e-Drug3D

1549

M FESOTERODINE


INN
FESOTERODINE

(is an active metabolite)

cas 207679-81-0
CLASS

ANTISPASMODICS
ANTIMUSCARINIC
MUSCARINIC ANTAGONIST
OVERACTIVE BLADDER WITH SYMPTOMS OF URGE URINARY INCONTINENCE
URINARY ANTISPASMODICS
GENITO
HYDROLYSIS BY NONSPECIFIC ESTERASES

ROUTE (list)

-

ATC code

G04BD11

PK parameters

F 52 PERCENT
Tmax 1.8 HOUR
Cmax 11.6 NANOMOLAR (8 MILLIGRAM)
VD 169 LITER
Cl 13.6 LITER / HOUR (EQN)
PPB 50 PERCENT
t1/2 8.59 HOUR

Target

TARGET MUSCARINIC RECEPTOR

DrugCentral

Muscarinic acetylcholine receptor M2 UNIPROT P08172 CHRM2

Muscarinic acetylcholine receptor M3 UNIPROT P20309 CHRM3

Download SDF file Benzenemethanol, 3-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-hydroxy-

Formula:
C22H31NO2

Calculated chemical properties:

MW 341.48
NB_atoms 25
XLogP 4.53
PSA 46.686
NB_HD 2
NB_HA 3
fsp3 0.45
Lipinski(0=no;1=yes) 1

FDA
-

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL

e-Drug3D

800

TOLTERODINE


INN
TOLTERODINE

(has an active metabolite)

cas 124937-51-5
CLASS

GENITO
ANTICHOLINERGIC
ANTI-INCONTINENCE AGENTS
ANTISPASMODICS
GENITOURINARY SMOOTH MUSCLE RELAXANTS
MUSCARINIC RECEPTOR ANTAGONISTS

ROUTE (list)

ORAL

ATC code

G04BD07

PK parameters

Tmax 1.5 HOUR
Cmax 4.92 NANOMOLAR
VD 113 LITER
Cl 534 LITER / HOUR
PPB 96.3 PERCENT
t1/2 2 HOUR

Solubility

IN WATER 12 MILLIGRAM / MILLILITER


Target

TARGET MUSCARINIC ACETYLCHOLINE RECEPTOR

DrugCentral

Muscarinic acetylcholine receptor M2 UNIPROT P08172 CHRM2

Muscarinic acetylcholine receptor M3 UNIPROT P20309 CHRM3

Download SDF file 2-[(1S)-3-(di(propan-2-yl)amino)-1-phenylpropyl]-4-methylphenol

Formula:
C22H31NO

Calculated chemical properties:

MW 325.48
NB_atoms 24
XLogP 5.34
PSA 25.324
NB_HD 1
NB_HA 2
fsp3 0.45
Lipinski(0=no;1=yes) 0

FDA
NDA 020771 (label) INN (TOLTERODINE TARTRATE) DETROL (UPJOHN) APPROVAL= AP YEAR= 1998 NEWMOLECULARENTITY
NDA 021228 (label) INN (TOLTERODINE TARTRATE) DETROL LA (UPJOHN) APPROVAL= AP YEAR= 2000
NDA 076953 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE (RANBAXY) APPROVAL= TA YEAR= 2005
NDA 078419 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (SANDOZ) APPROVAL= TA YEAR= 2011
NDA 200164 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (APOTEX CORP) APPROVAL= AP YEAR= 2012 DISCONTINUED
NDA 202641 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (PHARMOBEDIENT) APPROVAL= AP YEAR= 2012 DISCONTINUED
NDA 201486 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (AUROBINDO PHARMA USA) APPROVAL= AP YEAR= 2013 DISCONTINUED
NDA 077006 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (IVAX SUB TEVA PHARMS) APPROVAL= AP YEAR= 2015
NDA 203016 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (TORRENT) APPROVAL= AP YEAR= 2015
NDA 203409 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (MACLEODS PHARMS LTD) APPROVAL= AP YEAR= 2015
NDA 079141 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (TEVA PHARMS USA) APPROVAL= AP YEAR= 2016
NDA 206419 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (HETERO LABS LTD III) APPROVAL= AP YEAR= 2017
NDA 204562 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (INVENTIA HLTHCARE) APPROVAL= AP YEAR= 2019
NDA 210775 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (RISING) APPROVAL= AP YEAR= 2019
NDA 204721 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (UNIQUE) APPROVAL= AP YEAR= 2020
NDA 213397 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (AJANTA PHARMA LTD) APPROVAL= AP YEAR= 2020
NDA 205399 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (UNICHEM) APPROVAL= AP YEAR= 2020
NDA 213858 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (UTOPIC PHARMS) APPROVAL= AP YEAR= 2021
NDA 204397 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (HETERO LABS LTD V) APPROVAL= AP YEAR= 2021
NDA 216917 (pdf not found) INN (TOLTERODINE TARTRATE) TOLTERODINE TARTRATE (UNICHEM) APPROVAL= AP YEAR= 2024

