- March 15, 2022
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Brand Name :
Zydelig
Synonyms :
idelalisib
Class :
Antineoplastics and PI3K Inhibitors
Dosage forms & Strengths
Tablet
100mg
150mg
chronic lymphocytic leukemia (Cll)
150
mg
Orally
twice a day
Tablet
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Enough patients were not available for the confirmatory trial; hence the idelalisib was withdrawn in case of treatment of Small Lymphocytic Lymphoma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Enough patients were not available for the confirmatory trial; hence the idelalisib was withdrawn in case of treatment of Follicular B-cell Non-Hodgkin Lymphoma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 dosing
Refer to adult dosing
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 and Spectrum:
Actions:
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.
Spectrum:
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.
Frequency defined:
>10%
Skin rash
Abdominal pain
Decreased appetite
Diarrhea
Colitis
Nausea
Vomiting
Leukopenia
Lymphocytopenia
Neutropenia
Chills
Fatigue
Pneumonia
Fever
1-10%
Dehydration
Gastro reflux disease
Oral herpes simplex infection
Stomatitis
Urinary tract infection
Insomnia
Lethargy
Arthralgia
Bronchitis
Pneumonitis
Sinusitis
<1%
Cough
Hepatotoxicity
Intestinal perforation
Black-Box Warning:
One warning is regarding the risk of hepatotoxicity or liver damage. Severe and fatal cases of hepatotoxicity have occurred in 16% of treated patients. Therefore, it is important to monitor liver function before and during treatment with idelalisib and to interrupt or discontinue the medication as recommended if there is evidence of liver damage.
Another warning concerns the risk of diarrhea, colitis, or colon inflammation. Severe and fatal cases of diarrhea or colitis have occurred in 14% of treated patients. Therefore, it is essential to monitor for gastrointestinal symptoms and laboratory evidence of inflammation before and during treatment with idelalisib and to interrupt or discontinue the medication if symptoms or inflammation appear.
A third warning concerns the risk of pneumonitis or inflammation of the lungs. Severe and fatal cases of pneumonitis have occurred in 4% of treated patients. Therefore, it is important to monitor for pulmonary symptoms and bilateral interstitial infiltrates during treatment with idelalisib, and to interrupt or discontinue the medication if pneumonitis is suspected.
A fourth warning is regarding the risk of infections. Severe and fatal infections have occurred in 48% of treated patients. Therefore, it is essential to monitor for signs and symptoms of infection during treatment with idelalisib and to interrupt the medication if the infection is suspected.
Contraindication/Caution:
Contraindications:
idelalisib is contraindicated in patients with a history of severe allergic reactions to idelalisib or any of its components.
Caution:
Pregnancy consideration: The drug is toxic and unsafe for pregnant women and the developing fetus.
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.
Pregnancy category:
Pharmacology:
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.
Pharmacodynamics:
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.
Pharmacokinetics:
Absorption
Peak plasma is achieved in 1.5 hours (single fasting dose)
AUC increased 1.4-fold when administered with a high-fat meal
Distribution
Protein-bound is 84%
The volume of distribution is 23 L
Metabolism
idelalisib undergoes minor metabolism by UGT1A4
Metabolized to its major inactive metabolite, GS-563117, through aldehyde oxidase and CYP3A
Elimination and Excretion
Half-life is 8.2 hours
The systemic clearance rate is 14.9 L/hr
The drug is excreted 78% in feces; 14% in urine, and 45-50% excreted as a metabolite in both urine and feces
Administration:
idelalisib is an orally administered medication that is available in tablet form. The tablets should be swallowed whole with water and taken with or without food. If a dose of idelalisib is missed, the patient should take the missed dose as soon as possible. However, if it is close to the time for the next dose, the patient should skip the missed dose and resume the regular dosing schedule.
It is essential to avoid grapefruit and grapefruit juice while taking idelalisib, as they may increase the risk of side effects. Patients should also inform their healthcare provider about any other medications, supplements, or herbal products, as they may interact with idelalisib.
Patient information leaflet
Generic Name: idelalisib
Pronounced: Eye-DEL-a-LIS-ib
Why do we use idelalisib?
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.
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.
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