Idelalisib

Idelalisib (i-deh-luh-LIH-sib) is a drug used with rituximab to treat chronic lymphocytic leukemia (CLL) that has come back. It is also used to treat follicular B-cell non-Hodgkin lymphoma (NHL) and small lymphocytic lymphoma (SLL) that have come back after treatment with other anticancer therapy. It is also being studied in the treatment of other types of cancer. Idelalisib blocks certain proteins, which may help keep cancer cells from growing and may kill them. It is a type of kinase inhibitor. Also called Zydelig.

Information about Idelalisib

Idelalisib is an oral kinase inhibitor that is approved for use in combination with rituximab in relapsed or refractory chronic lymphocytic leukemia (CLL) and as monotherapy for relapsed follicular B cell and small lymphocytic lymphoma. 

Liver safety of Idelalisib

Idelalisib is associated with a high rate of minor serum enzyme elevations during therapy and has been reported to cause clinically apparent acute liver injury that can be severe and even fatal. 

Mechanism of action of Idelalisib

Idelalisib (eye del" a lis' ib) is an orally available, small molecule inhibitor of phosphatidylinositol 3-kinase delta (PI3Kδ), which is an essential component in the B cell signaling pathways that drive migration of B cells to lymph nodes and bone marrow.  Inhibition of this pathway inhibits B cell chemotaxis and adherence and reduces cell viability.  This pathway is upregulated in many B cell malignancies and has been shown to be critical for proliferation and survival of leukemia and lymphomatous malignant B lymphocytes. 

FDA approval information for Idelalisib

Idelalisib was approved for use in the United States as therapy for relapsed CLL in combination with rituximab and as monotherapy for indolent forms of non-Hodgkin’s lymphoma in 2014. 

Dosage and administration for Idelalisib

Idelalisib is available as tablets of 100 and 150 mg under the brand name Zydelig.  The recommended dose is 150 mg twice daily until disease progression or unacceptable toxicity. 

Side effects of Idelalisib

Side effects are common but usually mild-to-moderate in severity, and include nausea, diarrhea, headache, stomatitis, fever, pain, rash, infections, arthralgia and fatigue.  Common laboratory abnormalities can include cytopenias, liver enzyme elevations, hyper- or hypo-glycemia, and hyponatremia.  Severe adverse events can include liver failure, severe diarrhea, pneumonitis, intestinal perforation, severe skin rash, anaphylaxis, neutropenia and embryo-fetal toxicity.

 

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