Bortezomib is a dipeptidyl boronic acid that selectively inhibits the ubiquitin proteasome pathway, which plays a role in the degradation of many intracellular proteins. It is the first-in-class selective and reversible inhibitor of the 26S proteasome, with antiproliferative and antitumor activity. It exerts its anti-neoplastic action mainly via the inhibition of the nuclear factor-κB pathway components associated with cell proliferation, apoptosis, and angiogenesis. The drug has revolutionized the treatment of multiple myeloma and, more recently, mantle cell lymphoma. In 2003, bortezomib received accelerated approval from the US Food and Drug Administration for the treatment of relapsed/refractory multiple myeloma and in 2008 for patients with previously untreated multiple myeloma. In 2006, bortezomib was approved for the treatment of refractory/relapsed mantle cell lymphoma and, in 2014, for previously untreated mantle cell lymphoma. Bortezomib has also demonstrated clinical efficacy both as a single drug and in combination with other agents in light chain amyloidosis, lymphoplasmacytic lymphoma/Waldenstrom macroglobulinemia, and peripheral T-cell lymphomas. Furthermore, continued clinical studies are required to confirm its value for patients with indolent and aggressive B-cell non-Hodgkin lymphomas and acute leukemias.

中文翻译：

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硼替佐米治疗血液系统恶性肿瘤：15年后。

硼替佐米是一种二肽基硼酸，可选择性抑制泛素蛋白酶体途径，该途径在许多细胞内蛋白质的降解中起作用。它是26S蛋白酶体的一流选择性和可逆抑制剂，具有抗增殖和抗肿瘤活性。它主要通过抑制与细胞增殖，凋亡和血管生成有关的核因子-κB通路成分发挥其抗肿瘤作用。该药物彻底改变了多发性骨髓瘤和最近的套细胞淋巴瘤的治疗方法。2003年，硼替佐米获得了美国食品和药物管理局的加速批准，用于治疗复发/难治性多发性骨髓瘤，2008年获得了先前未治疗的多发性骨髓瘤患者的批准。在2006年，硼替佐米被批准用于治疗难治性/复发性套细胞淋巴瘤，并于2014年被批准用于先前未治疗的套细胞淋巴瘤。硼替佐米还已经证明在单一药物以及与其他药物联合治疗轻链淀粉样变性，淋巴浆细胞性淋巴瘤/ Waldenstrom巨球蛋白血症和外周T细胞淋巴瘤方面的临床疗效。此外，需要继续进行临床研究以确认其对惰性和侵袭性B细胞非霍奇金淋巴瘤和急性白血病患者的价值。