Multitarget Control of Drug Impact: A Therapeutic Imperative in Cancer Systems Biology

  • Ariel Fernández Stigliano


The etiological heterogeneity and complexity of cancer has inspired drug developers to seek for multipronged strategies for therapeutic attack. In fact, the quasi single-target drug/cancer combination imatinib/CML is illustrative of the exception rather than the rule. On the other hand, multidrug treatments, with their pharmacodynamics and kinetics uncertainties and incompatibilities, do not offer an attractive therapeutic possibility for multipronged attack, except in the context of therapeutic editors delineated in Chap. 12. Fuelled by systems biology insights, the burgeoning interest in multitarget drugs is motivating a reassessment of the therapeutic value of promiscuity. While drug efficacy may not correlate with specificity, it would be risky to take the opposite stance and welcome promiscuous compounds haphazardly, without a rational strategy to funnel their therapeutic impact. In this chapter, we survey approaches to control the therapeutic impact of multitarget kinase inhibitors to fulfill the therapeutic imperatives of human cancer. Thus, we advocate for the application of the wrapping design concept to turn multitarget kinase inhibitors into clinical opportunities through judicious chemical modifications.


Epidermal Growth Factor Receptor Chronic Myeloid Leukemia Selectivity Filter System Biology Perspective Promiscuous Compound 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


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Copyright information

© Springer International Publishing Switzerland 2015

Authors and Affiliations

  1. 1.National Research Council–CONICETBuenos AiresArgentina
  2. 2.Former Karl F. Hasselmann Endowed Chair Professor of BioengineeringRice UniversityHoustonUSA

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