Dosing & Uses
Follicular Lymphoma
In November 2023, copanlisib was voluntarily withdrawn for follicular lymphoma
The decision was based on recently updated CHRONOS-4 study that showed the addition of copanlisib to standard immunochemotherapy regimens did not improve progression-free survival
Pharmacology
Mechanism of Action
Pan class I phosphatidylinositol-3-kinase (PI3K) inhibitor with predominant inhibitory activity against PI3K-alpha and PI3K-delta isoforms expressed in malignant B cells; by inhibiting several key cell-signaling pathways may induce apoptosis and inhibition of proliferation of premalignant B cells and in turn cause tumor cell death
Absorption
Peak plasma concentration: 463 ng/mL
AUC (0-25): 1570 ng·hr/mL
Distribution
Protein binding: 84.2% (mainly albumin)
Vd: 871 L
Metabolism
Metabolism is mediated by CYP3A (~90%) and CYP1A1 (<10%)
Elimination
Half-life: 39.1 hr Clearance: 17.9 L/hr
Excreted ~50% as unchanged compound and 50% as metabolites
Excretion, unchanged compound: Feces (30%), urine (15%)
