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November 15, 2025
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Brand Name :
Zydelig
(United States) [Available]Synonyms :
idelalisib
Class :
Antineoplastics and PI3K Inhibitors
Brand Name :
Zydelig
(United States) [Available]Synonyms :
idelalisib
Class :
Antineoplastics and PI3K Inhibitors
AdultÂ
Dosage forms & StrengthsÂ
TabletÂ
100mgÂ
150mg Â
Chronic Lymphocytic Leukemia (Cll)
150
mg
Tablet
Orally 
twice a day
If severe symptomatic pneumonitis occurs, discontinue the usage of idelalisib
Enough patients were not available for the confirmatory trial; hence the idelalisib was withdrawn in case of treatment of Small Lymphocytic Lymphoma
Follicular B Cell Non Hodgkin Lymphoma
Enough patients were not available for the confirmatory trial; hence the idelalisib was withdrawn in case of treatment of Follicular B-cell Non-Hodgkin Lymphoma
Safety and efficacy of idelalisib are not found for pediatric dosingÂ
Refer to adult dosing Â
Idelalisib is contraindicated in the patients who are hypersensitive to any of the excipients in the formulation
when both drugs are combined, there may be an increased effect of nilotinib by affecting hepatic or intestinal enzyme cyp3a4 metabolism  
Idelalisib is contraindicated in the patients who are hypersensitive to any of the excipients in the formulation
may enhance the QTc-prolonging effect of each other when combined
It may enhance the effect when combined with irinotecan liposomal by affecting CYP3A4 metabolism
It may enhance when combined with oxycodone by affecting CYP3A4 metabolism
nafcillin will decrease the effect of action of idelalisib by affecting enzyme CYP3A4 metabolism.
cyclophosphamide effect of action decreased by affecting enzyme CYP3A4 metabolism.
the idelalisib interacting with brentuximab has its effect increased by altering the intestinal or hepatic CYP3A4 enzyme metabolism.
when both drugs are combined, there may be a reduced metabolism of idelalisib  
idelalisib itself causes diarrhea, and when taken with nivolumab, it increases the risk of fatal diarrhea.
when both drugs are combined, there may be an increased level or effect of romidepsin by affecting hepatic or intestinal enzyme cyp3a4 metabolism  
idelalisib increases the effect of lapatinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
CYP3A strong enhancers of the small intestine may reduce the bioavailability of idelalisib
idelalisib increases the effect of entrectinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
idelalisib increases the effect of encorafenib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
idelalisib increases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
idelalisib increases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
it increases the effect or level of palbociclib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it will increase the impact or level of regorafenib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
may increase the level by affecting the hepatic enzyme CYP3A4 metabolism
may increase the level of zonisamide by affecting hepatic enzyme CYP3A4 metabolism
aminosalicylic acid derivatives
they increase the myelosuppressive effect of the myelosuppressive agents
idelalisib increases the effect or level of abemaciclib by altering the intestinal/hepatic CYP3A4 metabolism
belzutifan decreases the effect or level of idelalisib by altering the intestinal/hepatic CYP3A4 metabolism
idelalisib increases the effect or level of capmatinib by altering the intestinal/hepatic CYP3A4 metabolism
idelalisib increases the effect or level of elvitegravir by altering the intestinal/hepatic CYP3A4 metabolism
idelalisib increases the effect or level of fedratinib by altering the intestinal/hepatic CYP3A4 metabolism
idelalisib increases the effect or level of gefitinib by altering the intestinal/hepatic CYP3A4 metabolism
idelalisib increases the effect or level of ivacaftor by altering the intestinal/hepatic CYP3A4 metabolism
