The historic change in medicine from a holistic approach to methods ba
sed on natural sciences still reverberates in current practice as well
as in the social and political framework of cancer treatment. Only re
cently has the perception of patients as suffering humans rather than
carriers of disease to be eradicated lead to the introduction of palli
ative care. Advances in general pharmacotherapy have much relied on th
e concept of specific interaction between drug and target molecule fir
st authored by Paul Ehrlich using the romantic term of a magic bullet.
This theme of specificity was explored and described in detail as dru
g protein interaction during the next century. Specific cellular targe
t proteins are ionic channels, enzymes, transporter proteins and recep
tors. While these may be targeted by antineoplastic agents they occur
not exclusively in tumour cells but also in normal stem cells. Nonethe
less, small differences in cellular behaviour after sustaining injurie
s have been exploited in such way that curative treatment regimens are
now available for several tumour entities even in advanced state. Dru
g screening and development as well as principles of cancer treatment
derived by empirical rationalism have been cornerstones in this proces
s lasting for about five decades. Molecular biology has helped to eluc
idate several mechanisms of drug resistance, and finally gave insight
how genes govern the checkpoints leading to either differentiation, pr
oliferation or cell death. The internal control of cellular fate may b
e influenced via signal transduction at the level of receptors or kina
ses and other enzymes. Ultimately the immense specificity of nucleic a
cid hybridisation opens new horizons for specific drug target interact
ion. Immunotherapy has originally been the most successful approach in
systemic therapy and is now being developed to an impressive range of
passive or active treatments including vaccination.