Disease relevance of TAUROMUSTINE

• Two phase III trials of tauromustine (TCNU) in advanced colorectal cancer [1].
• Phase II study of tauromustine in malignant glioma [2].
• Phase II study of tauromustine in disseminated malignant melanoma [3].
• Tumour uptake of a radiolabelled anticancer drug, tauromustine ([14C]TCNU), was investigated, using two different routes of administration in rats with colon adenocarcinomas implanted in the liver [4].
• 46 eligible patients with either anaplastic astrocytoma (AA) or glioblastoma (GBM) and clinical and computed-tomography-confirmed relapse following primary surgery and radiotherapy received oral tauromustine 130 mg/m2 every 5 weeks [2].

High impact information on TAUROMUSTINE

• Measurement and characterization of the denitrosation of tauromustine and related nitrosoureas by glutathione transferases in liver cytosol from various species [5].
• The denitrosation of a novel nitrosourea, 1-(2-chloroethyl)-3-[(2-dimethylaminosulfonyl)-ethyl]-1-nitrosoure a, tauromustine (TCNU), has been investigated in liver cytosol from various species and with a pool of cytosolic rat liver glutathione transferases (GSTs) [5].
• BACKGROUND: In preparation for a phase II trial we performed a dose-finding study involving tauromustine (TCNU), fluorouracil (5-FU) and leucovorin (LV), applied in patients with colon cancer [6].
• Combination chemotherapy with tauromustine (TCNU), 5-fluorouracil and leucovorin in advanced colorectal carcinoma: a dose-finding study [6].
• From a starting dose of 40 mg/m2/week, the long-term tolerated dose was 35 mg/m2/week, thus achieving a considerable increase of dose intensity without a significant increase of toxicity by employing this weekly schedule of tauromustine [7].

Chemical compound and disease context of TAUROMUSTINE

• 5-Fluorouracil plus tauromustine in advanced colorectal cancer: unexpected negative results [8].
• The antitumor effect of a novel nitrosourea, tauromustine, at intravenous administration in rat. Cure of hepatomas [9].
• Improved antitumor effect of the nitrosourea drugs tauromustine (TCNU) and carmustine (BCNU) on a rat liver adenocarcinoma after hepatic arterial administration with degradable starch microspheres [10].

Biological context of TAUROMUSTINE

• A novel nitrosourea, 1-(2-chloroethyl)-3-[2-(dimethylaminosulfonyl) ethyl]-1-nitrosourea (TCNU) tauromustine, has been investigated in a broad anti-tumour screen and, in depth toxicology and initial pharmacokinetics carried out [11].
• Chromosome aberrations and pharmacokinetics in patients receiving tauromustine as either a single or a repeated dose [12].
• Chemotherapy with tauromustine in advanced non-small cell lung cancer. A trial of the Phase II Study Group of the Association for Medical Oncology of the German Cancer Society [13].

Anatomical context of TAUROMUSTINE

• Metabolism of tauromustine in liver and lung microsomes from various species [14].
• The effect of estramustine, nor-nitrogen mustard and tauromustine on macromolecular labelling in the human prostatic tumour cell line 1013L [15].
• Other treatments under study include autologous bone marrow transplantation plus thiotepa, a combination regimen of chemotherapy and interferon, and newer agents such as taxol, tauromustine, and detrorubicin [16].

Gene context of TAUROMUSTINE

• 1. The cytochrome P450 (CYP)-mediated metabolism of tauromustine has been evaluated in liver and lung microsomes from various species [14].
• 5. In conclusion, the present results indicate a major role of CYP3A enzymes in the metabolism of tauromustine [14].

Analytical, diagnostic and therapeutic context of TAUROMUSTINE

• Tauromustine given at the time of relapse has demonstrable antitumour activity in patients not previously treated with chemotherapy [2].
• Plasma samples were taken over 24 h after administration and analysed for tauromustine by reversed-phase liquid chromatography [17].
• The initial effect of estramustine clearly differed from that obtained after treatment with nor-nitrogen mustard and tauromustine [15].
• TCNU (LS 2667), a new active drug in the treatment of advanced colorectal cancer. EORTC Early Clinical Trials Group [18].

References