Copanlisib — Drug Monograph

Brand names: Aliqopa

Drug class: PI3K Inhibitor

Mechanism of Action

Copanlisib is an intravenous inhibitor of phosphatidylinositol-3-kinase (PI3K) with predominant inhibitory activity against PI3K-alpha and PI3K-delta isoforms expressed in malignant B cells. By inhibiting these isoforms, it blocks several key cell signaling pathways including B-cell receptor signaling, CXCR12-induced chemotaxis of B-cells, and NF-kappaB signaling. This results in the inhibition of proliferation and induction of apoptosis in lymphoma cell lines. Its IV administration and pan-PI3K profile distinguish it from the delta-selective oral inhibitors.

FDA Indications

• Treatment of adult patients with relapsed follicular lymphoma (FL) who have received at least two prior systemic therapies

Common Side Effects

• Hyperglycemia
• Hypertension
• Diarrhea
• Decreased general strength and energy
• Neutropenia
• Nausea
• Lower respiratory tract infections
• Thrombocytopenia

Clinical Pearl

Copanlisib is unique among PI3K inhibitors because of its intravenous route and its potent alpha-isoform inhibition, which causes transient post-infusion hyperglycemia. Blood glucose levels often spike significantly following the infusion and usually return to baseline within 24 hours; acute management with insulin is occasionally needed. Unlike oral PI3K-delta inhibitors, it has a lower reported incidence of severe immune-mediated colitis. Prophylaxis for Pneumocystis jirovecii (PJP) should…

Related Therapies & Mechanisms

• Duvelisib (Copiktra) — PI3K Inhibitor · Lymphoma
• Gedatolisib (Revtorpyk) — PI3K Inhibitor
• Inavolisib (Itovebi) — PI3K Inhibitor
• Acalabrutinib (Calquence) — Lymphoma