idelalisib increases the effect or level of lopinavir by altering the intestinal/hepatic CYP3A4 metabolism
idelalisib increases the effect or level of marijuana by altering the intestinal/hepatic CYP3A4 metabolism
idelalisib increases the effect or level of sildenafil by altering the intestinal/hepatic CYP3A4 metabolism
idelalisib increases the effect or level of warfarin by altering the intestinal/hepatic CYP3A4 metabolism
idelalisib increases the effect or level of zanubrutinib by altering the intestinal/hepatic CYP3A4 metabolism
idelalisib: they may diminish the serum concentration of CYP3A4 Inducers
idelalisib: they may diminish the serum concentration of CYP3A4 Inducers
idelalisib: they may diminish the serum concentration of CYP3A4 Inducers
idelalisib: they may diminish the serum concentration of CYP3A4 Inducers
idelalisib: they may diminish the serum concentration of CYP3A4 Inducers
It may enhance the risk of adverse effects when combined with Fluoroquinolones
It may enhance the risk of adverse effects when combined with Fluoroquinolones
It may enhance the risk of adverse effects when combined with Fluoroquinolones
It may enhance the risk of adverse effects when combined with Fluoroquinolones
It may enhance the risk of adverse effects when combined with Fluoroquinolones
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both the drugs are combined, the risk or severity of adverse effects increases    
when both drugs are combined, there may be an increased risk of severe and life-threatening liver problems  
when both drugs are combined, there may be an increased risk of severe and life-threatening diarrhea  
when both drugs are combined, there may be an increased effect of abemaciclib by affecting hepatic or intestinal enzyme cyp3a4 metabolism  
ganaxolone with idelalisib, alters the intestinal/hepatic CYP3A4 metabolism
idelalisib, when taken with ixazomib, alters the intestinal/hepatic CYP3A4 enzyme metabolism
Actions:Â
The main action of idelalisib is to slow down or stop the growth of cancer cells by inhibiting the PI3K-delta pathway. The US FDA has approved it for treating relapsed or refractory chronic lymphocytic leukemia (CLL), follicular lymphoma, and small lymphocytic lymphoma in combination with other medications.Â
Spectrum:Â
Regarding its spectrum of activity, idelalisib is primarily used in treating CLL, a type of blood cancer affecting the white blood cells and bone marrow, as well as follicular lymphoma and small lymphocytic are both types of non-Hodgkin’s lymphoma.Â
Frequency definedÂ
>10%Â
Skin rashÂ
Abdominal painÂ
Decreased appetiteÂ
DiarrheaÂ
ColitisÂ
NauseaÂ
VomitingÂ
LeukopeniaÂ
LymphocytopeniaÂ
NeutropeniaÂ
ChillsÂ
FatigueÂ
PneumoniaÂ
FeverÂ
1-10%Â
DehydrationÂ
Gastro reflux diseaseÂ
Oral herpes simplex infectionÂ
StomatitisÂ
Urinary tract infectionÂ
InsomniaÂ
LethargyÂ
ArthralgiaÂ
BronchitisÂ
PneumonitisÂ
SinusitisÂ
<1%Â
Cough Â
HepatotoxicityÂ
Intestinal perforationÂ
Liver Toxicity: Life-threatening liver injury was seen in 16–18% of patients. Liver function should be assessed before and during therapy. If abnormalities arise, the drug should be paused and the dose adjusted or stopped.Â
Severe Diarrhea/Colitis: Serious gastrointestinal effects occurred in 14–20% of cases. Regular monitoring is essential. At the first sign of symptoms or lab abnormalities, treatment should be interrupted and adjusted or discontinued.Â
Pneumonitis: Around 4% of patients developed potentially fatal lung inflammation. Watch for symptoms like cough or shortness of breath and signs of interstitial lung disease. Discontinue treatment if pneumonitis is suspected.Â
Infections: Serious or fatal infections were reported in 21–48% of patients. Monitor closely for any signs of infection and pause treatment if one is suspected.Â
Intestinal Perforation: This rare but deadly complication necessitates immediate discontinuation of the drug if suspected.Â
Contraindicated:Â
idelalisib is contraindicated in the patients who are hypersensitive to any of the excipients in the formulationÂ
