Bosutinib

What it is and how it works

Mechanism of Action Bosutinib is a TKI. Bosutinib inhibits the BCR-ABL kinase that promotes 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 kinase expressed in murine myeloid cell lines. Bosutinib did not inhibit the T315I and V299L mutant cells.

Mechanism class: Bcr-Abl Tyrosine Kinase Inhibitors

Indications

Bosutinib tablets are indicated for the treatment of: Adult patients with chronic phase (CP) Philadelphia chromosome-positive chronic myelogenous leukemia (Ph+ CML), newly-diagnosed or resistant or intolerant to prior therapy . Adult patients with accelerated phase (AP), or blast phase (BP) Ph+ CML with resistance or intolerance to prior therapy . 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. Bosutinib tablets are a kinase inhibitor indicated for the treatment of adult patients with chronic phase Ph+ chronic myelogenous leukemia (CML), newly-diagnosed or resistant or intolerant to prior therapy. adult patients with accelerated, or blast phase Ph+ CML with resistance or intolerance to prior therapy.

Dosage and administration (summary)

Adult patients with newly-diagnosed chronic phase Ph+ CML: 400 mg orally once daily with food. Adult patients with chronic, accelerated, or blast phase Ph+ CML with resistance or intolerance to prior therapy: 500 mg orally once daily with food. 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. Adjust dosage for toxicity and organ impairment Recommended Dosage The recommended dosage is taken orally once daily with food. Swallow tablets whole. Do not cut, crush, break or chew tablets.

Contraindications

Bosutinib tablets are contraindicated in patients with a history of hypersensitivity to bosutinib. Reactions have included anaphylaxis . Hypersensitivity to bosutinib.

Warnings and precautions

Gastrointestinal Toxicity: Monitor and manage as necessary. Withhold, dose reduce, or discontinue bosutinib. ( 2.3, 5.1 ) Myelosuppression: Monitor blood counts and manage as necessary. Withhold, dose reduce, or discontinue bosutinib. ( 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. ( 2.3, 5.3 ) Cardiovascular Toxicity: Monitor and manage as necessary. Interrupt, dose reduce, or discontinue bosutinib. Fluid Retention: Monitor patients and manage using standard of care treatment.

Pregnancy

Pregnancy R isk Summary Based on findings from animal studies and its mechanism of action, bosutinib can cause fetal harm when administered to a pregnant woman . There are no available data in pregnant women to inform the drug-associated risk.

Storage and supply

Tablets - How Supplied Bosutinib tablets are supplied for oral administration in a single strength 400 mg orange, oval, biconvex, film-coated tablets debossed with “400” on one side and “B” on other side. Bosutinib tablets are available in the following packaging configurations with a child-resistant CR) closure (Table 17).

Source: Bosutinib (Bosutinib) — US FDA prescribing information, 2026-05-25, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.