Copanlisib

DB12483ApprovedInvestigationalSmall moleculeKinase Inhibitor

Copanlisib is a PI3K inhibitor used to treat relapsed follicular lymphoma in adults. Copanlisib is a selective pan-Class I phosphoinositide 3-kinase (PI3K) inhibitor with preferential activity against the alpha and delta isoforms.

Mechanism: 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 IC50 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.
Curator reviewed · 4 references
Primary indication: Copanlisib is indicated for the treatment of adults with relapsed follicular lymphoma (FL) who have received at least two prior systemic therapies.Curator reviewed · 1 structured indication
Formula / weight: C₂₃H₂₈N₈O₄ · 480.529 g/mol (avg)
First approval: United States, 2017
Also known as: 2-AMINO-N-(7-METHOXY-8-(3-(MORPHOLIN-4-YL)PROPOXY)-2,3-DIHYDROIMIDAZO(1,2-C)QUINAZOLIN-5-YL(PYRIMIDINE-5-CARBOXAMIDE · 2-AMINO-N-(7-METHOXY-8-(3-MORPHOLIN-4-YLPROPOXY)-2,3-DIHYDROIMIDAZO(1,2-C)QUINAZOLIN-5-YL)PYRIMIDINE-5-CARBOXAMIDE · 5-PYRIMIDINECARBOXAMIDE, 2-AMINO-N-(2,3-DIHYDRO-7-METHOXY-8-(3-(4-MORPHOLINYL)PROPOXY)IMIDAZO(1,2-C)QUINAZOLIN-5-YL)-
Code names: BAY 80-6946
Brand names: Aliqopa