Page last updated: 2024-12-07

idarubicinol

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

Description

idarubicinol: RN given refers to (7S-(7alpha,9alpha,9(R*))-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID21118312
CHEBI ID197279
SCHEMBL ID13147738
MeSH IDM0153726

Synonyms (7)

Synonym
idarubicinol
(7s,9s)-7-[(2r,4s,5s,6s)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy-6,9,11-trihydroxy-9-[(1s)-1-hydroxyethyl]-8,10-dihydro-7h-tetracene-5,12-dione
CHEBI:197279
z3gyr877xq ,
SCHEMBL13147738
(9s)-7-((2r,4s,5s,6s)-4-amino-5-hydroxy-6-methyltetrahydro-2h-pyran-2-yloxy)-6,9,11-trihydroxy-9-((s)-1-hydroxyethyl)-7,8,9,10-tetrahydrotetracene-5,12-dione
(7s,9s)-7-[(3-amino-2,3,6-trideoxy-alpha-l-lyxo-hexopyranosyl)oxy]-7,8,9,10-tetrahydro-6,9,11-trihydroxy-9-[(1r*)-1-hydroxyethyl]-5,12-naphthacenedione

Research Excerpts

Pharmacokinetics

The ratio of the areas under the curve (0-24) idarubicinol/idarubICin increased from day to day. Due to its protracted half-life (64 hr) this metabolite progressively accumulated.

ExcerptReferenceRelevance
" The IDAol terminal half-life and mean residence time (MRT) were significantly increased in patients with impaired kidney function [MRT: group N, 63."( Idarubicin metabolism and pharmacokinetics after intravenous and oral administration in cancer patients: a crossover study.
Camaggi, CM; Carisi, P; Efthymiopoulos, C; Guaraldi, M; Martoni, A; Pannuti, F; Strocchi, E; Strolin-Benedetti, M; Tononi, A, 1992
)
0.28
" Due to its protracted half-life (64 hr in this study), this metabolite progressively accumulated and the ratio of the areas under the curve (0-24) idarubicinol/idarubicin increased from day to day."( Pharmacokinetics of idarubicin after oral administration in elderly leukemic patients.
Huet, S; Hurteloup, P; Pris, J; Rigal-Huguet, F; Robert, J, 1990
)
0.28
" There was substantial variability in idarubicin elimination among patients, but no indication of dose-dependent or of schedule-dependent changes in pharmacokinetic parameters."( Plasma pharmacokinetics and cerebrospinal fluid concentrations of idarubicin and idarubicinol in pediatric leukemia patients: a Childrens Cancer Study Group report.
Ames, MM; Hammond, GD; Krailo, MD; Pendergrass, TW; Reid, JM, 1990
)
0.28
" No correlation was found between the pharmacokinetic parameters and the time to final progression."( Pharmacokinetics of oral idarubicin in breast cancer patients with reference to antitumor activity and side effects.
Bastholt, L; Dalmark, M; Ebbehøj, E; Elbaek, K; Jakobsen, A; Juul, P; Rasmussen, SN; Steiness, E, 1989
)
0.28
" For unchanged idarubicin, similar pharmacokinetic parameters were exhibited after the 1st and the 5th injection."( Pharmacokinetics of idarubicin after daily intravenous administration in leukemic patients.
Harousseau, JL; Huet, S; Hurteloup, P; Pris, J; Reiffers, J; Rigal-Huguet, F; Robert, J; Tamassia, V, 1987
)
0.27
" Although idarubicin was given in one-fifth of the dose, the intracellular peak concentration was 70% of that of daunorubicin."( Comparison of the intracellular pharmacokinetics of daunorubicin and idarubicin in patients with acute leukemia.
Paul, C; Sundman-Engberg, B; Tidefelt, U, 1994
)
0.29
" The average terminal half-life was 30."( Oral idarubicin pharmacokinetics--correlation of trough level with idarubicin area under curve.
Braess, J; Hiddemann, W; Kaufmann, CC; Kern, W; Kühn, S; Rührs, H; Schleyer, E; Sträubel, G; Unterhalt, M, 1996
)
0.29
" The plasma concentration time course of Ida was most properly described by the three-compartment pharmacokinetic model, independent of administration time."( Plasma pharmacokinetics of idarubicin and its 13-dihydro metabolite--a comparison of bolus versus 2 h infusion during a 3 day course.
Björkholm, M; Eksborg, S; Fagerlund, E; Hast, R, 1997
)
0.3
" The average terminal half-life was 30."( Oral idarubicin pharmacokinetics--correlation of trough level with idarubicin area under curve.
Braess, J; Hiddemann, W; Kaufmann, CC; Kern, W; Kühn, S; Rührs, H; Schleyer, E; Sträubel, G; Unterhalt, M, 1997
)
0.3
" With respect to cellular resistance mechanisms, 2 different pharmacodynamic phases can be distinguished: intracellular distribution and cellular reaction."( Intracellular pharmacokinetics of anthracyclines in human leukemia cells: correlation of DNA-binding with apoptotic cell death.
Brieden, T; Gieseler, F; Kunze, J; Nüssler, V; Valsamas, S, 1998
)
0.3
" Various pharmacokinetic profiles, with and without clinically relevant peak concentrations, were simulated in vitro."( Induction of apoptosis by idarubicin: how important is the plasma peak?
Clark, M; Gieseler, F; Puschmann, M; Stiebeling, K; Valsamas, S, 2000
)
0.31
" We simulated a bolus application and a continuous infusion using two different pharmacokinetic profiles of idarubicin with comparable AUCs (area under the time curve)."( Induction of apoptosis by idarubicin: how important is the plasma peak?
Clark, M; Gieseler, F; Puschmann, M; Stiebeling, K; Valsamas, S, 2000
)
0.31
"To clarify the pharmacokinetic properties of idarubicin (IDA) in Japanese patients and to clarify the relationship between the pharmacokinetic parameters of IDA or idarubicinol (IDAol), an active metabolite of IDA, and leukocytopenia or neutropenia, we examined the pharmacokinetics of IDA in patients with malignant lymphoma."( A pharmacokinetic study of idarubicin in Japanese patients with malignant lymphoma: relationship with leukocytopenia and neutropenia.
Fukushima, T; Goto, N; Kuraishi, Y; Ogawa, M; Ohno, R; Okabe, KI; Ueda, T; Urabe, A; Yamashita, T, 2001
)
0.31
" The plasma concentration-time data were analysed, assuming a biexponential disposition curve, both by the traditional (two-stage) method and by population pharmacokinetic modelling."( Pharmacokinetics and toxicity of idarubicin in the rat.
Hofmann, S; Kuhlmann, O; Weiss, M,
)
0.13
" The pharmacokinetic parameters of idarubicin found after duodenal administration of the two formulations were different: area under the curve of concentration versus time (AUC) and elimination half-life were approximately 21 times and 30 times, respectively, higher after IDA-SLN administration than after the solution administration."( Pharmacokinetics and tissue distribution of idarubicin-loaded solid lipid nanoparticles after duodenal administration to rats.
Bargoni, A; Cavalli, R; Fundarò, A; Gasco, MR; Vighetto, D; Zara, GP, 2002
)
0.31

