(boe-sue-ti nib) ,


(trade name)


Therapeutic: antineoplastics
Pharmacologic: kinase inhibitors
Pregnancy Category: D


Treatment of adults with chronic/accelerated/blast phase chronic myelogenous leukemia that it resistant/intolerant to previous therapies.


Acts as a kinase inhibitor, specifically inhibiting the kinase that promotes CML.

Therapeutic effects

Decreased progression of CML.


Absorption: Absorbed following oral administration
Distribution: Unknown.
Protein Binding: 96%
Metabolism and Excretion: Mostly metabolized, mainly by the CYP3A4 enzyme system; metabolites do not have antineoplastic activity.
Half-life: 22.5 hr

Time/action profile (beneficial hematologic response)

POwithin 8–12 wk4–6 hr (blood level)9–18 mo or longer


Contraindicated in: Hypersensitivity; Lactation: Breast feeding should be avoided; Obstetric: Pregnancy (may cause fetal harm);Concurrent use of moderate to strong CYP3A4 inbitors/inducers or P-gp inhibitors (may significantly alter drug effects).
Use Cautiously in: Hepatic impairment (dose ↓ recommended);Patients with reproductive potential (effective contraception is recommended); Pediatric: Safe and effective use in children <18 yr has not been established.

Adverse Reactions/Side Effects

Central nervous system

  • dizziness (most frequent)
  • fatigue (most frequent)
  • headache (most frequent)

Ear, Eye, Nose, Throat

  • tinnitus


  • cough (most frequent)


  • chest pain
  • fluid retention
  • pericarditis
  • prolonged QT interval


  • abdominal pain (most frequent)
  • ↓ appetite (most frequent)
  • diarrhea (most frequent)
  • nausea (most frequent)
  • vomiting (most frequent)
  • dysgeusia
  • gastritis
  • GI bleeding
  • hepatic toxicity
  • pancreatitis


  • itching (most frequent)
  • rash (most frequent)
  • acne

Fluid and Electrolyte

  • dehydration
  • hyperkalemia


  • anemia (most frequent)
  • neutropenia (most frequent)
  • thrombocytopenia (most frequent)


  • arthralgia (most frequent)
  • back pain (most frequent)
  • myalgia


  • allergic reactions including anaphlaxis
  • fever (most frequent)


Drug-Drug interaction

Concurrent use of moderate to strong CYP3A4 inibitors including amprenavir, aprepitant, atazanavir, bocepravir, ciprofloxacin, clarithromycin, conivaptan, crizotinib, darunavir, digoxin, diltiazem, erythromycin, fluconazole, fosamprenavir, imatinib, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, posiconazole, ritonavr, saquinavir, telaprevir, telithromcyin, verapamil and voriconazole ↑ blood levels and risk of toxicity and should be avoided.Concurrent use with CYP3A4 inducers including bosentan, carbamazepine, efavirenz, etravirine, modafinil, nafcillin, phenobarbital, phenytoin, rifabutin and rifampin may ↓ blood levels and beneficial effects and should be avoided.Proton pump inhibitors (PPIs) including esomeprazole, dexlansoprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole may ↓ blood levels and effectiveness and should be avoided, consider using short-acting antacids or histamine-H2 receptor blockers instead (these should be taken 2 hr before or 2 hr after bosutinib).May ↑ digoxin levels.Concurrent use with St. John's wort may ↓ blood levels and beneficial effects and should be avoided.Grapefruit juice may ↑ blood levels and the risk of toxicity and should be avoided.


Oral (Adults) 500 mg once daily, if complete hematologic response has not occurred by 8 wk, or complete cytologic response by 12 wk or there has been no occurrence of ≥Grade 3 adverse reactions, consider dose increase to 600 mg once daily. Dose adjustments should be made for toxicity (hematologic and non-hematologic).

