Antimetabolites for Cancer Treatment: Effects, Benefits, Risks

Medically Reviewed by Dr. K on 3 May 2021

Antimetabolites Cancer Treatment

If you or a loved one has been given an antimetabolite to treat cancer, you can learn everything you can about it, including the risks and benefits. Antimetabolites are a form of chemotherapy drug. They are one of the most widely used cancer treatments. They're also one of the oldest, dating back to the 1940s, when doctors used an antimetabolite-like drug to treat children with leukaemia.

How Does It Work

Since antimetabolites destroy cells, they are classified as a “cytotoxic" medication. They work by simulating the molecules required for cell growth. Antimetabolites are used instead of the usual building blocks of genetic material, RNA and DNA, to trick cells into taking in the drugs. The drugs prevent the cells from copying their DNA, preventing them from dividing into new cells. Antimetabolites are most effective against tumours that are rapidly developing since they attack cells only as they divide.

The following antimetabolites are widely used in cancer treatment:

  • 6-mercaptopurine
  • fludarabine
  • 5-fluorouracil
  • gemcitabine
  • cytarabine
  • pemetrexed
  • Methotrexate


Antimetabolites are widely used to treat leukemias, as well as cancers of the breast, ovary, and intestine. However, since the drugs delay the growth of any rapidly dividing cell type, they can also be used to treat a variety of other cancers.


Drug Administration

Depending on the medication and the form of cancer being treated, antimetabolite medications are administered in various ways.

Some antimetabolites come in the form of tablets or liquids that you can take every day.

Others are injected into a vein by an intravenous (IV) line inserted by a healthcare professional. A mediport, a form of IV line that sits in a wide, central vein, is frequently used.

Antimetabolites for skin cancer are available as creams to apply once or twice a day to the infected skin.

Benefits and Risks

The advantage of using antimetabolite drugs to treat cancer is that they destroy cancer cells, which will help you live longer and avoid or shrink your tumour.

Antimetabolites, on the other hand, don't function for everyone, and it's difficult for doctors to predict which tumours will react to them. Even though antimetabolites work well at first, tumours often develop resistance to them, which means they ultimately stop working.

Side Effects

Since antimetabolites involve a wide range of medications, side effects can vary. If you're considering using an antimetabolite to treat cancer, speak to your doctor about the potential side effects.

Antimetabolites have a variety of side effects, including:

  • Nausea, vomiting, or a lack of appetite
  • Muscle soreness, fatigue, or weakness
  • Dizziness and a headache
  • Inflammation of the mouth and lips
  • Increased levels of liver enzymes – could be a sign of liver injury
  • Hair loss
  • A rash or broken, dry skin
  • Constipation or diarrhea
  • Changes in vision or light exposure
  • Lower white blood cell counts – can increase the risk of infection.


Referenced on  20/4/2021

  1. Cancer & Metabolism: “Molecular features that predict the response to antimetabolite chemotherapies.”
  2. The New England Journal of Medicine: “Temporary Remissions in Acute Leukemia in Children Produced by Folic Acid Antagonist, 4-Aminopteroyl-Glutamic Acid (Aminopterin).”
  3. National Cancer Institute: “Types of Chemotherapy Drugs.”
  4. MedlinePlus: “methotrexate,” “flurouracil injection,” “cytarabine,” “gemcitabine.”
  5. Mayo Clinic: “Fluorouracil (topical route).”
  6. Avastin: “What are the benefits and risks of Avastin for metastatic colorectal cancer (mCRC)?”
  7. Cancer Immunotherapy: “Chapter 7 — Cytotoxic Chemotherapy in Clinical Treatment of Cancer.”

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