The restoration of the functions of the male reproductive system in type 2 diabetes mellitus (DM2) is one of the urgent problems of modern endocrinology. For this, both the drugs that improve glucose homeostasis and insulin sensitivity, primarily metformin, and the activators of luteinizing hormone receptor (LHR), such as human chorionic gonadotropin (hCG) and low-molecular-weight allosteric agonists of LHR, can be used. The aim of the work was to study the effect of metformin therapy (4 weeks, 120 mg/kg/day) on the stimulating steroidogenesis and spermatogenesis effects induced by 5-day administration of 5-amino-N-tert-butyl-2-(methylsulfanyl)-4-(3-(nicotinamido)phenyl)thieno[2,3-d]pyrimidine-6-carboxamide (TP03), an allosteric LHR agonist (15 mg/kg/day), and hCG (20 IU/rat/day) to male Wistar rats with DM2. The DM2 was induced by a high-fat diet and a low-dose streptozotocin (25 mg/kg). Metformin treatment partially restored testosterone levels and normalized spermatogenesis in DM2 rats. On the first day, metformin treatment enhanced the steroidogenic effects of TP03 and hCG, but on the following days its potentiating effect was not detected. After five days of treatment of diabetic rats with TP03 and hCG, the number of epididymal spermatozoa was restored, including those with progressive motility, and the proportion of the defective forms of spermatozoa was decreased. Spermatogenesis rates when treated with metformin or LHR agonists separately were comparable to those when they were used together. Thus, metformin therapy enhances the production of testosterone induced by TP03 and hCG on the first day of treatment with these drugs, but subsequently the steroidogenic and spermatogenic effects of LHR agonists in the groups of diabetic rats with and without metformin treatment did not differ significantly.