Compound-Compound Interactions

ExcerptReferenceRelevance
" In this work we compared in vitro the effects of IDA and 2HIDA used alone and in combination with 2 microM cyclosporin A (CyA) in the MDR leukemic cell lines FLCR and K562R and in their sensitive parent cell lines FLC and K562."( Comparative activity of idarubicin and idarubicinol in combination with cyclosporin A in multidrug-resistant leukemia cells.
Abbadessa, V; Cajozzo, A; Gancitano, RA; Musso, M; Perricone, R; Porretto, F; Tolomeo, M, 1996
)
0.29

Bioavailability

ExcerptReferenceRelevance
" administration of the drug in another study, the bioavailability of idarubicin alone can be estimated to about 21%, whereas the bioavailability of the sum idarubicin + idarubicinol is about 41%."( Pharmacokinetics of idarubicin after oral administration in elderly leukemic patients.
Huet, S; Hurteloup, P; Pris, J; Rigal-Huguet, F; Robert, J, 1990
)
0.28
" dose, and the bioavailability of the oral dose ranged between 9% and 39%."( Pharmacokinetics of 4-demethoxydaunorubicin in cancer patients.
D'Incalci, M; Erranti, D; Freshi, A; Tirelli, U; Zanette, L; Zucchetti, M, 1990
)
0.28
" These perspectives are somewhat hampered by the large variation in bioavailability between individual patients and the obvious requirement to monitor plasma concentration and area-under the curve values (AUC) for an appropriate adjustment of idarubicin dose."( Oral idarubicin pharmacokinetics--correlation of trough level with idarubicin area under curve.
Braess, J; Hiddemann, W; Kaufmann, CC; Kern, W; Kühn, S; Rührs, H; Schleyer, E; Sträubel, G; Unterhalt, M, 1996
)
0.29
" These perspectives are somewhat hampered by the large variation in bioavailability between individual patients and the obvious requirement to monitor plasma concentration and area-under-the-curve values (AUC) for an appropriate adjustment of idarubicin dose."( Oral idarubicin pharmacokinetics--correlation of trough level with idarubicin area under curve.
Braess, J; Hiddemann, W; Kaufmann, CC; Kern, W; Kühn, S; Rührs, H; Schleyer, E; Sträubel, G; Unterhalt, M, 1997
)
0.3
" The aim of this research was to study whether the bioavailability of idarubicin can be improved by administering IDA-SLN duodenally to rats."( Pharmacokinetics and tissue distribution of idarubicin-loaded solid lipid nanoparticles after duodenal administration to rats.
Bargoni, A; Cavalli, R; Fundarò, A; Gasco, MR; Vighetto, D; Zara, GP, 2002
)
0.31

Dosage Studied

ExcerptRelevanceReference
"We evaluated in vitro the toxicity of idarubicin and its active metabolite idarubicinol on haematopoietic progenitors, using human umbilical cord blood and peripheral blood progenitors to obtain dose-response curves."( Idarubicinol myelotoxicity: a comparison of in vitro data with clinical outcome in patients treated with high-dose idarubicin.
Cocorocchio, E; Corsini, C; D'Incalci, M; Ferrucci, PF; Ghielmini, M; Mancuso, P; Martinelli, G; Mezzetti, M; Mori, A; Paolucci, M; Riggi, M; Tealdo, F; Zucchetti, M, 2000
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
anthracyclineAnthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.
[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]

Research

Studies (51)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (9.80)18.7374
1990's31 (60.78)18.2507
2000's15 (29.41)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (18.52%)5.53%
Reviews1 (1.85%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other43 (79.63%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]