Renal Impairment

Oral (Adults) CCr <30 mL/min—300 mg once daily

Hepatic Impairment

Oral (Adults) Any degree of hepatic impairment—200 mg once daily


Tablets: 100 mg, 500 mg

Nursing implications

Nursing assessment

  • Monitor for diarrhea, nausea, vomiting, and abdominal pain. For Grade 3–4 diarrhea (↑ of ≥7 stools/day over baseline/pretreatment), withhold bosutinib until recovery to Grade ≤1.
  • Assess for signs and symptoms fluid retention (swelling in hands, ankles, or feet; weight gain; shortness of breath; cough; chest pain). May manifest as pericardial effusion, pleural effusion, pulmonary edema, and/or peripheral edema. Interrupt, reduce dose or discontinue bosutinib as necessary.
  • Monitor for signs of allergic reaction (rash, shortness of breath, respiratory tract infections, loss of appetite, headache, dizziness, back pain, joint pain, itching)
  • Lab Test Considerations: Monitor CBC weekly for first mo, then monthly thereafter. May cause thrombocytopenia, anemia, and neutropenia. If ANC <1000 x 106/L or platelets <50,000 x 106/L, withhold bosutinib until ANC ≥1000 x 106/L and platelets ≥50,000 x 106/L. Resume treatment with bosutinib at same dose if recovery occurs within 2 weeks. If blood counts remain low for >2 weeks, upon recovery, reduce dose by 100 mg and resume treatment. If cytopenia recurs, reduce dose by an additional 100 mg upon recovery and resume treatment.
    • Monitor hepatic function monthly for first 3 mo, then periodically during therapy as clinically indicated. If ↑ liver transaminases > 5 × institutional upper limit of normal (ULN) occur, withhold bosutinib until recovery to ≤2.5 × ULN and resume at 400 mg once daily thereafter. If recovery takes longer than 4 weeks, discontinue bosutinib. If transaminase ↑ ≥3 × ULN occur concurrently with bilirubin ↑ >2 × ULN and alkaline phosphatase <2 × ULN, discontinue bosutinib.

Potential Nursing Diagnoses

Risk for infection (Adverse Reactions)


  • Oral: Administer once daily with food. In patients who do not reach complete hematological response by week 8 or a complete cytogenetic response by week 12, who did not have Grade 3 or higher adverse reactions, and who are currently taking 500 mg daily, consider dose escalation to 600 mg once daily with food. Swallow tablets whole; do not crush, break or chew. Do not handle crushed or broken tablets.

Patient/Family Teaching

  • Instruct patient to take bosutinib as directed. Take missed doses as soon as remembered if within 12 hours, if longer than 12 hrs 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.
  • Advise patient to immediately report fever, jaundice (skin or the white part of your eyes turns yellow or dark “tea color” urine), symptoms of infection, fluid retention, unexpected bleeding or bruising, or blood in urine or stools occur. Advise patient to notify health care professional if diarrhea, nausea, vomiting, abdominal pain occur.
  • Inform patient to take medications that decrease stomach acid (cimetidine (Tagamet®), famotidine (Pepcid®), ranitidine (Zantac®), aluminum hydroxide/magnesium hydroxide (Maalox®), calcium carbonate (Tums®), calcium carbonate and magnesia (Rolaids®) 2 hrs before or 2 hrs after bosutinib and to avoid taking esomeprazole (Nexium®), esomeprazole strontium, dexlansoprazole (Dexilant®), lansoprazole (Prevacid®), omeprazole (Prilosec®, Vimovo®, Zegerid®), pantoprazole sodium (Protonix®), and rabeprazole (AcipHex®).
  • 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 to use effective contraception during and for at least 30 days following discontinuation of therapy. Advise patient to avoid pregnancy and breastfeeding; notify health care professional immediately if pregnancy is suspected.

Evaluation/Desired Outcomes

  • Decreased progression of CML.
Drug Guide, © 2015 Farlex and Partners
References in periodicals archive ?
[59] that demonstrates a protective role of bosutinib (src/c-Abl inhibitor) in motor neurons derived from iPSC of patients with familial or sporadic ALS.
Nilotinib, dasatinib, and bosutinib are some prominent examples of second generation TKIs and ponatinib are an example of a third generation of TKI.
He was switched to bosutinib and has been tolerating therapy well without any symptoms.
This is demonstrated in a report by Fujimi et al., in which a CML patient experienced reversible dasatinib-induced skin and hair depigmentation and then did not experience any depigmentation when subsequently treated with bosutinib [7].
The patient then switched to bosutinib 500 mg oral daily [9], reduced to 400mg oral daily after gastrointestinal toxicities, which resulted in an MMR within three months (BCR-ABL1/ABL1 IS 0.02%).
Kantarjian et al., "Bosutinib versus imatinib in newly diagnosed chronic-phase chronic myeloid leukemia: results from the BELA trial," Journal of Clinical Oncology, vol.
Bis[sulfosuccinimidyl]suberate (BS3), PP2, and bosutinib (the latter two being Src kinase inhibitors) and compound 56 (C56; an EGFR inhibitor) were obtained from Calbiochem (San Diego, CA, USA).
Generic Name Annual Cost Ponatinib $138,000 Bosutinib $118,000 Omacetaxine Over $100,000 Older anti-leukemia drugs like imatinib (Gleevec[R]) were initially priced at nearly $30,000 a year when released in 2001.
to conduct a global Phase 3 clinical trial of Pfizer's BOSULIF (bosutinib).
Of these, five are in the subclass of tyrosine kinase inhibitors (trade name; indication): axitinib (Inlyta; renal cancer), bosutinib (Bosulif; leukemia), cabozantinib (Cometriq; thyroid cancer), ponatinib (Iclusig; leukemia), and ziv-aflibercept (Zal-trap; colorectal cancer).
Key Words: Chronic myeloid leukemia, Tyrosine kinase inhibitor, Imatinib, Nilotinib, Dasatinib, Bosutinib, Ponatinib