• Capecitabine, inside the body, is converted to 5-fluorouracil (5-FU) through which it acts. (wikipedia.org)
  • Calcium folinate may enhance the therapeutic effects of capecitabine by means of synergising with its metabolite, 5-FU. (wikipedia.org)
  • The dihydropyrimidine dehydrogenase (DPD) enzyme is responsible for the detoxifying metabolism of fluoropyrimidines, a class of drugs that includes capecitabine, 5-fluorouracil and tegafur. (wikipedia.org)
  • Capecitabine is metabolised to 5-FU which in turn is a thymidylate synthase inhibitor, hence inhibiting the synthesis of thymidine monophosphate (ThMP), the active form of thymidine which is required for the de novo synthesis of DNA. (wikipedia.org)
  • 5-Fluorouracil is being increasing replaced in clinical trials with 3rd generation 5-FU drugs such as capecitabine. (dcu.ie)
  • Capecitabine is converted in the liver to 5-fluoro-5'- deoxyuridine (55FdU) and this is converted to 5-FU by thymidine phosphorylase whose over expression is induced by radiotherapy. (dcu.ie)
  • The product is uridine triacetate ( Vistogard , Wellstat Therapeutics Corporation), and it is approved for the emergency treatment of adults and children who have received an unintended overdose of 5-fluorouracil (5-FU) or capecitabine ( Xeloda ), an oral prodrug that is converted to 5-FU in the body. (medscape.com)
  • Fluorouracil (administered by infusion) and capecitabine (taken orally) are both widely used in the treatment of cancer, especially breast and colorectal cancers. (medscape.com)
  • An overdose of fluorouracil or capecitabine is rare, but when it occurs, the effects are serious and can be fatal, the FDA explains. (medscape.com)
  • The approval is based on data from two clinical trials involving 135 adult and pediatric cancer patients who either received an overdose of fluorouracil or capecitabine, or had early-onset, unusually severe, or life-threatening toxicities within 96 hours after receiving fluorouracil (not due to an overdose). (medscape.com)
  • It is important to recognize the signs of severe 5-FU and capecitabine toxicity early, which often include unexpected side effects on the first cycle - including gastrointestinal toxicities such as mucositis, central nervous system toxicities such as altered mental state, hematologic toxicities, and even cardiotoxicity. (medscape.com)
  • Worldwide, oral fluoropyrimidineshave become attractiveoptions in the treatmentof patients with colorectal cancer.Capecitabine (Xeloda), the only commerciallyavailable oral fluorouracil(5-FU) analog in the United States,was rationally designed to provideprolonged exposure to 5-FU and togenerate 5-FU preferentially withintumor tissue.Capecitabine is absorbedunchanged through the gastrointestinalwall and is converted to 5-FU viaa three-step enzymatic cascade. (cancernetwork.com)
  • Capecitabine is a prodrug that is converted to fluorouracil following oral administration, which in turn inhibits thymidylate synthetase, blocking the m. (arogga.com)
  • 5'-deoxy-5-fluorocytidine (5'-DFCR) is a cytidine analogue (metabolite of capecitabine), which is converted by CDA and subsequently by TYMP into 5-fluorouracil, a chemotherapeutic agent frequently used to treat solid tumors. (unibe.ch)
  • Capecitabine is a prodrug, that is enzymatically converted to 5-fluorouracil in the tumor, where it inhibits DNA synthesis and slows growth of tumor tissue. (med-chemist.com)
  • The activation of capecitabine follows a pathway with three enzymatic steps and two intermediary metabolites, 5'-deoxy-5-fluorocytidine (5'-DFCR) and 5'-deoxy-5-fluorouridine (5'-DFUR), to form 5-fluorouracil. (med-chemist.com)
  • The pre-planned three-year interim analysis of a randomised, prospective trial compared adjuvant capecitabine in combination with docetaxel and cyclophosphamide plus epirubicin for the treatment of early breast cancer with the standard, non-capecitabine regimen (docetaxel, epirubicin, cyclophosphamide and fluorouracil). (med-chemist.com)
