(trade name)


Therapeutic: antineoplastics
Pharmacologic: kinase inhibitors
Pregnancy Category: D


Treatment of relapsed Chronic Lymphocytic Leukemia (CLL) with rituximab.Treatment of relapsed follicular B-cell non-Hodgkin's Lymphoma in patients who have failed at least two previous systemic therapies.Treatment of relapsed small lymphocytic lymphoma (SLL) in patients who have failed at least two previous systemic therapies.


Acts as an inhibitor of phosphatidylinositol 3–kinase; induces apoptosis and inhibits cell proliferation in malignant B-cell and tumor cells, also inhibits come cell-signaling pathways, chemotaxis, adhesion and cell viability.

Therapeutic effects

Decreased progression of lymphoma.


Absorption: Well absorbed following oral administration.
Distribution: Unknown.
Metabolism and Excretion: Undergoes hepatic metabolism mostly by CYP3A and other systems. Metabolites are excreted in feces (78%) and urine (14%).
Half-life: 8.2 hr.

Time/action profile (increase in progression-free survival†)

PO2 mos6 mos10–12 mos
† Noted for CLL.


Contraindicated in: History of serious allergic reactions including anaphylaxis or toxic epidermal necrolysis; Strong inducer or substrates of CYP3A;Concurrent use of other hepatotoxic drugs; Concurrent use of drugs that cause diarrhea; Pregnancy (may cause fetal harm); Lactation: Discontinue idelalisib or discontinue breastfeeding.
Use Cautiously in: Renal impairment (CCr ≤15 mL/min); Underlying hepatic impairment (monitor for toxicity; safe and effective use in patients with baseline ALT or AST values >2.5 x ULN or bilirubin >1.5 x ULN not established); Strong inhibitors of CYP3A (monitor for idelalisib toxicity); Geriatric: Elderly patients may be more sensitive to drug effects; Women with child-bearing potential (effective contraception required); Pediatric: Safe and effective use in children <18 yr not established.

Adverse Reactions/Side Effects

Central nervous system

  • fatigue (most frequent)
  • headache (most frequent)
  • insomnia (most frequent)
  • weakness (most frequent)


  • pneumonitis (life-threatening)
  • cough (most frequent)
  • dyspnea (most frequent)
  • nasal congestion


  • peripheral edema (most frequent)


  • colitis/diarrhea
  • hepatotixicity (life-threatening)
  • intestinal perforation (life-threatening)
  • abdominal pain (most frequent)
  • ↑ liver enzymes (most frequent)
  • nausea (most frequent)
  • vomiting (most frequent)
  • stomatitis


  • toxic epidermal necrolysis
  • rash (most frequent)

Fluid and Electrolyte

  • hyponatremia (most frequent)


  • hyperglycemia (most frequent)
  • hypoglycemia


  • neutropenia (life-threatening)
  • anemia (most frequent)
  • thrombocytopenia (most frequent)


  • hypertriglyceridemia (most frequent)


  • athralgia


  • allergic reactions including anaphylaxis (life-threatening)
  • chills (most frequent)
  • fever (most frequent)
  • night sweats (most frequent)
  • pain


Drug-Drug interaction

Blood level and effectiveness may be ↓ by concurrent strong CYP3A inducers including carbamazepine,, phenytoin or rifampin and should be avoided.Concurrent use of strong inhibitors of CPY3A including ketoconazole may ↑ blood levels and risk of toxicity (careful monitoring recommended). Blood levels of substrates of CYP3A including midazolam may be ↑ by idelalisib, concurrent use should be avoided.


Oral (Adults) 150 mg twice daily, continued until disease progresses or unavoidable toxicity occurs; dose modification/interruption required for neutropenia or thrombocytopenia..


Tablets: 100 mg, 150 mg

Nursing implications

Nursing assessment

  • Monitor for diarrhea (stools increased by >6 more/day); may occur at any time. Responds poorly to antidiarrheal agents; may respond to corticosteroids. If moderate diarrhea (increase of 4–6 stools/day over baseline) occurs, maintain dose and monitor at least weekly until resolved. If severe diarrhea (increase of ≥7 stools/day over baseline) or diarrhea requiring hospitalization occurs, withhold dose and monitor at least weekly until resolved, then resume idelalisib at 100 mg twice daily. If life-threatening diarrhea occurs, discontinue idelalisib permanently.
  • Monitor for signs and symptoms of pneumonitis (cough, dyspnea, hypoxia, interstitial infiltrates, decline >5% in oxygen saturation). Discontinue therapy with any symptoms of pneumonitis and treat with corticosteroids.
  • Monitor for signs and symptoms of intestinal perforation (moderate to severe diarrhea, new or worsening abdominal pain, chills, fever, nausea, vomiting). Discontinue idelalisib permanently if intestinal perforation occurs.
  • Assess for cutaneous reactions (exfoliative dermatitis, rash, erythema, macular or maculo-papular rash, pruritus). Discontinue idelalisib if skin reactions occur.
  • Monitor for signs and symptoms of anaphylaxis (dyspnea, wheezing, facial swelling). Discontinue idelalisib if symptoms occur.
  • Lab Test Considerations: Monitor AST, ALT, and serum bilirubin every 2 wks for 3 mo, then every 4 wks for next 3 mo, then every 1–3 mo thereafter. If AST/ALT ↑ 3 times upper limit of normal, monitor weekly until resolved. If AST/ALT >3–5 times upper limit of normal or bilirubin >1.5–3 times upper limit of normal, maintain dose and monitor weekly until ≤ 1 times upper limit of normal. If AST/ALT >5–20 times upper limit of normal or bilirubin >3–10 times upper limit of normal, withhold dose. Monitor at least weekly until AST/ALT and/or bilirubin <1 times upper limit of normal, then resume dose at 100 mg twice daily. If AST/ALT >20 times upper limit of normal and/or if bilirubin >10 times upper limit of normal, discontinue idelalisib permanently. Usually occurs within first 12 wks of therapy and reversible with dose interruption.
    • Monitor CBC and platelet counts at least every 2 wks for first 3 mo. If neutropenia occurs and ANC is 1.0–<1.5 Gi/L, maintain idelalisib dose. If ANC 0.5–1.0 Gi/L, maintain dose and monitor ANC at least weekly. If ANC <0.5 Gi/L, interrupt idelalisib; monitor ANC at least weekly until ANC ≥0.5 Gi/L, then may resume idelalisib at 100 mg twice daily.
    • If thrombocytopenia occurs and platelets 50 to <75 Gi/L, maintain idelalisib dose. If platelets 25 to <50 Gi/L, maintain dose and monitor platelet count at least weekly. If platelets <25 Gi/L, interrupt idelalisib; monitor platelet counts at least weekly until platelet count ≥25 Gi/L, then may resume idelalisib at 100 mg twice daily.
    • May cause ↓ hemoglobin.

Potential Nursing Diagnoses

Diarrhea (Adverse Reactions)
Deficient knowledge, related to medication regimen (Patient/Family Teaching)


  • Avoid concurrent use of medications causing hepatotoxicity or diarrhea.
  • Oral: Administer twice daily without regard to food. Swallow tablets whole; do not crush, break, or chew.

Patient/Family Teaching

  • Instruct patient to take idelalisib as directed. If a dose is missed by less than 6 hrs take as soon as remembered; if missed by more than 6 hrs wait and take next scheduled dose at usual time. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes.
  • Advise patient to notify health care professional immediately if diarrhea (bowel movements increase by six or more/day), severe abdominal pain, severe skin reactions (painful sores or ulcers on skin, lips, or mouth; severe rash with blisters or peeling skin), signs and symptoms of anaphylaxis, fever or signs of infection occur, or if signs and symptoms of liver toxicity (yellowing of skin or whites of eyes, dark or brown urine, bruising, abdominal pain in upper right side, bleeding), pneumonitis (cough, dyspnea), occur.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
  • Caution female patient of teratogenic effects of idelalisib. Advise patient to use effective contraception and avoid breastfeeding during and for at least 1 mo after last dose of idelalisib. Advise patient to notify health care professional promptly if pregnancy is suspected.

Evaluation/Desired Outcomes

  • Decreased progression of lymphoma.
References in periodicals archive ?
Its only approved oncology asset is idelalisib, marketed as Zydelig, which is a second line therapy with boxed warning in three indications: Relapsed chronic lymphocytic leukemia (CLL), in combination with rituximab, in patients for whom rituximab alone would be considered appropriate therapy due to other co-morbidities; Relapsed follicular B-cell non-Hodgkin lymphoma in patients who have received at least two prior therapies; and Relapsed small lymphocytic lymphoma (SLL) in patients who have received at least two prior therapies.
Idelalisib has shown satisfactory activity with ORR of 57% and median duration of response of 12.
Adler discusses new targeted therapies like ibrutinib and idelalisib and describes how other treatments, including radiation therapy and stem cell transplants, have been modified, while others have been discontinued.
Idelalisib (Zydelig, Gilead, Foster City, California) is an inhibitor of the phosphatidylinositol-3-kinase d (PI3K[delta]) isoform approved for the treatment of patients with relapsed chronic lymphocytic leukemia/small cell lymphoma, follicular lymphoma, and indolent non-Hodgkin lymphoma.
This new oral chemotherapy Idelalisib allows me to do exactly that "live" with cancer and therefore still be able to dream and plan for the future with my family.
It includes new regimens like antineoplastic and antiemetic agents, advances in radiation therapy, new monoclonal antibodies, a new form of immunological therapy, new targeted therapies like ibrutinib and idelalisib, advances in stem cell transplants, and information on how other treatments have been modified or discontinued.
Gilead Sciences' Zydelig, also known as idelalisib, has been recommended by the National Institute for Health and Care Excellence as a treatment option for adults with chronic lymphocytic leukaemia (CLL) who have relapsed after two years.
The nine new antineoplastic agents and their indications are belinostat (Beleodaq) for peripheral T-cell lymphoma; blinatumomab (Blincyto) for acute lymphoblastic leukemia; ceritinib (Zykadia) for non-small cell lung cancer; idelalisib (Zydelig) for some types of leukemia and lymphoma; nivolumab (Opdivo) for metastatic melanoma; olaparib (Lynparza) for ovarian cancer; pembrolizumab (Keytruda) for unresectable or metastatic melanoma; ramucirumab (Cyramza) for gastric or gastroesophageal adenocarcinoma and metastatic non-small cell lung cancer; and siltuximab (Sylvant) for multicentric Castleman disease.
The launch of a premium-priced novel glycol-engineered antibody; obinutuzumab; the personalized vaccine dasiprotimut-T, mTOR inhibitor everolimus, and several kinase inhibitors including idelalisib and ibrutinib (which already gained FDA approval) are expected to have a significant impact on the market size.
While the current standard of care consists of chemoimmunotherapy, CLL disease management is poised for dramatic changes, particularly in the treatment of relapsed/refractory and elderly patients, as four new drugs (Gazyva, Imbruvica, idelalisib and IPI-145) will launch during the forecast period.
This study, and others we have conducted on idelalisib, demonstrates that we may no longer need to use chemotherapy in CLL.