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Capecitabine

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Capecitabine Basic information
Product Description Novel Oral Fluoride Pyrimidine Drugs Tegafur Gimeracil Oteracil Interactions Adverse reaction and attentions Overdose Uses
Product Name:Capecitabine
Synonyms:5'-DEOXY-5-FLUOROCYTISINE;5'-DEOXY-5-FLUORO-N-[(PENTYLOXY)CARBONYL]CYTIDINE;CAPECITABINE;RO-9-1978;pentyl [1-(3,4-dihydroxy-5-methyl-oxolan-2-yl)-5-fluoro-2-oxo-pyrimidin-4-yl]aminoformate;XELODA;Cpecitabine;5Deoxy-5-fluoro-N-[(pentyloxy)carbonyl]cytidine, Ro-9-1978, Xeloda
CAS:154361-50-9
MF:C15H22FN3O6
MW:359.35
EINECS:
Product Categories:Active Pharmaceutical Ingredients;Antineoplastic;Bases & Related Reagents;Intermediates & Fine Chemicals;Nucleotides;Pharmaceuticals;Antineoplastic drug, 5-FU analog;Anti-cancer;API;XELODA;Cardiovascular Drugs;Inhibitors
Mol File:154361-50-9.mol
Capecitabine Structure
Capecitabine Chemical Properties
mp 110-121°C
storage temp. -20°C Freezer
CAS DataBase Reference154361-50-9(CAS DataBase Reference)
Safety Information
Hazard Codes T
Risk Statements 45-60-61-68
Safety Statements 53-22-36/37-45
Hazardous Substances Data154361-50-9(Hazardous Substances Data)
MSDS Information
ProviderLanguage
Capecitabine English
Capecitabine Usage And Synthesis
Product DescriptionCapecitabine, developed by Roche Company and named as Rhoda, is a kind of fluorine pyrimidine carbamate deoxyuridine drug that can transform into 5 - FU in the body and inhibit cell division and disturb the synthesis of RNA and protein. Capecitabine applies to the further treatment of advanced primary or metastatic breast cancer that failed to respond to the paclitaxel or other chemotherapy regimens including anthracycline antibiotics. Its main usage is treating advanced primary or metastatic breast cancer, rectal cancer, colon cancer and stomach cancer.
The above information is edited by ChemicalBook Liu Jingjing.
Novel Oral Fluoride Pyrimidine DrugsAs a novel oral fluoride pyrimidine drug, Capecitabine interacts with tumor cells by transforming to 5-FU in a three-step polymerase chain reaction. Its curative effect obviously correlates with the expression level of TP and DPD enzymes of tumor tissues. The high expression level of TP in tumor tissues induces the drug gradient difference between tumor tissues and normal tissues thus achieving relatively selective tumor destruction effect. Animal experiments demonstrate that many drugs such as Taxanes (paclitaxel, docetaxel, mitomycin, cis-platinum etc.) can increase the expression level of TP enzyme, thus enhancing the anti-tumor effect of Capecitabine; and these drugs themselves also have good curative effect to stomach cancer which exhibit both efficiency and synergy after being used in combination with Capecitabine. So far, many II- and III-stage clinical trials released preliminary result, especially Real-2study, in which nearly 400 randomized controlled clinical result analyses indicate that the combination of pharmorubicin, cis-platinum or oxaliplatinm with Capecitabine has double effect compared to the combination of those with 5-FU; plus, the toxicity is reduced. Our II-stage trail of stomach cancer treatment using large-scale combination of Capecitabine and DDP also proved the advantages of high effect, low toxicity and low cost. These evidences indicate that as a convenient, safe and efficient anticancer drug exclusive of hand-food syndrome, Capecitabine might replace 5-FU and become the basic medicine of multidrug therapy for stomach cancer. Since the approval of its use on metastatic breast cancer by American FDA in 2001 and the European Agency for the Evaluation of Medicinal Products (EMEA) in 2002, Capecitabine has got recommendations from the authoritative guides of NICE and NCCN; many large-scale investigations in the world have also proved its survival benefit in stomach cancer, colon cancer and breast cancer. In China, Capecitabine has been successively approved for the use in the adjunctive treatment and first-line treatment of metastatic breast cancer and intestinal cancer in single-drug and combination therapies since its 8-year history in the market, and until last year, it has been approved for the use in the first-line treatment of late gastric cancer.