  • One such drug, capecitabine (Xeloda ®), is an oral fluoropyrimidine 5-fluorouracil carbamate. (uthscsa.edu)
  • Capecitabine is converted to 5-fluorouracil primarily in cancer tissue and it has been demonstrated to combine ease of administration, a manageable toxicity profile and potent antineoplastic activity. (uthscsa.edu)
  • Furthermore, tumor heterogeneity has a significant impact on both the immune microenvironment and the infiltration of various immune cells within tumors, such as cytotoxic T lymphocytes (CTLs) ( 5 ), myeloid antigen-presenting cells ( 6 ) and cancer-associated fibroblasts (CAFs) ( 7 ). (spandidos-publications.com)
  • The next stepoccurs in the liver and tumor tissue,where cytidine deaminase converts5'-DFCR to 5'-deoxy-5-fluorouridine(5'-DFUR). (cancernetwork.com)
  • In the front-line setting, two randomized trials of 5-FU and leucovorin, with or without oxaliplatin, demonstrated that the addition of oxaliplatin significantly increases response rate and time to tumor progression, but not survival, over 5-FU plus leucovorin alone. (cancernetwork.com)
  • Individualize the dose and dosing schedule of fluorouracil based on tumor type, the specific regimen administered, disease state, response to treatment, and patient risk factors. (nih.gov)
  • We have recently reported that certain chemotherapeutics, including 5-fluorouracil (5-FU), may in fact stimulate angiogenesis in the tumor-free rat mesenteric window assay. (unboundmedicine.com)
  • AU - Albertsson,Per, AU - Lennernäs,Bo, AU - Norrby,Klas, PY - 2008/10/22/pubmed PY - 2009/5/1/medline PY - 2008/10/22/entrez SP - 418 EP - 25 JF - Acta oncologica (Stockholm, Sweden) JO - Acta Oncol VL - 48 IS - 3 N2 - BACKGROUND: Tumor growth is angiogenesis-dependent. (unboundmedicine.com)
  • The 5-FU produced locally will diffuse through cellular membranes thereby increasing the cytotoxicity to neighboring tumor cells without increasing the risk of harmful systemic effects. (brainsciencefoundation.org)
  • The results at the conclusion of this project will provide us all the information necessary for a pilot phase I feasibility and safety study for treating brain tumor patients with mesenchymal stem cells that have been engineered to express cytosine deaminase (MSC-CD) followed by 5-FC therapy. (brainsciencefoundation.org)
  • These compounds increase histone acetylation, which correlates with the synergistic sensitization of those MDR tumor cells to conventional chemotherapeutic agents, including cisplatin, sorafenib, and 5-fluorouracil. (unamur.be)
  • In human colon cancer xenograft model, a single intratumoral inoculation of the recombinant Raccoonpox virus, in combination with 5-fluorocytosine administration, produced relevant tumor growth control. (oncotarget.com)
  • We have investigated the potential of the ECTA approach to circumvent the thymidylate synthase (TS) overexpression-based resistance of tumor cells to conventional fluoropyrimidine [i.e. 5-fluorouracil (5-FU)] cancer chemotherapy. (stanfordhealthcare.org)
  • NB1011 was synthesized and found to be at least 10-fold more cytotoxic to 5-FU-resistant, TS-overexpressing colorectal tumor cells than to normal cells. (stanfordhealthcare.org)
  • 5-fluorouracil hampers the synthesis of RNA and DNA in the cancer cells, which hampers their growth. (pharmeasy.in)
  • Fluorouracil is a nucleoside metabolic inhibitor that interferes with the synthesis of deoxyribonucleic acid (DNA) and to a lesser extent inhibits the formation of ribonucleic acid (RNA). (affygility.com)
  • CD is an enzyme found in bacteria and fungi that converts nontoxic drug 5-fluorocytosine (5-FC) to form the highly cytotoxic 5-fluorouracil (5-FU). (brainsciencefoundation.org)
  • 5-FU is a toxic compound commonly used as an anticancer drug. (invivogen.com)
  • The genetic changes triggered by Toca 511 cause the cancer cells to convert Toca FC into the anticancer drug 5-fluorouracil (5-FU). (iamtotallysick.com)
