How Do Antineoplastic PI3K Inhibitors Work?

Antineoplastic phosphoinositide 3-kinase (PI3K) inhibitors are a class of drugs used to treat certain types of cancers 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), follicular lymphoma (slow-growing blood cancer), marginal zone lymphoma (slow-growing cancer that begins in a type of white blood cells that normally fights infection), and breast cancer.

PI3K inhibitors are selective targeted anticancer agents that work by inhibiting PI3K enzymes which are part of the PI3K/AKT/mTOR pathway, a pathway that plays an important role in regulating cell growth and survival. The inhibition of this pathway prevents the proliferation of cancerous cells, resulting in tumor suppression and apoptosis (death of cells that occurs as a normal and controlled part of an organism's growth or development).

PI3K inhibitors are administered via intravenous (into a vein) and oral routes.

PI3K 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 signals that cause cancer cells to multiply which helps to stop the spread of cancer cells to other parts of the body.

Antineoplastic PI3K inhibitors are used to treat conditions such as:

• Follicular lymphoma (slow-growing blood cancer)
• Marginal zone lymphoma (slow-growing cancer that begins in a type of white blood cells that normally fights infection) 
• Breast cancer
• 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)

Some of the common side effects include:

• Nausea
• Vomiting
• Constipation
• Diarrhea
• Abdominal pain
• Headache
• Heartburn
• Tiredness/weakness
• Joint/muscle pain
• Mouth sores
• Loss of appetite

Other rare side effects include:

• Dizziness 
• Fatigue 
• Hair loss
• Weight loss
• Anemia (low red blood cell count)
• Insomnia 
• Shortness of breath
• Chills, sore throat, fever, or cough
• Thrombocytopenia (low blood platelet count)
• Peripheral edema (swelling of lower legs or hands)
• Hyperglycemia (high blood glucose level)
• Frequent, painful, or urgent urination
• Hypophosphatemia (low blood phosphate level)
• Rash/hives
• Increased serum creatinine 
• Hyperkalemia (high blood potassium level)
• Pneumonia (an infection that inflames the air sacs in one or both the lungs)

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 PI3K inhibitors include:

• Aliqopa
• Alpelisib
• Copanlisib
• Copiktra
• Duvelisib
• Idelalisib
• Piqray
• Ukoniq
• Umbralisib
• Zydelig