Etoposide chemical structure
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Etoposide

Etoposide phosphate (Eposin®, Etopophos®, Vepesid®, VP-16®) is an inhibitor of the enzyme topoisomerase II. It is used as a form of chemotherapy for malignancies such as lung cancer, testicular cancer, lymphoma, non-lymphocytic leukemia, and glioblastoma multiforme. It is often given in combination with other drugs. more...

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Chemically it derives from podophyllotoxin, a toxin found in the American Mayapple.

It is given intravenously or by mouth in capsule form. If the drug is given by IV it must be done slowly over a 30 to 60 minute period because it can lower blood pressure as it is being administered. Blood pressure is checked often during infusing. The physician may lengthen or shorten the time depending on circumstances.

Side Effects

Common are:

  1. low blood pressure
  2. hair loss
  3. pain and or burning at the IV site
  4. constipation or diarrhea
  5. metallic food taste
  6. Bone marrow suppression, leading to
    1. decreased white blood cell counts (leading to increased susceptibility to infections)
    2. low red blood cell counts (anemia)
    3. low platelet counts (leading to easy bruising and bleeding)

Less common are:

  1. nausea and vomiting
  2. allergic type reactions
  3. rash
  4. fever, often occurring shortly after IV administration and not due to infection
  5. mouth sores

Instruction

Patients are generally advised to call their doctor in case of fever, symptoms of infection or painful injection sites, as these may progress severely without adequate medical attention.

It is advised to drink lots of fluids after treatment to prevent damage to the bladder and kidneys, typically 1.5 to 3.5 litres of water on the day of treatment and for several days after.

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Soluble cancer drugs: just add phosphate - phosphate makes etoposide water-soluble - Brief Article
From Science News, 5/29/93 by Elizabeth Pennisi

Many anticancer drugs fail to live up to their potential simply because they do not dissolve well in water. Only by mixing these fat-soluble compounds in oils, detergents, and other substances that cause unwanted side effects can pharmacologists keep them in the bloodstream long enough to reach the tumor targets.

Now, by adding a phosphate side group to a commonly used anticancer compound called etoposide, researchers have managed to get rid of all other chemical baggage. As a result, cancer specialists can explore different and possibly more effective treatment regimens involving this compound, says Daniel R. Budman of North Shore University Hospital-Cornell Medical College in Manhasset, N.Y. The phosphate imparts a charge to the molecule so that it readily dissolves in water.

Budman and his colleagues administered the water-soluble version to 25 people whose solid tumors had not responded to other treatments. The researchers proved they could deliver the drug faster (in five, instead of 45, minutes) and in higher doses with fewer complications than is possible with etoposide in its original form, says Budman. After injection, enzymes in the blood chop off the compound's phosphate group and, within 10 minutes, restore the drug to its original, active form. "Then it [follows] the same pharmacology as the older drug," Budman explains. "[This form] is a lot more convenient."

The new version must undergo further evaluation, but Budman and others predict that pharmaceutical companies will soon begin making water-soluble versions of other drugs.

COPYRIGHT 1993 Science Service, Inc.
COPYRIGHT 2004 Gale Group

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