  • In the FDA notice about the new approval, the agency explains that uridine triacetate , which is taken orally, works by blocking the cell damage and cell death caused by fluorouracil chemotherapy. (medscape.com)
  • The mainstay of chemotherapy in colorectal cancer patients for the past 40 years has been fluorouracil (5-FU). (cancernetwork.com)
  • Chemotherapy-induced CDA expression renders resistant non-small cell lung cancer cells sensitive to 5'-deoxy-5-fluorocytidine (5'-DFCR). (unibe.ch)
  • We performed a small-scale screen of mitochondrial metabolism inhibitors, which revealed that 5'-DFCR selectively targets chemotherapy-resistant A549 paraclone cells characterized by high CDA and TYMP expression. (unibe.ch)
  • The addition of 5'-DFCR on the second day after MTA and cisplatin combination therapy was the most efficient treatment to eradicate chemotherapy-resistant NSCLC cells. (unibe.ch)
  • Chemotherapy increases CDA and TYMP expression thereby rendering resistant lung cancer cells susceptible to subsequent 5'-DFCR treatment. (unibe.ch)
  • Cell viability and colony formation assays were used to quantify the efficacy of MTA and cisplatin treatment in combination with schedule-dependent addition of 5'-DFCR on growth and survival of A549 paraclone cells and NSCLC cell lines. (unibe.ch)
  • 5-ALA is a prodrug that can be converted in situ into a highly fluorescent substance, protoporphyrin IX (PpIX), an effective photosensitizer by the heme biosynthetic pathway. (biomedcentral.com)
  • Crisantaspase is an enzyme preparation that converts the asparagine to aspartic acid so that cancer cells die because of lack of asparagine. (egpat.com)
  • We have developed an enzyme-catalyzed therapeutic agent (ECTA) approach in which an enzyme overexpressed within the resistant cells is recruited as an intracellular catalyst for converting a relatively non-toxic substrate to a toxic product. (stanfordhealthcare.org)
  • Fluorouracil is converted to three main active metabolites 5-fluoro-2′-deoxyuridine-5′-monophosphate (FdUMP), 5- fluorouridine-5′triphosphate (FUTP) and 5-fluoro-2′-deoxyuridine-5′-triphosphate (FdUTP). (affygility.com)
  • Numerous epidemiological and preclinical studies support a role of vitamin D compounds in cancer prevention and treatment in colorectal, breast, prostate, ovarian, bladder, lung and skin cancers and leukemia ( 1 , 5 , 6 ). (jcancer.org)
  • Fluorouracil is recommended for administration either as an intravenous bolus or as an intravenous infusion. (nih.gov)
  • The aim of the present study was to extend the investigation of the angiogenesis-modulating effects of 5-FU by prolonging the continuous infusion treatment time. (unboundmedicine.com)
  • The 14-days continuous infusion of 5-FU significantly stimulated angiogenesis. (unboundmedicine.com)
  • Albertsson P, Lennernäs B, Norrby K. Low-dose continuous 5-fluorouracil infusion stimulates VEGF-A-mediated angiogenesis. (unboundmedicine.com)
  • TY - JOUR T1 - Low-dose continuous 5-fluorouracil infusion stimulates VEGF-A-mediated angiogenesis. (unboundmedicine.com)
  • when administered by slow, continuous, intra-arterial infusion, it is converted to floxuridine monophosphate. (curehunter.com)
  • BACKGROUND: Developed as an antiviral drug in the 1960s and 1970s, the thymidine analogue 2'-deoxy-2'-fluoro-5-methyl-1-ß-D-arabinofuranosyluracil (FMAU) was translated to clinical application for treatment of herpes simplex virus infection. (bvsalud.org)
  • E)-5-(2-Bromovinyl)-2'-deoxy-5'-uridyl phenyl L-methoxyalaninylphosphoramidate (NB1011) is a pronucleotide analogue of (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVdU), an antiviral agent known to be a substrate for TS when in the 5'-monophosphorylated form. (stanfordhealthcare.org)
  • Phenotypes were characterised and 5-FU was found to induce and reduce invasion in various cell lines. (dcu.ie)
