Acromegaly is an endocrine disorder usually due to a growth hormone (GH)-secreting pituitary adenoma. This deforming disease is associated with several metabolic abnormalities and results in an elevated cardiovascular mortality. Pituitary transsesphenoidal surgery has been considered the treatment of choice, however, even in the most experienced hands this procedure succeeds in curing only 50 to 60% of the patients. Therefore, close to 50% of patients require an adjunctive form of treatment such as radiation therapy or the use of diverse medications that modulate GH secretion (somatostatin analogues) or action (GH receptor antagonists). The present review summarizes the clinical experience with these novel medications.