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Copanlisib: An Intravenous Phosphatidylinositol 3-Kinase (PI3K) Inhibitor for the Treatment of Relapsed Follicular Lymphoma

OBJECTIVE:

To review the mechanism of action, clinical efficacy, safety, dosage, administration, and role of copanlisib in the treatment of relapsed follicular lymphoma (FL).

DATA SOURCES:

Sources of information were identified through searches of PubMed (August 2014 to January 2019) using the key terms copanlisib, Aliqopa, PI3K inhibitor, and BAY 80-6946. Unpublished abstract information was obtained from the American Society of Clinical Oncology.

STUDY SELECTION AND DATA EXTRACTION:

Review articles and studies in the English language evaluating the pharmacology, efficacy, and safety of copanlisib were included.

DATA SYNTHESIS:

Copanlisib is the first intravenous phosphatidylinositol 3-kinase (PI3K) inhibitor approved for the treatment of relapsed FL in patients who have received at least 2 prior systemic therapies. The safety and efficacy of copanlisib has been studied in the multicenter, single-arm, phase II CHRONOS-1 study. The results reported for FL patients were an objective response rate of 59%, a complete response of 14%, median duration of response of 22.6 months, and median progression-free survival of 11.2 months. The most common adverse events reported were hyperglycemia and hypertension, which were infusion related and transient. Relevance to Patient Care and Clinical Practice: Copanlisib is unique in that it is a pan-class I PI3K inhibitor with preferential inhibitory activity against the PI3K-α and PI3K-δ isoforms. It has a more favorable safety profile than the other agents in its class with no late-onset toxicities.

CONCLUSIONS:

Copanlisib provides an alternative option for patients with relapsed FL. It is safe and effective and has an acceptable toxicity profile.

Related Products

Cat.No. Product Name Information
S2802 Copanlisib Copanlisib is a potent pan-class I PI3K with IC50 of 0.5, 3.7, 6.4, and 0.7 nM in cell-free assays for PI3Kα/β/γ/δ , respectively. Phase 3.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!

Related Targets

PI3K