Chemotherapy: Alkylating Agents

Reviewed by: HU Medical Review Board | Last reviewed: November 2023

Alkylating agents are a type of chemotherapy used to treat many cancers. They were one of the first types of drugs used against cancer. Alkylating agents treat lung cancer by affecting DNA and preventing cancer cells from dividing into new cancer cells.1-3

Alkylating agents are often combined with other types of chemotherapy. Talk to your doctor about your treatment plan and what to expect.4,5

How do alkylating agents work?

Alkylating agents act directly on DNA to change its structure. The term “alkylating” refers to a chemical tag called an “alkyl” group. Some alkylating agents tag certain DNA building blocks with alkyl groups. This changes how DNA strands interact with each other. It causes DNA to break apart.1-3

Other drugs classified as alkylating agents do not add alkyl groups. Instead, they create tight bonds (cross-links) between DNA strands. Platinum-based drugs (cisplatin and carboplatin) are examples.3,6

This changed DNA structure prevents cells from copying DNA, which makes it hard for cells to divide. Cancer cells then die without dividing. Alkylating agents work for various cancers and can be used to treat certain forms of lung cancer.1

Examples of alkylating agents

Three examples of alkylating agents used to treat lung cancer include:2,7-9

  • Paraplatin® (carboplatin)
  • Platinol® (cisplatin)
  • Zepzelca™ (lurbinectedin)

Treatment often combines carboplatin or cisplatin with another drug. For example, combinations with a mitotic inhibitor can treat non-small cell lung cancer (NSCLC). Combinations with a topoisomerase inhibitor can treat small cell lung cancer (SCLC).4,5,7,9

Lurbinectedin treats SCLC that has spread (metastasized) to other parts of the body. It is meant for people who have received platinum-based drugs that did not work or no longer work.4,8

What are the possible side effects?

Chemotherapy drugs, including alkylating agents, target cells that divide quickly. This is why they are effective on cancer cells. But they can also harm non-cancerous cells that divide quickly. This harm causes side effects.2

Side effects can vary depending on the specific drug you are taking. Common side effects of alkylating agents include:7-9

  • Nausea and vomiting
  • Diarrhea or constipation
  • Loss of appetite
  • Numbness, tingling, burning, or pain in the hands or feet
  • High blood sugar
  • Muscle and joint pain
  • Trouble breathing
  • Blood test changes
  • Low white blood cell counts, which can increase your risk of infection
  • Low platelets, which increase your risk of bleeding and bruising
  • Low red blood cell counts, which can cause fatigue

Serious side effects are possible. Cisplatin and carboplatin have boxed warnings, the strictest warning from the US Food and Drug Administration.7,9

Cisplatin has this warning because of an increased risk of:7

  • Severe kidney problems
  • Bone marrow problems resulting in low blood cell counts
  • Severe nausea and vomiting
  • Numbness, tingling, and/or pain in extremities

Carboplatin has a boxed warning because of an increased risk of:9

  • Bone marrow problems resulting in low blood cell counts
  • Vomiting
  • Serious allergic reactions
  • Complications that should be managed by an oncologist

Some of these risks can be related to the drug dose. Other serious side effects are possible.7,9

In addition, cancers can become resistant to anti-cancer drugs. This means that cancer cells adjust to survive during chemotherapy, and this may occur in some people with lung cancer. Combinations of different treatments can help lower the risk of resistance.10

These are not all the possible side effects of alkylating agents. Talk to your doctor about what to expect when taking these drugs. You should also call your doctor if you have any changes that concern you when receiving an alkylating agent.

Other things to know

Alkylating agents are given into a vein through an intravenous (IV) line. Your doctor will perform tests to check for side effects during treatment. They may stop treatment or change your dose or schedule if side effects occur.7-9

You may be prescribed other medicines during treatment with alkylating agents. These may include drugs to reduce nausea and vomiting. Your doctor may suggest avoiding eating certain foods during treatment. For example, avoid grapefruit-containing products during treatment with lurbinectedin.7-9

Before beginning treatment for lung cancer, tell your doctor about all your health conditions and any other drugs, vitamins, or supplements you take. This includes over-the-counter drugs. These can increase the risk of side effects in certain situations. Tell them about:7-9

  • History of blood or bone marrow problems
  • History of liver or kidney problems
  • Any active infections
  • Hearing problems
  • Any allergies
  • Pregnancy or plans to become pregnant
  • Breastfeeding or plans to breastfeed

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