- Class: PI3K inhibitor – primarily PI3K-α and PI3K-δ isoforms.Type: Small molecule, intravenous.
Mechanism of Action (MOA)
- Inhibits phosphatidylinositol 3-kinase (PI3K) signaling, mainly α and δ isoforms.
- Blocks AKT/mTOR pathway → reduces cell proliferation, survival, and angiogenesis.
- Active in B-cell malignancies with PI3K pathway activation.
Clinical Uses
- Relapsed follicular lymphoma – in patients refractory to at least two prior systemic therapies.
- Investigational in other B-cell lymphomas and solid tumors.
Dosing (Adults)
- 60 mg IV infusion on days 1, 8, and 15 of a 28-day cycle.
- Infuse over 1 hour.
- Dose modifications for toxicity (hematologic or hyperglycemia).
Toxicities
- Hyperglycemia – often transient; monitor blood glucose.
- Hypertension – monitor BP during infusion.
- Hematologic: neutropenia, thrombocytopenia, anemia.
- Fatigue, diarrhea, nausea.
- Rare: pneumonitis, hepatotoxicity.
Monitoring
- Blood glucose – baseline, during infusion, and post-infusion.
- Blood pressure – before and during infusion.
- CBC with differential prior to each cycle.
- Liver function tests.
- Monitor for signs of infection.
Summary
Copanlisib (Aliqopa®) is an IV PI3K-α/δ inhibitor used for relapsed follicular lymphoma. Key concerns are hyperglycemia, hypertension, and myelosuppression, requiring pre-infusion monitoring of glucose and BP, as well as ongoing CBC and LFT checks.