The currently available long-acting somatostatin analogs normalize serum growth hormone (GH) levels and insulin-like growth factor-I levels in approximately 60% of patients with acromegaly. The recently introduced GH receptor antagonist, pegvisomant, is able to normalize insulin-like growth factor-I levels in virtually all acromegalic subjects. Although no correlation between increased GH concentrations and tumor size has been found, long-term safety studies are still in progress. Also, pegvisomant monotherapy is administered once daily and is very costly. Combined treatment of a somatostatin analog with pegvisomant appears to be an effective and rational approach.