Molecular Classification
Chemical entity, Antineoplastic agent, DNA damaging agent
Disease Roles
CancerAutoimmune diseases

Alkylating Agent Overview

Alkylating agents are cytotoxic compounds that work primarily through covalent modification (“alkylation”) of cellular macromolecules—especially nucleic acids—leading directly or indirectly to inhibition of proliferation and induction of apoptosis. Their broad utility across many cancers is balanced by significant side effects related mainly to non-selective targeting.

Mechanism of Action

Covalent binding/alkylation of nucleic acids; inhibits replication/transcription

Biological Functions

DNA alkylation
Inhibition of DNA replication
Induction of apoptosis
Cytotoxicity

Disease Associations

Cancer
Autoimmune diseases

Safety Considerations

  • Bone marrow suppression
  • Gastrointestinal toxicity
  • Gonadal toxicity (infertility)
  • Secondary malignancies
  • Mutagenicity

Interacting Drugs

Cyclophosphamide
Chlorambucil
Melphalan
Carmustine
Lomustine
Busulfan
Dacarbazine
Temozolomide
Thiotepa
Cisplatin
Carboplatin