However, the combination was also more toxic than 5-FU alone, as evidenced by a higher incidence of grade 3 to 4 diarrhea (19.5% versus 8.5%) and conjunctivitis (26.5% versus 5.6%), as well as one recorded toxic death versus none. In a clinical study consisting of 148 patients with advanced untreated colorectal cancer, weekly administration of 5-FU (600 mg The exact mechanism of interaction is unknown.Īlthough enhancement of 5-FU cytotoxicity may be used to advantage in some cancer patients, increased toxicity should also be considered.ĭeaths from severe enterocolitis, diarrhea, and dehydration have been reported in elderly patients receiving weekly leucovorin and fluorouracil. MONITOR CLOSELY: Coadministration with folate therapy may potentiate the pharmacologic effects of 5-fluorouracil (5-FU). This metabolic error can interfere with RNA processing and protein synthesis through the production of fraudulent RNA. Secondly, nuclear transcriptional enzymes can mistakenly incorporate FUTP in place of uridine triphosphate (UTP) during the synthesis of RNA. Thymidylate is the necessary precursor of thymidine triphosphate, which is essential for the synthesis of DNA, therefore a deficiency of this compound can inhibit cell division.
This binding inhibits the formation of thymidylate from 2'-deaxyuridylate. First, FdUMP and the folate cofactor, N5-10-methylenetetrahydrofolate, bind to thymidylate synthase (TS) to form a covalently bound ternary complex. These metabolites cause cell injury by two different mechanisms. Fluorouracil is further metabolized to two active metabolites, 5-fluoro-2'-deoxyuridine 5'-monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP), within normal and tumour cells.
Oesophagogastric Cancer: Capsy is used for the first line treatment of patients with advanced oesophagogastric cancer.Ĭapsy is also used to associated treatment for these conditions: Duke's C Colon cancer, Esophageal Cancers, Hepatobiliary Cancers, Malignant Neoplasm of Stomach, Metastatic Breast Cancer, Metastatic Colorectal Carcinoma, Pancreatic Cancer Metastatic, Refractory Fallopian Tube Carcinoma, Metastatic pancreatic endocrine carcinoma, Refractory Ovarian cancer, Refractory peritoneal cancer, Refractory, metastatic Colorectal carcinomaĬapsy is a prodrug that is selectively tumour-activated to its cytotoxic moiety, fluorouracil, by thymidine phosphorylase, an enzyme found in higher concentrations in many tumors compared to normal tissues or plasma. Pancreatic Cancer: Capsy is used for the first line treatment of patients with locally advanced and metastatic pancreatic cancer in combination with gemcitabine. Monotherapy is also used for the treatment of patients with metastatic breast cancer resistant to both paclitaxel and an anthracycline-containing chemotherapy regimen or resistant to paclitaxel and for whom further anthracycline therapy is not used. It is used for first-line treatment of patients with metastatic colorectal carcinoma when treatment with fluoropyrimidine therapy alone is preferred.īreast Cancer: Capsy in combination with docetaxel is used for the treatment of patients with metastatic breast cancer after failure of prior anthracycline-containing chemotherapy.
Fluorouracil it then metabolized both normal and tumor cells to 5-fluoro-2′-deoxyuridine 5′-monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP).Ĭolorectal Cancer: Capsy is used for a single agent for adjuvant treatment in patients with Dukes' C colon cancer who have undergone complete resection of the primary tumor when treatment with fluoropyrimidine therapy alone is preferred. It is an orally administered systemic prodrug that has little pharmacologic activity until it is converted to fluorouracil by enzymes that are expressed in higher concentrations in many tumors. Additionally, FUTP interferes with RNA synthesis.Ĭapsy is a fluoropyrimidine carbamate with antineoplastic activity indicated for the treatment of metastatic breast cancer and colon cancer. FdUMP covalently binds to thymidylate synthase, inhibiting the formation of thymidilate, thus interfering with DNA synthesis. Capsy is a prodrug of fluorouracil, a pyrimidine antimetabolite, which is metabolised into 5-fluoro-2′-deoxyuridine-5′monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP).
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