Preterm delivery presents the main cause of neonatal morbidity and mortality worldwide. The rate of preterm delivery is 12% to 13% in the United States, of which 29% concerns preterm deliveries before 34 weeks of gestation. Basic parameter of prevention strategy is implementation of tocolytic therapy in cases of threatened preterm labor. Several therapeutic approaches have been proposed, among which betamimetic agonists, calcium channel blockers, magnesium sulfate, oxytocin receptor blockers, nitrates, and prostaglandin inhibitors, whereas new alternatives such as usage of thiocolchicoside have also been reported. This article is one among few that aims to review the comparative effectiveness of various tocolytic agents regarding prevention of preterm delivery, impact on perinatal morbidity and mortality, neonatal health status, and maternal complications. Main conclusions of recent randomized control trials and meta-analyses are summarized to assess about which agents consensus already exists on their effectiveness, which agents should be further studied to achieve conclusions, as well as those that are rather unlikely to have significant tocolytic impact or any other benefit on neonatal outcome.