Zydelig

Relapsed CLL with rituximab. Relapsed FL or SLL after 2+ prior systemic therapies.

150 mg orally twice daily.

Tablets: 100 mg, 150 mg

History of serious allergic reactions including anaphylaxis and TEN.

• Hepatotoxicity: Fatal cases reported. Monitor LFTs every 2 weeks for 3 months.
• Severe Diarrhea/Colitis: Including fatal cases.
• Pneumonitis: Fatal cases reported.
• Infections: Fatal infections including PJP and CMV. Provide PJP prophylaxis.
• Severe Cutaneous Reactions: Including SJS and TEN.

Diarrhea (47%), Pyrexia (28%), Nausea (24%), Fatigue (24%), Cough (22%), Pneumonia (20%), Rash (18%), ALT/AST Elevation (16%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

CYP3A Substrates: Idelalisib is a strong CYP3A inhibitor; avoid sensitive substrates.
CYP3A Inducers: Avoid.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Idelalisib selectively inhibits PI3K-delta, which is highly expressed in malignant B cells and important for proliferation, survival, homing, and retention. Inhibition leads to apoptosis in CLL and lymphoma cells.

Tmax: 1.5 hours. Protein binding: ~84%. Half-life: ~8 hours. Elimination: feces 78%, urine 15%.

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• Study 312-0116 — Idelalisib + rituximab vs placebo + rituximab in relapsed CLL. Phase III, n=220.
  🔬 NCT01539512 ↗ 📄 Primary Publication ↗

Zydelig has FDA-approved indications across the following cancer types covered on CancerDrugEvidence: