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Drugs. 2017 Dec;77(18):2057-2062. doi: 10.1007/s40265-017-0838-6.
Bayer are developing copanlisib (Aliqopa™)-a pan-class I phosphoinositide 3-kinase (PI3K) inhibitor-as a treatment for various haematological and solid malignancies. The US FDA has granted copanlisib accelerated approval for the treatment of adults with relapsed follicular lymphoma who have received at least two prior systemic therapies based on the results of a phase II trial. Phase III trials are underway evaluating copanlisib as treatment for relapsed/refractory diffuse large B-cell lymphoma and in combination with rituximab or rituximab-based chemotherapy or standard immunochemotherapy in patients with relapsed indolent B-cell non-Hodgkin's lymphoma. Phase I/II studies are underway in relapsed or refractory peripheral T-cell or NK/T-cell lymphoma, advanced cholangiocarcinoma, hormone receptor-positive HER2-negative stage I-IV breast cancer, HER2-positive breast cancer and recurrent and/or metastatic head and neck squamous cell carcinomas harbouring a PI3KCA mutation/amplification and/or a PTEN loss. This article summarizes the milestones in the development of copanlisib leading to this first approval for relapsed follicular lymphoma.
拜耳公司正在开发一种名为 copanlisib（AliqopaTM）的泛 PI3K 抑制剂，用于治疗各种血液系统恶性肿瘤和实体瘤。美国 FDA 基于 II 期临床试验结果，加速批准 copanlisib 用于治疗至少接受过两种基于系统的先前治疗的滤泡性淋巴瘤成人患者。III 期临床试验正在进行中，评估 copanlisib 作为复发/难治性弥漫性大 B 细胞淋巴瘤的治疗药物，以及与利妥昔单抗或利妥昔单抗为基础的化疗或标准免疫化疗联合治疗复发惰性 B 细胞非霍奇金淋巴瘤。I/II 期研究正在复发或难治性外周 T 细胞或 NK/T 细胞淋巴瘤、晚期胆管癌、激素受体阳性 HER2 阴性 I-IV 期乳腺癌、HER2 阳性乳腺癌以及携带 PI3KCA 突变/扩增和/或 PTEN 缺失的复发性和/或转移性头颈部鳞状细胞癌患者中进行。本文总结了导致此次滤泡性淋巴瘤复发首次获批的 copanlisib 开发的里程碑事件。
