5-hydroxymethyl tolterodine: a metabolite of tolterodine
ID Source | ID |
---|---|
PubMed CID | 9819382 |
CHEMBL ID | 3348932 |
CHEBI ID | 177454 |
SCHEMBL ID | 209062 |
MeSH ID | M0285124 |
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) |
Excerpt | Reference | Relevance |
---|---|---|
" 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 |
Excerpt | Reference | Relevance |
---|---|---|
" 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 |
Excerpt | Relevance | Reference |
---|---|---|
" 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 |
Class | Description |
---|---|
diarylmethane | Any 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] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, 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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 4 (12.12) | 18.2507 |
2000's | 6 (18.18) | 29.6817 |
2010's | 17 (51.52) | 24.3611 |
2020's | 6 (18.18) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (11.18) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 9 (27.27%) | 5.53% |
Reviews | 1 (3.03%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 23 (69.70%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |