TY - CHAP M1 - Book, Section TI - Idelalisib: A First-in-Class Specific Inhibitor of PI3Kδ for the Treatment of B-cell Lymphomas A1 - Hilal-Dandan, PhD, Department of Pharmacology, University of California, San Diego, Randa A2 - Brunton, Laurence L. A2 - Chabner, Bruce A. A2 - Knollmann, Björn C. Y1 - 2015 N1 - T2 - Goodman & Gilman's: The Pharmacological Basis of Therapeutics, 12e AB - Idelalisib (zydelig) is a first-in-class oral inhibitor of the enzyme phosphatidylinositol 3-kinase-δ (PI3Kδ) isoform that was approved by the FDA in July 2014 for the treatment of patients with relapsed or refractory B-cell malignancies (eFigure 62–1.1).1 The PI3Kδ isoform in the PI3K signaling pathway is constitutively activated in many B-cell malignancies, and inhibition of this pathway promotes apoptosis in these cancerous cells. The FDA granted idelalisib accelerated approval for treatment of relapsed follicular B-cell non-Hodgkin lymphoma (FL) and relapsed small lymphocytic lymphoma (SLL). Accelerated approval allows a drug to be used to treat a serious or life-threatening disease based on a surrogate end point predictive of a clinical benefit in patients. Idelalisib, in combination with rituximab, was also approved as a “breakthrough therapy” for relapsed chronic lymphocytic leukemia (CLL). Idelalisib, available in 100-mg and 150-mg tablets, is administered orally twice daily. Idelalisib may cause serious and sometimes fatal side effects, including liver toxicity, diarrhea, colon inflammation, lung inflammation, intestinal perforations, and skin toxicity. The drug carries a black box warning to caution patients and healthcare providers about these serious risks, and its use is conditional on employing a risk evaluation and mitigation strategy (REMS).2,3 SN - PB - McGraw-Hill Education CY - New York, NY Y2 - 2022/06/29 UR - accessbiomedicalscience.mhmedical.com/content.aspx?aid=1127872490 ER -