新一类蛋白酶体抑制剂bortezomib

Bortezomib: a new proteasome inhibitor

综述了bortezomib的药理作用、药动学及临床评价。本品是一种新型的蛋白酶体抑制剂,临床上用于复发性和难治性多发性骨髓瘤的治疗。

Bortezomib is a reversible inhibitor of the chymotrypsin-like activity of the 26S proteasome in mammalian cells. Inhibition of the 26S proteasome prevents this targeted proteolysis which can affect multiple signaling cascades within the cell. Clinical studies demonstrated that bortezomib causes a delay in tumor growth in vivo, including relapsed and refractory muhiple myeloma. This review presents the pharmacological action, pharmacokinetics and clinical evaluation of bortezomib.