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Indications ⬇

High Alert

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects ⬆ ⬇

CV: chest pain, HF, myocardial ischemia, pericardial effusion, pericarditis, peripheral edema, QT interval prolongation, tachycardia

Derm: itching, rash, acne, STEVENS-JOHNSON SYNDROME (SJS)

EENT: tinnitus

Endo: hypothyroidism

F and E: dehydration, hyperkalemia

GI: ↑liver enzymes, abdominal pain, diarrhea, nausea, vomiting, gastritis, GI bleeding, HEPATOTOXICITY, pancreatitis

GU: ↓fertility, renal impairment

Hemat: anemia, neutropenia, thrombocytopenia

Metab: ↓appetite

MS: arthralgia, back pain, myalgia

Neuro: dizziness, fatigue, headache, dysgeusia

Resp: cough, pulmonary edema

Misc: fever, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

Drug-Natural Products:

Drug-Food:

Availability ⬆ ⬇

(Generic available)
  • Capsules: 50 mg; 100 mg
  • Tablets: 100 mg; 400 mg; 500 mg

Route/Dosage ⬆ ⬇

Chronic Phase Ph+ CML Resistant/Intolerant to Previous Therapies

  • PO (Adults and Children ≥1 yr and BSA ≥1.1 m2): 500 mg once daily; if hematologic, cytogenetic, or molecular response is not achieved or maintained and there has been no occurrence of Grade ≥3 adverse reactions, consider ↑ dose in 100-mg/day increments up to max dose of 600 mg once daily. Continue until disease progression or unacceptable toxicity.
  • PO (Children ≥1 yr and BSA 0.9–<1.1 m2): 400 mg once daily; if hematologic, cytogenetic, or molecular response is not achieved after 3 mo, consider ↑ dose in 50-mg/day increments up to max dose of 500 mg once daily. Continue until disease progression or unacceptable toxicity.
  • PO (Children ≥1 yr and BSA 0.75–<0.9 m2): 350 mg once daily; if hematologic, cytogenetic, or molecular response is not achieved after 3 mo, consider ↑ dose in 50-mg/day increments up to max dose of 450 mg once daily. Continue until disease progression or unacceptable toxicity.
  • PO (Children ≥1 yr and BSA 0.63–<0.75 m2): 300 mg once daily; if hematologic, cytogenetic, or molecular response is not achieved after 3 mo, consider ↑ dose in 50-mg/day increments up to max dose of 400 mg once daily. Continue until disease progression or unacceptable toxicity.
  • PO (Children ≥1 yr and BSA 0.55–<0.63 m2): 250 mg once daily; if hematologic, cytogenetic, or molecular response is not achieved after 3 mo, consider ↑ dose in 50-mg/day increments up to max dose of 350 mg once daily. Continue until disease progression or unacceptable toxicity.
  • PO (Children ≥1 yr and BSA <0.55 m2): 200 mg once daily; if hematologic, cytogenetic, or molecular response is not achieved after 3 mo, consider ↑ dose in 50-mg/day increments up to max dose of 300 mg once daily. Continue until disease progression or unacceptable toxicity.

Renal Impairment

  • PO (Adults and Children ≥1 yr and BSA ≥1.1 m2): CCr 30–50 mL/min: 400 mg once daily; CCr <30 mL/min: 300 mg once daily.

Renal Impairment

  • (Children ≥1 yr and BSA 0.9–<1.1 m2): CCr 30–50 mL/min: 300 mg once daily; CCr <30 mL/min: 250 mg once daily.

Renal Impairment

  • (Children ≥1 yr and BSA 0.75–<0.9 m2): CCr 30–50 mL/min: 250 mg once daily; CCr <30 mL/min: 200 mg once daily.

Renal Impairment

  • (Children ≥1 yr and BSA 0.63–<0.75 m2): CCr 30–50 mL/min: 200 mg once daily; CCr <30 mL/min: 200 mg once daily.

Renal Impairment

  • (Children ≥1 yr and BSA 0.55–<0.63 m2): CCr 30–50 mL/min: 200 mg once daily; CCr <30 mL/min: 150 mg once daily.

Renal Impairment

  • (Children ≥1 yr and BSA <0.55 m2): CCr 30–50 mL/min: 150 mg once daily; CCr <30 mL/min: 100 mg once daily.

Hepatic Impairment

  • PO (Adults and Children ≥1 yr and BSA ≥1.1 m2): Mild, moderate, or severe hepatic impairment: 200 mg once daily.

Hepatic Impairment

  • (Children ≥1 yr and BSA 0.9–<1.1 m2): Mild, moderate, or severe hepatic impairment: 200 mg once daily.

Hepatic Impairment

  • (Children ≥1 yr and BSA 0.63–<0.9 m2): Mild, moderate, or severe hepatic impairment: 150 mg once daily.

Hepatic Impairment

  • (Children ≥1 yr and BSA <0.63 m2): Mild, moderate, or severe hepatic impairment: 100 mg once daily.

Newly Diagnosed Chronic Phase Ph+ CML

  • PO (Adults and Children ≥1 yr and BSA ≥1.1 m2): 400 mg once daily; if hematologic, cytogenetic, or molecular response is not achieved or maintained and there has been no occurrence of Grade ≥3 adverse reactions, consider ↑ dose in 100-mg/day increments up to max dose of 600 mg once daily. Continue until disease progression or unacceptable toxicity.
  • PO (Children ≥1 yr and BSA 0.9–<1.1 m2): 300 mg once daily; if hematologic, cytogenetic, or molecular response is not achieved after 3 mo, consider ↑ dose in 50-mg/day increments up to max dose of 400 mg once daily. Continue until disease progression or unacceptable toxicity.
  • PO (Children ≥1 yr and BSA 0.75–<0.9 m2): 250 mg once daily; if hematologic, cytogenetic, or molecular response is not achieved after 3 mo, consider ↑ dose in 50-mg/day increments up to max dose of 350 mg once daily. Continue until disease progression or unacceptable toxicity.
  • PO (Children ≥1 yr and BSA 0.55–<0.75 m2): 200 mg once daily; if hematologic, cytogenetic, or molecular response is not achieved after 3 mo, consider ↑ dose in 50-mg/day increments up to max dose of 300 mg once daily. Continue until disease progression or unacceptable toxicity.
  • PO (Children ≥1 yr and BSA <0.55 m2): 150 mg once daily; if hematologic, cytogenetic, or molecular response is not achieved after 3 mo, consider ↑ dose in 50-mg/day increments up to max dose of 250 mg once daily. Continue until disease progression or unacceptable toxicity.

Renal Impairment

  • (Adults and Children ≥1 yr and BSA ≥1.1 m2): CCr 30–50 mL/min: 300 mg once daily; CCr <30 mL/min: 200 mg once daily.

Renal Impairment

  • (Children ≥1 yr and BSA 0.9–<1.1 m2): CCr 30–50 mL/min: 200 mg once daily; CCr <30 mL/min: 200 mg once daily.

Renal Impairment

  • (Children ≥1 yr and BSA 0.75–<0.9 m2): CCr 30–50 mL/min: 200 mg once daily; CCr <30 mL/min: 150 mg once daily.

Renal Impairment

  • (Children ≥1 yr and BSA 0.63–<0.75 m2): CCr 30–50 mL/min: 150 mg once daily; CCr <30 mL/min: 100 mg once daily.

Renal Impairment

  • (Children ≥1 yr and BSA 0.55–<0.63 m2): CCr 30–50 mL/min: 150 mg once daily; CCr <30 mL/min: 100 mg once daily.

Renal Impairment

  • (Children ≥1 yr and BSA <0.55 m2): CCr 30–50 mL/min: 100 mg once daily; CCr <30 mL/min: 100 mg once daily.

Hepatic Impairment

  • (Adults and Children ≥1 yr and BSA ≥1.1 m2): Mild, moderate, or severe hepatic impairment: 200 mg once daily.

Hepatic Impairment

  • (Children ≥1 yr and BSA 0.9–<1.1 m2): Mild, moderate, or severe hepatic impairment: 150 mg once daily.

Hepatic Impairment

  • (Children ≥1 yr and BSA <0.9 m2): Mild, moderate, or severe hepatic impairment: 100 mg once daily.

Accelerated/Blast Phase Ph+ CML Resistant/Intolerant to Previous Therapies

  • PO (Adults ): 500 mg once daily; if hematologic, cytogenetic, or molecular response is not achieved or maintained and there has been no occurrence of Grade ≥3 adverse reactions, consider ↑ dose in 100-mg/day increments up to max dose of 600 mg once daily. Continue until disease progression or unacceptable toxicity.

Hepatic Impairment

  • PO (Adults ): Any degree of hepatic impairment: 200 mg once daily.

Renal Impairment

  • PO (Adults ): CCr 30–50 mL/min: 400 mg once daily; CCr <30 mL/min: 300 mg once daily.

US Brand Names ⬆ ⬇

Bosulif

Action ⬆ ⬇

  • Acts as a kinase inhibitor, specifically inhibiting the kinase that promotes CML.
Therapeutic effects:
  • Decreased progression of CML.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: 34% absorbed following oral administration; absorption ↑ with high-fat meal.

Distribution: Extensively distributed to tissues.

Protein Binding: 96%

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A4 isoenzyme; metabolites do not have antineoplastic activity.

Half-Life: 22.5 hr

Time/Action Profile ⬆ ⬇

(beneficial hematologic response)

ROUTEONSETPEAKDURATION
POwithin 8–12 wk4–6 hr (plasma concentrations)9–18 mo or longer

Patient/Family Teaching ⬆ ⬇

  • Explain the purpose and side effects of bosutinib. Instruct patient to take as directed. Take missed doses as soon as remembered if within 12 hr; if longer than 12 hr, skip dose and take usual prescribed dose on the following day. Do not stop taking bosutinib without consulting health care professional. Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes.
  • Advise patient to avoid grapefruit and grapefruit juice during therapy.
  • Warn patient to report signs/symptoms and seek treatment for HF or fluid retention.
  • Advise patient to immediately report signs/symptoms of hepatotoxicity.
  • Instruct patient to notify health care professional or call 911 immediately to seek medical care if swelling of face, eyes, lips, or tongue or if difficulty swallowing or breathing occur.
  • Advise patient to notify health care professional if fever, rash, diarrhea, nausea, vomiting, blood in stools, abdominal pain, or any signs of infection 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, especially St. John's wort.
  • Rep: May cause fetal harm. Advise women of reproductive potential to use effective contraception and to avoid breastfeeding during and for ≥2 wk after last dose of therapy. Advise patient to notify health care professional immediately if pregnancy is suspected. May impair fertility in men and women.

Pronunciation ⬆ ⬇

boe-SUE-ti nib

Code ⬆

NDC Code