Intended for healthcare professionals only.

ZYDELIG® (idelalisib) mechanism of action

ZYDELIG is the first oral phosphatidylinositol 3-kinase (PI3K) inhibitor approved in relapsed chronic lymphocytic leukemia (CLL)1,2

ZYDELIG inhibits PI3Kδ, a key driver of multiple B-cell processes1

  • ZYDELIG is thought to affect the life cycle of tumor cells derived from malignant B cells and primary tumor cells, and inhibit multiple cell signaling pathways involved in the trafficking and movement of B cells1

Inhibits multiple signaling pathways, including BCR, CXCR4, and CXCR51,3-5

ZYDELIG® inhibits multiple signaling pathways.

Inhibits proliferation and induces apoptosis1

ZYDELIG® inhibits proliferation and induces apoptosis.

Inhibits homing and adhesion1

ZYDELIG® inhibits homing and adhesion.

Mobilizes malignant B cells to the periphery, and may reduce lymph node burden1,6

ZYDELIG® mobilizes malignant B cells to the periphery.

Effects were observed in cell lines derived from malignant B cells and in primary tumor cells.1

Detailed visualization of the PI3K pathway.

For illustrative purposes only. Not all components of the pathway are illustrated.

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ZYDELIG dosing

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Adverse event monitoring &

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Call to learn more 1-844-622-2377

BCR=B-cell receptor; CLL=chronic lymphocytic leukemia; CXCR=C-X-C chemokine receptor; PI3Kδ=phosphatidylinositol 3-kinase delta.


  1. ZYDELIG® (idelalisib) [Prescribing Information]. Foster City, CA: Gilead Sciences, Inc.; rev February 2022.
  2. Hus I, Puła B, Robak T. PI3K inhibitors for the treatment of chronic lymphocytic leukemia: current status and future perspectives. Cancers (Basel). 2022;14(6):1571.
  3. Sharman JP, Coutré SE, Furman RR, et al. Efficacy of idelalisib in CLL subpopulations harboring del(17p) and other adverse prognostic factors: results from a phase 3, randomized, double-blind, placebo-controlled trial. Poster presented at: American Society of Clinical Oncology; May 30-June 3, 2014; Chicago, IL.
  4. Puri KD, Gold MR. Selective inhibitors of phosphoinositide 3-kinase delta: modulators of B-cell function with potential for treating autoimmune inflammatory diseases and B-cell malignancies. Front Immunol. 2012;3:256. doi:10.3389/fimmu.2012.00256
  5. Coutré SE, Barrientos JC, Brown JR, et al. Management of adverse events associated with idelalisib treatment: expert panel opinion. Leuk Lymphoma. 2015;56(10):2779-2786.
  6. Furman RR, Sharman JP, Coutré SE, et al. Idelalisib and rituximab in relapsed chronic lymphocytic leukemia. N Engl J Med. 2014;370(11):997-1007. doi:10.1056/NEJMoa1315226