The role of oxytocin and oxytocin receptors in preterm labor is perhaps more prominent than once thought. The blockade of oxytocin and/or oxytocin receptors has both a theoretical and clinical aspect. Initial trials with the oxytocin antagonist atosiban have been encouraging with respect to efficacy and side effect profile. Current trials are examining the efficacy and dosing regimens of atosiban. Additional work must be done with this drug. However, if subsequent data demonstrate that atosiban is as effective as ritodrine in obtaining uterine quiescence, on the basis of its milder side effect profile, it should be seriously considered as a tocolytic of choice for the treatment of preterm labor. Moreover, it may have significant appeal for combination use with other tocolytics, given its alternative mechanism of action to betamimetics and magnesium sulfate.