印度代购提示，本品硼替佐米是哺乳动物细胞中26S蛋白酶体糜蛋白酶样活性的可逆抑制剂。体外试验证明硼替佐米对多种类型的癌细胞具有细胞毒性。临床前肿瘤模型体内试验证明硼替佐米能够延迟包括多发性骨髓瘤在内的肿瘤生长。

Bortezomib is a reversible inhibitor of the protease-like activity of 26S proteasome chyme in mammalian cells. Bortezomib has been shown to be cytotoxic to many types of cancer cells in vitro. In vivo studies of preclinical tumor models have shown that bortezomib can delay tumor growth, including multiple myeloma.

硼替佐米

　　目前，多发性骨髓瘤仍然是不可治愈的疾病，这是治疗上的挑战，随着新药和新治疗手段的出现，使得MM治疗结局持续在改善。无论是否移植患者，诱导治疗目标：迅速减轻病人疾病负担，达到深度缓解。PI类药物头对头体外试验，硼替佐米抑制力最快显现；VRd方案治疗NDMM 1.1个月快速起效，可快速降低肿瘤负荷。

　　印度代购提示，本品根据目前国内可及的新药方案在治疗新诊断多发性骨髓瘤（NDMM）患者时的中位缓解时间可见，以硼替佐米为基础的方案快速起效，特别是VRd方案，仅需要1.1个月即可快速起效，实现诱导治疗需要快速降低肿瘤负荷的目标。2017年发表在《Bone Marrow Transplantation》上面的一项比较研究，共纳入1017例NDMM患者，患者接受不同方案的诱导治疗，比较患者的缓解质量（诱导后移植前）。

　　印度代购提示，本品结果显示：含硼替佐米方案诱导治疗后的缓解深度，显著优于不含硼替佐米方案。据NCCN、ESMO、中国多发性骨髓瘤指南推荐：以硼替佐米基础联合方案为NDMM诱导治疗一线用药， 2020 NCCN.V2首选推荐VRd和VCD。硼替佐米是一种蛋白酶体抑制剂，国内商品名为万珂。本品的推荐剂量为单次注射1.3 mg/m2，每周注射2次，连续注射2周（即在第1、4、8和11天注射）后停药10天（即从第12至第21天）。3周为1个疗程，两次给药至少间隔72小时。对于超过8个疗程的维持治疗，可按标准方案给药，也可以按每周1次、连续给药4周的维持方案（第1、8、15和22天），随后是13天的休息期（第23至25天）。

The results showed that the depth of remission after induction therapy with bortezomib was significantly better than that without bortezomib. According to NCCN, ESMO and Chinese guidelines for multiple myeloma, bortezomib based combination regimen is the first line of NDMM induction therapy, and 2020 NCCN.V2 first recommends VRd and VCD. Bortezomib is a kind of proteasome inhibitor, the domestic trade name is Wanke. The recommended dose is a single injection of 1.3 mg/m2, twice a week, for 2 consecutive weeks (i.e., on days 1, 4, 8 and 11) followed by 10 days of withdrawal (i.e., from day 12 to day 21). A course of 3 weeks was given at least 72 hours apart. For more than 8 courses of maintenance therapy, medication may be given as a standard regimen or as a weekly, continuous 4-week maintenance regimen (days 1, 8, 15, and 22) followed by a 13-day rest period (days 23 to 25).