Alkylating agents in chemotherapy refers to a form of treatment wherein alkylating chemotherapy drugs or agents are used. These alkylating agents are further classified into different classes however they all work on one chemical mechanism. Cancer cells are vulnerable to DNA damage and alkylating chemotherapy agents tend to target this weakness of cancer cells. Alkylating agents in chemotherapy interrupt the normal process of DNA production. In the normal process of DNA production, the proteins bind with each other to form a complex helix structure of a DNA molecule. Alkylating agents disrupt this process by adding an alkyl group to the DNA molecules and prevents the cell from producing the essential proteins. When the proteins don’t form and bind together, the DNA strands break up and the cancer cell is thus destroyed by alkylating agents in chemotherapy. The mechanism that is common to all classes of alkylating agents is mutation that prevents the cancer cells from diving and multiplying in numbers.

Alkylating agents is used in chemotherapy to treat different type of cancers because of its effect on the cancer cells. Alkylating agents in chemotherapy are found to be more beneficial to treat cancers that develop at a slow rate such as leukemia and solid tumors. Other cancers that benefit from alkylating agents used in chemotherapy include ovarian cancer, lung cancer, lymphomas, breast cancer, myelomas, Hodgkin’s disease and sarcomas, like chemotherapy for angiosarcoma.

Alkylating Agents in Chemotherapy

Given below are the common drugs which are used as alkylating agents in chemotherapy. There are five major classes of alkylating agents namely nitrogen mustards, alkyl sulfonates, nitrosoureas, ethylenimines and triazines. Nitrogen mustards are a kind of non-specific DNA alkylating agents that are similar to mustard gas. These compounds have been used as warfare agents in the past and that is when the use of it to treat cancer was discovered. Nitrosoureas are another class that is used as alkylating agents in chemotherapy. These compounds are also lipophilic in nature. It means that it has the ability to cross the blood-brain barrier, making it useful in the treatment of certain brain tumors. Apart from treating humans, these alkylating agents are also used for in chemotherapy for cats and other animals.

Some of the common drugs used as alkylating agents in chemotherapy are as follows:

Melphalan - Melphalan is an alkylating agent used in chemotherapy treatment and the brand name of this drug is Alkeran. Alternative names to this drug are phenylalanine mustard and L-PAM. It treats different conditions such as ovarian cancer, breast cancer, neuroblastoma, multiple myeloma and rhabdomyosarcoma. It is rarely administered via an injection and patients are usually advised to take the drugs orally.

Cyclophosphamide - Cyclophosphamide is one of the commonly used alkylating agents in chemotherapy and the patients who have been prescribed these drugs as part of their chemotherapy treatment are either given the drugs intravenously or orally. They are sold by the name of Cytoxan or Neosar in the market. Although the drug is usually administered intravenously or taken orally other administration options could also be followed. This is because cyclophosphamide is used in the treatment of many cancers. Burkitt’s lymphoma, AML or acute myelocytic leukemia (AML), acute lymphocytic leukemia (ALL), chronic lymphocytic leukemia (CLL), chronic myelocytic leukemia (CML), neuroblastoma, breast cancer, ovarian cancer, multiple myeloma, testicular cancer, Ewing’s sarcoma and lung cancer are some of the many cancers wherein cyclophosphamide is used as one of the alkylating agents in chemotherapy.

Lomustine - Lomustine is also referred to as CCNU. These drugs because of its lipophilic nature is used to treat brain tumors, non-Hodgkin’s lymphoma, Hodgkin’s disease and is also used in the treatment of colon cancer, lung cancer and melanoma.

Chlorambucil - Another alkylating agent used in chemotherapy treatments is chlorambucil. This drug is known by its brand name, Leukeran and is used in the treatment of Hodgkin’s disease, chronic lymphocytic leukemia (CLL) and malignant lymphomas. Chlorambucil has also found to be effective in the treatment of breast cancer, ovarian cancer and non-Hodgkin’s lymphoma. This drug is administered orally.

The use of alkylating agents in chemotherapy treatment is found to be effective as these agents or drugs disrupt the normal DNA formation. Although this is known to interrupt the production of DNA, certain cell types may also become resistant to alkylating agents and does not help in the chemotherapy treatment. An important point that was left to mention is that other than affecting the DNA formation in the cancerous cells, it also affects the healthy cells, resulting in side effects. Whether it is treatment for cervical cancer or chemotherapy treatment for any other type of cancer, most of the patients experience side effects.
Please note that none of the drugs mentioned above should be taken without consulting the doctor. All drug types do not suit every patient as which drugs to be administered depends on a variety of factors. Drugs are prescribed and administered depending upon the type of cancer, stage of cancer, age, overall health of the patient etc. Many tests are taken before finalizing a drug for chemotherapy treatment. If any severe side effects are noticed during the treatment the chemotherapy regimen may be changed for the patient.