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What is Idelalisib?

  • Idelalisib (Zydelig) is a kinase inhibitor used to treat certain blood cancers.

Idelalisib skeletal.svg

What are the uses of this medicine?

This medicine is used to treat people with:

Limitations of use:

  • Zydelig should not be used as the first medicine to treat people with CLL, FL, or SLL.
  • Zydelig should not be used in combination with bendamustine and or rituximab to treat people with FL.
  • It is not known if Zydelig is safe and effective in children less than 18 years of age.

How does this medicine work?

  • 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.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

  • serious hypersensitivity reactions to idelalisib, including anaphylaxis, or patients with a history of toxic epidermal necrolysis with any drug.

What drug interactions can this medicine cause?

  • Coadministration with strong CYP3A inhibitors may increase idelalisib concentrations. Use other drugs that are not strong CYP3A inhibitors. If unable to use alternative drugs, monitor patients more frequently for Zydelig adverse reactions
  • Avoid coadministration of Zydelig with strong CYP3A4 inducers.

Is this medicine FDA approved?

  • This medicine is approved in the year 2014.

How should this medicine be used?

Recommended Dosage:

  • The recommended dosage of Zydelig is 150 mg administered orally twice daily with or without food until disease progression or unacceptable toxicity.


  • Take Zydelig exactly as your doctor tells you to take it.
  • Your doctor may change your dose of Zydelig or tell you to stop taking Zydelig. Do not change your dose or stop taking Zydelig without first talking to your doctor.
  • Take Zydelig 2 times a day.
  • You may take Zydelig with or without food.
  • Take Zydelig tablets whole.
  • Do not miss a dose of Zydelig. If you miss a dose of Zydelig by less than 6 hours, take the missed dose right away. Then take your next dose as usual. If you miss a dose of Zydelig by more than 6 hours, wait and take the next dose of Zydelig at your usual time.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

  • As Tablets: 100 mg, 150 mg.

This medicine is available in fallowing brand namesː

  • Zydelig

What side effects can this medication cause?

The most common side effects of Zydelig when used alone include:

The most common side effects of Zydelig when used in combination with rituximab include:

Zydelig can cause serious side effects, including:

What special precautions should I follow?

  • Severe Cutaneous Reactions may occur. Monitor patients for the development of severe cutaneous reactions. Permanently discontinue Zydelig if confirmed.
  • Serious hypersensitivity reactions, including anaphylaxis, have been reported in patients on Zydelig. Permanently discontinue Zydelig and institute appropriate supportive measures.
  • Severe diarrhea or colitis (Grade 3 or higher) occurred in 14% of patients treated with Zydelig.
  • Fatal and serious pneumonitis occurred in patients treated with Zydelig. If symptomatic pneumonitis or organizing pneumonia is diagnosed, initiate appropriate treatment with corticosteroids and permanently discontinue Zydelig
  • Fatal and serious intestinal perforation occurred in Zydelig-treated patients. Discontinue Zydelig permanently in patients who experience intestinal perforation.
  • Neutropenia may occur. Monitor blood counts. Interrupt Zydelig until resolution and resume at reduced dose.
  • Based on findings in animals and its mechanism of action, Zydelig may cause fetal harm when administered to a pregnant woman. Advise females of reproductive potential of potential risk to a fetus and to use effective contraception.

What to do in case of emergency/overdose?

  • In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

Can this medicine be used in pregnancy?

  • Based on findings in animal studies and the mechanism of action , Zydelig may cause fetal harm when administered to a pregnant woman.

Can this medicine be used in children?

  • Safety and effectiveness of Zydelig in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

  • Active ingredient: idelalisib
  • Inactive ingredients: microcrystalline cellulose, hydroxypropyl cellulose, croscarmellose sodium, sodium starch glycolate, and magnesium stearate. The tablet coating contains polyethylene glycol, talc, polyvinyl alcohol, titanium dioxide and FD&C Yellow #6 or Sunset Yellow FCF Aluminum Lake (for the 100 mg tablet) and red iron oxide (for the 150 mg tablet).

Who manufactures and distributes this medicine?

  • Manufactured and distributed by: Gilead Sciences, Inc. Foster City, CA 94404

What should I know about storage and disposal of this medication?

  • Store Zydelig between 68°F to 86°F (20°C to 30°C).
  • Keep Zydelig in its original container.
  • Do not use Zydelig if the seal over the bottle opening is broken or missing.
  • Keep Zydelig and all medicines out of reach of children.

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