Bosutinib

Bosutinib is a TKI. Bosutinib inhibits the BCR-ABLkinase that promotes CML; it is also an inhibitor of Src-family kinases including Src, Lyn, and Hck.

• Bosutinib tablets are indicated for the treatment of: • Adult patients with chronic phase (CP) Philadelphia chromosome-positive chronic myelogenous leukemia (Ph+ CML), resistant or intolerant to prior therapy [see Clinical Studies (14.2)]. • Adult patients with accelerated phase (AP), or blast phase (BP) Ph+ CML with resistance or intolerance to prior therapy [see Clinical Studies (14.2)] .ICD-10: C95.90

• Bosutinib tablet is contraindicated in patients with a history of hypersensitivity to bosutinib. Reactions have included anaphylaxis [see Adverse Reactions (6.1)] .contraindicated

• Adult patients with chronic, accelerated, or blast phase Ph+ CML with resistance or intolerance to prior therapy: 500 mg orally once daily with food. ( 2.1 ) • Consider dose escalation by increments of 100 mg once daily to a maximum of 600 mg daily in adult patients who do not reach complete hematologic, cytogenetic, or molecular response and do not have Grade 3 or greater adverse reactions. ( 2.2 ) • Adjust dosage for toxicity and organ impairment ( 2 ) 2.1 Recommended Dosage The recommended dosage is taken orally once daily with food. Swallow tablets whole. Do not cut, crush, break or chew tablets. Continue treatment with bosutinib tablets until disease progression or intolerance to therapy. If a dose is missed beyond 12 hours, the patient should skip the dose and take the usual prescribed dose on the following day. Dosage in Adult Patients with CP, AP, or BP Ph+ CML with Resistance or Intolerance to Prior Therapy The recommended dosage of bosutinib tablet is 500 mg orally once daily with food. Pediatric use information is approved for PF PRISM CV’s BOSULIF® (bosutinib) tablets. However, due to PF PRISM CV’s marketing exclusivity rights, this drug product is not labeled with that information. 2.2 Dose Escalation In clinical studies of adult patients with Ph+ CML, dose escalation by increments of 100 mg once daily to a maximum of 600 mg once daily was allowed in patients who did not achieve or maintain a hematologic, cytogenetic, or molecular response and who did not have Grade 3 or higher adverse reactions at the recommended starting dosage.

• Gastrointestinal Toxicity: Monitor and manage as necessary. Withhold, dose reduce, or discontinue bosutinib tablets. ( 2.3 , 5.1 ) • Myelosuppression: Monitor blood counts and manage as necessary. Withhold, dose reduce or discontinue bosutinib tablets ( 2.4 , 5.2 ) • Hepatic Toxicity: Monitor liver enzymes at least monthly for the first 3 months and as needed. Withhold, dose reduce, or discontinue bosutinib tablets. ( 2.3 , 5.3 ) • Cardiovascular Toxicity: Monitor and manage as necessary. Interrupt, dose reduce, or discontinue bosutinib tablets. ( 5.4 ) • Fluid Retention: Monitor patients and manage using standard of care treatment. Interrupt, dose reduce, or discontinue bosutinib tablets. ( 2.3 , 5.5 ) • Renal Toxicity: Monitor patients for renal function at baseline and during therapy with bosutinib tablets. ( 5.6 ) • Embryo-Fetal Toxicity: Bosutinib tablets can cause fetal harm. Advise female patients of reproductive potential of potential risk to a fetus and to use effective contraception. ( 5.7 ) 5.1 Gastrointestinal Toxicity Diarrhea, nausea, vomiting, and abdominal pain occur with bosutinib tablets treatment. Monitor and manage patients using standards of care, including antidiarrheals, antiemetics, and fluid replacement. Among 546 adult patients in a single-arm study in patients with CML who were resistant or intolerant to prior therapy, the median time to onset for diarrhea (all grades) was 2 days and the median duration per event was 2 days.

The following clinically significant adverse reactions are discussed in greater detail in other sections of the labeling: Gastrointestinal toxicity [see Warnings and Precautions (5.1)] . Myelosuppression [see Warnings and Precautions (5.2)] . Hepatic toxicity [see Warnings and Precautions (5.3)] . Cardiovascular toxicity [see Warnings and Precautions (5.4)]. Fluid retention [see Warnings and Precautions (5.5)] . Renal toxicity [see Warnings and Precautions ( 5.6)] . • Most common adverse reactions (≥20%), in adult patients with CML are diarrhea, abdominal pain, vomiting, nausea, rash, fatigue, hepatic dysfunction, headache, pyrexia, and respiratory tract infection. The most common laboratory abnormalities (≥20%) in adult patients are creatinine increased, hemoglobin decreased, lymphocyte count decreased, platelets decreased, ALT increased, calcium decreased, white blood cell count decreased, AST increased, absolute neutrophil count decreased, glucose increased, phosphorus decreased, urate increased, alkaline phosphatase increased, lipase increased, creatine kinase increased, and amylase increased. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Alembic Pharmaceuticals Limited at 1-866-210-9797 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Lactation: Advise women not to breastfeed. ( 8.2 ) Pediatric use information is approved for PF PRISM CV’s BOSULIF® (bosutinib) tablets. However, due to PF PRISM CV’s marketing exclusivity rights, this drug product is not labeled with that information. 8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action, bosutinib tablets can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1)] . There are no available data in pregnant women to inform the drug-associated risk. In animal reproduction studies conducted in rats and rabbits, oral administration of bosutinib during organogenesis caused adverse developmental outcomes, including structural abnormalities, embryo-fetal mortality, and alterations to growth at maternal exposures (AUC) as low as 1.2 times the human exposure at the dose of 500 mg/day (see Data ) . Advise pregnant women of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies are 2 to 4% and 15 to 20%, respectively.