  • Flucytosine is also known as 5-FC. (medscape.com)
  • 5-Fluorocytosine, or Flucytosine, is a synthetic fluorinated pyrimidine analog that is used as an antifungal agent. (lktlabs.com)
  • It isfirst hydrolyzed in the liver by carboxylesteraseto 5'-deoxy-5-fluorocytidine(5'-DFCR). (cancernetwork.com)
  • In the skin, 7-dehydrocholesterol is converted to vitamin D 3 , which is hydroxylated to 25(OH)D 3 by 25-hydroxylase in the liver and then to 1,25(OH) 2 D 3 (1α, 25-dihydroxycholecalciferol, calcitriol), the hormonally active metabolite, by 1α-hydroxylase in the kidney ( 1 ). (jcancer.org)
  • 5-Fluorouracil produces oral and gastric ulceration which can be prevented by allopurinol mouthwash. (egpat.com)
  • Principal investigator of the Vistogard clinical development program, Wen Wee Ma, MD, associate professor of the oncology, GI cancers, and drug development program at the Roswell Park Cancer Institute in Buffalo, New York, commented in a statement: "Severe 5-FU toxicity has, historically, been difficult to treat and sometimes resulted in death for those affected. (medscape.com)
  • Withhold or permanently discontinue fluorouracil in patients with evidence of acute early-onset or unusually severe toxicity, which may indicate near complete or total absence of dipyrimidine dehydrogenase (DPD) activity. (nih.gov)
  • Withhold fluorouracil for cardiac toxicity. (nih.gov)
  • To increase the efficiency of the CD/5-FC pair, InvivoGen has fused the gene encoding uracil phosphoribosyl transferase (UPRT) to the CD gene. (invivogen.com)
  • Various reaction times, temperatures, and microwave powers were systematically explored to optimize the coupling reaction of 2-deoxy-2-[(18)F]fluoro-1,3,5-tri-O-benzoyl-d-arabinofuranose ([(18)F]-sugar) and bis-2,4-(trimethylsilyloxy)-5-methyluracil (silylated uracil) in the presence of a Friedel-Crafts catalyst, trimethylsilyl trifluoromethanesulfonate (TMSOTf). (bvsalud.org)
  • Levothyroxine Sodium Tablets, USP contain synthetic crystalline L-3,3',5,5'-tetraiodothyronine sodium salt [levothyroxine (T 4 ) sodium]. (nih.gov)
  • We found three compounds that convert the gene expression profiles of three HCC cell lines to gene expression profiles associated with good OS. (unamur.be)
  • 5-ALA ester derivatives which present more lipophilic properties have been synthesized, higher PpIX level in different cell cultures having been found for these compounds compared to 5-ALA itself [ 11 ]. (biomedcentral.com)
  • Few organofluorine compounds exist naturally ( C&EN, May 22, page 12 ), meaning that almost all must be made. (acs.org)
  • [ 5 ] Antibiotic treatment alone led to increased Candida colonization but did not affect dissemination. (medscape.com)
  • 1 ] Lesions are multifocal in about 5% of cases. (cancer.gov)
  • 1 , 2 , 4 , 5 Incidence and mortality rates for intrahepatic CC have risen steeply and steadily across the world over the past few decades with concomitant falls in extrahepatic CC rates. (bmj.com)
  • However, in advanced NSCLC, the 5-year survival rate is below 10%, mainly due to resistance to therapy. (unibe.ch)
  • The collective results from this virus study, include encouraging survival and excellent safety data, support the ongoing randomized phase 2/3 trial called Toca 5, and offer hope for a new treatment option for patients with brain cancer," Vogelbaum said. (iamtotallysick.com)
  • Differential regulated proteins were quantified using 2 dimensional difference gel electrophoresis (2D-DIGE) and differentially regulated proteins were identified using matrix-assisted laser desorption/ionization time of flight mass spectrometry (MALDI-ToF MS). Data shows the NHBE showed a dose dependent response to 5-FU treatment. (dcu.ie)
  • No fluorouracil dose has been proven safe in patients with absent DPD activity. (nih.gov)
  • Discontinue fluorouracil until resolved or decreased to Grade 1, then resume at a reduced dose. (nih.gov)
