Antimetabolites for Cancer: Effects, Benefits, Risks

If you or a loved one has been prescribed an antimetabolite to treat cancer, you’ll want to know all about this type of drug, including the risks and benefits. Antimetabolites are a form of chemotherapy drug. They’re one of the most commonly used therapies to treat cancer. And they’re one of the oldest, dating back to the 1940s, when doctors used a medication that’s now considered an antimetabolite to treat children with leukemia.

What Are Antimetabolites, and How Do They Work?

Antimetabolites are called a “cytotoxic” type of drug because they kill cells. They work by mimicking the molecules that a cell needs to grow. Cells are tricked into taking in the drugs and then using the antimetabolites instead of their normal building blocks of genetic material: RNA and DNA. With the drugs on board, the cells can no longer copy their DNA, so they can’t divide into new cells. Because antimetabolites target cells only as they are dividing, these medications are most effective against tumors that are growing quickly.

Some antimetabolites that are commonly used to treat cancer include:

What Cancers Do Antimetabolites Treat?

Antimetabolites are most commonly used to treat leukemias and cancers of the breast, ovary, and the intestinal tract. But since the drugs work to slow the growth of any quickly dividing cell type, they can be used to treat various others cancers, too.

How You Take Them

Different antimetabolite drugs are taken in different ways, depending on the drug and the type of cancer being treated.

Some antimetabolites are available as tablets or liquids you take by mouth every day.

Others are given by injection through an intravenous (IV) line that a health care professional inserts into a vein. Often, it’s a specific kind of IV line called a mediport that sits in a large, central vein.

Antimetabolites used for skin cancers are available as creams that you rub on the affected skin are once or twice a day.

Benefits and Risks

The benefit of taking antimetabolite drugs to treat cancer is that the drugs kill cancer cells, which can help you live longer and make your tumor stop growing or shrink.

But antimetabolites don’t work for everyone, and it can be hard for doctors to predict whose tumors will respond to these drugs. Even when antimetabolites first work well, tumors often become resistant to these drugs, which means they eventually don’t work anymore.

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Side Effects of Antimetabolites

Because antimetabolites include a variety of drugs, side effects may differ between drugs. If you’re going to take a particular antimetabolite to treat cancer, you should talk to your doctor about what side effects are common with that drug.

In general, side effects found in many antimetabolites include:

WebMD Medical Reference Reviewed by Sabrina Felson, MD on May 19, 2020

Sources

SOURCES:

Cancer & Metabolism: “Molecular features that predict the response to antimetabolite chemotherapies.”

The New England Journal of Medicine: “Temporary Remissions in Acute Leukemia in Children Produced by Folic Acid Antagonist, 4-Aminopteroyl-Glutamic Acid (Aminopterin).”

National Cancer Institute: “Types of Chemotherapy Drugs.”

American Cancer Society: "How Chemotherapy Drugs Work.”

Medscape: “murcaptopurine.”

MedlinePlus: “methotrexate,” “flurouracil injection,” “cytarabine,” “gemcitabine.”

Mayo Clinic: “Fluorouracil (topical route).”
Avastin: “What are the benefits and risks of Avastin for metastatic colorectal cancer (mCRC)?”

Cancer Immunotherapy: “Chapter 7 -- Cytotoxic Chemotherapy in Clinical Treatment of Cancer.”

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