Topic overview

Start with the big picture

Alkylating agents act as bifunctional electrophiles, primarily binding to N7 guanine and creating DNA cross-links and strand breaks that can lead to apoptosis. Although they are cell-cycle non-specific, their effects are greatest in rapidly dividing cells. The topic organizes these drugs into classes such as nitrogen mustards, nitrosoureas, alkyl-sulfonates, and triazines or imidazotetrazines, then relates class-wide adverse effects and resistance mechanisms to individual agents. Examples include hemorrhagic cystitis with cyclophosphamide or ifosfamide, pulmonary and hepatic risks with busulfan, and central nervous system penetration by nitrosoureas. The material also highlights supportive care and monitoring considerations, providing a framework for comparing clinical uses, distinctive toxicities, and key features across the class.