Chemotherapy for Colorectal Cancer

​​​​​Chemotherapy (also called chemo) uses drugs to destroy or damage fast-growing cells like cancer cells. It is used to shrink tumors, slow cancer’s growth, relieve symptoms, or help people live longer. Chemo drugs are given in different ways. This includes intravenously (IV into a vein), orally by a pill, or by injection. Chemotherapy given after surgery is called “adjuvant” treatment. Chemotherapy given before surgery is called “neoadjuvant” treatment. This helps to shrink the tumor before surgery.

These are the chemotherapy drugs that are used most often to treat colorectal cancer (CRC). New treatments become available all the time, so this may not be a complete list. 

Please note: The side effects listed here do not represent a comprehensive list. Each chemotherapy drug has its own set of side effects and ways of working. It's important to discuss all potential side effects of a drug with your healthcare team. Be sure to tell your healthcare team about any side effects you do have.

Search by Drug Name

IV (through a vein) =      Pill =

Treatment Type

Antimetabolite

Drug Name
Xeloda® (capecitabine) (Pill)
Important Things to Know
  • May lead to serious or life-threatening bleeding when taken with anticoagulants (blood thinners) such as warfarin (Coumadin®).
  • May lead to other side effects such as increased thirst, dizziness, and/or trouble falling asleep or staying asleep (insomnia).
  • Can be used alone or with other chemotherapies to treat patients whose CRC cannot be removed by surgery or has spread to other parts of the body.
  • Can be used alone or in combination with other chemotherapy treatments for patients who have had surgery to remove stage III CRC (adjuvant chemotherapy). This will help keep the cancer from coming back after surgery.
  • Can be used before the time of surgery (neoadjuvant chemotherapy) in combination with radiation therapy and other chemotherapy for adults whose CRC has spread to nearby tissues or lymph nodes.

Treatment Type

Antimetabolite

Drug Names
Carac® (IV)
Fluoroplex® (IV)
Tolak® (5-FU/ fluorouracil) (IV)
Important Things to Know
  • Can be used alone or with other chemotherapies to treat patients whose CRC cannot be removed by surgery or has spread to other parts of the body.
  • Can be used alone or in combination with other chemotherapy treatments for patients who have had surgery to remove stage III CRC (adjuvant chemotherapy), to help keep the cancer from coming back after surgery.
  • Can be used before the time of surgery (neoadjuvant chemotherapy) in combination with radiation therapy and other chemotherapy for adults whose CRC has spread to nearby tissues or lymph nodes.

Treatment Type

Folic Acid Analog

Drug Name
Leucovorin® (leucovorin calcium) (IV)
Important Things to Know
  • While this is technically not a chemotherapy drug, it is used during palliative care to help CRC patients with the side effects of advanced cancer.
  • Can be used alone or with other drugs, like 5-fluorouracil, to make the treatment more effective.
  • Used to help prevent the side effects caused by some medications, like methotrexate.
  • Adverse drug reactions may cause hives, itching, difficulty breathing or swallowing, and/or seizures. Seek medical attention for emergent reactions like these.

Treatment Type

Kinase Inhibitors

Drug Name
Stivarga® (regorafenib) (Pill)
Important Things to Know
  • This drug may cause liver damage, which can be severe or life-threatening.
  • Used to treat CRC that has spread to other areas of the body.
  • Used for patients whose CRC has not gotten better with other treatments.

Treatment Type

Platinum-containing Antineoplastic Agent

Drug Name
Eloxatin® (oxaliplatin) (IV)
Potential Severe Side Effects
Adverse drug reaction
Important Things to Know
  • May cause severe allergic reactions that can be life-threatening.
  • Used to treat CRC that is advanced like stage III colon cancer after surgery.
  • May lead to symptoms of anxiety and/or depression.
  • May lead to difficulty falling asleep or staying asleep (insomnia).

Treatment Type

Thymidine-based Nucleoside Analogues (trifluridine); Thymidine Phosphorylase Inhibitors (tipiracil)

Drug Name
Lonsurf® (trifluridine-tipiracil hydrochloride) (Pill)
Important Things to Know
  • Low blood counts are a potential side effect that may put you at risk for anemia, infection, or bleeding This medication can cause fetal harm.
  • This is used for people with CRC that has spread to other parts of the body (metastasized). 
  • Patients who receive this treatment have already been treated with other chemotherapy medications or cannot receive the other types of chemotherapies. 
  • This medication may be used with a type of immunotherapy called bevacizumab (Avastin®). 

Treatment Type

Topoisomerase I Inhibitors

Drug Name
Campostar® (irinotecan hydrochloride) (IV)
Important Things to Know
  • This drug is used alone or in combination with other medications to treat CRC.
  • You may experience severe diarrhea and/or "late diarrhea." This may occur more than 24 hours after you receive treatment. This type of diarrhea can be life threatening. It can put you at risk for dehydration, infection, kidney failure, and other problems.