How Do Antineoplastic Tyrosine Kinase Inhibitors Work?

Antineoplastic tyrosine kinase inhibitors are a class of drugs used to treat nonsmall cell lung cancer, gastrointestinal stromal tumors (a type of tumor that grows in the wall of the stomach and the intestine), mastocytosis (a disorder characterized by mast cell proliferation and accumulation within various organs, most commonly the skin), renal cell carcinoma (cancer that begins in the cells of the kidneys), mantle cell lymphoma (fast-growing cancer that begins in the cells of the immune system), chronic lymphocytic leukemia (a type of cancer that begins in the white blood cells), and small lymphocytic lymphoma (a cancer of the immune system), hepatocellular carcinoma, and thyroid cancer.

Antineoplastic tyrosine kinase inhibitors are a type of targeted therapy that identifies and attacks specific types of cancer cells while causing less damage to normal cells. Antineoplastic tyrosine kinase inhibitors work by blocking the action of enzymes called tyrosine kinases, responsible for the activation of proteins and a part of many cell functions, including cell signaling, growth, and division.

Antineoplastic tyrosine kinase inhibitors are administered via oral route.

Antineoplastic tyrosine kinase inhibitors work in the following ways:

• They belong to a class of drugs known as "kinase inhibitors that work by slowing or stopping the growth of cancer cells.
• They work by blocking the action of an abnormal protein that signals cancer cells to multiply which helps to slow down or stop the spread of cancer cells to other parts of the body.
• They target the abnormal BCR-ABL1 protein that causes uncontrolled chronic myeloid leukemia (CML) cell growth and blocks its function, causing the CML cells to die. 

Tyrosine kinase inhibitors are used to treat conditions such as:

• Chronic lymphocytic leukemia (a type of cancer of the blood and bone marrow)
• Small lymphocytic lymphoma (cancer of the immune system that affects infection-fighting white blood cells called B cells)
• Mantle cell lymphoma (fast-growing cancer that begins in the cells of the immune system)
• Nonsmall cell lung cancer
• Gastrointestinal stromal tumors (a type of tumor that grows in the wall of the stomach and the intestine)
• Systemic mastocytosis (a disorder characterized by mast cell proliferation and accumulation within various organs, most commonly the skin)
• Renal cell carcinoma
• Chronic myelogenous leukemia (an uncommon type of cancer of the bone marrow)
• Waldenstrom macroglobulinemia (a rare blood cell cancer characterized by an excess of abnormal white blood cells in the bone marrow)
• Marginal zone lymphoma (a group of indolent non-Hodgkin’s lymphoma B-cell lymphomas)
• Medullary thyroid cancer
• Hepatocellular carcinoma (liver cancer)
• Acute lymphoblastic leukemia (a type of cancer of the blood and bone marrow)
• Pancreatic cancer

Some of the common side effects include:

• Nausea
• Vomiting
• Constipation
• Diarrhea
• Abdominal pain
• Headache
• Heartburn
• Tiredness/weakness
• Back pain
• Altered taste sensation
• Joint/muscle pain
• Mouth sores
• Dry/itchy skin
• Loss of appetite

Other rare side effects include:

• Dizziness 
• Fatigue 
• Hair loss
• Weight gain
• Anemia (low red blood cell count)
• Insomnia 
• Shortness of breath
• Chills, sore throat, fever, or cough
• Chest pain
• Thrombocytopenia (low blood platelet count)
• Peripheral edema (swelling of lower legs or hands)
• Hyperglycemia (high blood glucose level)
• Hypophosphatemia (low blood phosphate level)
• Rash/hives
• Hypokalemia (low blood potassium level)
• Yellowing of skin or the eyes

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Generic and brand names of antineoplastic tyrosine kinase inhibitors include:

• Acalabrutinib
• Afatinib
• Alecensa
• Alectinib
• Avapritinib
• Axitinib
• Ayvakit
• Bosulif
• Bosutinib
• Brukinsa
• Cabometyx
• Cabozantinib
• Calquence
• Caprelsa
• Cometriq
• Crizotinib
• Dacomitinib
• Dasatinib
• Entrectinib
• Erlotinib
• Gilotrif
• Gilteritinib
• Gleevec
• Ibrutinib
• Iclusig
• Imatinib
• Imbruvica
• Inlyta
• Lapatinib
• Midostaurin
• Neratinib
• Nerlynx
• Nexavar
• Nilotinib
• Pacritinib
• Pazopanib
• Pexidartinib
• Ponatinib
• Quizartinib
• Regorafenib
• Rozlytrek
• Rydapt
• Sorafenib
• Sprycel
• Stivarga
• Sunitinib
• Surufatinib
• Sutent
• Tarceva
• Tasigna
• Tucatinib
• Tukysa
• Turalio
• Tykerb
• Vandetanib
• Vizimpro
• Votrient
• Xalkori
• Xospata
• Zaltrap
• Zanubrutinib
• Ziv-aflibercept