tezacitabine (MDL 101,731)

07/01/1995 - "Based on these data it seems that MDL 101,731 is effective when administered intravenously, twice weekly and is an excellent candidate for clinical development against solid tumors."
09/01/2000 - "We conducted a phase I trial of MDL 101,731 infusion in humans with advanced cancer to determine the maximum tolerated dose and the dose-limiting toxicities of this drug when administered on a twice-weekly schedule. "
05/01/2005 - "Tezacitabine blocks tumor cells in G1 and S phases of the cell cycle and induces apoptotic cell death."
01/01/1997 - "MDL 101,731 caused regression of MDA-MB-231 and PC-3 tumor xenografts, but only inhibition of growth (without regression) of MCF-7 xenografts. "
03/15/1994 - "Additionally, preliminary evidence raises the possibility that MDL 101,731 may induce apoptosis in MDA-MB-231 tumors. "

01/01/1998 - "The purpose of this study was to elucidate the mechanism of the antitumor activity of MDL 101,731 against human carcinoma cells through investigating metabolism and the target enzyme of MDL 101,731. "
01/01/1998 - "MDL 101,731 which shows antiproliferative activity against human cervical carcinoma HeLa S3 cells at nanomolar concentrations (IC50, 30-50 nM), was hardly metabolized to (E)-2'-deoxy-2'-(fluoromethylene)uridine (FMdU) which had no antiproliferative activity below 100 microM because of resistance to human cytidine deaminase. "
01/01/1998 - "Metabolism and ribonucleotide reductase inhibition of (E)-2'-deoxy-2'-(fluoromethylene)cytidine, MDL 101,731, in human cervical carcinoma HeLa S3 cells."
05/01/2005 - "Tezacitabine at a dose of 200 mg/m(2) in combination with CI 5-FU at a dose of 200 mg/m(2) per day was relatively well tolerated and had clinical activity in patients with advanced solid tumors, particularly in patients with esophageal and other gastrointestinal carcinomas."
01/01/2007 - "In the present study we have investigated the effect of the combination of tezacitabine and 5-fluorouracil (5-FU) or 5-fluoro-2'-deoxyuridine (FUdR) on HCT 116 human colon carcinoma cells and xenografts. "

05/01/2004 - "In this paper we describe mechanisms of action and possible clinical use in the treatment of hematological malignancies of these nucleoside analogs, which are now in different stages of clinical trials, namely tezacitabine, troxacitabine, clofarabine, nelarabine, decitabine, CNDAC and ECyD."
08/01/2002 - "Hydroxyurea, fludarabine and cladribine have established roles in the management of hematologic malignancies, while other ribonucleotide reductases inhibitors, such as gemcitabine, tezacitabine and heterocyclic carboxaldehyde thiosemicarbazones (e.g., triapine) are being evaluated in clinical trials."

09/01/2000 - "Despite closing enrollment for the NSCLC trial, as of October 1999, the phase II trial of tezacitabine in colorectal cancer was continuing to accrue patients [342009]. "

09/01/2000 - "A total of 30 patients with non-small cell lung cancer were expected to be enrolled by Matrix [316463]; however, in October 1999, Matrix closed enrollment in this trial (after 28 patients were enrolled); preliminary analysis of the evaluable patients did not show meaningful clinical activity with tezacitabine as a stand-alone therapy in this indication at the dose and regimen tested [342009]. "
09/01/2000 - "It is in phase II trials for colorectal and hematological cancer [333949,343071,353481] and was evaluated in a phase II trial for non-small cell lung cancer, for which enrollment was reported to have stopped [342009]; however, tezacitabine continues to be explored for this indication [378351]. "