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Antineoplastic (chemotherapy) drugs are medications used to treat cancer. They go by several other names such as anticancer or cytotoxic drugs. The National Cancer Institute’s SEER*RX database lists nearly 2000 antineoplastic drugs.

Chemotherapy drugs can be used in different ways in cancer treatment. They may be the primary treatment for your cancer or may be used to shrink tumors before or after other treatments. Your doctor may recommend antineoplastic drugs in combination with treatments such as:

The exact way antineoplastic drugs stop the spread of cancer depends on the specific medications used. They’re highly toxic and often lead to side effects such as hair loss, nausea, and fatigue.

Keep reading to learn how antineoplastic drugs work and when they’re used.

Antineoplastic agents are drugs used to treat cancer. These medications contain chemicals that kill cells that rapidly divide such as cancer cells. They may also kill healthy cells in your body that replicate quickly such as skin cells or cells in your hair follicles.

Antineoplastic drugs can be classified based on their method of action.

Alkylating and alkylating-like agents

Alkylating agents damage the DNA of cancer cells to keep them from replicating. They’re used to treat many types of cancer including

Antitumour antibiotics

These medications change the DNA inside cancer cells to keep them from replicating. High doses can potentially damage your heart, so lifetime limits are often imposed. Some types of cancer that they’re used to treat include:


Antimetabolites bind to the molecules in cancer cells that make up DNA and RNA to keep them from replicating. Some cancers that they’re commonly used to treat are:

  • leukemia
  • breast cancer
  • ovarian cancer
  • colon cancer

Plant alkaloids (topoisomerase inhibitors)

These drugs keep cancer cells from replicating by retaining enzymes that cancer cells need to make copies of themselves. They’re commonly used to treat:

Hormonal agents

Hormonal agents help kill cancers that are sensitive to hormone levels such as:

Miscellaneous agents

Many other antineoplastic drugs help kill cancer cells but don’t fit neatly into one of the other categories.

Antineoplastic drugs are used to treat cancer in a variety of situations and stages. Here are some of the ways it may be used.

  • Induction chemotherapy. Antineoplastic drugs used to shrink cancer cells before radiation therapy.
  • Adjuvant chemotherapy. Chemotherapy administered after other treatments to shrink remaining cancer cells.
  • Consolidation chemotherapy. Chemotherapy drugs administered after an induction therapy to kill remaining cancer cells.
  • Neoadjuvant treatment. Chemotherapy used to reduce cancer size before surgery.
  • Primary therapy. Chemotherapy used as the main treatment for your cancer.
  • Combination therapy. Chemotherapy drugs combined with one or more other treatments as the primary therapy
  • Maintenance therapy. Antineoplastic drugs administered after other therapies to prevent cancer relapse or to slow the growth of advanced cancer.
  • Palliative therapy. Chemotherapy used to extend life and increase overall wellness in people with cancers considered incurable.

According to the National Cancer Institute, antineoplastic drugs may be used as a primary treatment for cancers such as:

Antineoplastic drugs are usually administered at a hospital through an IV directly into a vein. Some medications used to treat skin cancer can be directly applied to your skin.

Some types of chemotherapy can be taken as oral pills. Others are delivered locally to your tumor either by injecting the medication into a nearby vein or by inserting a device near your cancer that slowly releases the medication.

Antineoplastic drugs are usually administered in cycles that last about 2 to 6 weeks. You receive antineoplastic drugs on certain days of the cycle and recover on the remaining days. For example, if you’re on a 2-week cycle, you may receive treatment on days 1, 2, and 3, and then have no treatment from days 4 to 14.

Chemotherapy generally takes about 3 to 6 months, depending on the number of cycles you need, but can vary widely depending on the type of cancer you have and your response to treatment.

Antineoplastic drugs can kill healthy cells in your body, especially those that replicate quickly such as cells in your hair follicles, the lining of your digestive tract, and skin. Damage to healthy cells leads to many of the side effects which include:

Most chemotherapy symptoms resolve once your treatment ends. It’s a good idea to let your doctor know which side effects you’re experiencing. It’s often possible to modify the dosage of antineoplastic drugs to lessen your side effects.

Antineoplastic drugs are one of the most common treatments for cancer. Their effectiveness depends on the type of cancer you have, how aggressive your cancer is, and what stage it’s in.

For some types of cancer, there’s lots of research backing the usage of chemotherapy for improving survival. But for other cancers, there’s little evidence showing that chemotherapy is more effective than other treatments.

A 2019 study examined the effectiveness of chemotherapy administered as adjuvant therapy for increasing the overall survival rate of patients with breast cancer discovered in various stages of screening. The researchers found that adjuvant chemotherapy may benefit patients with interval breast cancer. Interval breast cancer is cancer discovered between regularly scheduled mammograms and tends to have a poor prognosis.

A 2020 study found that induction chemotherapy may improve the overall survival rate of certain subgroups of people with high-grade extremity or trunk soft tissue sarcoma. Subgroups of people who may benefit include:

  • people over the age of 70
  • African Americans
  • people with large tumors
  • people who received radiation
  • people treated at high-volume centers

Antineoplastic drugs, also called chemotherapy drugs, help kill cancer cells. There are thousands of antineoplastic drugs used in cancer treatment.

These medications often improve the overall survival of people with cancer, but they also commonly cause side effects such as hair loss, fatigue, nausea, and vomiting.

Talk with your doctor before treatment to weigh the pros and cons for your specific type of cancer.