How Do Ankylating Antineoplastics Work?

Reviewed on 1/10/2022


Alkylating antineoplastics are a class of drugs used to treat various types of cancers such as multiple myeloma (a type of cancer of the bone marrow), ovarian cancer (cancer that begins in the female reproductive organs), brain tumors, Hodgkin's disease (a malignant though often curable disease of lymphatic tissues, typically causing painless enlargement of the lymph nodes, liver, and spleen), non-Hodgkin's lymphoma (cancer that begins in the cells of the immune system), certain types of leukemia (cancer of the white blood cells) including chronic lymphocytic leukemia and chronic myelogenous leukemia, and lung cancer.

Alkylating antineoplastics are administered orally once a day on an empty stomach and as a powder to be mixed with liquid to be injected intravenously (into a vein) over one minute or infused intravenously over 15 to 30 minutes.

Alkylating antineoplastics work in the following ways:

  • They belong to a class known as "alkylating agents" that work by stopping or slowing the growth of cancer cells in the body.
  • They belong to a class of medications called “platinum-containing antineoplastic agents” that work by suppressing the body's immune system.


Alkylating antineoplastics are used to treat conditions such as:

  • Multiple myeloma (a type of cancer of the bone marrow)
  • Ovarian cancer
  • Chronic lymphocytic leukemia (a type of cancer of the blood and bone marrow)
  • Non-Hodgkin’s lymphoma (a type of cancer that begins in your lymphatic system, which is part of the body's germ-fighting immune system)
  • Hodgkin's disease (cancer of the lymphatic system)
  • Recurrent glioblastoma (a type of tumor that occurs in the brain and spinal cord)
  • Malignant glioma (a type of brain tumor that originates from glial cells, which help support the function of the other main brain cell type—the neuron)
  • Chronic myelogenous leukemia (cancer of the blood and bone marrow)
  • Stem cell transplantation (bone marrow transplant)
  • Brain tumors
  • Metastatic testicular tumors
  • Advanced bladder cancer
  • Nephrotic syndrome (a kidney disorder that causes the body to pass too much protein in urine)
  • Breast cancer
  • Juvenile idiopathic arthritis/vasculitis (arthritis in kids and teens)
  • Lupus nephritis (a type of kidney disease caused by systemic lupus erythematosus)
  • Systemic sclerosis (an autoimmune disorder that affects the skin and internal organs)
  • Colorectal cancer
  • Pancreatic adenocarcinoma 
  • Cholangiocarcinoma (cancer that forms in the slender tubes [bile ducts] that carry the digestive fluid bile)
  • Germ cell testicular cancer
  • Bone sarcomas (primary bone tumors)
  • Soft tissue sarcomas
  • Small cell lung cancer
  • Mycosis fungoides (a type of blood cancer called cutaneous T-cell lymphoma)
  • Cutaneous T-cell lymphoma (a rare type of cancer that begins in white blood cells called T cells [T lymphocytes])
  • Anaplastic astrocytoma (a rare, malignant brain tumor that arises from astrocytes, the supportive cells in the nervous system)


Some of the common side effects include:

  • Nausea
  • Vomiting
  • Diarrhea
  • Hair loss
  • Loss of appetite
  • Joint, muscle, or back pain
  • Sores in the mouth and throat
  • Dry mouth

Other rare side effects include:

  • Shortness of breath
  • Dizziness (feeling faint, weak, or unsteady)
  • Fast, irregular, or pounding heartbeat
  • Dark-colored urine
  • Insomnia (trouble falling and/or staying asleep)
  • Yellowing of the skin or eyes
  • Pain in the upper right part of the stomach
  • Hives (a rash that appears as an allergic reaction)
  • Skin rash
  • Sweating
  • Confusion
  • Changes in vision
  • Decreased urination

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 alkylating antineoplastics include:


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