Disease relevance of pirarubicin

• Clinical pharmacology and toxicity of 4'-O-tetrahydropyranyladriamycin [1].
• The ability of the obtained compounds to revert MDR was evaluated on anthracycline-resistant erythroleukemia K 562 cells, measuring the uptake of THP-adriamycin (pirarubicin) by continuous spectrofluorometric monitoring of the decrease of the fluorescence signal of the anthracycline at 590 nm (lambdaex = 480 nm), after incubation with cells [2].
• Phase II study of pirarubicin (THP-adriamycin) in metastatic breast cancer patients [3].
• Exposure of L1210 mouse lymphocytic leukemia cells to adriamycin (ADM) or 4'-O-tetrahydropyranyladriamycin (THP) resulted in apoptosis in a dose-dependent manner: 5 microM ADM and 0.5 microM THP induced apoptosis efficiently, but the effects of 10 microM ADM and 5 microM THP were markedly decreased or completely absent [4].
• For the axillar metastasis we performed radiation and left subclavicular arterial infusion of cisplatin 70 mg, THP-adriamycin (THP) 50 mg and methotrexate 50 mg [5].

High impact information on pirarubicin

• In an effort to improve the selectivity of i.a. anthracycline chemotherapy, we compared pirarubicin (4'-O-tetrahydropyranyladriamycin, THP) and ADM in the surgically implanted VX2 rabbit tumor model [6].
• A linear correlation was observed between the dose and the areas under the concentration curves for THP-adriamycin in plasma (r2 = 0.97) and blood cells (r2 = 0.99) [1].
• The clinical pharmacology and toxicity of a novel anthracycline derivative, 4'-O-tetrahydropyranyladriamycin (THP-adriamycin), was investigated in patients with advanced malignant diseases [1].
• Chemotherapy consisted of 40 mg/m(2) i.v. pirarubicin (THP-Adriamycin), 750 mg/m(2) i.v. cyclophosphamide, and 1.0 mg/m(2) i.v. vincristine, on Day 1 and 40 mg/m(2) p.o. prednisone on Days 1-5 [7].
• The uptake and release of 4'-O-tetrahydropyranyladriamycin by drug-sensitive and drug-resistant K562 cells in the different phase of the cycle have been determined [8].

Chemical compound and disease context of pirarubicin

• Pirarubicin (4'-O-tetrahydropyranyldoxorubicin, THP-Adriamycin) is a new anthracycline antibiotic that has recently been developed because its reduced cardiac toxicity is associated with an antitumour efficacy similar to that of doxorubicin [9].
• For stage III neuroblastoma, surgical intervention at the primary site was performed in 18 of the 19 patients, 9 during and 9 after the first three cycles of A1 regimen, consisting of high-dose cyclophosphamide, vincristine, THP-adriamycin, and cis-platinum [10].
• Pirarubicin (4'-O-tetrahydropyranyladriamycin), a new anthracyline derivative, was administered as a single agent into the pleural cavity of 42 patients (total 46 courses) with malignant pleural effusion at a dose of 20, 40, 60 or 80 mg/body [11].

Biological context of pirarubicin

• We have calculated that the number of 4'-O-tetrahydropyranyladriamycin molecules, which are actively effluxed per cell and per second, is constant whatever the cell cycle phase [8].
• Pharmacokinetics of 4'-O-tetrahydropyranyladriamycin given on a weekly schedule in patients with advanced breast cancer [12].
• Two different methods were used to determine the kinetics of active efflux of THP-adriamycin: (1) at the steady-state, (2) directly, after the addition of glucose to cells first incubated with THP-adriamycin in the presence of N3- and in the absence of glucose [13].

Anatomical context of pirarubicin

• Circadian and seasonal rhythms in murine bone marrow colony-forming cells affect tolerance for the anticancer agent 4'-O-tetrahydropyranyladriamycin (THP) [14].
• THP-adriamycin was rapidly taken up by blood cell components, with concentrations in red blood cells (RBCs), lymphocytes, and polymorphonuclear cells exceeding those in plasma [15].
• Sequential but not simultaneous administration of taxol and THP-adriamycin showed synergistic effects to three cell lines [16].
• Rapid uptake by cultured tumor cells and intracellular behavior of 4'-O-tetrahydropyranyladriamycin [17].
• 4'-Epiadriamycin and 4'-O-tetrahydropyranyladriamycin (THP-adriamycin), derivatives of adriamycin, strongly inhibited in vitro reactions of DNA polymerases alpha and beta from calf thymus by competing with activated DNA (template-primer) [18].

Associations of pirarubicin with other chemical compounds

• The fluorescence emission spectra from anthracycline-treated cells suspended in buffer have been used to compare the membrane transport of five anthracycline derivatives: adriamycin, daunorubucin, 4'-o-tetrahydropyranyladriamycin, carminomycin and aclacinomycin in drug-sensitive and drug-resistant K562 cells [19].
• Through this catheter we started chemotherapy using THP-Adriamycin and cis-platinum [20].
• The THP-adriamycin uptake, monitored by fluorimetry, was diminished even when the revertant agent verapamil was added [21].
• The mechanism of endothelium-dependent relaxation induced by pirarubicin, (2''R)-4'-O-tetrahydropyranyladriamycin, THP, or carbachol was investigated in the rat isolated aorta [22].
• The effect of sodium chloride on the cytotoxicity of 4'-O-tetrahydropyranyldoxorubicin (pirarubicin), a novel anthracycline derivative, was investigated on P388 mouse leukemia cells in vitro [23].

Gene context of pirarubicin

• From 1991 to 1999, 134 cases of hepatoblastoma were treated by surgery and combination chemotherapy of cisplatin (CDDP) and THP-Adriamycin (THP-ADR) based on the JPLT-1 protocol [24].

Analytical, diagnostic and therapeutic context of pirarubicin

• Pharmacokinetics and disposition of 4'-O-tetrahydropyranyladriamycin in mice by HPLC analysis [25].
• The new adjuvant chemotherapy using THP-adriamycin and UFT was prescribed, and one year after surgery she remains in recession [26].

References