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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 Unpublished abstract information was obtained from the American Society of Clinical Oncology.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.

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Cat.No. Product Name Information Publications Customer Product Validation
S2802 Copanlisib (BAY 80-6946) Copanlisib (BAY 80-6946) 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. (7) (3)

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