Bleomycin antibiotics and their role in cancer chemotherapy

The bleomycins are a group of glycopeptide anticancer cytotoxic agents which have been used in the clinical treatment of several human malignancies as single or combination chemotherapy for over two decades. However, the risk of dose-dependent pulmonary toxicity, which ultimately results in pulmonary fibrosis, limits the scale of application. Meanwhile, the unique mechanism of the antitumour effects of bleomycins has also attracted considerable interest from biologists. Extensive studies at the molecular level have provided a guide to attempts to obviate the pulmonary toxicity. Recent progress made in the areas of drug delivery, electropermeabilisation and conjugate synthesis has provided valuable additional information to improve bleomycin chemotherapy. The patents and publications discussed in this review are selected from those covering the period from 1992 to date based on a Chemical Abstracts search.