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Copanlisib is a PI3K inhibitor used to treat relapsed follicular lymphoma in adults.
Copanlisib is a PI3K inhibitor used to treat relapsed follicular lymphoma in adults.
Phosphatidylinositol-3-kinase (PI3K) signalling pathway is implicated in cell proliferation and survival, as well as resistance to chemotherapeutic agents. PI3K isoforms are often overexpressed in B-cell malignancies, including follicular lymphoma. Copanlisib is a class I PI3K inhibitor with preferential activity against PI3K-α and PI3K-δ isoforms expressed in malignant B cells. It binds with IC values of 0.5, 3.7, 6.4, and 0.7 nmol/L against class I PI3K-α, β, γ, and δ isoforms, respectively. Copanlisibinduces tumour cell death by apoptosis, blocks cell cycle progression, and inhibits the proliferation of primary malignant B cell lines. Copanlisib inhibits several key cell signalling pathways, including B-cell receptor (BCR) signalling, CXCR12-mediated chemotaxis of malignant B cells, and NFκB signalling in lymphoma cell lines.
Copanlisib is indicated for the treatment of adults with relapsed follicular lymphoma (FL) who have received at least two prior systemic therapies. This indication was granted under accelerated approval; thus, continued approval may be contingent upon verification and description of clinical benefit in a confirmatory trial.
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