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Chemotherapy is the use of drugs to kill cancer (malignant) cells. Chemotherapy drugs work by targeting rapidly dividing cells, like cancer cells. The drugs travel throughout the body, making chemotherapy a systemic treatment that can kill cancer cells anywhere in the body. Chemotherapy drugs are often used in combination, and chemotherapy may be used along with other treatments for lung cancer, such as surgery, radiation therapy, or targeted therapy. Chemotherapy drugs are also called anti-neoplastic drugs because they are used to help prevent the development, growth or spread of neoplasms (tumors).1-3 Chemotherapy may be used:

  • Before surgery to reduce the size of a tumor to make it easier to remove
  • After surgery to kill any remaining cancer cells in the body
  • In combination with radiation therapy for lung cancers that cannot be removed with surgery
  • As the main treatment for patients who have advanced cancer or who aren’t healthy enough for surgery 1

Chemotherapy drugs for lung cancer can be broken down into categories based on their action, including alkylating agents, antimetabolites, antimicrotubule agents, and topoisomerase inhibitors.

Alkylating agents

Alkylating agents treat cancer by interfering with cell metabolism and growth.Examples of alkylating agents used for lung cancer treatment are carboplatin (Paraplatin®), cisplatin (Platinol®), and very rarely, mechlorethamine (Mustargen®).


Antimetabolites are similar in structure to substances that are essential for growth and division of both normal and cancerous cells. These drugs are most effective in blocking growth and division of rapidly growing tumors.2 Examples of antimetabolites used for lung cancer treatment are pemetrexed (Alimta®), gemcitabine (Gemzar®), and very rarely, methotrexate (Otrexup®, Rasuvo®, Rheumatrex®, or Trexall®).

Antimicrotubule agents

Antimicrotubule agents are drugs that block cell growth by stopping mitosis (cell division).4 Examples of antimicrotubule agents used for lung cancer treatment are paclitaxel (Taxol®), vinorelbine (Navelbine®), docetaxel (Taxotere®), and vinblastine (Velban®).

Topoisomerase inhibitors

Topoisomerase inhibitors block the enzymes that break and reconnect DNA strands (topoisomerases) that are needed for cell division and growth.Examples of topoisomerase inhibitors used for lung cancer treatment are irinotecan  (Camptosar®) and etoposide (VePesid®, Toposar®).

Possible side effects of chemotherapy

Because chemotherapy drugs attack all cells that are dividing quickly, they affect cancer cells as well as normal cells that divide quickly, such as cells in the bone marrow, the lining of the mouth and intestines, and hair follicles. While the side effects of chemotherapy are dependent on the type and dosage of drugs given, some common side effects include:

Generally, these side effects stop after treatment is completed. However, some side effects may develop later on such as other types of cancer, infertility or thyroid problems. In addition, there are drugs that can be given along with chemotherapy to reduce some of the side effects, such as drugs to prevent nausea and vomiting or drugs to boost the white blood cells. Patients should report all side effects to their doctor or nurse, who can suggest ways to alleviate and reduce the occurrence of side effects.1,3

Written by: Emily Downward | Last reviewed: January 2020.
  1. American Cancer Society. Accessed online on 9/25/16 at
  2. Taber’s Medical Dictionary. Accessed online on 9/25/16 at
  3. Chemocare. Accessed online on 9/25/16 at
  4. National Cancer Institute. Accessed online on 9/25/16 at