The biological synergism arising when administered in biosystem combinations of biologically active compounds (BAC) is the basis of some modes of modern chemotherapy of cancer. In this regard, manageability and predictability of response of biological systems on a combination of BAC is extremely important to promote further progress in the field of medical research. One of the most studied groups of BACs showing its biological synergies when used together, are aromatic compounds of DNA-directed action. Their mechanism of biological action is associated with the processes of non- covalent complexation: heteroassosiation of drugs and/or competition for DNA landing site. If the molecular complexation is the basis for the observed in the experiment biological synergy, there must be a quantitative relationship between biological and physic-chemical parameters. In either explicitly or implicitly search of this relationship held by many researchers that eventually allowed revealed some important correlation of biological and physic-chemical parameters in various private systems and to lay the foundations of the theory of interceptor-protector effect (IPE). The purpose of this paper is to create statistical-thermodynamic basis of the theory of generalized interceptor- protector effect in multicomponent DNA-binding BAC systems.