Bortezomib is the first proteasome inhibitor drug tested in human patients. Bortezomib demonstrates a particular clinical utility in the treatment of multiple myeloma (MM), where it is the only one of the new drugs administered as mono-therapy that prolongs survival. The significant problem for the consistent pursuit of bortezomib was neurotoxicity, which has been significantly reduced by registering subcutaneous administration or being administered once per week. Bortezomib is currently approved for the treatment of patients with progressive MM in mono-therapy and in combination with prednisone and melphalan in cases of untreated patients who are not candidates for autologous hematopoietic stem cell transplantation (AHSCT) and in combination with dexamethasone or dexamethasone and thalidomide in untreated MM patients, who are candidates for treatment AHSCT. Clinical research is focused on the combination of bortezomib with other new drugs with the hope of further optimizing the treatment of patients with multiple myeloma.