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Gestational diabetes mellitus (GDM) has been recognized as an important cause of fetomaternal morbidity and mortality, as well as various long-term endocrine-metabolic implications in both parts. Classically, insulin has dominated the therapeutic armamentarium for GDM. However, its adverse effects and related logistic inconvenients--such as multiple daily injections, cost, requirement for refrigeration, and the need for training in appropriate application--have propelled interest in the use of oral antidiabetics for GDM, especially metformin. Research has centered on this drug owing to its safe pharmacokinetic profile, along with its notorious insulin-sensitizing effect. Indeed, exacerbation of the physiological insulin resistance typically observed in pregnancy constitutes the fundamental pathophysiologic phenomenon in GDM. In this context, metformin use for the treatment of GDM has attracted an intense interest in the field of clinical research. Metformin has demonstrated to be effective at achieving satisfactory metabolic control in GDM. Likewise, it has been associated with various other beneficial secondary outcomes such as lower maternal weight gain, incidence of gestational hypertension, incidence of neonatal hypoglycemia, and frequency of admission into neonatal intensive care units. Furthermore, metformin may attenuate the deleterious endocrine-metabolic effects of GDM in offspring, although available evidence remains preliminary. Besides, although research is scarce, metformin appears to be more effective and safe in GDM than other oral antidiabetics, such as glibenclamide. Nevertheless, not all women appear to respond with equal effectiveness to treatment with metformin, and the identification of predicting factors, such as obesity and hyperglycemia severity, represent a key goal for research. [ABSTRACT FROM AUTHOR]