Monitor closely:Â
5-aminosalicylic acid derivatives:Â
they increase the myelosuppressive effect of the myelosuppressive agentsÂ
abemaciclib:Â
idelalisib increases the effect or level of abemaciclib by altering the intestinal/hepatic CYP3A4 metabolismÂ
belzutifan:Â Â
belzutifan decreases the effect or level of idelalisib by altering the intestinal/hepatic CYP3A4 metabolismÂ
capmatinib:Â
idelalisib increases the effect or level of capmatinib by altering the intestinal/hepatic CYP3A4 metabolismÂ
elvitegravir:Â
idelalisib increases the effect or level of elvitegravir by altering the intestinal/hepatic CYP3A4 metabolismÂ
fedratinib:Â
idelalisib increases the effect or level of fedratinib by altering the intestinal/hepatic CYP3A4 metabolismÂ
gefitinib:Â
idelalisib increases the effect or level of gefitinib by altering the intestinal/hepatic CYP3A4 metabolismÂ
ivacaftor:Â
idelalisib increases the effect or level of ivacaftor by altering the intestinal/hepatic CYP3A4 metabolismÂ
lopinavir:Â
idelalisib increases the effect or level of lopinavir by altering the intestinal/hepatic CYP3A4 metabolismÂ
marijuana:Â
idelalisib increases the effect or level of marijuana by altering the intestinal/hepatic CYP3A4 metabolismÂ
sildenafil:Â
idelalisib increases the effect or level of sildenafil by altering the intestinal/hepatic CYP3A4 metabolismÂ
warfarin:Â
idelalisib increases the effect or level of warfarin by altering the intestinal/hepatic CYP3A4 metabolismÂ
zanubrutinib:Â
idelalisib increases the effect or level of zanubrutinib by altering the intestinal/hepatic CYP3A4 metabolismÂ
Minor:Â
ganaxolone:Â
ganaxolone with idelalisib, alters the intestinal/hepatic CYP3A4 metabolismÂ
ixazomib:Â
ixazomib with idelalisib, alters the intestinal/hepatic CYP3A4 metabolismÂ
Pregnancy consideration: The drug is toxic and unsafe for pregnant women and the developing fetus.Â
Breastfeeding warnings: No data available regarding the excretion of idelalisib in breast milk. Due to the possibility of serious adverse effects, women are advised to breast feed one month after the last dose of idelalisib.Â
Pregnancy category:Â
Pharmacology:Â
idelalisib is a medication that belongs to a class of drugs called phosphoinositide 3-kinase (PI3K) inhibitors. It works by inhibiting a specific subtype of PI3K called PI3K-delta, which is involved in the signaling pathways that promote the growth and survival of cancer cells.Â
Pharmacodynamics:Â
The pharmacodynamic effects of idelalisib are primarily evaluated through biomarker analyses, including the measurement of PI3K delta inhibition, downstream signaling pathway inhibition, and modulation of immune function.Â
Pharmacokinetics:Â
AbsorptionÂ
Peak plasma is achieved in 1.5 hours (single fasting dose)Â
AUC increased 1.4-fold when administered with a high-fat mealÂ
DistributionÂ
Protein-bound is 84%Â
The volume of distribution is 23 LÂ
MetabolismÂ
idelalisib undergoes minor metabolism by UGT1A4Â
Metabolized to its major inactive metabolite, GS-563117, through aldehyde oxidase and CYP3AÂ
Elimination and ExcretionÂ
Half-life is 8.2 hoursÂ
The systemic clearance rate is 14.9 L/hrÂ
The drug is excreted 78% in feces; 14% in urine, and 45-50% excreted as a metabolite in both urine and fecesÂ
Administration:Â
It is orally administered medication that is available in tablet form. The tablets should be swallowed whole with water and taken with or without food.Â
Patient information leafletÂ
Generic Name: idelalisib Â
Pronounced: Eye-DEL-a-LIS-ibÂ
Why do we use idelalisib?Â
idelalisib is a medication used to treat certain types of blood cancers. It primarily treats chronic lymphocytic leukemia (CLL), follicular lymphoma, and small lymphocytic lymphoma.Â
idelalisib is combined with rituximab to treat CLL in patients who have received at least one prior therapy. In clinical trials, the combination of idelalisib and rituximab significantly improved progression-free survival compared to rituximab alone.Â
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