  • Using the Connectivity Map Tool, we were able to identify drugs that converted the gene expression profiles of HCC cell lines from ones matching patients with poor OS to profiles associated with good OS. (unamur.be)
  • Delivery systems that can improve the tissue penetration and retention of 5-ALA lead to a desirable accumulation of PpIX in the skin, optimizing the PDT in this way. (biomedcentral.com)
  • It is available as an oral suspension (200 mg/5 mL). (medscape.com)
  • Here the proteomic alterations induced by IC8o 5-FU treatment of normal and cancer cells of epithelial origin of the lung and breast are investigated. (dcu.ie)
  • According to the American Society of Clinical Oncology (ANCO) guidelines on breast cancer follow-up and management, symptoms of breast cancer recurrence include presence of new breast lumps, pain in the bone, chest or abdomen, dyspnea and constant headaches ( 5 ). (iiarjournals.org)
  • In addition, ASCO also recommends mammography for the early detection of relapse in breast cancer ( 5 ). (iiarjournals.org)
  • During the subsequent angiogenesis, 5-FU was delivered continuously for 14 days by an osmotic pump implanted subcutaneously. (unboundmedicine.com)
  • Photodynamic therapy (PDT) using 5-aminolevulinic acid (5-ALA) is a skin cancer therapy that still has limitations due to the low penetration of this drug into the skin. (biomedcentral.com)
  • The in vitro delivery performance provided by SCLLs lead to consider this systems adequate for the 5-ALA-PDT of skin cancer, since SCLLs have delivered 5-ALA to the target skin layers (viable epidermis + dermis) to be treated by topical PDT of skin cancer. (biomedcentral.com)
  • Afin d'estimer la faisabilité d'une évaluation de la qualité de vie dans une cohorte de patients cancéreux tunisiens, nous avons présenté le questionnaire QLQ-C30 de l'EORTC à 23 femmes traitées par chimiothérapie adjuvante en ambulatoire pour un cancer du sein à un stade précoce, au début du traitement et pendant le troisième cycle de chimiothérapie. (who.int)
  • Il est nécessaire d'améliorer encore l'infrastructure de soins et la sensibilisation du public en matière de cancer si l'on veut réaliser des études fiables sur la qualité de vie des cancéreux. (who.int)
  • However, only two proteomic experiments have been performed to date that look at the effect of 5-FU treatment. (dcu.ie)
  • Thus the possibility that the previously reported surprising proangiogenic effect of 5-FU reflected an insufficiently long treatment period can be ruled out. (unboundmedicine.com)
  • We have proposed in this work a delivery system for 5-ALA based on liposomes having lipid composition similar to the mammalian stratum corneum (SCLLs) in order to optimize its skin delivery in Photodynamic Therapy (PDT) of skin cancers. (biomedcentral.com)
  • RÉSUMÉ La recherche consacrée à la qualité de vie des patients cancéreux dans les pays en développement est limitée. (who.int)
  • The anti-metabolite - 5-Fluorouracil (5-FU) - is the most widely used chemotherapeutic drug. (dcu.ie)
  • It is converted to fluorouracil after penetrating fungal cells. (medscape.com)
  • TFFs are rapidly and coordinately secreted from mucus-secreting cells when the gastrointestinal mucosa suffers mechanical and/or chemical damage, and they respond to the mucosal injury ( 4 , 5 ). (spandidos-publications.com)
  • Capcita Tablet gets converted into 5-fluorouracil (active medicine) in the body. (pharmeasy.in)
  • Inside the body, this medicine gets converted into 5-fluorouracil (chemical). (arogga.com)
  • Niacin is converted to niacinamide when it is taken in amounts greater than what is needed by the body. (medlineplus.gov)
  • Resistance to 5-FU is a major clinical problem as mediated predominantly by over expression of Thymidylate Synthetase. (dcu.ie)
  • A variant of DLKP was generated by pulse selection with 55FdU and showed a ~4 fold resistance to 5-FU. (dcu.ie)