Insulin resistance is the main pathogenetic component of many metabolic diseases, including obesity, type 2 diabetes mellitus, gestational diabetes mellitus, and polycystic ovary syndrome (PCOS). Despite the fact that to date the mechanisms of insulin resistance formation have not been established, one of the promising directions at present is the search for potential therapeutic strategies for its correction, due to the fact that this also improves the course of the concomitant underlying disease. Insulin sensitizers are a generally recognized method of PCOS therapy due to their safety and effectiveness in normalizing the metabolic and endocrine profile of patients with polycystic ovary syndrome. The leading position in this direction is occupied by the combination of myo-inositol (MI) with D-chiro-inositol (DHI) in a ratio of 40:1, which, according to the conducted studies, is comparable to the concentration of inositols in the blood plasma of healthy women. This ratio of MI/DHI is effective both for normalization of the metabolic profile, and for regulation of the menstrual cycle and overcoming anovulatory infertility. An analysis of the literature has shown that a number of biologically active substances, such as folic acid, vitamin D and alpha-lipoic acid, in combination with insulin sensitizers, have additional advantages, which gives grounds for continuing research on their significance as components of combined treatment, as well as in the search for the optimal dose and duration of such therapy.