idelalisib

Contraindicated in:

History of serious allergic reactions including anaphylaxis or toxic epidermal necrolysis;
Concurrent use of other hepatotoxic drugs;
Concurrent use of drugs that cause diarrhea;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Renal impairment (CCr ≤15 mL/min);
Underlying hepatic impairment (monitor for toxicity; safety and effectiveness in patients with baseline ALT or AST values >2.5 times upper limit of normal [ULN] or bilirubin >1.5 times ULN not established);
Rep: Women of reproductive potential;
Pedi: Safety and effectiveness not established in children;
Geri: Older adults may be more sensitive to drug effects.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: rash, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), STEVENS-JOHNSON SYNDROME (SJS), TOXIC EPIDERMAL NECROLYSIS (TEN)

EENT: nasal congestion

Endo: hyperglycemia, hypoglycemia

F and E: hyponatremia

GI: ↑liver enzymes, abdominal pain, colitis/diarrhea, hepatotoxicity, nausea, vomiting, INTESTINAL PERFORATION, stomatitis

Hemat: anemia, neutropenia, thrombocytopenia

Metab: hypertriglyceridemia

MS: arthralgia, pain

Neuro: fatigue, headache, insomnia, weakness

Resp: cough, dyspnea, PNEUMONITIS

Misc: chills, fever, infection, night sweats, ANAPHYLAXIS

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A inducers, including carbamazepine,, phenytoin or rifampin, may ↓ levels and effectiveness; avoid concurrent use.
Strong CYP3A inhibitors, including ketoconazole, may ↑ levels and risk of toxicity; careful monitoring recommended.
May ↑ levels and risk of toxicity of CYP3A substrates, including midazolam; avoid concurrent use.

Availability ⬆ ⬇

Tablets: 100 mg; 150 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 150 mg twice daily; continue until disease progression or unacceptable toxicity.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

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

Therapeutic effects:

Decreased progression of CLL.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A isoenzymes. Metabolites are excreted in feces (78%) and urine (14%).

Half-Life: 8.2 hr.

Time/Action Profile ⬆ ⬇

(↑ in progression-free survival‡)

ROUTE	ONSET	PEAK	DURATION
PO	2 mo	6 mo	10–12 mo

‡Noted for CLL.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take idelalisib as directed. If a dose is missed by <6 hr, take as soon as remembered; if missed by >6 hr, 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 ↑ by 6 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, DRESS, 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) or 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.
Rep: May cause fetal harm. Advise females of reproductive potential to use effective contraception and avoid breastfeeding during therapy and for at least 1 mo after last dose of idelalisib. Advise patient to notify health care professional promptly if pregnancy is suspected. Advise males with female partners of reproductive potential to use effective contraception during therapy and for 3 mo after last dose.

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Indications ⬇

Contraind./Precautions ⬆ ⬇