Antisense therapy directed to protein kinase C-alpha (Affinitak, LY900003/ISIS 3521): potential role in breast cancer.

As our understanding of the biology of cancer increases, the attempts to target specific molecules associated with the promotion of cancer are accelerating. One of the targets currently being studied as an important tumor-promoting factor is protein kinase C-alpha (PKC-alpha). To specifically block PKC-alpha, antisense oligonucleotides have been developed, including LY900003 (Affinitak, ISIS-3521; Eli Lilly and Company, Indianapolis, IN), which is currently in clinical development. Although its single-agent activity in breast cancer is modest, its potential role may be in concert with traditional chemotherapy. This is a review of the pharmacology and current status of the clinical development of LY900003 and its potential role in treating patients with breast cancer.