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Idelalisib

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Small Molecules in Hematology

Part of the book series: Recent Results in Cancer Research ((RECENTCANCER,volume 212))

Abstract

Idelalisib (GS-1101, CAL-101, Zydelig®) is an orally bioavailable, small-molecule inhibitor of the delta isoform (p110δ) of the enzyme phosphoinositide 3-kinase (PI3K). In contrast to the other PI3K isoforms, PI3Kδ is expressed selectively in hematopoietic cells. PI3Kδ signaling is active in many B-cell leukemias and lymphomas. By inhibiting the PI3Kδ protein, idelalisib blocks several cellular signaling pathways that maintain B-cell viability. Idelalisib is the first PI3K inhibitor approved by the US Food and Drug Administration (FDA). Treatment with idelalisib is indicated in relapsed/refractory chronic lymphocytic leukemia (CLL), follicular lymphoma (FL), and small lymphocytic lymphoma (SLL). This review presents the preclinical and clinical activity of idelalisib with a focus on clinical studies in CLL.

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Authors and Affiliations

  1. Department of Medicine I: Hematology, Oncology, and Stem Cell Transplantation, University Medical Center Freiburg, Hugstetterstr. 55, 79106, Freiburg, Germany

    Katja Zirlik

  2. Tumor and Breast Center ZeTuP, St. Gallen, Switzerland

    Katja Zirlik

  3. Department of Hematology, Leiden University Medical Center, Leiden, The Netherlands

    Hendrik Veelken

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Correspondence to Hendrik Veelken .

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  1. MOLIT Institute, Cancer Center Heilbronn-Franken, SLK-Clinics, Heilbronn, Baden-Württemberg, Germany

    Uwe M. Martens

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Zirlik, K., Veelken, H. (2018). Idelalisib. In: Martens, U. (eds) Small Molecules in Hematology. Recent Results in Cancer Research, vol 212. Springer, Cham. https://doi.org/10.1007/978-3-319-91439-8_12

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