NCCN Guidelines for Patients® | Chronic Myeloid Leukemia

21 NCCN Guidelines for Patients ® : Chronic Myeloid Leukemia, 2018 Bosutinib Bosutinib is a second-generation TKI. It attaches to active and inactive sites on the BCR-ABL1 protein to block growth signals. It works against most BCL-ABL1 mutations. It also blocks SCR kinases. Ponatinib Ponatinib is third-generation TKI. It blocks many tyrosine kinases including BCR-ABL1. It works against all BCL-ABL1 mutations including T315I . What to expect TKIs for CML are alike in many ways. They are made in the form of a pill that is swallowed. You will need to avoid certain medicines, food, and drinks, such as grapefruit juice. Ask your treatment team for more information on how to take your TKI. Side effects A side effect is an unhealthy or unpleasant physical or emotional condition caused by treatment. Not every person gets the same side effects. Side effects depend on the drug, the amount taken, the length of treatment, and the person. There are side effects common among TKIs. These include low blood counts. You may feel nauseated, have diarrhea, and vomit. Changes in your skin may occur, such as a rash. You may feel tired and get headaches and fevers. Fluid buildup in limbs or around certain organs may occur. All TKIs can cause severe side effects. Your doctor will monitor your safety. Severe side effects include heart problems, liver problems, and kidney failure. Do not take TKIs while pregnant or breastfeeding. Not all side effects of TKIs are listed here. Please ask your treatment team for a complete list of common and rare side effects. If a side effect bothers you, tell your treatment team. There may be ways to help you feel better. There are also ways to prevent some side effects. 3 Overview of cancer treatments Tyrosine kinase inhibitors Figure 7 How TKIs work Kinases move chemicals, called phosphates, from one molecule to another. The phosphate “turns on” the next molecule in the signal pathway. TKIs block the transfer of phosphate and in turn stop cell growth signals. Copyright © 2017 National Comprehensive Cancer Network ® (NCCN ® ). www.nccn.org BCR-ABL1 protein in CML cells P TKI Molecule with phosphate has attached to BCR-ABL1. Signals for cell growth are sent. A TKI has attached to BCR-ABL1 and blocked the transfer of phosphate. No growth signals are sent.

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