Copanlisib: Novel PI3K Inhibitor for the Treatment of Lymphoma

医学 淋巴瘤 滤泡性淋巴瘤 不利影响 药代动力学 药理学 淋巴结 内科学 肿瘤科 化疗 癌症研究
作者
Anshul Kumar,Rohit Bhatia,Pooja A. Chawla,Durgadas Anghore,Vipin Saini,Ravindra K. Rawal
出处
期刊:Anti-cancer Agents in Medicinal Chemistry [Bentham Science Publishers]
卷期号:20 (10): 1158-1172 被引量:10
标识
DOI:10.2174/1871520620666200317105207
摘要

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.
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