Thursday 31 March 2016

Capecitabine, an anti-metabolite for the treatment of colorectal cancer

Capecitabine is a prodrug which gets converted into the chemotherapeutic drug 5-Fluorouracil in the body. 5-fluorouracil is a pyrimidine antagonist. Capecitabine is just one of the many generic oncology products that are available from Taj Accura Pharmaceuticals.
http://www.tajaccura.com/product/capecitabine-tablets-150mg/

What is Capecitabine used for?
Capecitabine is a mainstay of anti-cancer therapy. It is in frequent use for the treatment of various different types of cancer, including:
  • Metastatic colorectal cancer [i]
  • Metastatic breast cancer
  • Stomach cancer and
  • Oesophageal cancer.





How does Capecitabine work?
As we saw earlier, Capecitabine is a prodrug. This means that it is not active in and of itself but only starts to exert its effects after having been converted to the active form of the drug within the body. In this case, the active form is a drug called 5-fluorouracil.
Fluorouracil binds to a particular enzyme known as thymidylate synthase and inhibits its normal activity. Thymidylate synthase is involved in the synthesis of DNA within cells. The mechanism of 5-fluorouracil is referred to as suicide inhibition because the drug binds to the enzyme in an irreversible fashion. [ii]
Essentially, if a patient is given Capecitabine then the first step that occurs is the conversion of capecitabine to 5-fluorouracil. 5-FU will then bind to its target, the thymidylate synthase enzyme, thereby preventing it from manufacturing any additional DNA. The consequence of this is that the cancer cells are no longer capable of dividing so they begin to die off. [iii]

Are there any side effects associated with the use of Capecitabine?
Yes, side effects occur relatively frequently in patients being treated with Capecitabine. The reason for this is that chemotherapeutics are not capable of telling the difference between tumour cells and healthy cells. As a consequence, they will unfortunately kill some of the normal cells.
However, these side effects can be predicted so steps are always taken by the healthcare professionals administering the drug to limit the impact on the patient.
Some of the more common side effects include:
  • Anaemia (low red blood cell count)
  • Nausea and/or vomiting (there are medicines available now to treat this)
  • Hand-Foot Syndrome (pain, swelling and peeling of skin on palms of hands and soles of feet)
  • Loss of appetite and
  • diarrhoea (can be managed by drinking plenty of fluids).
Patients are advised to contact their doctor, pharmacist or nurse if they have any questions regarding treatment with Capecitabine.

How is Capecitabine taken?
Capecitabine tablets are taken within 30 minutes of a meal. They should be swallowed whole with a glass of water. They are normally taken for two weeks followed by a rest period lasting one week. The doctor calculates the required dose on the basis of the body surface area of the patient.
The dose can also change depending on the type of cancer, the weight of the patient and how well their liver and kidneys are functioning. Patients will take regular blood tests during treatment so that their healthcare team can monitor their response to the therapy and ensure their safety.

Conclusion
Capecitabine tablets
are available from Taj Accura Pharmaceuticals at doses of either 150 mg or 500 mg. Please visit www.tajaccura.com for further details.
Always remember to consult your Doctor or Healthcare Professional if you have any questions about your own health or medications.

Taj Accura Pharmaceuticals are committed to providing affordable pharmaceutical care solutions to health providers and patients globally. Our enthusiastic and highly skilled bi-lingual sales team in English and French are more than welcome to take your queries. We are contactable by emailing info@tajaccura.com, by phone at + 353 (1) 293 1882 or alternatively by fax at + 353 (1) 293 1883
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[i] Rossi, S, ed. (2013). Australian Medicines Handbook (2013 ed.). Adelaide: The Australian Medicines Handbook Unit Trust.
[ii] Longley D. B., Harkin D. P., Johnston P. G. (May 2003). “5-fluorouracil: mechanisms of action and clinical strategies”. Nat. Rev. Cancer 3 (5): 330–8.
[iii] Álvarez, P.; Marchal, J. A.; Boulaiz, H.; Carrillo, E.; Vélez, C.; Rodríguez-Serrano, F.; Melguizo, C.; Prados, J.; Madeddu, R.; Aranega, A. (February 2012). “5-Fluorouracil derivatives: a patent review”. Expert Opinion on Therapeutic Patents 22 (2): 107–123.

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