Overview
| Drugs | Mechanism of Action | Toxicity |
| Cyclophosphamide and ifosfamide | Crosslinks DNA | Hemorrhagic cytitis and myelosupression |
| Nitrosoureas | Crosslinks DNA | Dizziness and ataxia |
| Busulfan | Alkylates DNA | Pulmonary fibrosis and hyperpigmentation |
Cyclophosphamide and Ifosfamide
- Mechanism
- covalently crosslinks DNA
- at guanine N7 position
- between strands and within strands
- requires bioactivation by liver
- covalently crosslinks DNA
- Clinical use
- non-Hodgkin’s lymphoma
- breast cancer
- ovarian cancer
- immunosuppression
- Toxicity
- myelosuppression
Nitrosoureas (Carmustine, Lomustine, Semustine, and Streptozocin)
- Mechanism
- crosslinks DNA
- crosses BBB and enters CNS
- requires bioactivation
- Clinical use
- brain tumors
- including glioblastoma multiforme
- brain tumors
- Toxicity
- CNS toxicity
- dizziness
- CNS toxicity
- ataxia
Busulfan
- Mechanism
- alkylates DNA
- Clinical use
- CML
- was gold standard before imatinib was discovered
- hematopoietic stem cell transplants
- used for bone marrow ablation
- CML
- Toxicity
- pulmonary fibrosis
- hyperpigmentation