Department of Pharmaceutical Chemistry & Analysis, Indo-Soviet Friendship College of Pharmacy, Ferozepur G.T. Road, Moga-142 001, Punjab, India.
Maharishi Markandeshwar University, Solan-173229, Himachal Pradesh, India.
Anticancer Agents Med Chem. 2020;20(10):1158-1172. doi: 10.2174/1871520620666200317105207.
Lymphoma refers to a specialized category of blood cancers, which is characterized by lymph node enlargement, reduced body weight, prolonged tiredness, and fever associated with sweats. Traditional treatment strategies involve chemotherapy, radiation therapy, targeted therapy, and surgery. Copanlisib has emerged as a very potent drug which acts through inhibiting PI3K enzyme. The FDA has approved it for specific treatment of follicular Lymphoma in September 2017. Copanlisib induces tumor cell death along with the prevention of proliferation of dominant malignant β-cells. Copanlisib has a large volume of distribution i.e., 871L (%CV 47.4), plasma protein binding up to 15.8%, plasma half-life(t1/2) of 39.1h and the mean systemic plasma clearance 18.9 L/h (%CV 51.2). In the present review, various aspects related to Copanlisib have been summarized, which include pathophysiology, synthetic strategy, pharmacokinetics, pharmacodynamics and clinical studies. A special emphasis is paid on various reported adverse effects and in silico/in vivo studies conducted on Copanlisib.
淋巴瘤是一种特殊类型的血液癌，其特征是淋巴结肿大、体重减轻、持续疲劳和与出汗相关的发热。传统的治疗策略包括化疗、放射治疗、靶向治疗和手术。Copanlisib 是一种非常有效的药物，通过抑制 PI3K 酶发挥作用。FDA 已于 2017 年 9 月批准其用于特定的滤泡性淋巴瘤治疗。Copanlisib 诱导肿瘤细胞死亡，并防止主要恶性 β 细胞的增殖。Copanlisib 的分布容积很大，为 871L（%CV 47.4），血浆蛋白结合率高达 15.8%，血浆半衰期（t1/2）为 39.1 小时，平均全身血浆清除率为 18.9 L/h（%CV 51.2）。在本综述中，总结了与 Copanlisib 相关的各个方面，包括病理生理学、合成策略、药代动力学、药效学和临床研究。特别强调了各种已报道的不良反应以及对 Copanlisib 进行的计算和体内研究。
