The bleomycins are a group of glycopeptide anticancer cytotoxic agents
which have been used in the clinical treatment of several human malig
nancies as single or combination chemotherapy for over two decades. Ho
wever, the risk of dose-dependent pulmonary toxicity, which ultimately
results in pulmonary fibrosis, limits the scale of application. Meanw
hile, the unique mechanism of the antitumour effects of bleomycins has
also attracted considerable interest from biologists. Extensive studi
es at the molecular level have provided a guide to attempts to obviate
the pulmonary toxicity. Recent progress made in the areas of drug del
ivery, electropermeabilisation and conjugate synthesis has provided va
luable additional information to improve bleomycin chemotherapy. The p
atents and publications discussed in this review are selected from tho
se covering the period from 1992 to date based on a Chemical Abstracts
search.