Methanesulfonates & Nitrosureas
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What is busulfan's MOA?
Methanesulfonyloxy groups at each end of the molecule act as leaving groups after attack by nucleophilic sites on DNA. This forms INTER-STRAND DNA cross-links.
Busuflan is used for which types of cancers?
Almost exclusively for chronic myelogenous leukemia (CML).
What are the adverse effects associated with busulfan?
- - Significantly less N&V
- - Excessive myselosuppression that can result in irreversible bone marrow aplasia
- - Hyperpigmentation of the skin
- - Rare: pulmonary fibrosis (busulfan lung)
What are the three nitrosoureas?
- - Carmustine
- - Lomustine
- - Semustine
How do the nitrosoureas work?
DNA nucleophiles attack the molecule to cause bisalkylated adducts, aka INTER-STRAND cross-links. A seperate fragment of the molecule (alkyl isocyanate attacks the amino groups of proteins).
Nitrosoureas are highly (hydrophilic/lipophilic).
Lipophilic, and thus pass through the BBB fairly easy.
Which types of cancers may be treated with carmustine (a nitrosourea)?
Brain cancer, lymphomas, myelomas.
Which types of cancers may be treated with lomustine (a nitrosourea)?
Common adverse effects of carmustine (a nitrosourea) -
- - Delayed pulmonary fibrosis
- - Cumulative renal damage
Common adverse fx of lomustine (a nitrosourea) -
- - N&V
- - Delayed bone marrow toxicity
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