Tegafur Gimeracil OteracilTegafur Gimeracil Oteracil is a modified drug product of the Tegafur antitumor drug. In addition to this active ingredient, it also contains Oteracil potassium (Potassiumoxonate) and JMST which adjust the biology effect. The three substances compose the compound in molar ratio of 1:1:0.4, in which Tegafur (FT), the prodrug of 5-Fu, has excellent oral bioavailability and can convert into 5-Fu in the body; Gimeraci can inhibit the dissociation of 5-Fu, enhancing the antitumor activity; Oteracil potassium can decrease the toxicity and side effect of 5-Fu. Tegafur Gimeracil Oteracil Potassium which is composed of these two biochemical modulators functions to enable the patient’ body to obtain a higher 5-FU plasma concentration, decreasing digestive tract toxicity while increasing antitumor activity.
Differences exist between the application range of Capecitabine and Tegafur Gimeracil Oteracil. In addition to the main usages in breast and colorectal cancers, Rhoda can be used in other cancers as well. According to the findings, it also has good effectiveness on advanced gastric cancer and cardia cancers. Beijing has already included Capecitabine (Rhoda) in medical insurance scheme.
Tegafur Gimeracil Oteracil has been approved for the treatment of seven kinds of tumor diseases including advanced gastric cancer, head and neck cancer, rectal cancer, non-small cell lung cancer, metastatic breast cancer, and pancreatic cancer in Japan, and has become a Japanese first-line drug for advanced stomach cancer treatment. Its initial indication in China is unresectable locally advanced or metastatic gastric cancer, and it has not included in the national medical insurance yet.
InteractionsNo clinical side effect has been seen when it is used in combination with drugs such as antihistamines, NSAIDs, morphine, acetaminophen, aspirin, anti-nausea drugs, H2 receptor antagonist etc.
The serum protein binding of Capecitabine is relatively low (64%); the possibility of binding with drugs that bind tightly to protein through replacement is still unpredictable.
Interaction with cytochrome P450 emsyme: no influence of Capecitabine on human liver microsome P450 enzyme is found in vitro.
The dose may need to be reduced when any drug among phenytoin and coumarin derivative-type anticoagulants is used in combination with Rhoda.
Adverse reaction and attentionsCommon adverse reactions include nausea, vomit, oral ulcer, abdominal pain, diarrhea, loss of appetite and skin change; it is also reported that myelosuppression, trichomadesis, tear increase, headache and dizziness appear in some patient.
Capecitabine is a kind of marrow depressant; therefore, blood examination is needed for hemocyte detection and blood platelet count before each use.
It has liver toxic side effect; therefore periodical liver examination is needed. Besides, cardiac function should be detected to avoid irreversible toxic reaction. If venous transfusion is needed, assess of the suitability should be made on the aforementioned organs before medication.
Capecitabine may cause damage to the fetus; therefore it should not be used to pregnant women, and women who use it should not be pregnant, neither. It may have an influence on fertility even after even after treatment ends.
OverdoseNo side effect caused by drug overdose has been found in the clinic experiment of Capecitabine. But in the animal experiment (active treatment of monkeys with 25,679mg/m2/day) and human treatment with maximum tolerated dose (3,514mg/m2/day), the manifestations of overdose are nausea, vomit, diarrhea, gastrointestinal irritability, gastrointestinal bleedings, myelosuppression etc. Solutions should include dehydration with diuretic and dialysis if necessary. Although there is no report on the dialysis treatment for the overdose of Rhoda, dialysis may help to decrease the concentration of 5’-DFUR which is a low molecular weight metabolite of Capecitabine in the circulation.
Uses1. Noval oral fluoride pyrimidine drug.
2. Anticancer drug, mainly used in non-small cell lung cancer, pancreatic cancer, bladder cancer, breast cancer and other solid tumors.
Chemical PropertiesColourless solid
UsageAn antineoplastic agent. A prodrug of doxifluridine.
UsageCapecitabine is an antineoplastic agent. Capecitabine is a prodrug of Doxifluridine (D556750).
UsageAn antiproliferative 5-fluorouracil releasing compound
Capecitabine Preparation Products And Raw materials
Tag:Capecitabine(154361-50-9) Related Product Information
Pemetrexed disodium 1,2,3-Triacetyl-5-deoxy-D-ribose Gemcitabine hydrochloride Carbonyl iron powder Methyl salicylate RIBAVIRINA Cyclopentadienyl manganese tricarbonyl CARBONYL SULFIDE Methyl bromide 1,1'-Carbonyldiimidazole 2',3'-DI-O-ACETYL-5'-DEOXY-5-FLUORO-N4-(PENTOXY-D11-CARBONXYL)CYTIDINE 5`-deoxy-5-fluore-N-[(pentoyloxy)carbonyl]cytidine 2`,3`-diacetate Capecitabine Bensulfuron methyl Cytosine NICKEL CARBONYL Thiophanate-methyl 5-Fluorocytidine