How Do Antineoplastic DNA Methylation Inhibitors Work?

Antineoplastic DNA methylation inhibitors are a class of drugs used to treat a group of blood/bone marrow disorders such as myelodysplastic syndromes (group of cancers in which the bone marrow fails to produce healthy blood cells), including chronic myelomonocytic leukemia (a type of cancer that starts in blood-forming cells of the bone marrow). 

Myelodysplastic syndromes are a group of hematopoietic neoplasms that give rise to variable cytopenia (reduction in the number of mature blood cells) progressing to secondary acute myeloid leukemia (cancer of the blood and bone marrow), which is invariably fatal if untreated. People with myelodysplastic syndrome may have problems such as infections, anemia (low red blood cell count), and easy bleeding/bruising.

DNA methylation inhibitors belong to a class of medications called “demethylation agents” that work by helping the bone marrow to produce normal blood cells and killing abnormal cells in the bone marrow. They are used to treat myelodysplastic syndrome by inducing DNA hypomethylation and apoptosis (a type of cell death in which a series of molecular steps in a cell lead to its death) of cancerous cells.

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

DNA methylation inhibitors work in the following ways:

• They belong to a class of drugs called "hypomethylation agents" that work by helping the bone marrow produce normal blood cells and killing abnormal cells in the bone marrow.
• They help in slowing down or halting the growth of abnormal blood cells that grow very fast and do not work properly.
• In addition, they induce DNA hypomethylation and apoptosis of cancerous cells.

Antineoplastic DNA methylation inhibitors are used to treat conditions such as:

• Myelodysplastic syndromes (group of cancers in which the bone marrow fails to produce healthy blood cells)
• Acute myeloid leukemia (cancer of the blood and bone marrow)

Some of the common side effects include:

• Nausea
• Vomiting
• Constipation
• Diarrhea
• Abdominal pain
• Headache
• Tiredness/weakness
• Mouth sores
• Loss of appetite
• Joint/muscle pain
• Dry skin
• Pain, redness, swelling, hardness, or itching at the injection site

Other rare side effects include:

• Dizziness 
• Fatigue 
• Weight loss
• Chest pain
• Hair loss
• Anemia (low red blood cell count)
• Insomnia (trouble falling and/or staying asleep)
• Shortness of breath
• Chills, sore throat, fever, or cough
• Rash/hives/itching
• Swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
• Thrombocytopenia (low blood platelet count)
• Fast or pounding heartbeat
• Hyperglycemia (high blood glucose level)

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 DNA methylation inhibitors include:

• Azacitidine
• Cedazuridine/decitabine
• Dacogen
• Decitabine
• Inqovi
• Onureg
• Vidaza