4.4 Review

Copanlisib: Novel PI3K Inhibitor for the Treatment of Lymphoma

Journal

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
Volume 20, Issue 10, Pages 1158-1172

Publisher

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1871520620666200317105207

Keywords

Lymphoma; PI3K; copanlisib; systemic plasma clearance; lymph node enlargement; blood cancer

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Lymphoma refers to a specialized category of blood cancers, which 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 beta-cells. Copanlisib has a large volume of distribution i.e., 871L (%CV 47.4), plasma protein binding up to 15.8%, plasma hall-life(t(1/2)) or 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 silieo/in vivo studies conducted on Copanlisib.

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