Bosutinib

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[edit] BRAND NAMES

[edit] STRUCTURE

Bosutinib.jpg

[edit] MECHANISM OF ACTION

Bosutinib is a tyrosine kinase inhibitor. Bosutinib inhibits the Bcr-Abl kinase that promotes chronic myelogenous leukemia (CML); it is also an inhibitor of Src-family kinases including Src, Lyn, and Hck. Bosutinib inhibited 16 of 18 imatinib-resistant forms of Bcr-Abl expressed in murine myeloid cell lines. Bosutinib did not inhibit the T315I and V299L mutant cells. In mice, treatment with bosutinib reduced the size of CML tumors relative to controls and inhibited growth of murine myeloid tumors expressing several imatinib-resistant forms of Bcr-Abl.

[edit] INDICATIONS

Bosutinib is indicated for the treatment of adult patients with chronic, accelerated, or blast phase Ph+ chronic myelogenous leukemia (CML) with resistance or intolerance to prior therapy.

[edit] DOSAGE

  • Recommended Dose: 500 mg orally once daily with food.
  • Consider dose escalation to 600 mg daily in patients who do not reach complete hematologic response by week 8 or complete cytogenetic response by week 12 and do not have Grade 3 or greater adverse reactions.
  • Adjust dosage for hematologic and non-hematologic toxicity.
  • Adjust dosage for hepatic and renal impairment.

[edit] DOSAGE FORMS AND STRENGTHS

Tablets: 100 mg and 500 mg

[edit] CONTRAINDICATIONS

Hypersensitivity to Bosutinib

[edit] WARNINGS AND PRECAUTIONS

  • Gastrointestinal toxicity: Diarrhea, nausea, vomiting, and abdominal pain occur with Bosutinib treatment. Monitor and manage patients using standards of care, including antidiarrheals, antiemetics, and/or fluid replacement. Withhold, dose reduce, or discontinue Bosutinib.
  • Myelosuppression: Thrombocytopenia, anemia and neutropenia occur with Bosutinib treatment . Monitor blood counts and manage as necessary.
  • Hepatic toxicity: Monitor liver enzymes at least monthly for the first three months and as needed. Withhold, dose reduce, or discontinue Bosutinib.
  • Fluid retention: Fluid retention occurs with Bosutinib and may manifest as pericardial effusion, pleural effusion, pulmonary edema, and/or peripheral edema. Monitor patients and manage using standard of care treatment. Withhold, dose reduce, or discontinue Bosutinib as necessary.
  • Embryofetal toxicity: May cause fetal harm. Females of reproductive potential should avoid becoming pregnant while being treated with Bosutinib.

[edit] INTERACTIONS

  • CYP3A Inhibitors and Inducers: Avoid concurrent use of Bosutinib with strong or moderate CYP3A inhibitors and inducers.
  • Proton Pump Inhibitors: May decrease bosutinib drug levels. Consider short-acting antacids or H2 blockers instead of PPIs to avoid a reduction in bosutinib exposure.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category D (US). Bosutinib can cause fetal harm when administered to a pregnant woman. Studies in animals showed reproductive toxicities. If Bosutinib is used during pregnancy, or if the patient becomes pregnant while taking Bosutinib, the patient should be apprised of the potential hazard to the fetus.
  • Nursing Mothers: It is not known whether bosutinib is excreted in human milk. Bosutinib and/or its metabolites were excreted in the milk of lactating rats. Radioactivity was present in the plasma of suckling offspring 24 to 48 hours after lactating rats received a single oral dose of radioactive bosutinib. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from Bosutinib, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

[edit] SIDE EFFECTS

Most common adverse reactions (incidence greater than 20%) are diarrhea, nausea, thrombocytopenia, vomiting, abdominal pain, rash, anemia, pyrexia, and fatigue

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES