Page last updated: 2024-12-11

pnu 200577

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

5-hydroxymethyl tolterodine: a metabolite of tolterodine [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9819382
CHEMBL ID3348932
CHEBI ID177454
SCHEMBL ID209062
MeSH IDM0285124

Synonyms (62)

Synonym
HY-76569
207679-81-0
CHEBI:177454
desfesoterodine
2-[(1r)-3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenol
AKOS015841720
spm-7605
5-hmt
pnu-200577 ,
dd 01
AKOS005146249
(r)-5-hydroxymethyl tolterodine
3-[(1r)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-hydroxybenzenemethanol
(r)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol
pnu 200577
pnu200577
BCP0726000296
NCGC00346585-01
CS-0825
S2659
SCHEMBL209062
(r)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol
(r)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenol
(r)-4-hydroxymethyl-2-(3-diisopropylamino-1-phenylpropyl)-phenol
DUXZAXCGJSBGDW-HXUWFJFHSA-N
(r)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxy methyl phenol
(r)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxy methylphenol
(+)-n,n-diisopropyl-3-(2-hydroxy-5-hydroxymethylphenyl)-3-phenylpropylamine
r-5-hydroxymethyl tolterodine
desfesoterodine [who-dd]
desfesoterodine [inn]
yu871o78gr ,
benzenemethanol, 3-((1r)-3-(bis(1-methylethyl)amino)-1-phenylpropyl)-4-hydroxy-
5-hydroxymethyltolterodine
unii-yu871o78gr
(r)-(+)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenol
5-hydroxymethyl tolterodine (pnu 200577, 5-hmt, 5-hm)
AC-23943
(r)-5-hydroxymethyltolterodine
DTXSID40431319
intermediate of fesoterodine
spm 7605
CHEMBL3348932
5-hm
5-hydroxymethyl tolterodine
F31141
desfesoterodine (inn)
D10853
J-013606
SW219846-1
desfesoterodin
5-hydroxymethyl tolterodine (pnu 200577)
DB15578
BS-15813
BCP02922
mfcd09264524
HMS3884P12
5-hydroxymethyl-tolterodine
CCG-267936
benzenemethanol, 3-[(1r)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-hydroxy-
Q27294711
207679-81-0 (free base)

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic assessments were performed on day 14 based on plasma levels of ethinyl estradiol and levonorgestrel up to 24 hours after dosing and serum tolterodine levels at 1 to 3 hours after dosing."( The effect of tolterodine on the pharmacokinetics and pharmacodynamics of a combination oral contraceptive containing ethinyl estradiol and levonorgestrel.
Landgren, BM; Olsson, B, 2001
)
0.31
" There was no evidence of a pharmacokinetic interaction between tolterodine and the steroid hormones in the oral contraceptive used, nor did the oral contraceptive show any relevant pharmacokinetic interaction with tolterodine."( The effect of tolterodine on the pharmacokinetics and pharmacodynamics of a combination oral contraceptive containing ethinyl estradiol and levonorgestrel.
Landgren, BM; Olsson, B, 2001
)
0.31
" The peak concentration ratios for oxybutynin and metabolite also conformed to this range; those for tolterodine did not."( Effect of the proton pump inhibitor omeprazole on the pharmacokinetics of extended-release formulations of oxybutynin and tolterodine.
Chen, A; Dmochowski, R; Gidwani, S; Gupta, S; MacDiarmid, S; Sathyan, G, 2005
)
0.33
" The mean Cmax and AUC0-t in PMs were approximately twice those observed in EMs."( Pharmacokinetic profile of fesoterodine.
Gandelman, K; Guan, Z; Malhotra, B; Wood, N, 2008
)
0.35
"Fesoterodine demonstrated a pharmacokinetic (PK) profile that was favorable for once-daily dosing."( Pharmacokinetic profile of fesoterodine.
Gandelman, K; Guan, Z; Malhotra, B; Wood, N, 2008
)
0.35
"This head-to-head study confirmed the findings of reduced pharmacokinetic variability of fesoterodine and further delineates that tolterodine, and not 5-HMT, was the principal source of variability after administration of tolterodine extended release."( Comparison of pharmacokinetic variability of fesoterodine vs. tolterodine extended release in cytochrome P450 2D6 extensive and poor metabolizers.
Crownover, P; Darsey, E; Fang, J; Glue, P; Malhotra, B, 2011
)
0.37
" Ten pharmacokinetic studies and three efficacy/safety studies in overactive bladder (OAB) patients were pooled for the population pharmacokinetic analysis."( Population pharmacokinetics of the 5-hydroxymethyl metabolite of tolterodine after administration of fesoterodine sustained release tablet in Western and East Asian populations.
Malhotra, B; Oishi, M; Tomono, Y; Yamagami, H, 2014
)
0.4
" Potential drug-drug interactions (DDIs) following coadministration of these 2 overactive bladder treatments were estimated using physiologically based pharmacokinetic models, developed and verified by comparing predicted and observed pharmacokinetic profiles from clinical studies."( Physiologically Based Pharmacokinetic Modeling Suggests Limited Drug-Drug Interaction for Fesoterodine When Coadministered With Mirabegron.
Goosen, TC; Lin, J; Malhotra, B; Tse, S; Yamagami, H, 2019
)
0.51

Compound-Compound Interactions

ExcerptReferenceRelevance
" Potential drug-drug interactions (DDIs) following coadministration of these 2 overactive bladder treatments were estimated using physiologically based pharmacokinetic models, developed and verified by comparing predicted and observed pharmacokinetic profiles from clinical studies."( Physiologically Based Pharmacokinetic Modeling Suggests Limited Drug-Drug Interaction for Fesoterodine When Coadministered With Mirabegron.
Goosen, TC; Lin, J; Malhotra, B; Tse, S; Yamagami, H, 2019
)
0.51

Bioavailability

ExcerptReferenceRelevance
"This study assessed the effect of the proton pump inhibitor omeprazole on the bioavailability of the extended-release formulations of oxybutynin and tolterodine."( Effect of the proton pump inhibitor omeprazole on the pharmacokinetics of extended-release formulations of oxybutynin and tolterodine.
Chen, A; Dmochowski, R; Gidwani, S; Gupta, S; MacDiarmid, S; Sathyan, G, 2005
)
0.33
" A prodrug approach was necessary for systemic bioavailability of 5-HMT after oral administration."( The design and development of fesoterodine as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of tolterodine.
Gandelman, K; Malhotra, B; Michel, MC; Sachse, R; Wood, N, 2009
)
0.35
" We estimated the relative bioavailability of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of fesoterodine, following nighttime and daytime administration."( The pharmacokinetic profile of fesoterodine 8 mg with daytime or nighttime dosing.
Crownover, PH; Glue, P; LaBadie, R; MacDiarmid, SA; Malhotra, BK, 2010
)
0.36
" The data suggest that fesoterodine delivers 5-HMT consistently, regardless of CYP2D6 status, with up to 40% higher bioavailability compared with tolterodine."( Comparison of pharmacokinetic variability of fesoterodine vs. tolterodine extended release in cytochrome P450 2D6 extensive and poor metabolizers.
Crownover, P; Darsey, E; Fang, J; Glue, P; Malhotra, B, 2011
)
0.37
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Pharmacokinetic assessments were performed on day 14 based on plasma levels of ethinyl estradiol and levonorgestrel up to 24 hours after dosing and serum tolterodine levels at 1 to 3 hours after dosing."( The effect of tolterodine on the pharmacokinetics and pharmacodynamics of a combination oral contraceptive containing ethinyl estradiol and levonorgestrel.
Landgren, BM; Olsson, B, 2001
)
0.31
" At least partially due to the avoidance of variations in pharmacokinetic exposures observed with tolterodine, it was possible to develop fesoterodine with the flexibility of two efficacious and well-tolerated dosage regimens of 4 and 8 mg daily."( The design and development of fesoterodine as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of tolterodine.
Gandelman, K; Malhotra, B; Michel, MC; Sachse, R; Wood, N, 2009
)
0.35
"In this randomized, open-label, two-period, two-treatment crossover, single-dose study, healthy subjects received daytime and nighttime oral dosing of fesoterodine 8-mg sustained-release tablets, separated by a minimum 60-h washout period."( The pharmacokinetic profile of fesoterodine 8 mg with daytime or nighttime dosing.
Crownover, PH; Glue, P; LaBadie, R; MacDiarmid, SA; Malhotra, BK, 2010
)
0.36
" The 21% reduction in the C(max) for nighttime dosing is unlikely to be clinically relevant."( The pharmacokinetic profile of fesoterodine 8 mg with daytime or nighttime dosing.
Crownover, PH; Glue, P; LaBadie, R; MacDiarmid, SA; Malhotra, BK, 2010
)
0.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
diarylmethaneAny compound containing two aryl groups connected by a single C atom.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (29)

Assay IDTitleYearJournalArticle
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (33)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's4 (12.12)18.2507
2000's6 (18.18)29.6817
2010's17 (51.52)24.3611
2020's6 (18.18)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.18

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.18 (24.57)
Research Supply Index3.76 (2.92)
Research Growth Index4.94 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.18)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials9 (27.27%)5.53%
Reviews1 (3.03%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other23 (69.70%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]