Antineoplastic chemotherapy drugs contain chemicals that kill cells that rapidly divide, including cancer cells. Doctors use these medications to help treat some types of cancer.

There are many types of antineoplastic drugs. Which one a doctor recommends varies according to the type and stage of cancer a person has, the potential risks, and other treatments they are receiving, among other factors.

By working closely with a healthcare professional to monitor and respond to changes, such as side effects, antineoplastic chemotherapy may help many individuals fight cancer.

This article explores the different types of antineoplastic drugs, their uses, how healthcare professionals administer them, their side effects and risks, efficacy, and alternatives.

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There are many antineoplastic chemotherapy drugs available. The National Cancer Institute (NCI) Seer*Rx database lists over 1,900 antineoplastic drugs and their uses.

Doctors typically divide antineoplastic chemotherapy drugs according to their function or how they attack cancer cells.

Alkylating agents

Alkylating agents act directly on cell DNA. They damage DNA to prevent cells from multiplying.

Some examples include:

  • altretamine
  • bendamustine
  • busulfan
  • carmustine
  • chlorambucil
  • cyclophosphamide
  • dacarbazine
  • ifosfamide
  • lomustine
  • mechlorethamine
  • melphalan
  • procarbazine
  • streptozocin
  • temozolomide
  • thiotepa
  • trabectedin


Antimetabolites are a type of drug that inhibits the enzyme production necessary for DNA and RNA synthesis. This means they affect DNA synthesis and therefore interfere with cell division and tumor growth.

Antimetabolites include three types of drugs:

  • antifolates, including pemetrexed, pralatrexate, and methotrexate
  • purine analogs, such as azathioprine, cladribine, and fludarabine
  • pyrimidine analogs, including cytarabine, decitabine, and 5-fluorouracil

Plant alkaloids

Plant alkaloids are plant-derived drugs that stop a cancer cell’s ability to divide and multiply.

Examples of plant alkaloids for cancer therapy include:

  • actinomycin D
  • paclitaxel
  • vincristine
  • irinotecan

Antitumor antibiotics

Antitumor antibiotics alter DNA to prevent an important part of the cell process as it tries to create proteins. These drugs essentially cause parts of the DNA to unravel and hinder the cell from multiplying.

Some examples include:

  • bleomycin
  • dactinomycin
  • daunorubicin
  • doxorubicin
  • epirubicin
  • idarubicin
  • mitomycin
  • mitoxantrone
  • plicamycin
  • valrubicin

Antineoplastic chemotherapy drugs target cancerous cells by attacking the life cycle of a cell.

Cells go through different phases as they grow and multiply. Cancer cells tend to grow quickly, meaning they go through these phases quicker. By targeting these phases, healthcare professionals hope to kill these fast-growing cancer cells.

In some cases, antineoplastic chemotherapy drugs may be the main form of treatment. The NCI lists these drugs to treat:

Chemotherapy is also a highly common treatment for:

In other cases, doctors may also recommend different therapies or combinations of treatments with chemotherapy, such as:

  • Primary chemotherapy: When chemotherapy forms the main treatment for cancer.
  • Combination therapy: When chemotherapy combines with other therapies to form the cancer treatment. For example, chemoradiation combines chemotherapy with radiation therapy. Combination therapy can also include immunotherapy or targeted agents.
  • Adjuvant chemotherapy: A person will receive adjuvant chemotherapy after the primary treatment. It aims to prevent recurrence and reduce micrometastases, when the cancer spreads but there are too few cells for testing to pick up.
  • Neoadjuvant chemotherapy: When doctors use chemotherapy to shrink cancer before using other treatments such as surgery or radiation. Neoadjuvant chemotherapy can mean that the main treatment — often surgery — may not need to be as extensive.
  • Maintenance therapy: When doctors recommend chemotherapy to help prevent relapse after treatment or slow the growth of advanced cancer.
  • Palliative therapy: Palliative chemotherapy primarily aims to relieve or delay cancer symptoms, promote comfort, manage cancer-related symptoms, such as pain from a large tumor or reaccumulation of cancerous fluid, and improve quality of life. It may also extend a person’s life.

Depending on the type, location, and severity of cancer, healthcare professionals may also combine chemotherapy with other forms of treatment, such as:

Antineoplastic drugs come in different forms for different uses, such as:

  • capsules or pills that people take orally
  • liquid injections into the muscle tissue, under the skin, or into a vein or the spinal fluid
  • liquids that healthcare professionals administer directly into an organ or body cavity, such as the bladder or liver

The NCI notes that IV liquid drugs are the most common form of chemotherapy drug administration. This is because they are an efficient way to get the most medication into the bloodstream.

Chemotherapy typically requires many “cycles,” or rounds, of therapy. A person will receive antineoplastic drugs on certain days in their cycle and then recover for the remaining days.

Chemotherapy can take time, and a person can sometimes expect months of these cycles, depending on the type and severity of cancer and treatment.

Because chemotherapy drugs cannot distinguish between cancerous cells and healthy cells, they can attack other cells in the body. This can lead to several side effects.

The side effects may occur in other areas of the body where cells rapidly divide, such as the hair follicles, digestive system, liver, and mucus membranes.

Side effects can include:

  • bone marrow suppression
  • bruising easily
  • anemia
  • hair loss
  • nausea and vomiting
  • loss of appetite
  • diarrhea and constipation
  • changes in mood
  • dry mouth
  • fertility issues
  • sexual issues
  • urinary and bladder issues
  • changes to the skin and nails
  • nerve damage
  • issues with memory or concentration
  • mouth sores
  • taste changes
  • allergic reactions

Not everyone will experience the same side effects. They can vary depending on a person’s overall health and the strength of the treatment.

Long-term effects from antineoplastic drugs include:

  • damage to the bone marrow
  • liver and kidney damage
  • damage to the lungs
  • damage and risks for the heart
  • damage to the reproductive system
  • temporary or permanent infertility
  • hearing impairment
  • sexual dysfunction

However, not all people will experience long-term effects.

The efficacy of chemotherapy drugs will depend on the type and stage of a person’s cancer.

Chemotherapy drugs are generally effective, but their exact effectiveness is difficult to determine. Part of the reason for this is that people with cancer often receive more than one type of therapy at once. For example, they may undergo radiation therapy or surgery in addition to chemotherapy. This can make it hard to establish which treatment is causing the results.

A person’s overall health may also play a role in the treatment’s effectiveness. Generally, those who are healthier respond better to chemotherapy treatment.

The success rates of chemotherapy for different cancer types will also vary. Additionally, the stage of cancer and how aggressive it is will play a role in the effectiveness of treatment.

If a person does not wish to undergo chemotherapy, doctors may recommend alternatives, such as:

However, some alternatives may not yield the same results as chemotherapy.

Antineoplastic chemotherapy drugs attack cancer cells to keep them from multiplying. However, they can also attack healthy cells and cause side effects.

Doctors may recommend antineoplastic chemotherapy drugs alone or in combination with other therapies to treat cancer. The exact treatment timeline will vary in each case, but some people may require weeks or even months of chemotherapy.

Individuals can discuss their treatment options with a healthcare professional.