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The concept of nontraditional biomedical screening of chemical compounds as potential drugs for various diseases is presented. This concept, based on ideas developed by L.A. Piruzyan, envisages (i) the maximum possible similarity of the testing conditions to the conditions in the human body affected by pathology and (ii) novel approaches to screening: (1) tests using molecular targets or biological test objects (BTOs) obtained from patients; (2) obtaining of BTOs from patients with (a) the disease stage and (b) the patient's ethnicity being taken into account in order to determine the characteristic features of the pathological process at different stages of disease and in different populations; (3) mapping of patients with a given disease with respect to the corresponding markers; (4) selection of substances that normalize the values of the markers to control levels; and (5) clinical trials of these substances. Published data on the properties, dynamics, and pathogenetic significance of biochemical markers of atherosclerosis, diabetes mellitus, and progeria are systematized. Theoretical grounds are presented for the possibility of nontraditional biomedical screening of potential agents for “molecular/biochemical treatment” for these diseases.