Modern cancer therapy is often multimodal, including chemotherapy, surgery, and radiotherapy.

Chemotherapeutics can be categorized based on structure and function:

Alkylating agents, such as nitrogen mustard derivatives and nitrosureas, contain highly reactive alkyl groups that form covalent bonds with DNA, resulting in cross-linking events that lead to cell death by impeding DNA replication.

Antimetabolites, such as the antifolate methotrexate and the purine analogs, induce cell death predominantly through interference with DNA synthesis.

Topoisomerase inhibitors, such as podophyllotoxins and anthracyclines, induce cell death by interfering with the maintenance of DNA supercoiling.