• Leukemias, lymphomas, and other hematologic cancers

Zydelig Generic Name & Formulations

General Description

Idelalisib 100mg, 150mg; tabs.

Pharmacological Class

Phosphatidylinositol 3-kinase inhibitor.

How Supplied



Generic Availability


Zydelig Indications


Relapsed chronic lymphocytic leukemia (CLL), in combination with rituximab, in patients for whom rituximab alone would be considered appropriate due to other co-morbidities.

Limitations of Use

Not recommended for first-line treatment of CLL, small lymphocytic lymphoma (SLL), follicular lymphoma (FL), and other indolent non-Hodgkin lymphomas, or in combination with bendamustine and/or rituximab for FL, SLL, and other indolent non-Hodgkin lymphomas.

Zydelig Dosage and Administration


Swallow whole. ≥18yrs: initially 150mg twice daily (max); continue until disease progression or unacceptable toxicity. Dose modifications: see full labeling.


<18yrs: not established.

Zydelig Contraindications


History of toxic epidermal necrolysis (TEN) with any drug.

Zydelig Boxed Warnings

Boxed Warning

Fatal and serious toxicities: hepatic, severe diarrhea, colitis, pneumonitis, infections, and intestinal perforation.

Zydelig Warnings/Precautions


Hepatotoxicity: monitor ALT/AST every 2 weeks for the first 3 months, every 4 weeks for the next 3 months, then every 1–3 months thereafter; if ALT/AST >3×ULN, monitor weekly until resolved; if ALT/AST >5×ULN, withhold and continue monitoring weekly until resolved; if ALT/AST >20×ULN or bilirubin >10×ULN, discontinue permanently. Monitor for diarrhea or colitis; withhold if severe or hospitalization; discontinue permanently if life-threatening. Pneumonitis: monitor for pulmonary symptoms or a decline by >5% in oxygen saturation; if diagnosed, treat and discontinue permanently. Infections: monitor and interrupt if Grade ≥3. Treat infections before starting. Provide Pneumocystis jirovecii pneumonia (PJP) prophylaxis during treatment; interrupt if PJP infection is suspected and permanently discontinue if confirmed. Monitor patients with history of CMV infection or (+) baseline CMV serology; interrupt if CMV PCR (+) until resolved; if resumed, monitor for reactivation at least monthly. Discontinue permanently if intestinal perforation occurs. Monitor for severe cutaneous (eg, SJS, TEN, DRESS) or serious hypersensitivity reactions; permanently discontinue if occur. Monitor CBCs at least every 2 weeks for the first 6 months, and at least weekly if neutrophils <1.0Gi/L. Hepatic impairment: monitor. Embryo-fetal toxicity. Advise to use effective contraception during and for at least 1 month (females) or 3 months (males w. female partners) after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 1 month after the last dose).



Zydelig Pharmacokinetics

See Literature

Zydelig Interactions


Avoid concomitant drugs that can cause hepatotoxicity or diarrhea. May be potentiated by strong CYP3A inhibitors (eg, ketoconazole); use alternatives or monitor frequently for idelalisib toxicity. May be antagonized by strong CYP3A inducers (eg, rifampin); avoid. May potentiate CYP3A substrates (eg, oral midazolam); avoid.

Zydelig Adverse Reactions

Adverse Reactions

Diarrhea, pyrexia, fatigue, nausea, cough, pneumonia, abdominal pain, chills, rash, neutropenia, ALT/AST elevations.

Zydelig Clinical Trials

See Literature

Zydelig Note

Not Applicable

Zydelig Patient Counseling

See Literature