Because regional chemotherapy has been useful in treatment and palliation o
f many cancer types, the concept of delivering drugs by inhalation for the
treatment of cancers in the lung is attractive. Much higher local drug expo
sure can be achieved with total doses considerably lower than those require
d for systemic administration, resulting in lower exposure of nonrespirator
y tract tissues to potentially toxic drugs. Regional delivery of chemothera
py to the respiratory tract has been shown to have activity in preclinical
and clinical studies. Technical improvements in delivery methods have now m
ode it possible to conduct trials of inhalational agents, both to treat can
cers affecting the respiratory tract and to deliver other drugs used in can
cer patients. This review discusses the rationale of drug delivery by the i
nhalational route, its technical challenges, preclinical and clinical exper
iences, limitations, and promise. (C) 2001 by American Society of Clinical
Oncology.