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL

e-Drug3D

1452

FESOTERODINE


INN
FESOTERODINE

(has an active metabolite)

cas 286930-02-7
CLASS

ANTISPASMODICS
ANTIMUSCARINIC
MUSCARINIC ANTAGONIST
OVERACTIVE BLADDER WITH SYMPTOMS OF URGE URINARY INCONTINENCE
URINARY ANTISPASMODICS
GENITO
HYDROLYSIS BY NONSPECIFIC ESTERASES

ROUTE (list)

ORAL

ATC code

G04BD11

PK parameters

Solubility

FREELY SOLUBLE IN WATER


Target

TARGET MUSCARINIC RECEPTOR ANTAGONIST

DrugCentral

Muscarinic acetylcholine receptor M2 UNIPROT P08172 CHRM2

Muscarinic acetylcholine receptor M3 UNIPROT P20309 CHRM3

Download SDF file Propanoic acid, 2-methyl-, 2-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl ester

Formula:
C26H37NO3

Calculated chemical properties:

MW 411.57
NB_atoms 30
XLogP 5.38
PSA 47.623
NB_HD 1
NB_HA 4
fsp3 0.50
Lipinski(0=no;1=yes) 0

FDA
NDA 022030 (label) INN (FESOTERODINE FUMARATE) TOVIAZ (PFIZER) APPROVAL= AP YEAR= 2008
NDA 204844 (pdf not found) INN (FESOTERODINE FUMARATE) FESOTERODINE FUMARATE (SANDOZ INC) APPROVAL= TA YEAR= 2015
NDA 204893 (pdf not found) INN (FESOTERODINE FUMARATE) FESOTERODINE FUMARATE (LUPIN LTD) APPROVAL= TA YEAR= 2015 OBSOLETE
NDA 205032 (pdf not found) INN (FESOTERODINE FUMARATE) FESOTERODINE FUMARATE (SUN PHARM INDS INC) APPROVAL= TA YEAR= 2015
NDA 204827 (pdf not found) INN (FESOTERODINE FUMARATE) FESOTERODINE FUMARATE (ALKEM LABS LTD) APPROVAL= AP YEAR= 2015
NDA 205007 (pdf not found) INN (FESOTERODINE FUMARATE) FESOTERODINE FUMARATE (AUROBINDO PHARMA) APPROVAL= AP YEAR= 2017
NDA 204946 (pdf not found) INN (FESOTERODINE FUMARATE) FESOTERODINE FUMARATE (ZYDUS PHARMS) APPROVAL= AP YEAR= 2017
NDA 204975 (pdf not found) INN (FESOTERODINE FUMARATE) FESOTERODINE FUMARATE (DR REDDYS) APPROVAL= AP YEAR= 2019
NDA 204504 (pdf not found) INN (FESOTERODINE FUMARATE) FESOTERODINE FUMARATE (ANI PHARMS) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 204868 (pdf not found) INN (FESOTERODINE FUMARATE) FESOTERODINE FUMARATE (ACTAVIS LABS FL INC) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 204973 (pdf not found) INN (FESOTERODINE FUMARATE) FESOTERODINE FUMARATE (ALEMBIC) APPROVAL= AP YEAR= 2023
NDA 204983 (pdf not found) INN (FESOTERODINE FUMARATE) FESOTERODINE FUMARATE (CHARTWELL RX) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 205002 (pdf not found) INN (FESOTERODINE FUMARATE) FESOTERODINE FUMARATE (AMNEAL PHARMS NY) APPROVAL= AP YEAR= 2023
NDA 205012 (pdf not found) INN (FESOTERODINE FUMARATE) FESOTERODINE FUMARATE (ACCORD HLTHCARE) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 204792 (pdf not found) INN (FESOTERODINE FUMARATE) FESOTERODINE FUMARATE (HETERO LABS LTD V) APPROVAL= AP YEAR= 2024

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL