• Newly diagnosed Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL) (in combination with chemotherapy).
• T315I-positive Ph+ ALL.
• Ph+ ALL when no other kinase inhibitor is indicated.
• T315I-positive chronic myeloid leukemia (CML) (chronic phase, accelerated phase, or blast phase).
• Accelerated phase or blast phase CML when no other kinase inhibitor is indicated.
• Chronic phase CML in patients who have resistance or intolerance to 2 prior kinase inhibitors.

Contraindicated in:

• Moderate to severe hepatic impairment
• Newly diagnosed chronic phase CML
• OB: Pregnancy
• Lactation: Lactation.

Use Cautiously in:

• History of ischemia, thromboembolic disease, diabetes, dyslipidemia, hypertension, peripheral arterial disease, HF, or arrhythmias
• History of liver disease or pancreatitis
• Impending elective surgery
• Rep: Women of reproductive potential
• Pedi: Safety and effectiveness not established in children
• Geri: ↑risk of adverse reactions in older adults; consider age, organ function, concurrent disease states, and medications.

CV: arrhythmias, arterial thrombosis, hypertension, mI, peripheral arterial disease, peripheral edema, DEEP VEIN THROMBOSIS (DVT), pericardial effusion, HF.

Derm: dry skin, rash, ERYTHEMA MULTIFORME, impaired wound healing, STEVENS-JOHNSON SYNDROME.

EENT: blindness, blurred vision, cataracts, dry eye, eye pain, glaucoma, iritis, macular edema, retinal hemorrhage, retinal vein occlusion, ulcerative keratitis.

Endo: hyperglycemia, hypothyroidism.

F and E: hyperkalemia, hypocalcemia, hypokalemia, hyponatremia, hypophosphatemia.

GI: abdominal pain, constipation, diarrhea, hepatotoxicity, nausea, mucositis, pancreatitis, ↓ appetite, FISTULA FORMATION, GI PERFORATION.

GU: ↓fertility (females).

Hemat: anemia, bleeding, leukopenia, neutropenia, thrombocytopenia, LYMPHOPENIA.

MS: arthralgia, back pain, bone pain, extremity pain, muscle spasm, myalgia, muscle weakness.

Neuro: dizziness, fatigue, headache, peripheral neuropathy, weakness, insomnia, POSTERIOR REVERSIBLE ENCEPHALOPATHY SYNDROME (PRES), STROKE.

Resp: pleural effusion, PULMONARY EMBOLISM (PE).

Misc: fever, TUMOR LYSIS SYNDROME.

Drug-Drug:

• CYP3A4 inhibitors, including clarithromycin, conivaptan, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, posaconazole, ritonavir, and voriconazole, may ↑ levels and risk of toxicity; avoid concurrent use.
• CYP3A4 inducers, including carbamazepine, phenytoin, and rifampin, may ↓ levels and effectiveness; avoid concurrent use.
• Drugs that ↑ gastric pH, including proton pump inhibitors, H₂ blockers, and antacids, may ↓ levels and effectiveness; avoid concurrent use.

Natural-Natural Products:

• St. John's wort may ↓ levels and effectiveness; avoid concurrent use.

Drug-Food:

• Grapefruit juice may ↑ levels and risk of toxicity; avoid concurrent use.

(Generic available)

• Tablets (contain lactose): 10 mg; 15 mg; 30 mg; 45 mg;

Newly Diagnosed Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia

• PO (Adults): 30 mg once daily. ↓ to 15 mg once daily on achievement of minimum residual disease-negative (0.01% BCR::ABL1/ABL1) complete remission at the end of induction. Continue in combination with chemotherapy for up to 20 cycles until loss of response or unacceptable toxicity. Concurrent use of strong CYP3A4 inhibitor: If current dose 30 mg once daily, ↓ to 15 mg once daily. If current dose 15 mg once daily, ↓ to 10 mg once daily. If current dose 10 mg once daily, avoid concurrent use.

Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia for Whom No Other Kinase Inhibitors Are Indicated or T315I-Positive Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia

• PO (Adults): 45 mg once daily. Continue until loss of response or unacceptable toxicity. Consider discontinuing therapy if hematologic response has not occurred within 3 mo. Concurrent use of strong CYP3A4 inhibitor: If current dose 45 mg once daily, ↓ to 30 mg once daily. If current dose 30 mg once daily, ↓ to 15 mg once daily. If current dose 15 mg once daily, ↓ to 10 mg once daily. If current dose 10 mg once daily, avoid concurrent use.

Chronic Phase Chronic Myeloid Leukemia

• PO (Adults): 45 mg once daily; ↓ to 15 mg once daily on achievement of 1% BCR::ABL1I. If loss of response occurs, may then ↑ to 30 mg once daily or 45 mg once daily. Continue until loss of response at re-escalated dose or unacceptable toxicity. Consider discontinuing therapy if hematologic response has not occurred within 3 mo. Concurrent use of strong CYP3A4 inhibitor: If current dose 45 mg once daily, ↓ to 30 mg once daily. If current dose 30 mg once daily, ↓ to 15 mg once daily. If current dose 15 mg once daily, ↓ to 10 mg once daily. If current dose 10 mg once daily, avoid concurrent use.

