Alkylating Agents Pharmacology (Examples, MOA, Adverse Effects)

Alkylating agents are medications that are mainly used to treat cancer. They are effective against hematologic malignancies, such as leukemia, lymphoma, and multiple myeloma, as well as solid tumors, like breast, ovarian, uterus, lung, and bladder cancer.
The most commonly used alkylating agents are nitrogen mustards like cyclophosphamide, bendamustine, and ifosfamide; nitrosoureas like carmustine, lomustine, and streptozocin; triazenes, such as dacarbazine and temozolomide; and other alkylating agents, including busulfan and procarbazine.
Alkylating agents are cell-cycle phase nonspecific, which means they work by causing damage to the DNA of cancer cells in all phases of the cell-cycle, ultimately leading to cancer cell death. There are two primary ways they do this. First, they can attach an alkyl group to one of the DNA bases of cancer cells. Repair enzymes recognize there’s something wrong, so they jump in to replace the alkylated bases and cause DNA fragmentation, which eventually results in DNA damage and cancer cell death.
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