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The ’90s… advent of TMZ has changed the paradigm
Oral alkylating agent
Rapidly and completely adsorbed after
oral administration
Spontaneous conversion into the active
metabolite without the need for liver
demethylation (Advantage over
dacarbazine)
Excellent
penetration
into all body
tissues,
including the brain
Mechanism of
resistance to TMZ is
mediated
through O
6
-methylguanine-
DNA methyltransferase (
MGMT
).
Many
brain tumors express low concentrations
of this enzyme
.
Newlands ES. et al. Canc Treat Rev 1997;23