Acute Phase Chronic Myeloid Leukemia or Blast Phase Chronic Myeloid Leukemia

• PO (Adults): 45 mg once daily. In patients with acute phase CML, consider ↓ dose on achievement of major cytogenetic response. Continue until loss of response or unacceptable toxicity. Consider discontinuing therapy if hematologic response has not occurred within 3 mo. Concurrent use of strong CYP3A4 inhibitor: If current dose 45 mg once daily, ↓ to 30 mg once daily. If current dose 30 mg once daily, ↓ to 15 mg once daily. If current dose 15 mg once daily, ↓ to 10 mg once daily. If current dose 10 mg once daily, avoid concurrent use.

Iclusig

• Inhibits kinases, which are involved in various stages of cell proliferation.

• Decreased progression of leukemia with improved survival.

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Absorption: Well absorbed following oral administration; absorption is pH dependent (↑ gastric pH may ↓ absorption).

Distribution: Unknown.

Protein Binding: >99%.

Metabolism/Excretion: Primarily metabolized in the liver via the CYP3A4 isoenzyme; metabolites eliminated in feces (87%) and urine (5%).

Half-life: 24 hr (range 12–66 hr).

(response as noted by disease markers)

*For resistant/intolerant chronic phase CML

†For accelerated/blast phase CML or Ph+ALL

• Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Instruct patient to take as directed and not to change dose or stop taking unless advised by health care professional. If a dose is missed, omit and take next dose the next day in the morning. Do not double doses to make up for missed dose.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• Caution patient to notify health care professional immediately if symptoms suggestive of a blood clot (chest pain, shortness or breath, weakness on one side of the body, speech problems, leg pain, leg swelling), liver failure (yellowing of eyes or skin, tea-colored urine, drowsiness), HF, pancreatitis (nausea, vomiting, abdominal pain or discomfort), neuropathy, unusual bleeding, easy bruising, fluid retention (leg swelling, abdominal swelling, weight gain, shortness of breath), or fever occurs.
• Advise patient to notify health care professional if signs of slow HR (fainting, dizziness, chest pain) or signs of rapid HR (palpitations, dizziness) occur.
• Instruct patient to maintain adequate hydration to minimize risk of tumor lysis syndrome.
• Advise patient to notify health care professional of therapy prior to surgery or if had recent surgery.
• Rep: May cause fetal harm. Advise females of reproductive potential to use effective contraception during and for 3 wk after final dose of therapy and to notify health care professional if pregnancy is planned or suspected. Advise patient to avoid breastfeeding during and for 6 days after last dose of therapy. May impair fertility in female patients.

poe-NA-ti-nib

NDC Code^*

• 63020- Millennium Pharmaceuticals, Inc.
  • 63020-533- Iclusig
    • 63020-533-30- 30 TABLET, FILM COATED in 1 BOTTLE (63020-533-30)

• 63020- Millennium Pharmaceuticals, Inc.
  • 63020-534- Iclusig
    • 63020-534-30- 30 TABLET, FILM COATED in 1 BOTTLE (63020-534-30)

• 63020- Millennium Pharmaceuticals, Inc.
  • 63020-535- Iclusig
    • 63020-535-30- 30 TABLET, FILM COATED in 1 BOTTLE (63020-535-30)

• 63020- Millennium Pharmaceuticals, Inc.
  • 63020-535- Iclusig
    • 63020-535-60- 60 TABLET, FILM COATED in 1 BOTTLE (63020-535-60)

• 76189- ARIAD Pharmaceuticals, Inc.
  • 76189-533- Iclusig
    • 76189-533-30- 30 TABLET, FILM COATED in 1 BOTTLE (76189-533-30)

• 76189- ARIAD Pharmaceuticals, Inc.
  • 76189-534- Iclusig
    • 76189-534-30- 30 TABLET, FILM COATED in 1 BOTTLE (76189-534-30)

• 76189- ARIAD Pharmaceuticals, Inc.
  • 76189-534- Iclusig
    • 76189-534-90- 90 TABLET, FILM COATED in 1 BOTTLE (76189-534-90)

• 76189- ARIAD Pharmaceuticals, Inc.
  • 76189-535- Iclusig
    • 76189-535-30- 30 TABLET, FILM COATED in 1 BOTTLE (76189-535-30)

• 76189- ARIAD Pharmaceuticals, Inc.
  • 76189-535- Iclusig
    • 76189-535-60- 60 TABLET, FILM COATED in 1 BOTTLE (76189-535-60)

• 76189- ARIAD Pharmaceuticals, Inc.
  • 76189-535- Iclusig
    • 76189-535-80- 180 TABLET, FILM COATED in 1 BOTTLE (76189-535-80)