Raw material intermediate Capecitabine Powder

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Capecitabine Usage and Synthesis.

Capecitabine, an antimetabolising fluoropyrimidine deoxyriboside carbamate that can be converted to 5-FU in vivo, was developed by Roche under the trade name Shiroda to inhibit cell division and interfere with RNA and protein synthesis (proteins). It is indicated for further treatment of advanced primary or metastatic breast cancer that has failed treatment with paclitaxel and chemotherapy regimens that include anthracycline antibiotics. Mainly used in the treatment of advanced primary or metastatic breast cancer,rectal cancer, colon cancer and gastric cancer.

Uses and functions of Capecitabine.

1. Adjuvant chemotherapy for colon cancer: Capecitabine is suitable for single-agent adjuvant therapy for colon cancer patients with Dukes' C stage, after radical surgery of the primary tumour, and suitable for receiving fluoropyrimidines alone. Its treatment has a disease-free survival (DFS) that is no less favourable than the combination regimen of 5-fluorouracil and formyltetrahydrofolate (5-FU/LV).

Neither capecitabine alone nor in combination with other agents in chemotherapy prolongs overall survival (OS), but trial data are available to show that capecitabine improves disease-free survival compared to 5-FU/LV in combination chemotherapy regimens.

Physicians may refer to these findings when prescribing capecitabine monotherapy for the adjuvant treatment of Dukes' stage C colon cancer.

Data used to support this indication are from foreign clinical studies.

2、Colorectal cancer: capecitabine alone or in combination with oxaliplatin (XELOX) is indicated for the first-line treatment of metastatic colorectal cancer.

Breast cancer combination chemotherapy: Capecitabine can be used in combination with doxorubicin for the treatment of metastatic breast cancer that has failed chemotherapy with anthracycline-containing drug regimen.

4、Breast cancer single-agent chemotherapy: Capecitabine can also be used alone for the treatment of metastatic breast cancer patients who are resistant to both paclitaxel and anthracycline-containing chemotherapy regimens, or who are resistant to paclitaxel and can no longer be treated with anthracycline-containing medications (e.g., those who have received a cumulative dose of 400 mg/m2 of adriamycin or adriamycin analogues).

Resistance is defined as continued disease progression during treatment (with or without initial remission) or relapse within 6 months of completion of adjuvant chemotherapy containing anthracyclines.

5, Gastric cancer: Capecitabine is indicated for the first-line treatment of inoperable advanced or metastatic gastric cancer.

Pharmacological Effect of Capecitabine.

Both normal and tumour cells metabolise 5-FU to 5-fluoro-2-deoxyuridylic acid monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). These metabolites cause cellular damage by two different mechanisms.

First, FdUMP and the folate co-factor N5,10-methylenetetrahydrofolate bind to thymidylate synthase (TS) to form a covalently bound triple complex.

This binding inhibits the formation of thymidylate from 2'-deoxyuridine [pyrimidine nucleotide] glycosides.

Thymine nucleotides are essential precursors to thymine nucleoside triphosphate, which is required for DNA synthesis, so that deficiency of this compound inhibits cell division.

Secondly, during RNA synthesis nuclear transcriptase may incorrectly programme FUTP at the site of uridine triphosphate (UTP).

This metabolic error would interfere with RNA processing and protein synthesis.

Drug interactions of  Bulk Capecitabine Powder.

No clinically significant side effects were seen in combination with antihistamines, NSAIDs, morphine,paracetamol, aspirin, antiemetics, and H2 receptor antagonists.

Capecitabine has a low binding to serum proteins (64%) The likelihood of interactions with drugs that bind tightly to proteins by displacement is unpredictable.

Interactions with Cytochrome P450 Enzymes: In in vitro experiments, capecitabine was not found to affect human hepatic microsomal P450 enzymes.

Dosage reductions may be required when either of the phenytoin and coumarin derivative anticoagulants are used in combination with Xeloda.

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