PD-083176

Considerable progress has been made with tyrosine kinase inhibitors. After long and sustained efforts, several tyrosine kinase inhibitors with convincing in vivo experimental antitumour properties such as CP-358,774, ZD 1839, CEP-751 are entering Phase I clinical trials. Significant in vivo experimental antitumour activity has also been described for two new families of farnesyl transferase inhibitors (SCH 59228 and PD 083176 series). Novel inhibitors of tubulin polymerisation are on the verge of entering clinical trials. These include F12458, an analogue of vinorelbine, and C52/C55 cryptophycin derivatives.