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INTRODUCTION. Sexual activity is an important component of the overall quality of life. Erectile dysfunction (ED) has recently been considered an epidemic of the 21st century and is an extremely common pathology that has been observed throughout all periods of the development of our civilization. The frequency of ED is increasing significantly every year, which is associated with an increase in the population of men suffering from ED. There are many models of ED treatment, of which metabolic therapy occupies an important place. MATERIALS AND METHODS. A systematic analytical review of the scientific literature on the effect of the amino acids arginine and citrulline on erectile function was conducted for the period 2015–2025 in the databases PubMed, Scopus, Google Scholar, ISSWSH. RESULTS AND DISCUSSION. The main pathophysiological mechanism leading to the formation of ED is a violation of cavernous hemodynamics. The key factors that shape the occurrence of an erection include hemodynamic changes, relaxation of smooth muscles and the regulatory effect of neurotransmitters, among which nitric oxide (NO) is the most influential universal secondary messenger. A decrease in the ability of endothelial cells to produce NO is most often the main cause of ED, as it causes impaired blood flow and a decrease in various functions of the male genitalia. During sexual stimulation, its concentration is released in the endothelium of blood vessels and smooth muscle cells, which leads to dilation of the vessels of the penis, the corpus cavernosum and the onset of an erection. The amino acid arginine is a metabolic substrate for the synthesis of the primary mediator NO. Arginine acts on the vascular system and participates in the regulation of testosterone synthesis, and a decrease in its level is a risk factor for the development of vascular pathology of the genital organs. One of the possible ways to eliminate endothelial dysfunction is to enhance the synthesis of NO by adding exogenous L-arginine. To date, it is believed that phosphodiesterase type 5 inhibitors (PDE5 inhibitors) are the first-line therapy for most men with ED. Certain groups of patients who have a burdened health condition in the form of severe diabetes mellitus, arterial hypertension, secondary hypogonadism are difficult to treat exclusively with PDE5 inhibitors, taking into account systemic disorders of endothelial function. In the event of such clinical circumstances, the search for new drugs becomes particularly promising. Oral administration of L-arginine in high doses causes a significant subjective improvement in sexual function in men with organic ED only under conditions of reduced excretion or production of NO. The benefits of L-arginine in the treatment of various male sexual dysfunctions are confirmed by a number of scientific studies, and the intake of L-citrulline increases the level of L-arginine in the blood serum and has a positive effect on the synthesis of nitric oxide, as a key metabolite of the endothelial function of the cavernous tissue of the penis. L-citrulline is converted to L-arginine in the kidneys, which justifies the need for its addition in ED as a donor of the L-arginine/NO/cGMP pathway. The use of L-citrulline improves the ratio of intra-abdominal pressure/microfibrillar pressure, the ratio of body weight/collagen, and increases the level of NOx. In Ukraine, the drug VALARGIN PLUS is registered — a dosage form containing L-arginine — 1500 mg and L — citrulline — 1500 mg (mg). CONCLUSIONS. Based on the above, it can be assumed that the use of L-arginine in combination with L-citrulline in the treatment of erectile dysfunction in men is a more effective method than monotherapy with L-arginine. The combination of L-arginine and L-citrulline (Valagrin Plus) is an effective component of the complex treatment of patients with erectile dysfunction.