How is capecitabine metabolized?

Metabolized by thymidine phosphorylase to fluoruracil. Capecitabine and its metabolites are predominantly excreted in urine; 95.5% of administered capecitabine dose is recovered in urine. Fecal excretion is minimal (2.6%). The major metabolite excreted in urine is FBAL which represents 57% of the administered dose.

What class of drug is capecitabine?

Drug Type: Capecitabine is an anti-cancer (“antineoplastic” or “cytotoxic”) chemotherapy drug. Capecitabine is classified as an “antimetabolite.” (For more detail, see “How Capecitabine Works” section below).

What is capecitabine converted to?

DESCRIPTION: XELODA (capecitabine) is a fluoropyrimidine carbamate with antineoplastic activity. It is an orally administered systemic prodrug of 5′-deoxy-5-fluorouridine (5′-DFUR) which is converted to 5-fluorouracil.

Is capecitabine an inducer of CYP2C9?

Capecitabine/FU inhibits the CYP2C9 enzyme, which is responsible for the metabolism of the more potent S-isomer of warfarin. This can lead to substantial increases in international normalized ratio (INR) values and a high risk of bleeding complications.

Can capecitabine be dissolved in water?

Tell your doctor if you find it difficult to swallow the tablets. They may suggest that you dissolve the capecitabine tablets in water. In this case, dissolve the tablets in a 200ml glass of warm water. Stir the water with a spoon until the tablets are completely dissolved and then drink it immediately.

Where is capecitabine absorbed?

Capecitabine is fully absorbed from the gastrointestinal tract (particularly from the small intestines) unaltered and converted to 5′-DFCR and 5′-DFUR to 5-fluorouracil (Kochi et al 2007) The absorption of oral fluoropyrimidines is unaffected by gastrectomy (Camidge et al 2005) Clearly, patients who have significant …

What is the function of capecitabine?

Capecitabine is used to treat breast, colon, or rectal cancer. It works by slowing or stopping the growth of cancer cells.

Does capecitabine cause hair loss?

Hair loss. When used on its own, capecitabine occasionally causes some temporary hair thinning. It very rarely causes complete hair loss. If capecitabine is taken in combination with another chemotherapy drug, most people will lose all their hair including eyebrows, eyelashes and body hair.

What is the main advantage of using capecitabine instead of fluorouracil?

Compared with the 5-FU/LV group, patients in the capecitabine group experienced a significantly lower incidence of any grade diarrhea, stomatitis, nausea, and alopecia, but a higher incidence of HFS and hyperbilirubinemia [19].

Is there an alternative to capecitabine?

Possible alternative treatment options to be considered are to replace the oral capecitabine or intravenous 5-FU by a 5-FU bolus regimen, by uracil-tegafur or tegafur/gimeracil/oteracil, both oral fluoropyrimidines combining a 5-FU prodrug with a dihydropyrimidine dehydrogenase (DPD) inhibitor, or by raltitrexed, a …

How effective is capecitabine?

At 3 years, 82.8% of capecitabine patients were alive and free from recurrence or second cancer, compared with 73.9% of control patients. At 5 years, these rates were 74.1% and 67.6%.

How long does it take for capecitabine to leave your system?

The chemotherapy itself stays in the body within 2 -3 days of treatment but there are short-term and long-term side effects that patients may experience.

How is capecitabine metabolized in tumor cells?

Capecitabine. As a prodrug, capecitabine is selectively activated by tumor cells to its cytotoxic moiety, 5-fluorouracil ( 5-FU ); subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate ( FdUMP) and 5-fluorouridine triphosphate ( FUTP) by both tumor cells and normal cells.

How are the pharmacokinetics of capecitabine used in medicine?

Clinical pharmacokinetics of capecitabine Capecitabine is a novel oral fluoropyrimidine carbamate that is preferentially converted to the cytotoxic moiety fluorouracil (5-fluorouracil; 5-FU) in target tumour tissue through a series of 3 metabolic steps. After oral administration of 1250 mg/m2, capecitabine is rapidly and extensively absorbe …

Is there a generic name for capecitabine?

Brand Name: Xeloda®. Capecitabine is the generic name for the trade name drug Xeloda. In some cases, health care professionals may use the trade name Xeloda when referring to the generic drug name capecitabine. Drug Type: Capecitabine is an anti-cancer (“antineoplastic” or “cytotoxic”) chemotherapy drug.

How is capecitabine converted into a carbonyl derivative?

Capecitabine is a carbamate ester that is cytidine in which the hydrogen at position 5 is replaced by fluorine and in which the amino group attached to position 4 is converted into its N- (penyloxy)carbonyl derivative. Capecitabine is a antineoplastic agent used in the treatment of cancers.