How Do EZH2 Inhibitors Work?

Enhancer of zeste 2 polycomb repressive complex 2 subunit (EZH2) inhibitors are drugs used for treating various cancers.

EZH2 is a gene that makes an enzyme called histone-lysine N-methyltransferase EZH2 protein (EZH2 enzyme). This enzyme is involved in the suppression of gene activity, essential for the normal development of cells. Mutation of the EZH2 gene has been linked to various types of cancers. Some changes can enhance the activity of the EZH2 enzyme or give it a new atypical function. Due to the overactivity of the EZH2 enzyme, cell growth becomes uncontrolled leading to the development of cancers.

EZH2 inhibitors are drugs used in the treatment of:

• Follicular lymphoma: Cancer of the lymphocytes (a type of white blood cells that help the body fight infections).
• Epithelial sarcoma: A rare soft tissue cancer affecting the hands and arms.

The side effects of EZH2 inhibitors may include:

• Pain
• Low hemoglobin level
• Fatigue
• Decreased white blood cell count
• Increased cholesterol
• Nausea
• Decreased electrolytes
• Vomiting
• Constipation
• Cough
• Headache
• Anemia
• Decreased weight
• Shortness of breath
• Diarrhea
• Abdominal pain
• Hemorrhage

The 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 EZH2 inhibitors include:

• Tazemetostat
• Tazverik