A pro-drug that is converted to 5-FU via three enzymatic steps in the liver or tumor tissue.

Trade name Xeloda.

Converted through a series of enzymatic steps to 5′-deoxy-5-fluoridine and eventually to 5-fluorouracil.

Without conversion is an inactive drug.

Rapidly and extensively absorbed orally.

Generates fluorouracil preferentially in tumor tissue.

Associated with lower incidence of serious gastrointestinal adverse events compared with 5-fluorouracil.

Converted to 5-fluorouracil in tumor sites by the enzyme thymidine phosphorylase.

As first-line treatment for metastatic colon cancer has a response rate of 26%.

In a trial of monotherapy with first line treatment of patients with HER-2 negative metastatic breast cancer progression free survival and time to progression were in the range of 6-7.9 months and median overall survival within the range of 18.6-29.4 months (O’Shaughnessy JA et al).

Indicated with docetaxel for patients when anthracycline containing chemotherapy has failed, and as monotherapy for patients when taxanes and anthracycline containing chemotherapy have failed or for whom further anthracycline continuing therapy is not indicated.

It is often given as first chemotherapy agent for patients with estrogen receptor positive breast cancer, that is progress during anti-estrogen therapy.

Capecitabine improves both disease-free and overall survival (DFS and OS) when used as an add-on to other standard chemotherapy, either before or after surgery for triple negative breast cancer.

The meta-analysis showed that adding capecitabine to standard chemotherapy in TNBC improves DFS by 18% and OS by 22%.

In a randomized clinical trial of patients with early-stage triple negative breast cancer who receives standard adjuvant treatment, low-dose  capecitabine maintenance therapy for one year, compared with observation, resulted in significantly higher five-year disease free survival of 82.8% versus 73% percent for risk of recurrence or death.

In first line metastatic colorectal cancer at least as active as bolus 5 FU, and infusional 5 FU.

Time to progression in metastatic colorectal cancer comparing to 5 FU/LV is 4.6 months vs. 4.7 months, respectively.

Median time to treatment failure in metastatic colorectal cancer 4.2 months vs. 3.6 months with 5 FU/LV and median survival 12.9 vs 12.8 months, respectively.

As effective as 5FU/LV in adjuvant treatment for Dukes C colon cancer with 3-year DFS of 64%.

In heavily pretreated patients with metastatic breast cancer it has a response rate of 26% and a disease control rate of 57%, with a median time to progression of 3.2 months and a median survival of 12.2 months (Blum JL et al).

Produces hand-foot syndrome.

The over the counter nonsteroidal anti-inflammatory gel containing 1% diclofenac reduces the incidence of hand-foot syndrome by 75% among patients with cancer being treated with capecitabine.

An oral agent with a recommended dose of 1250 mg/m2 twice daily days 1-14 every 3 weeks in repeated cycles.

Improved safety profile compared to 5-FU with less diarrhea, stomatitis, neutropenia and nausea but more hand-foot syndrome.

In combination with oxaliplatin (CAPOX) is equivalent to infusional FOLFOX in metastatic colon cancer.

G.I. toxicity is higher in patients 80 years or older.

Higher incidence of G.I. adverse reactions observed in individuals with higher baseline folate levels.

Higher folate levels in the United States may account for the fact that there is a higher incidence of gastrointestinal adverse reactions in the United States compared to other nations.

Has efficacy for breast cancer brain metastases (Ekenel M).

Effective with temozolimide in neuroendocrine tumors.

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