Pharmacokinetics of idarubicin (4‐demethoxydaunorubicin; IMI‐30; NSC 256439) following intravenous and oral administration in patients with advanced cancer.

Gillies, HC; Herriott, D; Liang, Raymond; Ohashi, Kazushi; Rogers, H. J.; Harper, P.

doi:10.1111/j.1365-2125.1987.tb03049.x

Cited by 41 publications

(7 citation statements)

References 11 publications

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“…Computation of the published results gives a bioavailability value for drug plus metabolite of 45, 36,40, 43, 41 and 34%, respectively, in the works of Berman et al (1983), Speth et al (1986), Smith et al (1987), Gillies et al (1987), Eksborg et al (1990) and Robert et al (1990), and were 46 and 48% in the works of Camaggi et al (1992) and Zanette et al (1990), respectively. This indicates that the ratio of oral dose: intravenous doses necessary to obtain similar total AVC values (and potentially similar drug effects) must be 2.5 to 3: I.…”

Section: Bioavailabilitymentioning

confidence: 97%

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Clinical Pharmacokinetics of Idarubicin

Robert

1993

Clinical Pharmacokinetics

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Idarubicin (4-demethoxy-daunorubicin) is a new commercially available anthracycline antibiotic which is more active than daunorubicin, the accepted reference drug, in the treatment of acute myelogenous leukaemia, which generally involves the combination of an anthracycline and cytarabine [corrected]. It is characterised by metabolic transformation into a 13-dihydro derivative, idarubicinol, which is as active as the parent drug in in vitro models. The pharmacokinetics of idarubicin follow a 2- or 3-compartment plasma disappearance with half-life (t1/2) values of 13 min, 2.4h and 16h, clearance approximately 60 L/h/m2 and volume of distribution at steady-state of 1,500 L/m2. Idarubicinol is characterised by a very long elimination t1/2 of 55h. The ratio of metabolite: parent drug area under the plasma concentration-time curve is often > 2 and is even higher after 2 or 3 daily injections of the drug, the normal drug protocol used in induction or consolidation treatments of acute leukaemias. Idarubicin can also be administered orally and the pharmacokinetics are similar to those after intravenous administration, except that the idarubicinol: idarubicin ratio is increased, probably due to a liver first-pass effect. The bioavailability of idarubicin is 20 to 25%, but if the activity of idarubicinol is taken into account, it is effectively about 40%. After idarubicin administration by either route, there is a progressive accumulation of idarubicinol after multiple once-daily but not after once-weekly doses. About 10% of the injected dose is recovered in urine as idarubicin and idarubicinol, and only slightly higher proportions are recovered in bile. This suggests that other unidentified metabolites must be excreted by either or by both pathways.

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Section: Bioavailabilitymentioning

confidence: 97%

“…In comparative noncrossover studies, values of 23, 30, 21 and 21 % were obtained by Eksborg et al (1990), Gillies et al (1987), Robert et al (1990) and Speth et al (1986), respectively. All the results were calculated on the basis of idarubicin alone.…”

Section: Bioavailabilitymentioning

confidence: 99%

Clinical Pharmacokinetics of Idarubicin

Robert

1993

Clinical Pharmacokinetics

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“…Idarubicin (4‐demethoxydaunorubicin) is an anthracycline agent that is more lipid soluble than daunorubicin or doxorubicin 1. The drug is available for administration by the intravenous (iv) and oral routes, and is rapidly absorbed following oral administration, with drug concentrations detectable in the plasma within 30 min 2,3. Idarubicin differs from daunorubicin and doxorubicin, which are not absorbed to any appreciable degree following oral administration.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics and Tissue Distribution of Idarubicin-Loaded Solid Lipid Nanoparticles After Duodenal Administration to Rats

Zara

Bargoni

Cavalli

et al. 2002

Journal of Pharmaceutical Sciences

122

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“…This was particularly useful in the patients with CML, who were able to spend the majority of their treatment period at home, and in two cases, return to work for short periods. These results indicate that oral idarubicin used as a single agent, despite a wide individual variation in bioavailability (Gillies et al, 1987), can be useful in the palliative management of AML and CML in accelerated phase or blast crisis.…”

Section: Discussionmentioning

confidence: 94%

Oral idarubicin in the treatment of acute myelogenous leukaemia and the blast phase of chronic myeloid leukaemia

Malik

Tucker

Rohatiner

et al. 1989

Hematological Oncology

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Fourteen patients with poor-risk acute myelogenous leukaemia (AML) and five patients with accelerated phase/blast crisis chronic myeloid leukaemia (CML) were treated with 3 days of oral idarubicin (25 mg/m2/day). No complete remissions or return to chronic phase CML were observed. A fall in the peripheral blast count was seen in all patients with the first cycle of treatment, and with subsequent cycles in CML patients, but all responses were transient, with eventual reemergence of peripheral blasts. In some patients, there was a clear cut improvement in symptoms such as bone and splenic pain. Five of the AML patients and all of the CML patients were treated as out-patients. In this group of patients oral idarubicin was found to be a useful drug for palliative treatment.

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Pharmacokinetics of idarubicin (4‐demethoxydaunorubicin; IMI‐30; NSC 256439) following intravenous and oral administration in patients with advanced cancer.

Abstract: 1 The plasma pharmacokinetics of idarubicin (4-demethoxydaunorubicin) were studied in 20 patients with advanced malignant disease after intravenous (21 occasions)

Cited by 41 publications

References 11 publications

Clinical Pharmacokinetics of Idarubicin

Clinical Pharmacokinetics of Idarubicin

Pharmacokinetics and Tissue Distribution of Idarubicin-Loaded Solid Lipid Nanoparticles After Duodenal Administration to Rats

Oral idarubicin in the treatment of acute myelogenous leukaemia and the blast phase of chronic myeloid leukaemia

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