Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0278488 (metastatic breast cancer)
 7,812 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Docetaxel (TXT) has been shown to be an up-regulator of human pyrimidine nucleoside phosphorylase (PyNPase) in tumors. We have tried to use the combination of low-dose weekly TXT with 5'-DFUR (LD + D) in patients with advanced or metastatic breast cancer. In this study, we compared the clinical efficacy of LD + D with that of conventional full-dose TXT (FD) and that of low-dose weekly TXT (LD). Twenty-one patients received 3 or 4 cycles of FD 60 mg/m2 every 3 or 4 weeks (group I), 14 patients received 8 cycles of LD 20-30 mg/m2 every week (group II) and 25 patients received 8 cycles of LD 20-30 mg/m2 weekly with oral 5'-DFUR 600-1,200 mg per day (group III). The overall response rates of groups I, II and III were 29%, 29% and 52% (p = 0.24), respectively. Grade 3-4 neutropenia was observed in 91% of group I, 6% of group II and 3% of group III. Nausea was present in 27% of group I, 28% of group II and 40% of group III. Higher incidence of gastrointestinal symptoms was found in LD + D, but the symptoms abated when the doses of 5'-DFUR were reduced. Low-dose weekly TXT with oral 5'-DFUR produced a higher response rate, but less hematologic toxicity than full-dose TXT, suggesting that this combination therapy is clinically useful and may be effective for patients with advanced or metastatic breast cancer.
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PMID:[Clinical efficacy of low-dose weekly docetaxel combined with oral 5'-deoxy-5-fluorouridine (5'-DFUR) in advanced or metastatic breast cancer: a pilot trial]. 1079 Oct

Xeloda (Capecitabine), a prodrug of antitumor agent 5-fluorouracil, is the first and only oral fluoropyrimidine to be approved for use as second-line therapy in metastatic breast cancer, colorectal cancer, and other solid malignancies. Fluorine-18 labeled Xeloda may serve as a novel radiotracer for positron emission tomography (PET) to image enzymes such as thymidine phosphorylase and uridine phosphorylase in cancers. The precursor 2',3'-di-O-acetyl-5'-deoxy-5-nitro-N(4)-(pentyloxycarbonyl)cytidine (11) was synthesized from D-ribose and cytosine in 8 steps with approximately 18% overall chemical yield. The reference standard 5'-deoxy-5-fluoro-N(4)-(pentyloxycarbonyl)cytidine (Xeloda; 1) was synthesized from D-ribose and 5-fluorocytosine in eight steps with approximately 28% overall chemical yield. The target radiotracer 5'-deoxy-5-[(18)F]fluoro-N(4)-(pentyloxycarbonyl)cytidine ([(18)F]Xeloda; [(18)F]1) was prepared by nucleophilic substitution of the nitro-precursor with K(18)F/Kryptofix 2.2.2 followed by a quick deprotection reaction and purification with the HPLC method in 20-30% radiochemical yields.
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PMID:Synthesis of [18F]Xeloda as a novel potential PET radiotracer for imaging enzymes in cancers. 1560 85