate	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1934	TABLET, FILM COATED	10 mg	ORAL	ANDA	26 sections
Solifenacin succinate	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3795	TABLET, FILM COATED	5 mg	ORAL	ANDA	26 sections
Solifenacin succinate	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3795	TABLET, FILM COATED	5 mg	ORAL	ANDA	26 sections
Solifenacin succinate	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3795	TABLET, FILM COATED	5 mg	ORAL	ANDA	26 sections
Solifenacin succinate	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3796	TABLET, FILM COATED	10 mg	ORAL	ANDA	26 sections
Solifenacin succinate	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3796	TABLET, FILM COATED	10 mg	ORAL	ANDA	26 sections
Solifenacin succinate	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3796	TABLET, FILM COATED	10 mg	ORAL	ANDA	26 sections
solifenacin succinate	Human Prescription Drug Label	1	27241-037	TABLET, FILM COATED	5 mg	ORAL	ANDA	26 sections
solifenacin succinate	Human Prescription Drug Label	1	27241-038	TABLET, FILM COATED	10 mg	ORAL	ANDA	26 sections

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