Metabolism

Bosutinib pharmacokinetics were assessed following oral dosing with food in adult patients with CML and were presented as geometric mean (CV%), unless otherwise specified. Bosutinib exhibits dose proportional increases in C max and AUC over the oral dose range of 200 to 800 mg (0.33 to 1.3 times the maximum approved recommended dosage of 600 mg).

Experience with bosutinib tablets overdose in clinical studies was limited to isolated cases. There were no reports of any serious adverse events associated with the overdoses. Patients who take an overdose of bosutinib tablets should be observed and given appropriate supportive treatment.

• Sep 4, 2012NDANDA203341Pf Prism Cv
• Sep 26, 2023NDANDA217729Pf Prism Cv
• May 23, 2025ANDAANDA209543Alembic

The 10 most recently updated of 81 ClinicalTrials.gov registrations naming Bosutinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study on the Tolerability, Safety and Effectiveness of Asciminib in Patients With Philadelphia Chromosome-positive Chronic Myeloid Leukemia in the Chronic Phase in Germany
  Recruiting · Observational · 380 enrolled · Novartis Pharmaceuticals
  NCT07549516updated 2026-06-12
• Asciminib Roll-over Study
  Recruiting · Phase 4 · Interventional · 347 enrolled · Novartis Pharmaceuticals
  NCT04877522updated 2026-06-10
• A Study of Oral Asciminib Versus Other TKIs in Adult Patients With Newly Diagnosed Ph+ CML-CP
  Active not recruiting · Phase 3 · Interventional · 405 enrolled · Novartis Pharmaceuticals
  NCT04971226updated 2026-06-08
• Safety And Efficacy Of TKI Cessation For CML Patients With Stable Molecular Response In A Real World Population
  Active not recruiting · Phase 2 · Interventional · 17 enrolled · Baylor College of Medicine
  NCT04626024updated 2026-05-04
• A Study to Learn About the Study Medicine Bosulif in Adult Patients With Chronic Myeloid Leukemia(CML).
  Recruiting · Observational · 600 enrolled · Pfizer
  NCT06297161updated 2026-04-14
• Treatment Free Remission After Combination Therapy With Ruxolitinib Plus Tyrosine Kinase Inhibitors
  Active not recruiting · Phase 2 · Interventional · 24 enrolled · H. Lee Moffitt Cancer Center and Research Institute
  NCT03610971updated 2026-04-02
• Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR)
  Recruiting · Phase 2 · Interventional · 720 enrolled · Canadian Cancer Trials Group
  NCT03297606updated 2026-03-27
• Testing the Addition of Ruxolitinib to the Usual Treatment (Tyrosine Kinase Inhibitors) for Chronic Myeloid Leukemia
  Active not recruiting · Phase 2 · Interventional · 81 enrolled · SWOG Cancer Research Network
  NCT03654768updated 2025-12-18
• Treatment Patterns and Outcomes Among Patients With Chronic Myeloid Leukemia (CML) in All Lines of Treatment
  Completed · Observational · 2,298 enrolled · Novartis Pharmaceuticals
  NCT07188428updated 2025-09-23
• Bosutinib in Pediatric Patients With Newly Diagnosed Chronic Phase or Resistant/Intolerant Ph + Chronic Myeloid Leukemia
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 60 enrolled · Children's Oncology Group
  NCT04258943updated 2025-09-18

Frequently asked questions

How does Bosutinib work?

Bosutinib is a TKI. Bosutinib inhibits the BCR-ABLkinase that promotes CML; it is also an inhibitor of Src-family kinases including Src, Lyn, and Hck.

What is Bosutinib used for?

According to FDA labeling, Bosutinib carries indications including: Bosutinib tablets are indicated for the treatment of: • Adult patients with chronic phase (CP) Philadelphia chromosome-positive chronic myelogenous leukemia (Ph+ CML), resistant or intolerant to prior therapy [see Clinical Studies (14.2)]. • Adult patients with accelerated phase (AP), or blast phase (BP) Ph+ CML with resistance or intolerance to prior therapy [see Clinical Studies (14.2)] .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Bosutinib?

Bosutinib is classified as BCR-ABL tyrosine kinase inhibitors, Kinase Inhibitor, Bcr-Abl Tyrosine Kinase Inhibitors, Tyrosine Kinase Inhibitors, Cellular Proliferation Alteration.

What are the brand names for Bosutinib?

Bosutinib is marketed under brand names including Bosulif.

What are the contraindications for Bosutinib?

Bosutinib labeling lists contraindications including: Bosutinib tablet is contraindicated in patients with a history of hypersensitivity to bosutinib. Reactions have included anaphylaxis [see Adverse Reactions (6.1)] .. Always consult the full prescribing information and a clinician.