What You Should Know About Breast Cancer Chemotherapy Pills

By | August 23, 2025

Breast cancer treatment has come a long way. While many people still associate chemotherapy with intravenous (IV) infusions at a hospital or clinic, oral chemotherapy—also called chemo pills—offers a convenient alternative for some patients. Alongside chemo pills, oral medications can include antihormone therapies and targeted therapies, expanding the options for personalized breast cancer care.

What Are Breast Cancer Chemotherapy Pills?

Not all chemotherapy drugs are available in pill form. Understanding the differences between oral medications is crucial for making informed treatment decisions. According to Dr. Hannah Luu, a California-based oncologist and founder of OncoGambit, oral breast cancer medications generally fall into three categories:

  1. Chemotherapy pills – directly kill fast-growing cancer cells.
  2. Antihormone pills – block hormones that fuel certain types of breast cancer.
  3. Targeted therapy pills – interfere with specific pathways that cancer cells use to grow.

Each therapy works differently, and not every option is suitable for everyone. The right choice depends on factors such as your cancer type, stage, overall health, and other medications you may be taking.

For a deeper dive, visit Breast Cancer Hub for more information.

Common Types of Breast Cancer Chemo Pills

Several chemotherapy drugs have been formulated as pills, making at-home treatment more manageable. Here are some of the most commonly prescribed:

Capecitabine (Xeloda)

Capecitabine is often used to treat metastatic breast cancer, either alone or in combination with targeted therapies. When ingested, it remains inactive until enzymes in cancer cells convert it to 5-fluorouracil, a compound that stops cancer cells from multiplying (NIH source).

Possible side effects include:

  • Nausea and vomiting
  • Diarrhea
  • Mouth sores
  • Appetite loss
  • Changes in menstrual cycles
  • Hand-foot syndrome (swelling, redness, and blistering of hands/feet)

Patients on blood thinners may need careful monitoring, and capecitabine isn’t recommended for those who are pregnant or have severe liver or kidney problems.

Cyclophosphamide (Cytoxan)

Cyclophosphamide is part of the CMF regimen (cyclophosphamide, methotrexate, fluorouracil) and can also be given orally. It works by blocking cancer cell growth.

Potential side effects:

  • Hair loss
  • Nausea and vomiting
  • Diarrhea
  • Mouth sores
  • Unintentional weight loss

It should not be used by pregnant women or those with urinary blockages, as it can cause severe complications.

Methotrexate

Methotrexate is a cytotoxic drug, meaning it kills cells, and is used in combination with other chemotherapy medications. Oral methotrexate offers an alternative to IV administration, though it may still cause nausea, mouth ulcers, and loss of appetite (NIH source).

Targeted Therapy vs. Chemotherapy

Oral targeted therapies differ significantly from traditional chemotherapy:

  • Chemotherapy kills fast-growing cells in general, affecting both healthy and cancerous cells, which can lead to more side effects.
  • Targeted therapy focuses specifically on cancer cells by interfering with the pathways that drive their growth, sparing most healthy cells.

Targeted therapies can be used alone or alongside chemotherapy. Some of the main types include:

  • Monoclonal antibodies: Attach to cancer cell targets to deliver drugs or toxins directly. Examples include trastuzumab (Herceptin) and pertuzumab (Perjeta) for HER2-positive breast cancer.
  • Small-molecule inhibitors: Penetrate cancer cells to block proteins that promote cell growth.
  • Angiogenesis inhibitors: Prevent new blood vessel formation that tumors need to grow.

Oral options like neratinib (Nerlynx), lapatinib (Tykerb), and tucatinib (Tukysa) are increasingly used in advanced HER2-positive cases.

Key Takeaways

  • Chemo pills such as capecitabine (Xeloda) and cyclophosphamide (Cytoxan) provide an at-home alternative to IV chemotherapy.
  • Targeted therapies are designed to attack only cancer cells, reducing the risk of damaging healthy cells.
  • Treatment decisions are highly personalized, based on cancer type, stage, and patient health.

Always discuss options thoroughly with your oncologist to find the best treatment plan for your situation.

For further reading on breast cancer treatments, visit American Cancer Society and NIH Breast Cancer Resources.

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