The experimental antitumor activity of the alkylphosphocholines, a new class of signal transduction inhibitors, has been demonstrated repeatedly. The alkylphosphocholines have inhibitory activities on protein kinase C (PKC) and phospholipase C. The PKC pathway of signal transduction may be involved in cellular differentiation and in the induction of apoptosis. Moreover, PKC inhibition by miltefosine may affect tumor invasion and metastasis formation. Miltefosine may also interfere with immunological mechanisms. Finally, in addition to its antitumor activity, miltefosine also exerts substantial effects on a number of Leishmania strains. In brief, miltefosine and other alkylphosphocholines interact with signal transduction components of cellular functions such as differentiation, growth control, migration, tumor promotion and cell death. Due to these activities, this new class of pharmacophores has a great potential in the treatment of cancer and certain parasitic diseases. (C) 1999 Prous Science. All rights reserved.