Growth factor receptors as targets for drug development: monoclonals beat kinase inhibitors to market, but are they better drugs?

Abstract

Some growth factor receptors have been shown to be overexpressed or mutated in quite a wide range of common solid tumours. Preclinical experiments have demonstrated that they are one of the causes of cell transformation and thus, represent targets for drug development. Two entirely separate strategies have been pursued to make antireceptor drugs. Surprisingly, no antagonists of their natural ligands have so far been made. Instead overexpression has been exploited to selectively target cancer cells, and small molecule inhibitors of tyrosine kinase (TK) activity have been developed to inhibit their influence on cell growth. The Type 1 family, the most prominent members of which are epidermal growth factor receptor and the c-erbB-2 or HER-2 proteins, are manifestly involved in cancer. Antibodies and TK inhibitors directed to both are currently in clinical evaluation.

• c-erbB-2
• cancer
• epidermal growth factor receptor
• growth factor receptors
• HER-2
• tyrosine kinase