Idelalisib (Zydelig)

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General information

Class/mechanism: Isoform-selective PI3K (phosphatidylinositol 3-kinase) inhibitor. Idelalisib inhibits class I isoform p110 delta (p110δ), which is one of the mediators of activation of the PI3K pathway and is expressed at high levels by hematopoietic cells, particularly leukocytes. Inhibition of the PI3Kδ kinase pathway affects B-cell receptor (BCR), CXCR4, and CXCR5 signaling, disrupting trafficking and homing of B-cells to the lymph nodes and bone marrow. Lymphoma cells treated with idelalisib have been observed to have impaired chemotaxis, adhesion properties, and cell viability.[1][2][3][4][5][6]
Route: PO
Extravasation: n/a

For conciseness and simplicity, currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]

Diseases for which it is established (work in progress)

Diseases for which it is used

Diseases for which it was used

Patient drug information

Suggestions for SAE monitoring/prevention

  • Administer PCP/PJP prophylaxis throughout treatment
  • Monitor for CMV infection (positive PCR or antigen test) and discontinue treatment if any evidence of infection
  • Monitor blood counts at least every 2 weeks for the first 6 months of treatment
    • Increase monitoring to at least weekly if ANC < 1000/mm3

History of changes in FDA indication

Chronic lymphocytic leukemia - PARTIALLY WITHDRAWN

Follicular lymphoma - WITHDRAWN

History of changes in EMA indication

  • 2014-09-18: Initial authorization
  • Zydelig is indicated in combination with an anti-CD20 monoclonal antibody (rituximab or ofatumumab) for the treatment of adult patients with chronic lymphocytic leukaemia (CLL) who have received at least one prior therapy.
  • Zydelig is indicated in combination with an anti-CD20 monoclonal antibody (rituximab or ofatumumab) for the treatment of adult patients with chronic lymphocytic leukaemia (CLL) as first line treatment in the presence of 17p deletion or TP53 mutation in patients who are not eligible for any other therapies.
  • Zydelig is indicated as monotherapy for the treatment of adult patients with follicular lymphoma (FL) that is refractory to two prior lines of treatment.

History of changes in Health Canada indication

  • 2015-03-27: Initial notice of compliance with conditions
  • 2020-04-21: Conditions were met

Also known as

  • Code names: CAL-101, GS-1101
  • Brand name: Zydelig


  1. 1.0 1.1 1.2 Idelalisib (Zydelig) package insert
  2. Idelalisib (Zydelig) package insert (locally hosted backup)
  3. Zydelig manufacturer's website
  4. S. E. Coutre, J. C. Byrd, R. R. Furman, J. R. Brown, D. M. Benson, N. D. Wagner-Johnston, I. W. Flinn, B. S. Kahl, S. E. F. Spurgeon, B. J. Lannutti, H. K. W. Hsu, R. Ulrich, S. Peterman, L. Holes, L. L. Miller, A. S. Yu. Phase I study of CAL-101, an isoform-selective inhibitor of phosphatidylinositol 3-kinase P110d, in patients with previously treated chronic lymphocytic leukemia. 2011 ASCO Annual Meeting abstract 6631.
  5. I. W. Flinn, J. C. Byrd, R. R. Furman, J. R. Brown, T. S. Lin, C. Bello, N. A. Giese, A. S. Yu. Preliminary evidence of clinical activity in a phase I study of CAL-101, a selective inhibitor of the p1108 isoform of phosphatidylinositol 3-kinase (P13K), in patients with select hematologic malignancies. 2009 ASCO Annual Meeting abstract 3543.
  6. Lannutti BJ, Meadows SA, Herman SE, Kashishian A, Steiner B, Johnson AJ, Byrd JC, Tyner JW, Loriaux MM, Deininger M, Druker BJ, Puri KD, Ulrich RG, Giese NA. CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood. 2011 Jan 13;117(2):591-4. Epub 2010 Oct 19. PubMed